course
Anticonvulsants, Gabapentin
Drugs for neuropathic pain and peripheral neuropathy
at the DEA level
undertake
describe
Oral analogue of GABA.
Adjunctive therapy for restless legs syndrome, postherpetic neuralgia, and partial seizures; orphan drug for the treatment of amyotrophic lateral sclerosis (ALS).
Monitor for new or worsening suicidal thoughts or behaviors and/or depression.
common brand
Active-PAC με Gabapentin, Gralise, Horizant, Neurontin
how to provide
Active-PAC with Gabapentin/Gabapentin/Neurontin Oral Caps: 100mg, 300mg, 400mg
Gabapentin/Gralise/Neurontin oral tablet: 300mg, 450mg, 600mg, 750mg, 800mg, 900mg
Gabapentin/Neurontin oral solution: 5mL, 250mg
Horizont oral tablet ER: 300mg, 600mg
Dosage and indications
For the adjunctive treatment of partial-onset seizures with or without secondary generalized tonic-clonic seizures.
Oral dose (immediate-release formulations only, eg Neurontin)
adults and teenagers
Initially, 300 mg PO 3 times daily. May be increased to 300, 400, 600 or 800 mg orally 3 times daily. The effective dose is 900-1800 mg/day, but the maximum long-term use can reach 2400 mg/day. Doses of 3600 mg/day have been administered to a limited number of patients for a relatively short period of time. Dosing should not be less frequent than every 12 hours. No dose adjustment of other anticonvulsants was required. Doses should be based on CrCl if appropriate.
Children aged 3-12 years (adjunctive therapy)
Initially, 10-15 mg/kg/day, orally, in 3 divided doses; gradually titrate to effective dose over 3 days. If > 5 years, the effective dose is 25-35 mg/kg/day orally in 3 divided doses. If the child is 3-4 years old, the effective dose is 40 mg/kg/day taken orally in 3 divided doses. Dosing should not be less frequent than every 12 hours. Continue titration to 50 mg/kg/day PO as needed based on clinical response; occasionally use higher doses. In one study, the dose was further increased to a maximum of 50 mg/kg/day in refractory patients if clinically indicated.
For the treatment of moderate to severe primary restless legs syndrome (RLS).
Oral dose (gabapentin etacabil extended-release, Horizant only)
adult
You take 600 mg by mouth every evening around 5:00 pm. with the food. If the recommended time is missed, the next dose should be taken the next day as prescribed. Doses of 1,200 mg/day have been studied but did not provide additional benefit and an increase in adverse effects was observed. Limitations of Use: Not recommended for patients who need to sleep during the day and stay awake at night. Due to differences in chemical form and pharmacokinetic properties, the different formulations of gabapentin are not interchangeable.
For the treatment of Amyotrophic Lateral Sclerosis (ALS)†.
Note: Gabapentin has been designated an orphan drug by the FDA for this indication.
oral dose
adult
In a case-control study of 110 patients, gabapentin 1000 mg/day orally in divided doses for 6 months slowed the decline in muscle strength and showed a trend toward increased survival compared with controls.
For horror†.
For the treatment of postural tremor†.
oral dose
adult
In a limited trial of 4 patients, an initial dose of 100 mg PO three times daily titrated to 2400 mg/day orally in divided doses was effective in reducing postural tremor. Crossover with placebo resulted in relapse of tremor in all patients.
For the treatment of essential tremor†.
oral dose
adult
Clinical practice guidelines from the American Academy of Neurology suggest that gabapentin may be effective as monotherapy in the treatment of essential tremor. Initial doses range from 300-400 mg/day PO (single or divided doses). The dose is then titrated to 400-600 mg PO 3 times daily for 4-7 days and then further titrated to a maximum target dose of 1800-3600 mg/day PO in 3 divided doses. In these small trials, gabapentin treatment showed variable efficacy; however, the data suggest modest overall clinical and functional improvement. The drug may provide a treatment option for patients who have had an inadequate response or intolerance to standard treatments such as beta-blockers (eg propranolol). At the dose studied, gabapentin improved the Clinical Tremor Rating Scale and other clinical measures of tremor compared with placebo. There were no significant differences between gabapentin and propranolol in these outcomes. One study showed that higher doses of gabapentin 3600 mg/day PO improved activities of daily living (ADL) and global scores compared with lower total daily doses. Common side effects include nausea, fatigue and drowsiness. Larger, well-controlled trials are needed to determine the role and optimal dosing strategy of gabapentin in the treatment of essential tremor.
For the treatment of nystagmus†.
For the treatment of acquired pendulum nystagmus†.
oral dose
adult
Limited short-term data suggest that dose titration from 300 mg PO once daily to 300 mg PO 3 to 4 times daily may be effective. Gabapentin reduces eye tremors and the frequency of eye tremors and improves vision.
For the treatment of congenital nystagmus†.
oral dose
Adults and Youth 16 years and older
In a small retrospective analysis, 900 mg/day PO (in divided doses) was administered initially and increased to 2400 mg/day PO as indicated. Infantile nystagmus (n = 2) and nystagmus associated with ocular pathology (n = 5) patients had reduced nystagmus amplitude after treatment. Vision improved in all infant patients with nystagmus, vision improved in 4 patients with eye lesions.
For the treatment of episodic symptoms and cramps caused by multiple sclerosis†.
oral dose
adult
In an open-label trial, 18 of 21 MS patients treated with PO 600-1200 mg/day in divided doses reported improvements in trigeminal neuralgia, paresthesias, spasticity, and ocular ataxia. The authors concluded that further research is needed on the role of gabapentin for the treatment of paroxysmal symptoms in multiple sclerosis.
For hot flashes† associated with menopause† or in women who have been treated for breast cancer.
To reduce hot flashes associated with natural menopause†.
oral dose
adult woman
Initially, 300 mg/day PO is recommended, titrated to 300 mg PO 3 times daily if the patient continues to experience hot flashes on lower doses. The North American Menopause Society (NAMS) guidelines for nonhormonal therapy indicate that gabapentin is an effective option for the management of menopausal vasomotor symptoms when hormonal therapy is not required or contraindicated. Doses up to 2700 mg/day have been studied. Data from a small randomized controlled trial of 59 postmenopausal women showed that gabapentin treatment for 12 weeks significantly reduced the frequency of hot flashes (45% reduction in the gabapentin group vs. 29% reduction in the placebo group, p = 0.02) as well as the frequency and severity of hot flashes (54% reduction in the gabapentin group vs. 31% reduction in the placebo group, p = 0.01). A study of 60 postmenopausal women showed no difference in the frequency or severity of hot flashes between those receiving conjugated estrogens 0.625 mg/day and those receiving gabapentin 2400 mg/day (conjugated estrogens vs. gabapentin 2400 mg Composite hot flush score was reduced by 72% compared to 1 day). 71% for gabapentin, p = 0.63), but there was a significant difference in both treatment groups compared to placebo. The overall incidence of adverse events was similar between the two treatments; however, gabapentin use was associated with a higher incidence of symptom clusters such as headache, dizziness, and disorientation. When data from the available studies were pooled, oral gabapentin 900 mg daily was associated with an overall reduction of 2 hot flashes compared with placebo (mean difference -2.05, 95% CI -2.80 to -1.30 ).
To reduce hot flashes in women with breast cancer†.
oral dose
adult woman
Initially, 300 mg/day PO is recommended, titrated to 300 mg PO 3 times daily if the patient continues to experience hot flashes on lower doses. The North American Menopause Society (NAMS) guidelines for nonhormonal therapy indicate that gabapentin is an effective option for the management of menopausal vasomotor symptoms when hormonal therapy is not required or contraindicated. Doses up to 2700 mg/day have been studied. Data from a randomized clinical trial of 420 women with breast cancer (71% who received tamoxifen) showed that gabapentin significantly reduced the mean daily frequency of hot flashes by -2.10 (90% CI -2.95 to -1.23, p less than 0.0001) with placebo after 8 weeks, the mean percentage change in hot flush severity was -30% (95% CI -44% to -16%, p less than 0.0001); these effects were seen as early as 4 weeks after the drug started to show. Gabapentin at a PO dose of 300 mg/day had no effect on the frequency or severity of hot flashes compared with placebo. In a trial of vitamin E versus gabapentin, hot flashes were reduced to a significantly greater extent with gabapentin than with vitamin E, and 35% of the vitamin E group discontinued the trial due to lack of efficacy. When data from the available studies were pooled, oral gabapentin 900 mg daily was associated with an overall reduction of 2 hot flashes compared with placebo (mean difference -2.05, 95% CI -2.80 to -1.30 ).
For the treatment of pruritus†, including pruritus associated with chronic kidney disease (CKD-aP)†.
For the treatment of pruritus associated with chronic kidney disease (CKD-aP)† in patients undergoing hemodialysis.
oral dose (immediate release)
adult
300 mg PO 3 times weekly after hemodialysis.
For the treatment of brachial pruritus†.
oral dose (immediate release)
adult
300 to 1,800 mg/day orally in divided doses.
For the treatment of neuropathic pain, including complex peripheral pain syndrome†, diabetic neuropathy†, postherpetic neuralgia (PHN) and trigeminal neuralgia†.
For the treatment of diabetic neuropathy†.
oral dose (immediate release)
adult
Initially, 300 mg PO 3 times daily. Dose titration based on clinical response and tolerability. Maximum: 3,600 mg/day. In clinical trials, the average effective and tolerated daily dose was reported to be approximately 1,500 mg/day in divided doses. The guidelines suggest that gabapentin may be effective in the treatment of painful diabetic neuropathy.
For the treatment of postherpetic neuralgia (PHN).
Note: Gabapentin products are not interchangeable due to differences in pharmacokinetic profile.
oral dose
adult
300 mg PO once daily for 1 day, then 300 mg PO twice daily for 1 day, then 300 mg PO 3 times daily. The dose can be increased as needed for pain. Maximum: 600 mg PO 3 times daily.
Oral dose (Extended-release tablet, Gralise)
Note: Gabapentin products are not interchangeable due to differences in pharmacokinetic profile.
adult
300 mg PO qd for 1 day, then 600 mg PO qd for 1 day, then 900 mg PO qd for 4 days, then 1,200 mg PO qd for 4 days, then 1,500 mg PO once daily for 4 days and then 1,800 mg PO once daily. Maximum: 1,800 mg/day.
Oral Dose (Extended-release tablet; Horizant)
Note: Gabapentin products are not interchangeable due to differences in pharmacokinetic profile.
adult
600 mg PO once daily for 3 days, then 600 mg PO twice daily. Maximum: 1,200 mg/day.
For the treatment of trigeminal neuralgia†.
oral dose (immediate release)
adult
Initially, 100 mg PO 3 times daily or 300 mg PO once daily. Increase dose by 300 mg/day as needed. Usual maximum dose: 1,800 mg/day. Maximum: 3,600 mg/day.
For the treatment of complex regional pain syndrome†.
oral dose (immediate release)
adult
600 mg PO once daily for 2 days, then 600 mg PO twice daily for 2 days, then 600 mg PO 3 times daily. Lower starting doses and doses up to 3,600 mg/day have been used.
For the treatment of fibromyalgia†.
oral dose
adult
Start treatment with 300 mg at bedtime for 1 week. After 1 week, gradually increase to target dose (2400 mg/day) according to the following schedule: 300 mg twice daily for 1 week, 300 mg twice daily, 600 mg at bedtime for 2 weeks, 600 mg daily 3 times for 2 weeks, 600 mg twice daily, 1200 mg at bedtime. If discontinuation is required, gradually reduce the dose to 300 mg/day. The safety and efficacy of gabapentin in the treatment of fibromyalgia were evaluated in a randomized, double-blind, placebo-controlled, parallel-group study. Adult patients meeting the American College of Rheumatology criteria for fibromyalgia with a mean pain severity item score ≥4 on the Brief Pain Inventory (BPI) were randomized 1:1 to receive either gabapentin for 12 weeks (n = 75) or placebo. n = 75). Acetaminophen, nonprescription nonsteroidal anti-inflammatory drugs, and intermittent use of sedative antihistamines were permitted during the trial. Antidepressants were not allowed and required a 2-week washout period before study initiation; fluoxetine required a 30-day washout period. The primary outcome was pain severity as measured by the mean BPI Pain Severity Score (0-10, none to severe); a positive response to treatment required a score reduction of >= 30%. Pain interference with activities such as general mood, interpersonal relationships, work, and sleep was also assessed. Various other secondary outcomes were assessed, including the overall impact of fibromyalgia on several components of health status assessed by the Fibromyalgia Impact Questionnaire (FIQ) (0–80, higher score = more negative impact). Analysis using intention-to-treat. Thirty-one patients (21%) withdrew before completion of the study. The average daily dose of gabapentin is 1800 mg/day. Pain severity scores were significantly reduced (from about 5.7 to 3.2) at 12 weeks of gabapentin treatment compared with placebo (6 to 4.6). The estimated difference between groups was -0.92 (95% CI -1.75 to -0.71, p = 0.015). Pain interference scores were also significantly lower in the gabapentin group than in the placebo group (from about 4.7 to 2.2) (from 5.3 to 3.6); the estimated between-group difference was -0 .81 (95% CI -1.56 to -0.07, p = 0.032). Fifty-one percent of patients in the gabapentin group and 31% in the placebo group (p = 0.014) responded to treatment. FIQ total score also favored gabapentin (26.2 +/- 15.1 vs 37.3 +/- 18.1), with an estimated difference of -8.4 (95% CI -13 to -3.3, p = 0.001). A total of 19 patients discontinued treatment due to adverse events during the trial (12 in the gabapentin group and 7 in the placebo group). The most common adverse effects of gabapentin were headache (26.7%), dizziness (25.3%), sedation (24%), and nausea (21.3%).
To treat hiccups (hiccup)†.
oral dose
adult
300 mg PO 3 times daily titrated in response to 1200 mg/day, alternatively, 400 mg PO 3 times daily for 3 days, then 400 mg PO qd for 3 days.
For the treatment of autonomic dysfunction after severe traumatic brain injury†.
Oral dose (immediate release formulation)
adult
300 mg orally twice daily. Titrate to desired clinical outcome. Doses up to 600 mg PO three times daily have been used.
For long-term prophylaxis of short-term unilateral neuralgia-like headache with injection and conjunctival tearing (SUNCT)†.
oral dose
adult
Limited case series and case reports suggest that doses ranging from 300 mg PO twice daily to 300 mg to 1200 mg PO three times daily may be effective in reducing or eliminating SUNCT symptoms. Most patients require a dose of at least 900 mg/day PO. Titration to response and tolerance.
For the treatment of alcohol dependence†.
Oral dose (immediate release product)
adult
Initially, 300 mg orally at bedtime on Day 1; then 300 mg orally twice daily on Day 2; then 300 mg orally 3 times daily on Day 3; then titrated over 4 to 7 days to reach the final dosage plan. PO doses ranging from 600 mg/day to 1,800 mg/day are beneficial for treating symptoms of alcohol dependence, such as increased abstinence and nonabuse rates, fewer heavy drinking days, and fewer drinks per day. Although the overall quality of the studies was low, gabapentin works well for alcohol use disorder (AUD), especially at higher doses, and may be considered as a treatment option. The American Psychiatric Association's evidence-based practice guidelines for the medication of patients with alcohol use disorder indicate that gabapentin can be offered to patients with moderate to severe alcohol use disorder who aim to reduce or achieve abstinence from alcohol and prefer gabapentin or naltrex Ketone and acamprosate were intolerant or unresponsive and there were no contraindications to gabapentin.
For the treatment of alcohol withdrawal†.
oral dose (immediate release)
adult
Initial dose of 1,200 mg PO loading dose followed by 600 mg PO orally every 6 hours on day 1 or 400 mg PO three times daily for 1 to 3 days, then tapered to 300 to 600 mg/day for 4 days to 7 days. Additional doses may be given as needed.
†Denotes off-label use
maximum dose
adult
3600 mg/day PO (immediate-release products such as Neurontin), 1800 mg/day PO (extended-release, Gralise only), 1200 mg/day PO (extended-release, Horizant only).
Geriatrics
3600 mg/day PO (immediate-release products such as Neurontin), 1800 mg/day PO (extended-release, Gralise only), 1200 mg/day PO (extended-release, Horizant only).
young
3600 mg/day PO (immediate-release products such as Neurontin); safety and efficacy of extended-release gabapentin products have not been established.
children
3-12 years: An immediate-release oral product of 50 mg/kg/day is recommended, and higher doses are occasionally used in resistant patients. The safety and efficacy of extended-release gabapentin products have not been established.
< 3 years: Safety and efficacy not established.
baby
Safety and efficacy have not been established.
newborn
Safety and efficacy have not been established.
Dosage Considerations
liver damage
Dose adjustment does not appear to be necessary unless renal impairment is present. Gabapentin is not metabolized.
Renal failure
• Immediate-release dose adjustments for adults and adolescents over 12 years of age:
Note: Immediate-release gabapentin has not been studied in children younger than 12 years of age with impaired renal function.
CrCl >= 60 mL/min: No dose adjustment required.
CrCl > 30-59 mL/min: Total dose ranges from 400-1400 mg/day, orally, divided into 2 divided doses.
CrCl > 15-29 mL/min: Total dose ranges from 200-700 mg/day, orally, once daily.
CrCl = 15 mL/min: total dose range 100–300 mg/day, orally, in daily doses of 100, 125, 150, 200, or 300 mg.
CrCl < 15 mL/min: Reduce daily dose according to CrCl (eg, CrCl = 7.5 mL/min should receive half the dose that a patient with CrCl 15 mL/min receives).
• Dose adjustments for extended-release tablets (Gralise tablets only, recommended for adults):
CrCl >= 60 mL/min: No dose adjustment required.
CrCl 30-59 mL/min: 600-1800 mg/day orally daily, based on tolerability and desired clinical benefit.
CrCl < 30 mL/min: Not recommended.
• Dose adjustments for extended-release tablets (Horizant tablets only, recommended for adults):
CrCl >= 60 mL/min: No dose adjustment required. For dose reduction prior to discontinuation, reduce dose to 600 mg PO once daily for 1 week prior to discontinuation.
CrCl 30–59 mL/min: For RLS, start at 300 mg/day PO and increase to 600 mg/day PO as needed. For PHN, start with 300 mg PO in the morning for 3 days and increase to 300 mg PO twice daily. Increase to 600 mg PO twice daily as needed. To taper before stopping, reduce the maintenance dose to once daily in the morning for 1 week before stopping.
CrCl 15—29 mL/min: For RLS, 300 mg/day orally. For PHN, 300 mg orally on days 1 and 3, followed by a maintenance dose of 300 mg orally each morning. Increase dose to 300 mg PO twice daily as needed. For dose reduction, if the patient is taking 300 mg twice daily, reduce the dose to 300 mg PO once daily in the morning for 1 week before discontinuing the drug. If a patient is taking 300 mg daily, it does not need to be reduced.
CrCl < 15 mL/min: For RLS and PHN, 300 mg orally every other day. For PHN, the dose may be increased to 300 mg PO once daily in the morning if needed. There is no need to gradually reduce the dose before stopping the drug.
intermittent hemodialysis
• Immediate release formulation (adults):
Patients undergoing hemodialysis should receive a PO maintenance dose based on CrCl, as indicated for patients with renal failure. A supplemental post-dialysis dose ranging from 125-350 mg PO (based on maintenance dose and CrCl) should be given every 4 hours after dialysis (see manufacturer's package label).
• Extended-release tablets (Gralise tablets, for adults only):
Not recommended.
• Extended-release tablets (Tablet Horizant, for adults only):
Patients should receive 300 mg PO orally after each dialysis session. The dose may be increased to 600 mg PO after each dialysis session if needed.
administrative
Medical guidelines discuss the proper use and precautions of gabapentin, as well as the risk of suicidal thoughts and behaviors associated with anticonvulsant use. This MedGuide should be distributed with each new prescription and refill.
Oral administration
oral solid dosage form
Administering an immediate-release capsule or tablet (such as Neurontin):
Administration may be administered without regard to meals, however, administration with meals minimizes adverse gastrointestinal effects.
In the treatment of epilepsy, the maximum time between doses should not exceed 12 hours.
The 600 mg and 800 mg tablets can be broken along the score line if desired. Advise patients to take the unused half tablet and the next dose as prescribed. Unused halves within 28 days of breaking a scored tablet should be discarded.
Oral capsules should be swallowed whole with plenty of water.
For patients with dysphagia: In one study, gabapentin capsules were opened and the contents mixed with drink (such as orange juice) or food (such as applesauce) in patients who could not swallow the capsules. Alternatively, a scored tablet can be cut in half and the other half used or discarded within 28 days.
Extended-release tablets (such as Gralise or Horizant) give:
Caution: Due to differences in pharmacokinetic profile and chemical composition, do not interchange Gralise or Horizant.
Take with food; bioavailability is significantly reduced if taken on an empty stomach. Once-daily patients should be instructed to take the tablets with the evening meal (around 5pm).
Swallow the extended-release tablet whole; do not break, crush, or chew the tablet.
oral liquid formulation
Measurements are taken with calibrated equipment prior to dosing to ensure accurate dosing.
Administration may be administered without regard to meals, however, administration with meals minimizes adverse gastrointestinal effects.
In the treatment of epilepsy, the maximum time between doses should not exceed 12 hours.
Save
Active-PAC with Gabapentin:
- Storage between 68 and 77 degrees Fahrenheit, with excursions allowed to 59 to 86 degrees Fahrenheit
Gaborone:
- Store at 77°F, allow excursions at 59-86°F
Glaris:
- Store between 20 and 25 degrees C (68 and 77 degrees F), allow movement between 15 and 30 degrees C (59 and 86 degrees F) USP controlled room temperature
Horizontal line:
- Waterproof
- Store at 77°F, allow excursions at 59-86°F
Neurons:
- Store between 20 and 25 degrees C (68 and 77 degrees F), allow movement between 15 and 30 degrees C (59 and 86 degrees F) USP controlled room temperature
Contraindications/Precautions
General information
Gabapentin is contraindicated in patients allergic to gabapentin or any component of the product.
Due to differences in chemical and pharmacokinetic profiles, Gralise or Horizant extended-release tablets are not interchangeable with each other or with other gabapentin products.
depression, suicidal ideation
Monitor closely for development or worsening of depression or suicidal ideation in all patients starting antiepileptic drug (AED) therapy or currently receiving gabapentin. Advise patients and caregivers of increased risk of suicidal thoughts and behaviors, and promptly report new or worsening depression, suicidal thoughts or behaviors, thoughts of self-harm, or other unusual changes in mood or behavior. AEDs should be prescribed in amounts consistent with good patient management practices to reduce the risk of overdose. Epilepsy and many other conditions treated with AEDs are associated with an increased risk of suicidal thoughts and behaviors. If suicidal thoughts and behaviors develop during treatment, consider whether the patient's symptoms may be related to the disorder being treated. Patients receiving AEDs for epilepsy, psychiatric disorders, or other medical conditions (eg, migraine, neuropathic pain) are at increased risk of suicidal ideation and behavior. The primary analysis included 199 placebo-controlled clinical studies with a total of 27,863 patients in the drug treatment group and 16,029 patients (5 years and older) in the placebo group. Four patients in the drug treatment group completed suicide, compared with none in the placebo group. Patients receiving AEDs had approximately twice the risk of suicidal behavior or ideation compared with patients receiving placebo (0.43% vs 0.24%, respectively; RR 1.8, 95% CI: 1.2 to 2.7 ). Compared with patients with other disorders, patients with epilepsy have a higher relative risk of suicide; however, absolute risk differences were similar in trials for epilepsy and psychiatric indications. Age is not a determining factor. An increased risk of suicidal ideation and behavior was observed between 1 and 24 weeks after initiation of treatment. However, the longer duration of treatment should not rule out a possible association with this drug, as most of the studies included in the analysis did not last longer than 24 weeks.
Dialysis, renal failure, renal failure
Gabapentin is known to be mainly excreted by the kidneys. The dose of gabapentin should be adjusted in patients with renal insufficiency or renal insufficiency undergoing hemodialysis (eg hemodialysis).
drive or operate machinery
Because gabapentin may cause drowsiness and dizziness, advise patients not to drive or operate machinery until they have sufficient experience with gabapentin to assess whether gabapentin impairs their ability to perform such tasks. A driving performance study using a prodrug of gabapentin (gabapentin etacabir) showed that gabapentin can cause significant impairment in driving. The ability of patients to assess their own driving ability and to estimate the degree of drowsiness caused by gabapentin may be imperfect. The duration of driving impairment after initiation of gabapentin therapy is unknown. Whether this disorder is related to somnolence or other effects of gabapentin is unknown.
Sudden withdrawal
Avoid abrupt discontinuation of gabapentin to reduce discontinuation and the potential for increased seizure frequency. Gradually discontinue gabapentin for at least 1 week or more. Patients taking gabapentin encarbil 600 mg or less may be discontinued without tapering.
drug abuse
When using gabapentin, carefully assess patients for a history of substance abuse and monitor for signs and symptoms of gabapentin abuse or misuse (eg, development of tolerance, self-escalation, and drug-seeking behavior). A small number of post-marketing cases of gabapentin misuse and abuse have been reported. These people were taking higher than recommended doses of gabapentin for off-label uses. Most of the individuals described in these reports had a history of multiple substance abuse or were using gabapentin to relieve withdrawal symptoms from other substances.
Chronic obstructive pulmonary disease (COPD), concomitant use with other CNS depressants, pulmonary disease, respiratory depression
In elderly patients, patients with underlying lung disease such as chronic obstructive pulmonary disease (COPD) and when coadministered with other CNS depressants, initiate gabapentin at the lowest recommended dose and monitor for symptoms of respiratory depression and sedation. Gabapentin has been reported to cause severe, life-threatening, and fatal respiratory depression. Most cases involved concomitant administration of another CNS depressant, particularly an opioid, in patients with underlying respiratory failure or advanced age. Respiratory depression, if left untreated, can lead to respiratory arrest and death. Treatment of respiratory depression should include observation, supportive measures as needed, and reduction or withdrawal of CNS depressants, including gabapentin. Reduce the dose of gabapentin used for analgesia or seizure control before stopping the drug.
Geriatrics
Ξεκινήστε τη γκαμπαπεντίνη στη χαμηλότερη συνιστώμενη δόση και παρακολουθήστε τους ηλικιωμένους ασθενείς για συμπτώματα αναπνευστικής καταστολής και καταστολής. Η γκαμπαπεντίνη έχει αναφερθεί ότι προκαλεί σοβαρή, απειλητική για τη ζωή και θανατηφόρα αναπνευστική καταστολή. Οι περισσότερες περιπτώσεις αφορούσαν την ταυτόχρονη χορήγηση άλλου κατασταλτικού του ΚΝΣ, ιδιαίτερα ενός οπιοειδούς, σε ασθενείς με υποκείμενη αναπνευστική ανεπάρκεια ή προχωρημένη ηλικία. Η αναπνευστική καταστολή, εάν αφεθεί χωρίς θεραπεία, μπορεί να οδηγήσει σε αναπνευστική διακοπή και θάνατο. Η θεραπεία της αναπνευστικής καταστολής θα πρέπει να περιλαμβάνει παρατήρηση, υποστηρικτικά μέτρα όπως απαιτείται και μείωση ή απόσυρση των κατασταλτικών του ΚΝΣ, συμπεριλαμβανομένης της γκαμπαπεντίνης. Μειώστε τη δόση της γκαμπαπεντίνης που χρησιμοποιείται για την αναλγησία ή τον έλεγχο των επιληπτικών κρίσεων πριν διακόψετε το φάρμακο. Συνολικά, κλινικές δοκιμές διαφόρων χρήσεων της γκαμπαπεντίνης και άλλη αναφερόμενη κλινική εμπειρία δεν δείχνουν γενικές διαφορές στην ασφάλεια και την αποτελεσματικότητα της γκαμπαπεντίνης σε ηλικιωμένους έναντι νεότερων ενηλίκων. Ορισμένες κλινικές δοκιμές, όπως αυτές για την επιληψία ή το σύνδρομο ανήσυχων ποδιών (RLS), δεν έχουν συμπεριλάβει αρκετά άτομα 65 ετών και άνω για να προσδιορίσουν εάν ανταποκρίνονται διαφορετικά από τα νεότερα άτομα. Η γκαμπαπεντίνη είναι γνωστό ότι απεκκρίνεται σχεδόν αποκλειστικά από τους νεφρούς και οι ασθενείς με μειωμένη νεφρική λειτουργία μπορεί να διατρέχουν μεγαλύτερο κίνδυνο ανεπιθύμητων ενεργειών σε αυτό το φάρμακο. Προσαρμόστε τη δόση με βάση την εκτιμώμενη κάθαρση κρεατινίνης· μπορεί να είναι χρήσιμο για την παρακολούθηση της νεφρικής λειτουργίας. Σύμφωνα με τα κριτήρια της Beers, τα αντισπασμωδικά φάρμακα θεωρούνται δυνητικά ακατάλληλα φάρμακα (PIM) σε ηλικιωμένους ασθενείς με ιστορικό πτώσεων ή καταγμάτων και θα πρέπει να αποφεύγονται σε αυτές τις ομάδες ασθενών εκτός από τη θεραπεία της επιληψίας και των διαταραχών της διάθεσης, επειδή τα αντισπασμωδικά φάρμακα μπορούν να προκαλέσουν αταξία και ψυχοκινητική δυσλειτουργία. Δυσλειτουργία, συγκοπή και επιπλέον πτώσεις. Εάν πρέπει να χρησιμοποιηθεί γκαμπαπεντίνη, εξετάστε το ενδεχόμενο μείωσης της χρήσης άλλων φαρμάκων που δρουν στο ΚΝΣ που αυξάνουν τον κίνδυνο πτώσεων και καταγμάτων και εφαρμόστε στρατηγικές για τη μείωση του κινδύνου πτώσεων. [63923] Ο ομοσπονδιακός νόμος για τον προϋπολογισμό του Διαμεσολαβητή (OBRA) ρυθμίζει τη χρήση φαρμάκων σε κατοίκους εγκαταστάσεων μακροχρόνιας φροντίδας· η χρήση οποιουδήποτε αντισπασμωδικού για οποιαδήποτε πάθηση θα πρέπει να βασίζεται στην αναγνώριση της πάθησης και της υποκείμενης αιτίας της. Η αποτελεσματικότητα και η ανεκτικότητα προσδιορίστηκαν με αξιολόγηση των συμπτωμάτων και χρησιμοποιήθηκαν ως βάση για προσαρμογές της δόσης στους περισσότερους ασθενείς. Τα περισσότερα αντισπασμωδικά δεν απαιτούν ούτε επιτρέπουν την παρακολούθηση των θεραπευτικών φαρμάκων. Οι συγκεντρώσεις του φαρμάκου στον ορό, εάν είναι διαθέσιμες, μπορεί να βοηθήσουν στον εντοπισμό της τοξικότητας. Παρακολουθήστε την αποτελεσματικότητα του φαρμάκου και τις παρενέργειες σε ασθενείς που λαμβάνουν θεραπεία. Τα αντισπασμωδικά μπορεί να προκαλέσουν ποικίλες παρενέργειες, μερικά μπορεί να αυξήσουν τον κίνδυνο πτώσεων. Όταν χρησιμοποιούνται αντισπασμωδικά για τον έλεγχο της συμπεριφοράς, τη σταθεροποίηση της διάθεσης ή τη θεραπεία ψυχιατρικών παθήσεων, τα ιδρύματα θα πρέπει να επιχειρούν να μειώνουν περιοδικά τη δόση του φαρμάκου ή να παρέχουν τεκμηρίωση της ιατρικής αναγκαιότητας, όπως περιγράφεται στις οδηγίες της OBRA. [60742]
Pregnant
Δεν υπάρχουν επαρκείς και καλά ελεγχόμενες μελέτες για τη γκαμπαπεντίνη σε έγκυες γυναίκες. Τα δεδομένα από μελέτες κοόρτης που περιγράφουν τους νεογνικούς κινδύνους της θεραπείας με γκαμπαπεντίνη κατά τη διάρκεια της εγκυμοσύνης είναι ασαφή. Η γκαμπαπεντίνη διασχίζει ενεργά τον πλακούντα. Σε έξι νεογνά που γεννήθηκαν από μητέρες που λάμβαναν γκαμπαπεντίνη (εύρος δόσης 900 έως 3.200 mg/ημέρα), η αναλογία συγκέντρωσης του ομφάλιου λώρου προς το πλάσμα της μητέρας κατά τον τοκετό κυμαινόταν από 1,3 έως 2,11 (μέση τιμή 1,74). Έως τις 24 ώρες μετά τον τοκετό, οι συγκεντρώσεις της γκαμπαπεντίνης στα νεογνά μειώθηκαν κατά μέσο όρο στο 27% των συγκεντρώσεων στο αίμα του ομφάλιου λώρου (εύρος, 12% έως 36%). Ένα μωρό γεννήθηκε πρόωρα στις 33 εβδομάδες, ωστόσο, όλοι οι τοκετοί ήταν χωρίς προβλήματα και όλα τα νεογέννητα γεννήθηκαν καλά στην υγεία τους. Σε μια προοπτική μελέτη κοόρτης, η συχνότητα εμφάνισης μειζόνων νεογνικών δυσπλασιών ήταν παρόμοια μεταξύ 223 εγκύων γυναικών που είχαν εκτεθεί σε γκαμπαπεντίνη και 223 εγκύων γυναικών που δεν είχαν εκτεθεί σε γκαμπαπεντίνη (4,1% στο 2,5% των εγκύων γυναικών που είχαν εκτεθεί σε γκαμπαπεντίνη, p = 0,555). Οι κύριες δυσπλασίες περιελάμβαναν 2 κοιλιακά διαφραγματικά ελαττώματα, ανεγκεφαλία, μακροκεφαλία, μικρογναθία, δέρμα Marmora, πυλωρική στένωση, αμφοτερόπλευρη ιπποειδίτιδα και κρυψορχία. Σε όλες τις περιπτώσεις σοβαρής δυσπλασίας, οι γυναίκες έλαβαν ταυτόχρονη θεραπεία με άλλα φάρμακα κατά τη διάρκεια της εγκυμοσύνης· επομένως, δεν μπορούσε να τεκμηριωθεί αιτιολογική σχέση με τη γκαμπαπεντίνη. Δεν παρουσιάστηκαν σημαντικές δυσπλασίες σε νεογνά που γεννήθηκαν από γυναίκες που έλαβαν μονοθεραπεία με γκαμπαπεντίνη κατά τη διάρκεια της εγκυμοσύνης (n = 36). Συγκρίθηκαν υψηλότερα ποσοστά πρόωρου τοκετού (10,5% έναντι 3,9%, p = 0,019), χαμηλού βάρους γέννησης (λιγότερο από 2.500 g) (10,5% έναντι 4,4%, p = 0,033) και εισαγωγής σε εντατική ή ειδική φροντίδα νεογνών με το ποσοστό των βρεφονηπιακών σταθμών μεταξύ των νεογνών που εκτέθηκαν στη γκαμπαπεντίνη σε σύγκριση με τα μη εκτεθειμένα νεογνά (38% έναντι 2,9%, p<0,001). Υπήρχαν δύο πιθανά νεογνικά δυσπροσαρμοστικά σύνδρομα σε νεογνά που εκτέθηκαν στη γκαμπαπεντίνη στο τέλος της εγκυμοσύνης αλλά όχι σε βρέφη που δεν εκτέθηκαν στη γκαμπαπεντίνη· αυτά τα δύο νεογνά εκτέθηκαν επίσης σε άλλα ψυχοφάρμακα. Σε μια ομάδα 39 γυναικών που εκτέθηκαν στη γκαμπαπεντίνη κατά τη διάρκεια του πρώτου τριμήνου (97%) και καθ' όλη τη διάρκεια της εγκυμοσύνης (81,8%), 3 από τις 44 γεννήσεις ζωντανών γεννήσεων είχαν δυσμορφία. Τα νεογνά που εκτέθηκαν σε γκαμπαπεντίνη και βαλπροϊκό οξύ έχουν αναφερθεί ότι ανέπτυξαν υποσπαδία, νεογνά που εκτέθηκαν σε γκαμπαπεντίνη και φαινοβαρβιτάλη για να αναπτύξουν νεφρική ανεπάρκεια και νεογνά που εκτέθηκαν σε γκαμπαπεντίνη και λαμοτριγίνη για να αναπτύξουν μια ελαφρά παραμόρφωση του αριστερού έξω ακουστικού πόρου και μια μικρή ετικέτα δέρματος 2 A . Επειδή κατά τη διάρκεια αυτών των εγκυμοσύνων εμφανίστηκαν πολλαπλές εκθέσεις σε αντισπασμωδικά φάρμακα, δεν ήταν δυνατό να τεκμηριωθεί αιτιολογική σχέση με τη γκαμπαπεντίνη. Έντεκα ασθενείς που έλαβαν μονοθεραπεία με γκαμπαπεντίνη κατά τη διάρκεια της εγκυμοσύνης δεν εμφάνισαν δυσπλασίες. Σε μελέτες σε ζώα, η γκαμπαπεντίνη ήταν εμβρυοτοξική σε δόσεις 1 έως 4 φορές τη μέγιστη συνιστώμενη δόση για τον άνθρωπο (σε βάση mg/m2) κατά τη διάρκεια της οργανογένεσης. Όταν σε έγκυα ποντίκια χορηγήθηκε από το στόμα γκαμπαπεντίνη (500, 1.000 ή 3.000 mg/kg/ημέρα) κατά τη διάρκεια της οργανογένεσης, η σκελετική οστεοποίηση καθυστέρησε στο κρανίο, τα άκρα και τους σπονδύλους. Το NOEAD (500 mg/kg/ημέρα) ήταν κάτω από τη μέγιστη συνιστώμενη ανθρώπινη δόση (MRHD) των 3.600 mg/kg με βάση την επιφάνεια του σώματος (mg/m2). Σε μελέτες σε αρουραίους που έλαβαν από του στόματος γκαμπαπεντίνη (500 έως 2.000 mg/kg/ημέρα), παρατηρήθηκε αυξημένη συχνότητα εμφάνισης υδροουρητή και/ή υδρονέφρωσης σε όλες τις δόσεις που δοκιμάστηκαν. Όταν σε έγκυα κουνέλια χορηγήθηκε από το στόμα γκαμπαπεντίνη (60, 300 ή 1.500 mg/kg) κατά τη διάρκεια της οργανογένεσης, υπήρξε επίσης αυξημένη συχνότητα απώλειας εμβρύου σε όλες τις δόσεις που εξετάστηκαν. Υπάρχει ένα Μητρώο Έκθεσης Κύησης που παρακολουθεί τα αποτελέσματα σε εγκύους ασθενείς που εκτίθενται στη γκαμπαπεντίνη· για πληροφορίες σχετικά με το μητρώο, επισκεφθείτε τη διεύθυνση www.aedpregnancyregistry.org ή καλέστε στο 1-888-233-2334.
Breastfeeding
Gabapentin is excreted in human milk, however, it is unknown whether gabapentin derived from gabapentin etacab is excreted in human milk. The maximum dose to which a nursing infant can be exposed to gabapentin is approximately 1 mg/kg/day. There are no data on the effects of gabapentin on nursing infants or milk production. Consider the developmental and health benefits of breastfeeding, the mother's clinical need for gabapentin, and any adverse effects of gabapentin or the mother's underlying condition on the nursing infant. Use gabapentin in nursing women only if the benefits clearly outweigh the risks. [27986] [43322][43905] Infant doses of gabapentin excreted in breast milk were examined in 4 infants, 3 infants 2 to 3 weeks of age and 1 infant approximately 3 months of age. The mean daily maternal dose of gabapentin was 1,575 mg (range: 600 to 2,100 mg/day). Obtain a single sample of milk approximately 10 to 15 hours after the last dose. Assuming a breast milk consumption of 150 mL/kg/day, the relevant infant dose of gabapentin is estimated to be 0.2 to 1.3 mg/kg/day, approximately 1.3% to 3.8% of the weight-adjusted maternal dose . Two to three weeks postpartum, plasma gabapentin concentrations were detectable and within the normal quantitative range in 2 infants and undetectable in 1 infant. At 3 months, another infant had gabapentin plasma concentrations below the normal quantitative range. No side effects were reported. [62571]
Unwanted actions
serious
Suicidal ideation/delay/0-0.1
Unknown teratogenicity/delay/incidence
Angioedema / rapid / unknown incidence
Stevens-Johnson syndrome/delay/effect unknown
Anaphylactoid/rapid/unknown effect
Erythema multiforme / late onset / unknown incidence
Drug reaction with eosinophilia and systemic symptoms (DRESS)/Delayed/Unknown effect
Rhabdomyolysis/late onset/incidence unknown
ease
Disorder/Delay/3.0-13.0
Peripheral edema / Delayed / 0-8.0
Nystagmus / Latency / 8.0-8.0
enmity/early/5.2-8.0
Blurred vision/early/0-5.0
Constipation/Delay/1.4-4.0
Amblyopia/Retardation/3.0-4.0
Cognitive Impairment/Early/1.7-2.7
Amnesia/Latency/2.0-2.0
Dysarthria/Retardation/2.0-2.0
Peripheral Vasodilation / Rapid / 1.1-1.1
Dystonic response / delayed / 0.1-1.0
Conjunctivitis / Delayed / 1.0-1.0
Hyperglycemia / Delayed / 1.0-1.0
Withdraw/Early/0-1.0
Tolerance/Delay/0-1.0
Chorioacetosis / Latent period / 0-0.1
depression/retardation/1.8
unintended motion/delay/0.1
chaos/early/1.0
memory impairment/lag/1.0
hepatitis / delayed / 1.0
Dyspnea/Early/1.0
Hypertension/Early/1.0
Dehydration/delay/unknown effect
Jaundice/delay/unknown effect
Hyponatremia/delay/unknown effect
Eosinophilia/delay/unknown effect
Bullous rash/early stage/incidence unknown
Respiratory depression/rapid/unknown effect
Moderate
Dizziness/Early/3.0-30.0
Sleepiness / Early / 4.5-27.0
Headache/Early/0-15.0
Fatigue/Early/3.0-11.0
Weakness/Delay/4.0-10.0
Nausea/Early/4.0-8.0
Vomiting/Early/3.0-8.0
Insomnia / Early / 0-7.0
horror/early/0-7.0
Diarrhea/early/3.3-6.0
Diplopia/Early/1.0-6.0
Weight Gain/Delay/2.0-5.0
Dormancy/Early/0-2.0
Decreased/delayed libido/0-2.0
back pain/delay/1.0
nervous/retarded/2.0
stun/early/1.4
Appetite Stim/Delay/2.0
Dyspepsia/Early/1.0
Anorexia/Delay/2.0
Xerostomia / Early / 2.0
flatulence / early / 2.0
cough/lag/2.0
Rhinitis / Early / 1.0
infection/delay/1.0
Pharyngitis/Delay/1.0
Rash/Early/1.0
Emotional instability/early stage/unknown impact
Agitation/early stage/effect unknown
Fever/early stage/incidence unknown
Skin irritation/early/unknown effect
drug interactions
Acetaminophen, Aspirin, Diphenhydramine:(Moderate) Monitor for excessive sedation and somnolence during coadministration of diphenhydramine and gabapentin. Concomitant use may cause further central nervous system depression.
Acetaminophen, Caffeine, Dihydrocodeine:Concomitant use of (major) opioid agonists with gabapentin may cause excessive sedation, drowsiness and respiratory depression. Avoid prescribing opioid cough suppressants in patients receiving gabapentin. Only use opioid analgesics in combination with gabapentin and only in patients with insufficient alternative treatment options. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Use the lowest effective dose and shortest duration of treatment necessary to achieve the desired clinical effect. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Acetaminophen, Caffeine, Pyramine:(Moderate) Monitor for excessive sedation and somnolence during coadministration of pyrilamine and gabapentin. Concomitant use may cause further central nervous system depression.
Acetaminophen, Chlorpheniramine:(Moderate) Monitor for excessive sedation and somnolence during coadministration of chlorpheniramine and gabapentin. Concomitant use may cause further central nervous system depression.
Acetaminophen, Chlorpheniramine, Dextromethorphan:(Moderate) Monitor for excessive sedation and somnolence during coadministration of chlorpheniramine and gabapentin. Concomitant use may cause further central nervous system depression.
Acetaminophen, Chlorpheniramine, Dextromethorphan, Phenylephrine:(Moderate) Monitor for excessive sedation and somnolence during coadministration of chlorpheniramine and gabapentin. Concomitant use may cause further central nervous system depression.
Acetaminophen, Chlorpheniramine, Dextromethorphan, Pseudoephedrine:(Moderate) Monitor for excessive sedation and somnolence during coadministration of chlorpheniramine and gabapentin. Concomitant use may cause further central nervous system depression.
Acetaminophen, Chlorpheniramine, Phenylephrine:(Moderate) Monitor for excessive sedation and somnolence during coadministration of chlorpheniramine and gabapentin. Concomitant use may cause further central nervous system depression.
Acetaminophen, Codeine:Concomitant use of (major) opioid agonists with gabapentin may cause excessive sedation, drowsiness and respiratory depression. Avoid prescribing opioid cough suppressants in patients receiving gabapentin. Only use opioid analgesics in combination with gabapentin and only in patients with insufficient alternative treatment options. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Use the lowest effective dose and shortest duration of treatment necessary to achieve the desired clinical effect. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Acetaminophen, Dextromethorphan, Doxylamine:(Moderate) Monitor for excessive sedation and somnolence during coadministration of doxylamine and gabapentin. Concomitant use may cause further central nervous system depression.
Acetaminophen, Diphenhydramine:(Moderate) Monitor for excessive sedation and somnolence during coadministration of diphenhydramine and gabapentin. Concomitant use may cause further central nervous system depression.
Acetaminophen, Hydrocodone:Concomitant use of (major) opioid agonists with gabapentin may cause excessive sedation, drowsiness and respiratory depression. Avoid prescribing opioid cough suppressants in patients receiving gabapentin. Only use opioid analgesics in combination with gabapentin and only in patients with insufficient alternative treatment options. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Use the lowest effective dose and shortest duration of treatment necessary to achieve the desired clinical effect. In addition, coadministration of gabapentin with hydrocodone decreased hydrocodone exposure in a dose-dependent manner. Consider possible reduction in hydrocodone exposure and effects when starting or stopping gabapentin in patients taking hydrocodone. After 125 mg gabapentin (n = 48), hydrocodone (10 mg, n = 50) Cmax and AUC values decreased by 3% to 4%, respectively, and after 500 mg gabapentin, Cmax and AUC values decreased by 21 % to 22%, respectively % . Hydrocodone increased gabapentin AUC by 14%. The extent of the interaction and the mechanism of interaction at other doses are unknown.
Acetaminophen, Oxycodone:Concomitant use of (major) opioid agonists with gabapentin may cause excessive sedation, drowsiness and respiratory depression. Only use opioid analgesics in combination with gabapentin and only in patients with insufficient alternative treatment options. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Use the lowest effective dose and shortest duration of treatment necessary to achieve the desired clinical effect. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Acetaminophen, Pamabromide, Pyrilamine:(Moderate) Monitor for excessive sedation and somnolence during coadministration of pyrilamine and gabapentin. Concomitant use may cause further central nervous system depression.
Aclastin, Pseudoephedrine:(Primarily) avoid concomitant use of avastatin and gabapentin due to the risk of superimposed CNS depression. If concomitant use cannot be avoided, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of sedation and somnolence during coadministration. Educate patients about the risks and symptoms of excessive CNS depression.
Alfentanil:Concomitant use of (major) opioid agonists with gabapentin may cause excessive sedation, drowsiness and respiratory depression. The use of alfentanil in combination with gabapentin should be limited to patients for whom alternative treatment options are inadequate. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Use the lowest effective dose and shortest duration of treatment necessary to achieve the desired clinical effect. The magnitude and duration of the central nervous system and cardiovascular effects of alfentanil may be enhanced. Monitor patients for hypotension or prolonged respiratory depression and sedation. The respiratory depressant effects of alfentanil may outlast the measured analgesic effects; consider the total dose of all opioid agonists before ordering opioid analgesics during recovery from anesthesia. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Alprazolam:Concomitant use of (mainly) benzodiazepines with gabapentin may cause excessive sedation, drowsiness and respiratory depression. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Aluminum hydroxide:(Moderate) Gabapentin should be taken at least 2 hours after taking an antacid. Antacids have been shown to reduce the oral bioavailability of gabapentin by approximately 20%. When gabapentin is administered 2 hours after antacids, bioavailability is reduced by approximately 5%.
Aluminum hydroxide, magnesium carbonate:(Moderate) Gabapentin should be taken at least 2 hours after taking an antacid. Antacids have been shown to reduce the oral bioavailability of gabapentin by approximately 20%. When gabapentin is administered 2 hours after antacids, bioavailability is reduced by approximately 5%.
Aluminum Hydroxide, Magnesium Hydroxide:(Moderate) Gabapentin should be taken at least 2 hours after taking an antacid. Antacids have been shown to reduce the oral bioavailability of gabapentin by approximately 20%. When gabapentin is administered 2 hours after antacids, bioavailability is reduced by approximately 5%.
Aluminum Hydroxide, Magnesium Hydroxide, Simethicone:(Moderate) Gabapentin should be taken at least 2 hours after taking an antacid. Antacids have been shown to reduce the oral bioavailability of gabapentin by approximately 20%. When gabapentin is administered 2 hours after antacids, bioavailability is reduced by approximately 5%.
Aluminum Hydroxide, Magnesium Trisilicate:(Moderate) Gabapentin should be taken at least 2 hours after taking an antacid. Antacids have been shown to reduce the oral bioavailability of gabapentin by approximately 20%. When gabapentin is administered 2 hours after antacids, bioavailability is reduced by approximately 5%.
Amobarbital:Concomitant use of (mainly) barbiturates with gabapentin may cause excessive sedation, drowsiness and respiratory depression. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Amoxapine:(Major) Initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of sedation and somnolence when gabapentin and amoxapine are coadministered. Concomitant use of gabapentin and amoxapine may result in cumulative central nervous system depression. Educate patients about the risks and symptoms of excessive CNS depression.
Antacids:(Moderate) Gabapentin should be taken at least 2 hours after taking an antacid. Antacids have been shown to reduce the oral bioavailability of gabapentin by approximately 20%. When gabapentin is administered 2 hours after antacids, bioavailability is reduced by approximately 5%.
Apomorphine:Start gabapentin at the lowest recommended dose (primarily) and monitor patients for symptoms of sedation and somnolence when coadministering gabapentin and apomorphine. Concomitant use of gabapentin and apomorphine may result in cumulative central nervous system depression. Educate patients about the risks and symptoms of excessive CNS depression. Dopaminergic drugs such as apomorphine have also been associated with sleepiness during activities of daily living (such as driving), which in some cases has led to accidents. Reassess patients periodically throughout treatment for somnolence or hypersomnia, especially since somnolence or hypersomnia may occur long after initiation of therapy.
Aripiprazole:(Moderate) Monitor for respiratory depression and sedation during coadministration of aripiprazole and gabapentin; consider starting gabapentin at a low dose. Concomitant administration increases the risk of central nervous system depression.
Asenapine:(Moderate) Monitor for excessive sedation and somnolence during coadministration of asenapine and gabapentin. Concomitant use may cause further central nervous system depression.
Aspirin, ASA, butalbital, caffeine:Concomitant use of (mainly) barbiturates with gabapentin may cause excessive sedation, drowsiness and respiratory depression. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Aspirin, ASA, caffeine, orphenadine:(Major) Initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of sedation and somnolence during coadministration of gabapentin and orphenadine. Coadministration of gabapentin and orphenadine may result in cumulative central nervous system depression. Educate patients about the risks and symptoms of excessive CNS depression.
Aspirin, ASA, Carisoprodol:(Major) Initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of sedation and somnolence when coadministering gabapentin and carisoprodol. Concomitant use of gabapentin and carisoprodol may cause cumulative central nervous system depression. Educate patients about the risks and symptoms of excessive CNS depression.
Aspirin, ASA, Carisoprodol, Codeine:Concomitant use of (major) opioid agonists with gabapentin may cause excessive sedation, drowsiness and respiratory depression. Avoid prescribing opioid cough suppressants in patients receiving gabapentin. Only use opioid analgesics in combination with gabapentin and only in patients with insufficient alternative treatment options. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Use the lowest effective dose and shortest duration of treatment necessary to achieve the desired clinical effect. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression. (Major) Initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of sedation and somnolence when coadministering gabapentin and carisoprodol. Concomitant use of gabapentin and carisoprodol may cause cumulative central nervous system depression. Educate patients about the risks and symptoms of excessive CNS depression.
Aspirin, ASA, Citric acid, Sodium bicarbonate:(Moderate) Antacids have been shown to decrease the oral bioavailability of gabapentin by approximately 20%. When gabapentin is administered 2 hours after antacids, bioavailability is reduced by approximately 5%. It is recommended to take gabapentin at least 2 hours after taking antacids to avoid significant interactions.
Aspirin, ASA, Oxycodone:Concomitant use of (major) opioid agonists with gabapentin may cause excessive sedation, drowsiness and respiratory depression. Only use opioid analgesics in combination with gabapentin and only in patients with insufficient alternative treatment options. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Use the lowest effective dose and shortest duration of treatment necessary to achieve the desired clinical effect. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
atropine:(Moderate) Monitor for excessive sedation and somnolence during coadministration of atropine and gabapentin. Concomitant use may cause further central nervous system depression.
Atropine, Benzoic Acid, Hyoscyamine, Urotropin, Methylene Blue, Phenyl Salicylate:(Moderate) Monitor for excessive sedation and somnolence during coadministration of atropine and gabapentin. Concomitant use may cause further central nervous system depression.
Atropine, Diphenoxin:(Moderate) Monitor for excessive sedation and somnolence during coadministration of atropine and gabapentin. Concomitant use may cause further central nervous system depression.
Atropine, ephenonium chloride:(Moderate) Monitor for excessive sedation and somnolence during coadministration of atropine and gabapentin. Concomitant use may cause further central nervous system depression.
Azelastine:(Major) Initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of sedation and somnolence when coadministering gabapentin and azelastine. Concomitant use of gabapentin and azelastine may lead to cumulative central nervous system depression. Educate patients about the risks and symptoms of excessive CNS depression.
Azelastine, Fluticasone:(Major) Initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of sedation and somnolence when coadministering gabapentin and azelastine. Concomitant use of gabapentin and azelastine may lead to cumulative central nervous system depression. Educate patients about the risks and symptoms of excessive CNS depression.
Baclofen:(Primary) Initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of sedation and somnolence during coadministration of gabapentin and baclofen. Concomitant use of gabapentin and baclofen may result in cumulative central nervous system depression. Educate patients about the risks and symptoms of excessive CNS depression.
Barbiturates:Concomitant use of (mainly) barbiturates with gabapentin may cause excessive sedation, drowsiness and respiratory depression. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Belladonna, Opium:Concomitant use of (major) opioid agonists with gabapentin may cause excessive sedation, drowsiness and respiratory depression. Only use opioid analgesics in combination with gabapentin and only in patients with insufficient alternative treatment options. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Use the lowest effective dose and shortest duration of treatment necessary to achieve the desired clinical effect. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
phenhydrocodone, acetaminophen:Concomitant use of (major) opioid agonists with gabapentin may cause excessive sedation, drowsiness and respiratory depression. Only use opioid analgesics in combination with gabapentin and only in patients with insufficient alternative treatment options. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Use the lowest effective dose and shortest duration of treatment necessary to achieve the desired clinical effect. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Benzodiazepines:Concomitant use of (mainly) benzodiazepines with gabapentin may cause excessive sedation, drowsiness and respiratory depression. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Bripiprazole:(Major) Initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of sedation and somnolence during coadministration of gabapentin and brepiprazole. Concomitant use of gabapentin and brepiprazole may lead to cumulative central nervous system depression. Educate patients about the risks and symptoms of excessive CNS depression.
Brompheniramine:(Moderate) Monitor for excessive sedation and somnolence during coadministration of brompheniramine and gabapentin. Concomitant use may cause further central nervous system depression.
Brompheniramine, Dextromethorphan, Guaifenesin:(Moderate) Monitor for excessive sedation and somnolence during coadministration of brompheniramine and gabapentin. Concomitant use may cause further central nervous system depression.
Brompheniramine, Dextromethorphan, Phenylephrine:(Moderate) Monitor for excessive sedation and somnolence during coadministration of brompheniramine and gabapentin. Concomitant use may cause further central nervous system depression.
bromephramine, phenylephrine:(Moderate) Monitor for excessive sedation and somnolence during coadministration of brompheniramine and gabapentin. Concomitant use may cause further central nervous system depression.
Brompheniramine, Pseudoephedrine:(Moderate) Monitor for excessive sedation and somnolence during coadministration of brompheniramine and gabapentin. Concomitant use may cause further central nervous system depression.
Bromopheniramine, Pseudoephedrine, Dextromethorphan:(Moderate) Monitor for excessive sedation and somnolence during coadministration of brompheniramine and gabapentin. Concomitant use may cause further central nervous system depression.
Buprenorphine:Concomitant use of (mainly) buprenorphine with gabapentin may cause excessive sedation, drowsiness, and respiratory depression. Limit the use of buprenorphine in combination with gabapentin only to patients for whom alternative treatment options are inadequate. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Use the lowest effective dose and shortest duration of treatment necessary to achieve the desired clinical effect. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Buprenorphine, Naloxone:Concomitant use of (mainly) buprenorphine with gabapentin may cause excessive sedation, drowsiness, and respiratory depression. Limit the use of buprenorphine in combination with gabapentin only to patients for whom alternative treatment options are inadequate. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Use the lowest effective dose and shortest duration of treatment necessary to achieve the desired clinical effect. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Butabarbital:Concomitant use of (mainly) barbiturates with gabapentin may cause excessive sedation, drowsiness and respiratory depression. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
butalbital, acetaminophen:Concomitant use of (mainly) barbiturates with gabapentin may cause excessive sedation, drowsiness and respiratory depression. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Butalbital, Acetaminophen, Caffeine:Concomitant use of (mainly) barbiturates with gabapentin may cause excessive sedation, drowsiness and respiratory depression. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Butalbital, Acetaminophen, Caffeine, Codeine:Concomitant use of (mainly) barbiturates with gabapentin may cause excessive sedation, drowsiness and respiratory depression. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression. Concomitant use of (major) opioid agonists with gabapentin may cause excessive sedation, drowsiness and respiratory depression. Avoid prescribing opioid cough suppressants in patients receiving gabapentin. Only use opioid analgesics in combination with gabapentin and only in patients with insufficient alternative treatment options. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Use the lowest effective dose and shortest duration of treatment necessary to achieve the desired clinical effect. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Butalbital, Aspirin, Caffeine, Codeine:Concomitant use of (mainly) barbiturates with gabapentin may cause excessive sedation, drowsiness and respiratory depression. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression. Concomitant use of (major) opioid agonists with gabapentin may cause excessive sedation, drowsiness and respiratory depression. Avoid prescribing opioid cough suppressants in patients receiving gabapentin. Only use opioid analgesics in combination with gabapentin and only in patients with insufficient alternative treatment options. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Use the lowest effective dose and shortest duration of treatment necessary to achieve the desired clinical effect. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Butorphanol:Concomitant use of (mainly) butorphanol with gabapentin may cause excessive sedation, drowsiness, and respiratory depression. The use of butorphanol in combination with gabapentin is limited to patients for whom alternative treatment options are inadequate. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Use the lowest effective dose and shortest duration of treatment necessary to achieve the desired clinical effect. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Calcium carbonate:(Moderate) antacids (eg aluminum hydroxide, magnesium hydroxide) have been shown to decrease the oral bioavailability of gabapentin by approximately 20%. When gabapentin is administered 2 hours after antacids, bioavailability is reduced by approximately 5%. It is recommended to take gabapentin at least 2 hours after taking antacids to avoid significant interactions.
Calcium Carbonate, Famotidine, Magnesium Hydroxide:(Moderate) antacids (eg aluminum hydroxide, magnesium hydroxide) have been shown to decrease the oral bioavailability of gabapentin by approximately 20%. When gabapentin is administered 2 hours after antacids, bioavailability is reduced by approximately 5%. It is recommended to take gabapentin at least 2 hours after taking antacids to avoid significant interactions.
Calcium Carbonate, Magnesium Hydroxide:(Moderate) antacids (eg aluminum hydroxide, magnesium hydroxide) have been shown to decrease the oral bioavailability of gabapentin by approximately 20%. When gabapentin is administered 2 hours after antacids, bioavailability is reduced by approximately 5%. It is recommended to take gabapentin at least 2 hours after taking antacids to avoid significant interactions.
Calcium Carbonate, Magnesium Hydroxide, Simethicone:(Moderate) antacids (eg aluminum hydroxide, magnesium hydroxide) have been shown to decrease the oral bioavailability of gabapentin by approximately 20%. When gabapentin is administered 2 hours after antacids, bioavailability is reduced by approximately 5%. It is recommended to take gabapentin at least 2 hours after taking antacids to avoid significant interactions.
Calcium Carbonate, Risedronate Sodium:(Moderate) antacids (eg aluminum hydroxide, magnesium hydroxide) have been shown to decrease the oral bioavailability of gabapentin by approximately 20%. When gabapentin is administered 2 hours after antacids, bioavailability is reduced by approximately 5%. It is recommended to take gabapentin at least 2 hours after taking antacids to avoid significant interactions.
Calcium Carbonate, Simethicone:(Moderate) antacids (eg aluminum hydroxide, magnesium hydroxide) have been shown to decrease the oral bioavailability of gabapentin by approximately 20%. When gabapentin is administered 2 hours after antacids, bioavailability is reduced by approximately 5%. It is recommended to take gabapentin at least 2 hours after taking antacids to avoid significant interactions.
Calcium, Magnesium, Potassium, Sodium oxalate:Concomitant use of (mainly) sodium oxybate with gabapentin may cause excessive sedation, drowsiness, and respiratory depression. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Calcium, Vitamin D:(Moderate) antacids (eg aluminum hydroxide, magnesium hydroxide) have been shown to decrease the oral bioavailability of gabapentin by approximately 20%. When gabapentin is administered 2 hours after antacids, bioavailability is reduced by approximately 5%. It is recommended to take gabapentin at least 2 hours after taking antacids to avoid significant interactions.
Cannabidiol:(Moderate) Monitor for excessive sedation and somnolence during coadministration of cannabidiol and gabapentin. Concomitant use may cause further central nervous system depression.
Capsaicin, Metaxalone:(Major) Initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of sedation and somnolence during coadministration of gabapentin and metaxalone. Concomitant use of gabapentin and metaxalone may result in cumulative central nervous system depression. Educate patients about the risks and symptoms of excessive CNS depression.
Carbidopa, Levodopa:(Major) Initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of sedation and somnolence during coadministration of gabapentin and levodopa. Concomitant use of gabapentin and levodopa may lead to cumulative central nervous system depression. Educate patients about the risks and symptoms of excessive CNS depression. Dopaminergic drugs such as levodopa have also been linked to sleepiness during activities of daily living (such as driving), which in some cases has led to accidents. Reassess patients periodically throughout treatment for somnolence or hypersomnia, especially since somnolence or hypersomnia may occur long after initiation of therapy.
Carbidopa, Levodopa, Entacapone:(Major) Initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of sedation and somnolence when coadministering gabapentin and entacapone. Concomitant use of gabapentin and entacapone may lead to cumulative central nervous system depression. Educate patients about the risks and symptoms of excessive CNS depression. Dopaminergic drugs such as entacapone have also been associated with sleepiness during activities of daily living (such as driving), which in some cases has led to accidents. Reassess patients periodically throughout treatment for somnolence or hypersomnia, especially since somnolence or hypersomnia may occur long after initiation of therapy. (Major) Initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of sedation and somnolence during coadministration of gabapentin and levodopa. Concomitant use of gabapentin and levodopa may lead to cumulative central nervous system depression. Educate patients about the risks and symptoms of excessive CNS depression. Dopaminergic drugs such as levodopa have also been linked to sleepiness during activities of daily living (such as driving), which in some cases has led to accidents. Reassess patients periodically throughout treatment for somnolence or hypersomnia, especially since somnolence or hypersomnia may occur long after initiation of therapy.
Carbenzamine:(Moderate) Monitor for excessive sedation and somnolence during coadministration of carbinoxamine and gabapentin. Concomitant use may cause further central nervous system depression.
Carbinoxamine, Dextromethorphan, Pseudoephedrine:(Moderate) Monitor for excessive sedation and somnolence during coadministration of carbinoxamine and gabapentin. Concomitant use may cause further central nervous system depression.
Carbinoxamine, Phenylephrine:(Moderate) Monitor for excessive sedation and somnolence during coadministration of carbinoxamine and gabapentin. Concomitant use may cause further central nervous system depression.
Carbinoxamine, Pseudoephedrine:(Moderate) Monitor for excessive sedation and somnolence during coadministration of carbinoxamine and gabapentin. Concomitant use may cause further central nervous system depression.
Cariprazine:(Moderate) Monitor for excessive sedation and somnolence during coadministration of cariprazine and gabapentin. Concomitant use may cause further central nervous system depression.
Kalipunto:(Major) Initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of sedation and somnolence when coadministering gabapentin and carisoprodol. Concomitant use of gabapentin and carisoprodol may cause cumulative central nervous system depression. Educate patients about the risks and symptoms of excessive CNS depression.
Celecoxib, Tramadol:Concomitant use of (major) opioid agonists with gabapentin may cause excessive sedation, drowsiness and respiratory depression. Only use opioid analgesics in combination with gabapentin and only in patients with insufficient alternative treatment options. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Use the lowest effective dose and shortest duration of treatment necessary to achieve the desired clinical effect. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Sinofibrate:(Moderate) Monitor for excessive sedation and somnolence during coadministration of quinofibrate and gabapentin. Concomitant use may cause further central nervous system depression.
Cetirizine:(Moderate) Monitor for respiratory depression and sedation during coadministration of cetirizine and gabapentin; consider starting gabapentin at a low dose. Concomitant administration increases the risk of central nervous system depression.
Cetirizine, Pseudoephedrine:(Moderate) Monitor for respiratory depression and sedation during coadministration of cetirizine and gabapentin; consider starting gabapentin at a low dose. Concomitant administration increases the risk of central nervous system depression.
Chlorophenol, Dexbromopheniramine:(Moderate) Monitor for excessive sedation and somnolence during coadministration of dexbromopheniramine and gabapentin. Concomitant use may cause further central nervous system depression.
Chlorophenol, Dexchlorpheniramine, Pseudoephedrine:(Moderate) Monitor for excessive sedation and somnolence during coadministration of dexchlorpheniramine and gabapentin. Concomitant use may cause further central nervous system depression.
Chlorocyclazine:(Moderate) Monitor for excessive sedation and somnolence during coadministration of chlorcyclazine and gabapentin. Concomitant use may cause further central nervous system depression.
Chlorodiazepoxide:Concomitant use of (mainly) benzodiazepines with gabapentin may cause excessive sedation, drowsiness and respiratory depression. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Chlordiazepoxide, Amitriptyline:Concomitant use of (mainly) benzodiazepines with gabapentin may cause excessive sedation, drowsiness and respiratory depression. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Chlorodiazepoxide, Ammonium Chloride:Concomitant use of (mainly) benzodiazepines with gabapentin may cause excessive sedation, drowsiness and respiratory depression. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
chlorpheniramine:(Moderate) Monitor for excessive sedation and somnolence during coadministration of chlorpheniramine and gabapentin. Concomitant use may cause further central nervous system depression.
Chlorpheniramine, Codeine:Concomitant use of (major) opioid agonists with gabapentin may cause excessive sedation, drowsiness and respiratory depression. Avoid prescribing opioid cough suppressants in patients receiving gabapentin. Only use opioid analgesics in combination with gabapentin and only in patients with insufficient alternative treatment options. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Use the lowest effective dose and shortest duration of treatment necessary to achieve the desired clinical effect. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression. (Moderate) Monitor for excessive sedation and somnolence during coadministration of chlorpheniramine and gabapentin. Concomitant use may cause further central nervous system depression.
Chlorpheniramine, Dextromethorphan:(Moderate) Monitor for excessive sedation and somnolence during coadministration of chlorpheniramine and gabapentin. Concomitant use may cause further central nervous system depression.
Chlorpheniramine, Dextromethorphan, Phenylephrine:(Moderate) Monitor for excessive sedation and somnolence during coadministration of chlorpheniramine and gabapentin. Concomitant use may cause further central nervous system depression.
Chlorpheniramine, Dextromethorphan, Pseudoephedrine:(Moderate) Monitor for excessive sedation and somnolence during coadministration of chlorpheniramine and gabapentin. Concomitant use may cause further central nervous system depression.
Chlorpheniramine, Dihydrocodeine, Phenylephrine:Concomitant use of (major) opioid agonists with gabapentin may cause excessive sedation, drowsiness and respiratory depression. Avoid prescribing opioid cough suppressants in patients receiving gabapentin. Only use opioid analgesics in combination with gabapentin and only in patients with insufficient alternative treatment options. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Use the lowest effective dose and shortest duration of treatment necessary to achieve the desired clinical effect. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression. (Moderate) Monitor for excessive sedation and somnolence during coadministration of chlorpheniramine and gabapentin. Concomitant use may cause further central nervous system depression.
Chlorpheniramine, Hydrocodone:Concomitant use of (major) opioid agonists with gabapentin may cause excessive sedation, drowsiness and respiratory depression. Avoid prescribing opioid cough suppressants in patients receiving gabapentin. Only use opioid analgesics in combination with gabapentin and only in patients with insufficient alternative treatment options. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Use the lowest effective dose and shortest duration of treatment necessary to achieve the desired clinical effect. In addition, coadministration of gabapentin with hydrocodone decreased hydrocodone exposure in a dose-dependent manner. Consider possible reduction in hydrocodone exposure and effects when starting or stopping gabapentin in patients taking hydrocodone. After 125 mg gabapentin (n = 48), hydrocodone (10 mg, n = 50) Cmax and AUC values decreased by 3% to 4%, respectively, and after 500 mg gabapentin, Cmax and AUC values decreased by 21 % to 22%, respectively % . Hydrocodone increased gabapentin AUC by 14%. The extent of the interaction and the mechanism of interaction at other doses are unknown. (Moderate) Monitor for excessive sedation and somnolence during coadministration of chlorpheniramine and gabapentin. Concomitant use may cause further central nervous system depression.
Chlorpheniramine, Ibuprofen, Pseudoephedrine:(Moderate) Monitor for excessive sedation and somnolence during coadministration of chlorpheniramine and gabapentin. Concomitant use may cause further central nervous system depression.
Chlorpheniramine, Phenylephrine:(Moderate) Monitor for excessive sedation and somnolence during coadministration of chlorpheniramine and gabapentin. Concomitant use may cause further central nervous system depression.
Chlorpheniramine, pseudoephedrine:(Moderate) Monitor for excessive sedation and somnolence during coadministration of chlorpheniramine and gabapentin. Concomitant use may cause further central nervous system depression.
Chlorpromazine:(Major) Initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of sedation and somnolence during coadministration of gabapentin and chlorpromazine. Concomitant use of gabapentin and chlorpromazine may result in cumulative central nervous system depression. Educate patients about the risks and symptoms of excessive CNS depression.
Chlorthalidone, Clonidine:(Major) Initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of sedation and somnolence when coadministering gabapentin and clonidine. Concomitant use of gabapentin and clonidine may result in cumulative central nervous system depression. Educate patients about the risks and symptoms of excessive CNS depression.
Chlorzoxazone:(Major) Initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of sedation and somnolence when coadministering gabapentin and chlorzoxazone. Concomitant use of gabapentin and chlorzoxazone may result in cumulative central nervous system depression. Educate patients about the risks and symptoms of excessive CNS depression.
Clemastine:(Moderate) Monitor for excessive sedation and somnolence during coadministration of clemastine and gabapentin. Concomitant use may cause further central nervous system depression.
Clovazami:Concomitant use of (mainly) clobazam with gabapentin may cause excessive sedation, drowsiness and respiratory depression. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Clonazepam:Concomitant use of (mainly) benzodiazepines with gabapentin may cause excessive sedation, drowsiness and respiratory depression. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Clonidine:(Major) Initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of sedation and somnolence when coadministering gabapentin and clonidine. Concomitant use of gabapentin and clonidine may result in cumulative central nervous system depression. Educate patients about the risks and symptoms of excessive CNS depression.
Chloracilate:Concomitant use of (mainly) benzodiazepines with gabapentin may cause excessive sedation, drowsiness and respiratory depression. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Clozapine:(Major) Initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of sedation and somnolence when coadministering gabapentin and clozapine. Concomitant use of gabapentin and clozapine may result in cumulative central nervous system depression. Educate patients about the risks and symptoms of excessive CNS depression.
Codeine:Concomitant use of (major) opioid agonists with gabapentin may cause excessive sedation, drowsiness and respiratory depression. Avoid prescribing opioid cough suppressants in patients receiving gabapentin. Only use opioid analgesics in combination with gabapentin and only in patients with insufficient alternative treatment options. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Use the lowest effective dose and shortest duration of treatment necessary to achieve the desired clinical effect. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Codeine, Guaifenesin:Concomitant use of (major) opioid agonists with gabapentin may cause excessive sedation, drowsiness and respiratory depression. Avoid prescribing opioid cough suppressants in patients receiving gabapentin. Only use opioid analgesics in combination with gabapentin and only in patients with insufficient alternative treatment options. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Use the lowest effective dose and shortest duration of treatment necessary to achieve the desired clinical effect. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Codeine, Guaifenesin, Pseudoephedrine:Concomitant use of (major) opioid agonists with gabapentin may cause excessive sedation, drowsiness and respiratory depression. Avoid prescribing opioid cough suppressants in patients receiving gabapentin. Only use opioid analgesics in combination with gabapentin and only in patients with insufficient alternative treatment options. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Use the lowest effective dose and shortest duration of treatment necessary to achieve the desired clinical effect. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Codeine, Phenylephrine, Promethazine:Concomitant use of (major) opioid agonists with gabapentin may cause excessive sedation, drowsiness and respiratory depression. Avoid prescribing opioid cough suppressants in patients receiving gabapentin. Only use opioid analgesics in combination with gabapentin and only in patients with insufficient alternative treatment options. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Use the lowest effective dose and shortest duration of treatment necessary to achieve the desired clinical effect. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression. (Major) Initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of sedation and somnolence when coadministering gabapentin and promethazine. Concomitant use of gabapentin and promethazine may result in cumulative central nervous system depression. Educate patients about the risks and symptoms of excessive CNS depression.
Codeine, Promethazine:Concomitant use of (major) opioid agonists with gabapentin may cause excessive sedation, drowsiness and respiratory depression. Avoid prescribing opioid cough suppressants in patients receiving gabapentin. Only use opioid analgesics in combination with gabapentin and only in patients with insufficient alternative treatment options. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Use the lowest effective dose and shortest duration of treatment necessary to achieve the desired clinical effect. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression. (Major) Initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of sedation and somnolence when coadministering gabapentin and promethazine. Concomitant use of gabapentin and promethazine may result in cumulative central nervous system depression. Educate patients about the risks and symptoms of excessive CNS depression.
Collevelen:(Moderate) The manufacturer of colesevelam recommends monitoring of serum drug concentrations and/or clinical effects, as changes in serum blood concentrations may have clinically significant effects on safety or efficacy. To minimize the potential for interactions, consider taking an oral anticonvulsant such as gabapentin at least 1 hour before or at least 4 hours after colesevelam.
Cyclohexazine:(Moderate) Monitor for excessive sedation and somnolence during coadministration of cyclizine and gabapentin. Concomitant use may cause further central nervous system depression.
Cyclobenzaprine:(Major) Initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of sedation and somnolence when coadministering gabapentin and cyclobenzaprine. Concomitant use of gabapentin and cyclobenzaprine may result in cumulative central nervous system depression. Educate patients about the risks and symptoms of excessive CNS depression.
Cyproheptadine:(Moderate) Monitor for excessive sedation and somnolence during coadministration of cyproheptadine and gabapentin. Concomitant use may cause further central nervous system depression.
Danteros:(Major) Concomitant use of dantrolene with gabapentin may cause excessive sedation, drowsiness, and respiratory depression. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Tetrabenazine:(Moderate) Monitor for excessive sedation and somnolence during coadministration of deutetrabenazine and gabapentin. Concomitant use may cause further central nervous system depression.
Dexbromopheniramine:(Moderate) Monitor for excessive sedation and somnolence during coadministration of dexbromopheniramine and gabapentin. Concomitant use may cause further central nervous system depression.
Dexbrompheniramine, Pseudoephedrine:(Moderate) Monitor for excessive sedation and somnolence during coadministration of dexbromopheniramine and gabapentin. Concomitant use may cause further central nervous system depression.
Dexchlorpheniramine:(Moderate) Monitor for excessive sedation and somnolence during coadministration of dexchlorpheniramine and gabapentin. Concomitant use may cause further central nervous system depression.
Dexchlorpheniramine, Dextromethorphan, Pseudoephedrine:(Moderate) Monitor for excessive sedation and somnolence during coadministration of dexchlorpheniramine and gabapentin. Concomitant use may cause further central nervous system depression.
Dexmedetomidine:(Moderate) Monitor for excessive sedation, somnolence, and respiratory depression during coadministration of dexmedetomidine and gabapentin. Concomitant use may cause central nervous system arousal and respiratory depression.
Dextromethorphan, Diphenhydramine, Phenylephrine:(Moderate) Monitor for excessive sedation and somnolence during coadministration of diphenhydramine and gabapentin. Concomitant use may cause further central nervous system depression.
Jixi Pan:Concomitant use of (mainly) benzodiazepines with gabapentin may cause excessive sedation, drowsiness and respiratory depression. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Defelik Farin:(Moderate) If concomitant use of difelicfarin and CNS depressants is indicated, monitor for dizziness, somnolence, changes in mental status, and disturbances in gait. Concomitant administration may increase the risk of these side effects.
Dimenhydrin:(Moderate) Monitor for excessive sedation and somnolence during coadministration of dimenhydrinate and gabapentin. Concomitant use may cause further central nervous system depression.
Diphenhydramine:(Moderate) Monitor for excessive sedation and somnolence during coadministration of diphenhydramine and gabapentin. Concomitant use may cause further central nervous system depression.
Diphenhydramine, Ibuprofen:(Moderate) Monitor for excessive sedation and somnolence during coadministration of diphenhydramine and gabapentin. Concomitant use may cause further central nervous system depression.
Diphenhydramine, Naproxen:(Moderate) Monitor for excessive sedation and somnolence during coadministration of diphenhydramine and gabapentin. Concomitant use may cause further central nervous system depression.
Diphenhydramine, Phenylephrine:(Moderate) Monitor for excessive sedation and somnolence during coadministration of diphenhydramine and gabapentin. Concomitant use may cause further central nervous system depression.
Diphenoxylate, Atropine:(Moderate) Monitor for excessive sedation and somnolence during coadministration of atropine and gabapentin. Concomitant use may cause further central nervous system depression.
Doxylamine:(Moderate) Monitor for excessive sedation and somnolence during coadministration of doxylamine and gabapentin. Concomitant use may cause further central nervous system depression.
doxylamine, pyridoxine:(Moderate) Monitor for excessive sedation and somnolence during coadministration of doxylamine and gabapentin. Concomitant use may cause further central nervous system depression.
Droperidol:(Major) Initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of sedation and somnolence during coadministration of gabapentin and droperidol. Concomitant use of gabapentin and droperidol may lead to cumulative central nervous system depression. Educate patients about the risks and symptoms of excessive CNS depression.
Endcapone:(Major) Initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of sedation and somnolence when coadministering gabapentin and entacapone. Concomitant use of gabapentin and entacapone may lead to cumulative central nervous system depression. Educate patients about the risks and symptoms of excessive CNS depression. Dopaminergic drugs such as entacapone have also been associated with sleepiness during activities of daily living (such as driving), which in some cases has led to accidents. Reassess patients periodically throughout treatment for somnolence or hypersomnia, especially since somnolence or hypersomnia may occur long after initiation of therapy.
prose:(Moderate) Closely monitor patients receiving esketamine and gabapentin for sedative and other CNS depressant effects. Instruct patients receiving a dose of esketamine not to drive or engage in other activities requiring alertness until the next rest day.
For estazol:Concomitant use of (mainly) benzodiazepines with gabapentin may cause excessive sedation, drowsiness and respiratory depression. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Ezopiclone:(Primary) Initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of sedation and somnolence when gabapentin and eszopiclone are coadministered. Concomitant use of gabapentin and eszopiclone may result in additional central nervous system depression and complex sleep-related behaviors (eg, driving, talking, eating, or other activities while not fully awake). Educate patients about the risks and symptoms of excessive CNS depression. Advise patients to contact their provider immediately if sleep-related symptoms or behaviors occur.
Ethanol:Patients are (mostly) advised to avoid alcohol while taking gabapentin. Concomitant use of alcohol with gabapentin may cause excessive sedation, drowsiness, and respiratory depression. Alcohol can cause gabapentin to be released faster than etacar from extended-release tablets, which can increase the risk of side effects. In an in vitro dissolution study, 63% of the gabapentin enakabi dose was released within 1 hour at the highest alcohol concentration studied (40%). In 5% alcohol, 43% of the dose is released in 1 hour.
Etomidate:Concomitant use of (primary) general anesthetics with gabapentin may cause excessive sedation, drowsiness and respiratory depression. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of excessive respiratory depression. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Fenfluramine:(Moderate) Monitor for excessive sedation and somnolence during coadministration of fenfluramine and gabapentin. Concomitant use may cause further central nervous system depression.
Fentanyl:Concomitant use of (major) opioid agonists with gabapentin may cause excessive sedation, drowsiness and respiratory depression. Only use opioid analgesics in combination with gabapentin and only in patients with insufficient alternative treatment options. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Use the lowest effective dose and shortest duration of treatment necessary to achieve the desired clinical effect. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Flibenther's:(Moderate) Monitor for excessive sedation and somnolence during coadministration of flibanserin and gabapentin. Concomitant use may cause further central nervous system depression.
Fluphenazine:(Moderate) Monitor for excessive sedation and somnolence during coadministration of fluphenazine and gabapentin. Concomitant use may cause further central nervous system depression.
Fluazepam:Concomitant use of (mainly) benzodiazepines with gabapentin may cause excessive sedation, drowsiness and respiratory depression. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
food:Patients are (mostly) advised to avoid cannabis when taking CNS depressants due to the risk of superimposed CNS depression and possible other cognitive side effects.
General anesthetics:Concomitant use of (primary) general anesthetics with gabapentin may cause excessive sedation, drowsiness and respiratory depression. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of excessive respiratory depression. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Guaifenesin, Hydrocodone:Concomitant use of (major) opioid agonists with gabapentin may cause excessive sedation, drowsiness and respiratory depression. Avoid prescribing opioid cough suppressants in patients receiving gabapentin. Only use opioid analgesics in combination with gabapentin and only in patients with insufficient alternative treatment options. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Use the lowest effective dose and shortest duration of treatment necessary to achieve the desired clinical effect. In addition, coadministration of gabapentin with hydrocodone decreased hydrocodone exposure in a dose-dependent manner. Consider possible reduction in hydrocodone exposure and effects when starting or stopping gabapentin in patients taking hydrocodone. After 125 mg gabapentin (n = 48), hydrocodone (10 mg, n = 50) Cmax and AUC values decreased by 3% to 4%, respectively, and after 500 mg gabapentin, Cmax and AUC values decreased by 21 % to 22%, respectively % . Hydrocodone increased gabapentin AUC by 14%. The extent of the interaction and the mechanism of interaction at other doses are unknown.
Guanfacine:(Moderate) Monitor for excessive sedation and somnolence during coadministration of guanfacine and gabapentin. Concomitant use may cause further central nervous system depression.
Haloperidol:(Major) Initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of sedation and somnolence during coadministration of gabapentin and haloperidol. Concomitant use of gabapentin and haloperidol may lead to cumulative central nervous system depression. Educate patients about the risks and symptoms of excessive CNS depression.
Omatropine, Hydrocodone:Concomitant use of (major) opioid agonists with gabapentin may cause excessive sedation, drowsiness and respiratory depression. Avoid prescribing opioid cough suppressants in patients receiving gabapentin. Only use opioid analgesics in combination with gabapentin and only in patients with insufficient alternative treatment options. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Use the lowest effective dose and shortest duration of treatment necessary to achieve the desired clinical effect. In addition, coadministration of gabapentin with hydrocodone decreased hydrocodone exposure in a dose-dependent manner. Consider possible reduction in hydrocodone exposure and effects when starting or stopping gabapentin in patients taking hydrocodone. After 125 mg gabapentin (n = 48), hydrocodone (10 mg, n = 50) Cmax and AUC values decreased by 3% to 4%, respectively, and after 500 mg gabapentin, Cmax and AUC values decreased by 21 % to 22%, respectively % . Hydrocodone increased gabapentin AUC by 14%. The extent of the interaction and the mechanism of interaction at other doses are unknown.
Hydrochlorothiazide, HCTZ, Methyldopa:(Moderate) Monitor for excessive sedation and somnolence during coadministration of methyldopa and gabapentin. Concomitant use may cause further central nervous system depression.
Hydrocodone:Concomitant use of (major) opioid agonists with gabapentin may cause excessive sedation, drowsiness and respiratory depression. Avoid prescribing opioid cough suppressants in patients receiving gabapentin. Only use opioid analgesics in combination with gabapentin and only in patients with insufficient alternative treatment options. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Use the lowest effective dose and shortest duration of treatment necessary to achieve the desired clinical effect. In addition, coadministration of gabapentin with hydrocodone decreased hydrocodone exposure in a dose-dependent manner. Consider possible reduction in hydrocodone exposure and effects when starting or stopping gabapentin in patients taking hydrocodone. After 125 mg gabapentin (n = 48), hydrocodone (10 mg, n = 50) Cmax and AUC values decreased by 3% to 4%, respectively, and after 500 mg gabapentin, Cmax and AUC values decreased by 21 % to 22%, respectively % . Hydrocodone increased gabapentin AUC by 14%. The extent of the interaction and the mechanism of interaction at other doses are unknown.
Hydrocodone, Ibuprofen:Concomitant use of (major) opioid agonists with gabapentin may cause excessive sedation, drowsiness and respiratory depression. Avoid prescribing opioid cough suppressants in patients receiving gabapentin. Only use opioid analgesics in combination with gabapentin and only in patients with insufficient alternative treatment options. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Use the lowest effective dose and shortest duration of treatment necessary to achieve the desired clinical effect. In addition, coadministration of gabapentin with hydrocodone decreased hydrocodone exposure in a dose-dependent manner. Consider possible reduction in hydrocodone exposure and effects when starting or stopping gabapentin in patients taking hydrocodone. After 125 mg gabapentin (n = 48), hydrocodone (10 mg, n = 50) Cmax and AUC values decreased by 3% to 4%, respectively, and after 500 mg gabapentin, Cmax and AUC values decreased by 21 % to 22%, respectively % . Hydrocodone increased gabapentin AUC by 14%. The extent of the interaction and the mechanism of interaction at other doses are unknown.
Hydrocodone, Pseudoephedrine:Concomitant use of (major) opioid agonists with gabapentin may cause excessive sedation, drowsiness and respiratory depression. Avoid prescribing opioid cough suppressants in patients receiving gabapentin. Only use opioid analgesics in combination with gabapentin and only in patients with insufficient alternative treatment options. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Use the lowest effective dose and shortest duration of treatment necessary to achieve the desired clinical effect. In addition, coadministration of gabapentin with hydrocodone decreased hydrocodone exposure in a dose-dependent manner. Consider possible reduction in hydrocodone exposure and effects when starting or stopping gabapentin in patients taking hydrocodone. After 125 mg gabapentin (n = 48), hydrocodone (10 mg, n = 50) Cmax and AUC values decreased by 3% to 4%, respectively, and after 500 mg gabapentin, Cmax and AUC values decreased by 21 % to 22%, respectively % . Hydrocodone increased gabapentin AUC by 14%. The extent of the interaction and the mechanism of interaction at other doses are unknown.
Hydromorphone:Concomitant use of (major) opioid agonists with gabapentin may cause excessive sedation, drowsiness and respiratory depression. Only use opioid analgesics in combination with gabapentin and only in patients with insufficient alternative treatment options. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Use the lowest effective dose and shortest duration of treatment necessary to achieve the desired clinical effect. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Hydroxychloroquine:(Moderate) Monitor seizure activity in epileptic patients during concomitant use of gabapentin and hydroxychloroquine. Hydroxychloroquine may lower the seizure threshold, therefore, the activity of concomitant antiepileptic drugs may be affected.
Hydroxyzine:Initiate gabapentin at the lowest recommended dose (primarily) and monitor patients for symptoms of sedation and somnolence when coadministering gabapentin and hydroxyzine. When co-administered with hydroxyzine intramuscular injection, reduce gabapentin dose by 50% or more. Concomitant use of gabapentin and hydroxyzine may result in cumulative central nervous system depression. Educate patients about the risks and symptoms of excessive CNS depression.
Ibuprofen, Oxycodone:Concomitant use of (major) opioid agonists with gabapentin may cause excessive sedation, drowsiness and respiratory depression. Only use opioid analgesics in combination with gabapentin and only in patients with insufficient alternative treatment options. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Use the lowest effective dose and shortest duration of treatment necessary to achieve the desired clinical effect. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Iloperidone:(Moderate) Monitor for excessive sedation and somnolence during coadministration of iloperidone and gabapentin. Concomitant use may cause further central nervous system depression.
Isocarboxazid:(Moderate) Monitor for respiratory depression and sedation during concomitant use of monoamine oxidase inhibitors (MAOIs) and gabapentin; consider starting gabapentin at a low dose. Concomitant administration increases the risk of central nervous system depression.
Isoflurane:Concomitant use of (primary) general anesthetics with gabapentin may cause excessive sedation, drowsiness and respiratory depression. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of excessive respiratory depression. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Ketamine:Concomitant use of (primary) general anesthetics with gabapentin may cause excessive sedation, drowsiness and respiratory depression. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of excessive respiratory depression. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Lanthanum Carbonate:Oral compounds known to (mostly) interact with antacids (such as gabapentin) should not be taken within 2 hours of taking lanthanum carbonate. If these drugs are used at the same time, please separate the dosage interval appropriately. Monitor serum concentrations and clinical status.
Officially:(Moderate) Monitor for excessive sedation and somnolence during coadministration of lamistan and gabapentin. Concomitant use may cause further central nervous system depression.
Citric acid:(Moderate) Monitor for excessive sedation and somnolence during concomitant use of leborexant and gabapentin. When leborexant and gabapentin are co-administered, dose adjustment may be required due to the potential for additive CNS effects. The risk of next-day impairment, including impairment of driving, is increased if leborexant is taken with other CNS depressants.
Left Nishika Toriya:(Moderate) Monitor for respiratory depression and sedation during coadministration of cetirizine and gabapentin; consider starting gabapentin at a low dose. Concomitant administration increases the risk of central nervous system depression.
Levodopa:(Major) Initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of sedation and somnolence during coadministration of gabapentin and levodopa. Concomitant use of gabapentin and levodopa may lead to cumulative central nervous system depression. Educate patients about the risks and symptoms of excessive CNS depression. Dopaminergic drugs such as levodopa have also been linked to sleepiness during activities of daily living (such as driving), which in some cases has led to accidents. Reassess patients periodically throughout treatment for somnolence or hypersomnia, especially since somnolence or hypersomnia may occur long after initiation of therapy.
Levorphanol:Concomitant use of (major) opioid agonists with gabapentin may cause excessive sedation, drowsiness and respiratory depression. Only use opioid analgesics in combination with gabapentin and only in patients with insufficient alternative treatment options. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Reduce the initial dose of levorphanol by about 50% or more. Use the lowest effective dose and shortest duration of treatment necessary to achieve the desired clinical effect. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Lofexidine:(Moderate) Monitor for excessive sedation and somnolence during coadministration of lofexidine and gabapentin. Concomitant use may cause further central nervous system depression.
Lorazepam:Concomitant use of (mainly) benzodiazepines with gabapentin may cause excessive sedation, drowsiness and respiratory depression. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Loxapine:(Moderate) Monitor for excessive sedation and somnolence during coadministration of loxapine and gabapentin. Concomitant use may cause further central nervous system depression.
Lumateperone:(Moderate) Monitor for excessive sedation and somnolence during coadministration of luteperone and gabapentin. Concomitant use may cause further central nervous system depression.
Lurasidone:(Moderate) Monitor for excessive sedation and somnolence during coadministration of lurasidone and gabapentin. Concomitant use may cause further central nervous system depression.
magnesium hydroxide:(Moderate) Gabapentin should be taken at least 2 hours after taking an antacid. Antacids have been shown to reduce the oral bioavailability of gabapentin by approximately 20%. When gabapentin is administered 2 hours after antacids, bioavailability is reduced by approximately 5%.
Maprotiline:(Major) Initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of sedation and somnolence when coadministering gabapentin and maprotiline. Concomitant use of gabapentin and maprotiline may lead to cumulative central nervous system depression. Educate patients about the risks and symptoms of excessive CNS depression.
Meclizine:(Moderate) Monitor for excessive sedation and somnolence during coadministration of meclizine and gabapentin. Concomitant use may cause further central nervous system depression.
Mefloquine:(Moderate) It is unclear whether mefloquine alters the activity of gabapentin, as gabapentin is not appreciably metabolized and generally does not interfere with the metabolism of other drugs. Concomitant use of mefloquine and certain anticonvulsants has been reported to result in lower than expected anticonvulsant concentrations and uncontrolled seizures. If the drug is monitored with therapeutic drug monitoring, monitoring of anticonvulsant serum concentrations is recommended. Gabapentin concentrations are not usually monitored. Mefloquine can also cause central nervous system side effects that may cause seizures or altered mood or behavior.
melatonin:(Moderate) Monitor for excessive sedation and somnolence during coadministration of melatonin and gabapentin. Concomitant use may cause further central nervous system depression.
Pethidine:Concomitant use of (major) opioid agonists with gabapentin may cause excessive sedation, drowsiness and respiratory depression. Only use opioid analgesics in combination with gabapentin and only in patients with insufficient alternative treatment options. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Use the lowest effective dose and shortest duration of treatment necessary to achieve the desired clinical effect. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Next step:(Moderate) Monitor for excessive sedation and somnolence during coadministration of meprovamate and gabapentin. Concomitant use may cause further central nervous system depression.
Metaxalone:(Major) Initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of sedation and somnolence during coadministration of gabapentin and metaxalone. Concomitant use of gabapentin and metaxalone may result in cumulative central nervous system depression. Educate patients about the risks and symptoms of excessive CNS depression.
Methadone:Concomitant use of (major) opioid agonists with gabapentin may cause excessive sedation, drowsiness and respiratory depression. Only use opioid analgesics in combination with gabapentin and only in patients with insufficient alternative treatment options. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Use the lowest effective dose and shortest duration of treatment necessary to achieve the desired clinical effect. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Methocarbamol:(Major) Initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of sedation and somnolence when coadministering gabapentin and methocarbamol. Concomitant use of gabapentin and methocarbamol may lead to cumulative central nervous system depression. Educate patients about the risks and symptoms of excessive CNS depression.
Mid-life:Concomitant use of (mainly) barbiturates with gabapentin may cause excessive sedation, drowsiness and respiratory depression. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Methyldopa:(Moderate) Monitor for excessive sedation and somnolence during coadministration of methyldopa and gabapentin. Concomitant use may cause further central nervous system depression.
Metoclopramide:(Moderate) Monitor for excessive sedation and somnolence during coadministration of metoclopramide and gabapentin. Concomitant use may cause further central nervous system depression.
Midazolam:Concomitant use of (mainly) benzodiazepines with gabapentin may cause excessive sedation, drowsiness and respiratory depression. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Mirtazapine:(Major) Initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of sedation and somnolence during coadministration of gabapentin and mirtazapine. Concomitant use of gabapentin and mirtazapine may lead to cumulative central nervous system depression. Educate patients about the risks and symptoms of excessive CNS depression.
Morinone:(Primary) Initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of sedation and somnolence when gabapentin and morpholino are coadministered. Concomitant use of gabapentin and morpholone may lead to cumulative central nervous system depression. Educate patients about the risks and symptoms of excessive CNS depression.
Monoamine oxidase inhibitors:(Moderate) Monitor for respiratory depression and sedation during concomitant use of monoamine oxidase inhibitors (MAOIs) and gabapentin; consider starting gabapentin at a low dose. Concomitant administration increases the risk of central nervous system depression.
morphine:Concomitant use of (major) opioid agonists with gabapentin may cause excessive sedation, drowsiness and respiratory depression. Only use opioid analgesics in combination with gabapentin and only in patients with insufficient alternative treatment options. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. For extended-release morphine (MS Contin and Morphabond), start with 15 mg every 12 hours. Morphine; Naltrexone should be started at one-third to one-half of the recommended starting dose. Use the lowest effective dose and shortest duration of treatment necessary to achieve the desired clinical effect. In addition, coadministration of morphine and gabapentin may increase gabapentin concentrations and may require dose adjustment. When the 60 mg controlled-release morphine capsules were administered 2 hours before the 60 mg gabapentin capsules, the mean AUC of gabapentin was increased by 44% (n = 12). Morphine pharmacokinetic parameter values were not affected by gabapentin administered 2 h after morphine. The extent of the interaction at other doses is unknown.
Morphine, Naltrexone:Concomitant use of (major) opioid agonists with gabapentin may cause excessive sedation, drowsiness and respiratory depression. Only use opioid analgesics in combination with gabapentin and only in patients with insufficient alternative treatment options. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. For extended-release morphine (MS Contin and Morphabond), start with 15 mg every 12 hours. Morphine; Naltrexone should be started at one-third to one-half of the recommended starting dose. Use the lowest effective dose and shortest duration of treatment necessary to achieve the desired clinical effect. In addition, coadministration of morphine and gabapentin may increase gabapentin concentrations and may require dose adjustment. When the 60 mg controlled-release morphine capsules were administered 2 hours before the 60 mg gabapentin capsules, the mean AUC of gabapentin was increased by 44% (n = 12). Morphine pharmacokinetic parameter values were not affected by gabapentin administered 2 h after morphine. The extent of the interaction at other doses is unknown.
Lost:(Major) Monitor for excessive sedation and somnolence during coadministration of nabilone and gabapentin. Concomitant use may cause further central nervous system depression.
Nabuphine:Concomitant use of (mainly) nalbuphine with gabapentin may cause excessive sedation, drowsiness and respiratory depression. Use nalbuphine only in combination with gabapentin and only in patients with insufficient alternative treatment options. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Use the lowest effective dose and shortest duration of treatment necessary to achieve the desired clinical effect. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Nefazodone:(Primary) Initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of sedation and somnolence when gabapentin and nefazodone are coadministered. Concomitant use of gabapentin and nefazodone may result in cumulative central nervous system depression. Educate patients about the risks and symptoms of excessive CNS depression.
Olanzapine:(Major) Initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of sedation and somnolence during coadministration of gabapentin and olanzapine. Concomitant use of gabapentin and olanzapine may lead to cumulative central nervous system depression. Educate patients about the risks and symptoms of excessive CNS depression.
Olanzapine, Fluoxetine:(Major) Initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of sedation and somnolence during coadministration of gabapentin and olanzapine. Concomitant use of gabapentin and olanzapine may lead to cumulative central nervous system depression. Educate patients about the risks and symptoms of excessive CNS depression.
Olanzapine, Salmidorphine:(Major) Initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of sedation and somnolence during coadministration of gabapentin and olanzapine. Concomitant use of gabapentin and olanzapine may lead to cumulative central nervous system depression. Educate patients about the risks and symptoms of excessive CNS depression.
Oxythidine:Concomitant use of (major) opioid agonists with gabapentin may cause excessive sedation, drowsiness and respiratory depression. Only use opioid analgesics in combination with gabapentin and only in patients with insufficient alternative treatment options. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Use the lowest effective dose and shortest duration of treatment necessary to achieve the desired clinical effect.
Omeprazole, Sodium Bicarbonate:(Moderate) Antacids have been shown to decrease the oral bioavailability of gabapentin by approximately 20%. When gabapentin is administered 2 hours after antacids, bioavailability is reduced by approximately 5%. It is recommended to take gabapentin at least 2 hours after taking antacids to avoid significant interactions.
Opie Capone:(Major) Initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of sedation and somnolence when coadministering gabapentin and apicapone. Concomitant use of gabapentin and opioids may result in cumulative central nervous system depression. Educate patients about the risks and symptoms of excessive CNS depression. Dopaminergic drugs, such as opioids, have also been associated with sudden sleepiness during activities of daily living (such as driving), which in some cases can lead to accidents. Reassess patients periodically throughout treatment for somnolence or hypersomnia, especially since somnolence or hypersomnia may occur long after initiation of therapy.
Ofena June:(Major) Initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of sedation and somnolence during coadministration of gabapentin and orphenadine. Coadministration of gabapentin and orphenadine may result in cumulative central nervous system depression. Educate patients about the risks and symptoms of excessive CNS depression.
Oxazepam:Concomitant use of (mainly) benzodiazepines with gabapentin may cause excessive sedation, drowsiness and respiratory depression. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Oxycodone:Concomitant use of (major) opioid agonists with gabapentin may cause excessive sedation, drowsiness and respiratory depression. Only use opioid analgesics in combination with gabapentin and only in patients with insufficient alternative treatment options. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Use the lowest effective dose and shortest duration of treatment necessary to achieve the desired clinical effect. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Oxymorphon:Concomitant use of (major) opioid agonists with gabapentin may cause excessive sedation, drowsiness and respiratory depression. Only use opioid analgesics in combination with gabapentin and only in patients with insufficient alternative treatment options. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Use oxymorphone at an initial dose of 1/3 to 1/2 the usual dose and titrate based on clinical response. Use the lowest effective dose and shortest duration of treatment necessary to achieve the desired clinical effect. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Paliperidone:(Moderate) Monitor for excessive sedation and somnolence during coadministration of paliperidone and gabapentin. Concomitant use may cause further central nervous system depression.
Pentazocine:Concomitant use of (mainly) pentazocine with gabapentin may cause excessive sedation, drowsiness, and respiratory depression. The use of pentazocine in combination with gabapentin alone is limited to patients for whom alternative treatment options are inadequate. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Use the lowest effective dose and shortest duration of treatment necessary to achieve the desired clinical effect. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Pentazocine, Naloxone:Concomitant use of (mainly) pentazocine with gabapentin may cause excessive sedation, drowsiness, and respiratory depression. The use of pentazocine in combination with gabapentin alone is limited to patients for whom alternative treatment options are inadequate. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Use the lowest effective dose and shortest duration of treatment necessary to achieve the desired clinical effect. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Pentobarbital:Concomitant use of (mainly) barbiturates with gabapentin may cause excessive sedation, drowsiness and respiratory depression. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Perapanel:(Moderate) Monitor for excessive sedation and somnolence during coadministration of perapanel and gabapentin. Concomitant use may cause further central nervous system depression.
Perphenazine:(Moderate) Monitor for excessive sedation and somnolence during coadministration of perphenazine and gabapentin. Concomitant use may cause further central nervous system depression.
Perphenazine, Amitriptyline:(Moderate) Monitor for excessive sedation and somnolence during coadministration of perphenazine and gabapentin. Concomitant use may cause further central nervous system depression.
Phenelzine:(Moderate) Monitor for respiratory depression and sedation during concomitant use of monoamine oxidase inhibitors (MAOIs) and gabapentin; consider starting gabapentin at a low dose. Concomitant administration increases the risk of central nervous system depression.
Phenobarbital:Concomitant use of (mainly) barbiturates with gabapentin may cause excessive sedation, drowsiness and respiratory depression. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Phenobarbital, Hyoscyamine, Atropine, Scopolamine:Concomitant use of (mainly) barbiturates with gabapentin may cause excessive sedation, drowsiness and respiratory depression. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression. (Moderate) Monitor for excessive sedation and somnolence during coadministration of atropine and gabapentin. Concomitant use may cause further central nervous system depression. (Moderate) Monitor for excessive sedation and somnolence during coadministration of scopolamine and gabapentin. Concomitant use may cause further central nervous system depression.
From Selin the Horse:(Moderate) Monitor for excessive sedation and somnolence when coadministering pima vanserin and gabapentin. Concomitant use may cause further central nervous system depression.
Pimozide:(Major) Initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of sedation and somnolence when gabapentin and pimozide are coadministered. Concomitant use of gabapentin and pimozide may lead to cumulative central nervous system depression. Educate patients about the risks and symptoms of excessive CNS depression.
Pramipexole:(Major) Initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of sedation and somnolence during coadministration of gabapentin and pramipexole. Concomitant use of gabapentin and pramipexole may lead to cumulative central nervous system depression. Educate patients about the risks and symptoms of excessive CNS depression. Dopaminergic drugs such as pramipexole have also been linked to sudden sleepiness during activities of daily living (such as driving), which in some cases has led to accidents. Reassess patients periodically throughout treatment for somnolence or hypersomnia, especially since somnolence or hypersomnia may occur long after initiation of therapy.
Pregabalin:Concomitant use of (mainly) gabapentin with pregabalin may cause excessive sedation, drowsiness and respiratory depression. If concomitant use is required, initiate pregabalin and gabapentin at the lowest recommended doses and monitor patients for symptoms of respiratory depression and sedation. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Primidone:Concomitant use of (mainly) barbiturates with gabapentin may cause excessive sedation, drowsiness and respiratory depression. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Prochlorperazine:(Major) Initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of sedation and somnolence during coadministration of gabapentin and prochlorperazine. Concomitant use of gabapentin and prochlorperazine may result in cumulative central nervous system depression. Educate patients about the risks and symptoms of excessive CNS depression. Concomitant administration of prochlorperazine is contraindicated in patients receiving high doses of CNS depressants.
Promethazine:(Major) Initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of sedation and somnolence when coadministering gabapentin and promethazine. Concomitant use of gabapentin and promethazine may result in cumulative central nervous system depression. Educate patients about the risks and symptoms of excessive CNS depression.
Promethazine, Dextromethorphan:(Major) Initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of sedation and somnolence when coadministering gabapentin and promethazine. Concomitant use of gabapentin and promethazine may result in cumulative central nervous system depression. Educate patients about the risks and symptoms of excessive CNS depression.
Promethazine, Phenylephrine:(Major) Initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of sedation and somnolence when coadministering gabapentin and promethazine. Concomitant use of gabapentin and promethazine may result in cumulative central nervous system depression. Educate patients about the risks and symptoms of excessive CNS depression.
Propofol:Concomitant use of (primary) general anesthetics with gabapentin may cause excessive sedation, drowsiness and respiratory depression. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of excessive respiratory depression. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Propranolol:(Minus) The combination of propranolol and gabapentin may cause dystonia through pharmacodynamic interactions.
propranolol, hydrochlorothiazide, HCTZ:(Minus) The combination of propranolol and gabapentin may cause dystonia through pharmacodynamic interactions.
Pseudoephedrine, Triprolidine:(Moderate) Monitor for excessive sedation and somnolence during coadministration of triprolidine and gabapentin. Concomitant use may cause further central nervous system depression.
Pyramine:(Moderate) Monitor for excessive sedation and somnolence during coadministration of pyrilamine and gabapentin. Concomitant use may cause further central nervous system depression.
Quazepam:Concomitant use of (mainly) benzodiazepines with gabapentin may cause excessive sedation, drowsiness and respiratory depression. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Quetiapine:(Major) Initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of sedation and somnolence during coadministration of gabapentin and quetiapine. Concomitant use of gabapentin and quetiapine may lead to cumulative central nervous system depression. Educate patients about the risks and symptoms of excessive CNS depression.
Ramelteon:(Moderate) Monitor for excessive sedation and somnolence during coadministration of ramelteon and gabapentin. Concomitant use may cause further central nervous system depression.
Rasagiline:(Major) Initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of sedation and somnolence when coadministering gabapentin and rasagiline. Concomitant use of gabapentin and rasagiline may result in cumulative central nervous system depression. Educate patients about the risks and symptoms of excessive CNS depression. Dopaminergic drugs such as rasagiline have also been associated with sudden sleepiness during activities of daily living (such as driving), which has led to accidents in some cases. Reassess patients periodically throughout treatment for somnolence or hypersomnia, especially since somnolence or hypersomnia may occur long after initiation of therapy.
Remifentanil:Concomitant use of (major) opioid agonists with gabapentin may cause excessive sedation, drowsiness and respiratory depression. Limit the use of remifentanil in combination with gabapentin in patients for whom alternative treatment options are inadequate. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Use the lowest effective dose and shortest duration of treatment necessary to achieve the desired clinical effect. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Remimazolam:Concomitant use of (mainly) benzodiazepines with gabapentin may cause excessive sedation, drowsiness and respiratory depression. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Risperidone:(Major) Initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of sedation and somnolence during coadministration of gabapentin and risperidone. Concomitant use of gabapentin and risperidone may lead to cumulative central nervous system depression. Educate patients about the risks and symptoms of excessive CNS depression.
Ropinirole:(Primary) Initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of sedation and somnolence when gabapentin and ropinirole are coadministered. Concomitant use of gabapentin and ropinirole may lead to cumulative central nervous system depression. Educate patients about the risks and symptoms of excessive CNS depression. Dopaminergic drugs such as ropinirole have also been linked to sudden sleepiness during activities of daily living (such as driving), which has led to accidents in some cases. Reassess patients periodically throughout treatment for somnolence or hypersomnia, especially since somnolence or hypersomnia may occur long after initiation of therapy.
Rotigotine:(Major) Initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of sedation and somnolence during coadministration of gabapentin and rotigotine. Concomitant use of gabapentin and rotigotine may lead to cumulative central nervous system depression. Educate patients about the risks and symptoms of excessive CNS depression. Dopaminergic drugs such as rotigotine have also been linked to sudden sleepiness during activities of daily living (such as driving), which in some cases has led to accidents. Reassess patients periodically throughout treatment for somnolence or hypersomnia, especially since somnolence or hypersomnia may occur long after initiation of therapy.
Safinamide:(Major) Initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of sedation and somnolence during coadministration of gabapentin and safinamide. Concomitant use of gabapentin and safinamide may result in cumulative central nervous system depression. Educate patients about the risks and symptoms of excessive CNS depression. Dopaminergic drugs such as safinamide have also been associated with sudden sleepiness during activities of daily living (such as driving), which in some cases has led to accidents. Reassess patients periodically throughout treatment for somnolence or hypersomnia, especially since somnolence or hypersomnia may occur long after initiation of therapy.
Scopolamine:(Moderate) Monitor for excessive sedation and somnolence during coadministration of scopolamine and gabapentin. Concomitant use may cause further central nervous system depression.
Secobarbital:Concomitant use of (mainly) barbiturates with gabapentin may cause excessive sedation, drowsiness and respiratory depression. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Slaijilan:(Moderate) Monitor for excessive sedation and somnolence during coadministration of selegiline and gabapentin. Concomitant use may cause further central nervous system depression.
Sevoflurane:Concomitant use of (primary) general anesthetics with gabapentin may cause excessive sedation, drowsiness and respiratory depression. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of excessive respiratory depression. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Sodium Bicarbonate:(Moderate) Antacids have been shown to decrease the oral bioavailability of gabapentin by approximately 20%. When gabapentin is administered 2 hours after antacids, bioavailability is reduced by approximately 5%. It is recommended to take gabapentin at least 2 hours after taking antacids to avoid significant interactions.
Sodium Acetate:Concomitant use of (mainly) sodium oxybate with gabapentin may cause excessive sedation, drowsiness, and respiratory depression. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Dot toll:(Moderate) Monitor for excessive sedation and somnolence during coadministration of cetopentol and gabapentin. Concomitant use may cause further central nervous system depression.
Sufentanil:Concomitant use of (major) opioid agonists with gabapentin may cause excessive sedation, drowsiness and respiratory depression. The combination of sufentanil and gabapentin alone should be limited to patients with insufficient alternative treatment options. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Use the lowest effective dose and shortest duration of treatment necessary to achieve the desired clinical effect. Concomitant use of sufentanil with CNS depressants may result in decreased pulmonary artery pressure and hypotension. As a postoperative analgesia, concomitant use increases the risk of hypotension, respiratory depression, deep sedation, coma and death. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Suwaksan:(Moderate) Monitor for excessive sedation and somnolence during coadministration of suvorexant and gabapentin. Concomitant use may cause further central nervous system depression.
He sprayed him more:Concomitant use of (major) opioid agonists with gabapentin may cause excessive sedation, drowsiness and respiratory depression. Only use opioid analgesics in combination with gabapentin and only in patients with insufficient alternative treatment options. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Use the lowest effective dose and shortest duration of treatment necessary to achieve the desired clinical effect. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Tasi Meiqiong:(Moderate) Monitor for excessive sedation and somnolence during coadministration of tasimelteon and gabapentin. Concomitant use may cause further central nervous system depression.
Temazepam:Concomitant use of (mainly) benzodiazepines with gabapentin may cause excessive sedation, drowsiness and respiratory depression. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Tetrabenazine:(Moderate) Monitor for excessive sedation and somnolence during coadministration of tetrabenazine and gabapentin. Concomitant use may cause further central nervous system depression.
Thalidomide:(Primarily) avoid concomitant use of thalidomide and gabapentin due to the risk of superimposed CNS depression. If concomitant use cannot be avoided, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of sedation and somnolence during coadministration. Educate patients about the risks and symptoms of excessive CNS depression.
Thioridazine:(Major) Initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of sedation and somnolence when coadministering gabapentin and thioridazine. Concomitant administration of gabapentin and thioridazine may result in cumulative central nervous system depression. Educate patients about the risks and symptoms of excessive CNS depression.
Thiothioxene:(Moderate) Monitor for excessive sedation and somnolence during coadministration of thiothixene and gabapentin. Concomitant use may cause further central nervous system depression.
Tizanidine:(Major) Initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of sedation and somnolence when coadministering gabapentin and tizanidine. Concomitant use of gabapentin and tizanidine may lead to cumulative central nervous system depression. Educate patients about the risks and symptoms of excessive CNS depression.
Tolcapone:(Major) Initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of sedation and somnolence during coadministration of gabapentin and tolcapone. Concomitant use of gabapentin and tolcapone may lead to cumulative central nervous system depression. Educate patients about the risks and symptoms of excessive CNS depression. Dopaminergic drugs such as tolcapone have also been linked to sudden sleepiness during activities of daily living such as driving, which in some cases has led to accidents. Reassess patients periodically throughout treatment for somnolence or hypersomnia, especially since somnolence or hypersomnia may occur long after initiation of therapy.
Tramadol:Concomitant use of (major) opioid agonists with gabapentin may cause excessive sedation, drowsiness and respiratory depression. Only use opioid analgesics in combination with gabapentin and only in patients with insufficient alternative treatment options. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Use the lowest effective dose and shortest duration of treatment necessary to achieve the desired clinical effect. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
tramadol, acetaminophen:Concomitant use of (major) opioid agonists with gabapentin may cause excessive sedation, drowsiness and respiratory depression. Only use opioid analgesics in combination with gabapentin and only in patients with insufficient alternative treatment options. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Use the lowest effective dose and shortest duration of treatment necessary to achieve the desired clinical effect. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Tranylcypromine:(Moderate) Monitor for respiratory depression and sedation during concomitant use of monoamine oxidase inhibitors (MAOIs) and gabapentin; consider starting gabapentin at a low dose. Concomitant administration increases the risk of central nervous system depression.
Trazodone:(Major) Initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of sedation and somnolence during coadministration of gabapentin and trazodone. Concomitant use of gabapentin and trazodone may result in cumulative central nervous system depression. Educate patients about the risks and symptoms of excessive CNS depression.
Triazolam:Concomitant use of (mainly) benzodiazepines with gabapentin may cause excessive sedation, drowsiness and respiratory depression. If concomitant use is required, initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of respiratory depression and sedation. Educate patients about the dangers and symptoms of excessive CNS and respiratory depression.
Tricyclic antidepressants:(Major) Initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of sedation and somnolence when coadministering gabapentin with tricyclic antidepressants. Concomitant use of gabapentin with tricyclic antidepressants may lead to cumulative central nervous system depression. Educate patients about the risks and symptoms of excessive CNS depression.
Trifluoperazine:(Moderate) Monitor for excessive sedation and somnolence during coadministration of trifluoperazine and gabapentin. Concomitant use may cause further central nervous system depression.
Triprolidine:(Moderate) Monitor for excessive sedation and somnolence during coadministration of triprolidine and gabapentin. Concomitant use may cause further central nervous system depression.
Valerian, valerian:(Moderate) Monitor for excessive sedation and somnolence during coadministration of valerian and gabapentin. Concomitant use may cause further central nervous system depression.
Valproic acid, divalproex sodium:(Moderate) Monitor for excessive sedation and somnolence during coadministration of valproic acid and gabapentin. Concomitant use may cause further central nervous system depression.
Zaleplon:(Major) Initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of sedation and somnolence during coadministration of gabapentin and zaleplon. Concomitant use of gabapentin and zaleplon may result in additional central nervous system depression and complex sleep-related behaviors (eg, driving, talking, eating, or other activities while not fully awake). Educate patients about the risks and symptoms of excessive CNS depression. Advise patients to contact their provider immediately if sleep-related symptoms or behaviors occur.
Ziprasidone:(Moderate) Monitor for excessive sedation and somnolence during coadministration of ziprasidone and gabapentin. Concomitant use may cause further central nervous system depression.
Zolpidem:(Major) Initiate gabapentin at the lowest recommended dose and monitor patients for symptoms of sedation and somnolence during coadministration of gabapentin and zolpidem. For patients receiving concomitant CNS depressants, the recommended dose of zolpidem sublingual tablets is 1.75 mg/night. Concomitant use of gabapentin with zolpidem may result in further central nervous system depression and complex sleep-related behaviors (eg, driving, talking, eating, or other activities while not fully awake). Educate patients about the risks and symptoms of excessive CNS depression. Advise patients to contact their provider immediately if sleep-related symptoms or behaviors occur.
pregnancy and lactation
Pregnant
Δεν υπάρχουν επαρκείς και καλά ελεγχόμενες μελέτες για τη γκαμπαπεντίνη σε έγκυες γυναίκες. Τα δεδομένα από μελέτες κοόρτης που περιγράφουν τους νεογνικούς κινδύνους της θεραπείας με γκαμπαπεντίνη κατά τη διάρκεια της εγκυμοσύνης είναι ασαφή. Η γκαμπαπεντίνη διασχίζει ενεργά τον πλακούντα. Σε έξι νεογνά που γεννήθηκαν από μητέρες που λάμβαναν γκαμπαπεντίνη (εύρος δόσης 900 έως 3.200 mg/ημέρα), η αναλογία συγκέντρωσης του ομφάλιου λώρου προς το πλάσμα της μητέρας κατά τον τοκετό κυμαινόταν από 1,3 έως 2,11 (μέση τιμή 1,74). Έως τις 24 ώρες μετά τον τοκετό, οι συγκεντρώσεις της γκαμπαπεντίνης στα νεογνά μειώθηκαν κατά μέσο όρο στο 27% των συγκεντρώσεων στο αίμα του ομφάλιου λώρου (εύρος, 12% έως 36%). Ένα μωρό γεννήθηκε πρόωρα στις 33 εβδομάδες, ωστόσο, όλοι οι τοκετοί ήταν χωρίς προβλήματα και όλα τα νεογέννητα γεννήθηκαν καλά στην υγεία τους. Σε μια προοπτική μελέτη κοόρτης, η συχνότητα εμφάνισης μειζόνων νεογνικών δυσπλασιών ήταν παρόμοια μεταξύ 223 εγκύων γυναικών που είχαν εκτεθεί σε γκαμπαπεντίνη και 223 εγκύων γυναικών που δεν είχαν εκτεθεί σε γκαμπαπεντίνη (4,1% στο 2,5% των εγκύων γυναικών που είχαν εκτεθεί σε γκαμπαπεντίνη, p = 0,555). Οι κύριες δυσπλασίες περιελάμβαναν 2 κοιλιακά διαφραγματικά ελαττώματα, ανεγκεφαλία, μακροκεφαλία, μικρογναθία, δέρμα Marmora, πυλωρική στένωση, αμφοτερόπλευρη ιπποειδίτιδα και κρυψορχία. Σε όλες τις περιπτώσεις σοβαρής δυσπλασίας, οι γυναίκες έλαβαν ταυτόχρονη θεραπεία με άλλα φάρμακα κατά τη διάρκεια της εγκυμοσύνης· επομένως, δεν μπορούσε να τεκμηριωθεί αιτιολογική σχέση με τη γκαμπαπεντίνη. Δεν παρουσιάστηκαν σημαντικές δυσπλασίες σε νεογνά που γεννήθηκαν από γυναίκες που έλαβαν μονοθεραπεία με γκαμπαπεντίνη κατά τη διάρκεια της εγκυμοσύνης (n = 36). Συγκρίθηκαν υψηλότερα ποσοστά πρόωρου τοκετού (10,5% έναντι 3,9%, p = 0,019), χαμηλού βάρους γέννησης (λιγότερο από 2.500 g) (10,5% έναντι 4,4%, p = 0,033) και εισαγωγής σε εντατική ή ειδική φροντίδα νεογνών με το ποσοστό των βρεφονηπιακών σταθμών μεταξύ των νεογνών που εκτέθηκαν στη γκαμπαπεντίνη σε σύγκριση με τα μη εκτεθειμένα νεογνά (38% έναντι 2,9%, p<0,001). Υπήρχαν δύο πιθανά νεογνικά δυσπροσαρμοστικά σύνδρομα σε νεογνά που εκτέθηκαν στη γκαμπαπεντίνη στο τέλος της εγκυμοσύνης αλλά όχι σε βρέφη που δεν εκτέθηκαν στη γκαμπαπεντίνη· αυτά τα δύο νεογνά εκτέθηκαν επίσης σε άλλα ψυχοφάρμακα. Σε μια ομάδα 39 γυναικών που εκτέθηκαν στη γκαμπαπεντίνη κατά τη διάρκεια του πρώτου τριμήνου (97%) και καθ' όλη τη διάρκεια της εγκυμοσύνης (81,8%), 3 από τις 44 γεννήσεις ζωντανών γεννήσεων είχαν δυσμορφία. Τα νεογνά που εκτέθηκαν σε γκαμπαπεντίνη και βαλπροϊκό οξύ έχουν αναφερθεί ότι ανέπτυξαν υποσπαδία, νεογνά που εκτέθηκαν σε γκαμπαπεντίνη και φαινοβαρβιτάλη για να αναπτύξουν νεφρική ανεπάρκεια και νεογνά που εκτέθηκαν σε γκαμπαπεντίνη και λαμοτριγίνη για να αναπτύξουν μια ελαφρά παραμόρφωση του αριστερού έξω ακουστικού πόρου και μια μικρή ετικέτα δέρματος 2 A . Επειδή κατά τη διάρκεια αυτών των εγκυμοσύνων εμφανίστηκαν πολλαπλές εκθέσεις σε αντισπασμωδικά φάρμακα, δεν ήταν δυνατό να τεκμηριωθεί αιτιολογική σχέση με τη γκαμπαπεντίνη. Έντεκα ασθενείς που έλαβαν μονοθεραπεία με γκαμπαπεντίνη κατά τη διάρκεια της εγκυμοσύνης δεν εμφάνισαν δυσπλασίες. Σε μελέτες σε ζώα, η γκαμπαπεντίνη ήταν εμβρυοτοξική σε δόσεις 1 έως 4 φορές τη μέγιστη συνιστώμενη δόση για τον άνθρωπο (σε βάση mg/m2) κατά τη διάρκεια της οργανογένεσης. Όταν σε έγκυα ποντίκια χορηγήθηκε από το στόμα γκαμπαπεντίνη (500, 1.000 ή 3.000 mg/kg/ημέρα) κατά τη διάρκεια της οργανογένεσης, η σκελετική οστεοποίηση καθυστέρησε στο κρανίο, τα άκρα και τους σπονδύλους. Το NOEAD (500 mg/kg/ημέρα) ήταν κάτω από τη μέγιστη συνιστώμενη ανθρώπινη δόση (MRHD) των 3.600 mg/kg με βάση την επιφάνεια του σώματος (mg/m2). Σε μελέτες σε αρουραίους που έλαβαν από του στόματος γκαμπαπεντίνη (500 έως 2.000 mg/kg/ημέρα), παρατηρήθηκε αυξημένη συχνότητα εμφάνισης υδροουρητή και/ή υδρονέφρωσης σε όλες τις δόσεις που δοκιμάστηκαν. Όταν σε έγκυα κουνέλια χορηγήθηκε από το στόμα γκαμπαπεντίνη (60, 300 ή 1.500 mg/kg) κατά τη διάρκεια της οργανογένεσης, υπήρξε επίσης αυξημένη συχνότητα απώλειας εμβρύου σε όλες τις δόσεις που εξετάστηκαν. Υπάρχει ένα Μητρώο Έκθεσης Κύησης που παρακολουθεί τα αποτελέσματα σε εγκύους ασθενείς που εκτίθενται στη γκαμπαπεντίνη· για πληροφορίες σχετικά με το μητρώο, επισκεφθείτε τη διεύθυνση www.aedpregnancyregistry.org ή καλέστε στο 1-888-233-2334.
Gabapentin is excreted in human milk, however, it is unknown whether gabapentin derived from gabapentin etacab is excreted in human milk. The maximum dose to which a nursing infant can be exposed to gabapentin is approximately 1 mg/kg/day. There are no data on the effects of gabapentin on nursing infants or milk production. Consider the developmental and health benefits of breastfeeding, the mother's clinical need for gabapentin, and any adverse effects of gabapentin or the mother's underlying condition on the nursing infant. Use gabapentin in nursing women only if the benefits clearly outweigh the risks. [27986] [43322][43905] Infant doses of gabapentin excreted in breast milk were examined in 4 infants, 3 infants 2 to 3 weeks of age and 1 infant approximately 3 months of age. The mean daily maternal dose of gabapentin was 1,575 mg (range: 600 to 2,100 mg/day). Obtain a single sample of milk approximately 10 to 15 hours after the last dose. Assuming a breast milk consumption of 150 mL/kg/day, the relevant infant dose of gabapentin is estimated to be 0.2 to 1.3 mg/kg/day, approximately 1.3% to 3.8% of the weight-adjusted maternal dose . Two to three weeks postpartum, plasma gabapentin concentrations were detectable and within the normal quantitative range in 2 infants and undetectable in 1 infant. At 3 months, another infant had gabapentin plasma concentrations below the normal quantitative range. No side effects were reported. [62571]
Mechanism
The exact mechanism by which gabapentin exerts its anticonvulsant action is unknown but appears to be independent of its development as a GABA analog. Animal studies have shown that gabapentin binds with high affinity to the brain, but does not act on GABA receptors and does not inhibit sustained repetitive firing of sodium action potentials. Gabapentin appears to interact with cortical neurons of voltage-sensitive calcium channel accessory subunits, but the relationship of this effect to functional activity is unclear. Gabapentin crosses the lipid membranes of brain cells via the L-system amino acid transporter. In vitro actions include modulation of GABA synthase, glutamate synthase, glutamate decarboxylase, and branched-chain amino acid transaminase. In animals, gabapentin increases GABA responses at non-synaptic sites of neural tissue and decreases the release of monoamine neurotransmitters. In humans, NMR spectroscopy has shown that gabapentin increases GABA synthesis. In animal models, gabapentin was more effective in suppressing maximal shock-induced seizures and was also found to reduce the mean effective dose of phenytoin, carbamazepine, valproic acid, and primidone. Gabapentin attenuates pain responses in multiple animal models of hyperalgesia and prevents neuronal death in models of amyotrophic lateral sclerosis (ALS). Animal models have also shown the anxiolytic effect of gabapentin.
Pharmacokinetics
Gabapentin is given orally. Plasma concentrations > 2 mcg/mL are considered therapeutic; however, monitoring of gabapentin plasma concentrations is not necessary to optimize therapy. Protein binding of gabapentin is < 3%. Due to its high lipid solubility, gabapentin is easily distributed to the central nervous system. Gabapentin is not metabolized and is excreted intact in the urine. Patients with normal renal function receive 1200 to 3000 mg of immediate-release gabapentin daily with an elimination half-life of 5 to 7 hours.
Gabapentin and enacabi did not prolong QTc to clinically relevant levels at a dose of 6000 mg.
oral route
Gabapentin is rapidly absorbed in the proximal small intestine, in part, via the saturable L-amino acid transport system. Bioavailability decreases with increasing dose. The absolute bioavailability of immediate-release gabapentin was 60% for the 300 mg dose and 35% for the 1600 mg dose; bioavailability values for an extended-release tablet formulation (Gralise) were not reported. The mean bioavailability of Horizant (gabapentin enacabi) extended-release tablets in the fed state is approximately 75%. A pharmacokinetic study evaluated the bioavailability of immediate-release gabapentin after mixing the contents of an opened capsule with water, fruit juice, applesauce, or pudding. Food does not affect the absorption of immediate-release gabapentin, even when the capsules are opened for ease of administration. However, extended-release gabapentin should be taken with food; the rate and extent of absorption are increased when taken with a fatty meal. Unlike immediate-release gabapentin, Gralise extended-release tablets swell in gastric fluid, releasing the drug gradually, which slows the absorption of the drug. The use of 1800 mg of gabapentin extended-release (Gralise) once daily produced a higher Cmax (9,585 +/- 2,326 ng/mL) vs. 8,536 +/- - 1,715 ng/mL) and a longer median time to peak plasma concentration (8 [range : 3-12] hours vs. 2 [range: 1-5] hours). A steady state is achieved within 2 days of taking Horizant extended-release tablets daily.
Note: Due to different pharmacokinetic profiles, neither Gralise tablets nor Horizant extended-release tablets are interchangeable with other gabapentin formulations or with each other.