Gabapentin


Description

Gabapentin (brand name Neurontin) is a medication originally developed for the treatment of epilepsy. Presently, gabapentin is widely used to relieve pain, especially neuropathic pain. Gabapentin is well tolerated in most patients, has a relatively m...

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Pharmacology

Indication

For the management of postherpetic neuralgia in adults and as adjunctive therapy in the treatment of... Read more

Pharmacodynamic

Gabapentin, an analog of GABA, is used as an anticonvulsant to treat partial seizures, amyotrophic l... Read more

Mechanismofaction

Gabapentin interacts with cortical neurons at auxillary subunits of voltage-sensitive calcium channe... Read more

Absorption

Rapid. Absorbed in part by the L-amino acid transport system, which is a carrier-mediated, saturable... Read more

Proteinbinding

Less than 3% of gabapentin circulates bound to plasma protein.

Volumeofdistribution

58±6 L

Clearance

190 mL/min

Halflife

5-7 hours

Routeofelimination

Gabapentin is eliminated from the systemic circulation by renal excretion as unchanged drug.
Gabape...
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Toxicity

Symptoms of overdose include ataxia, labored breathing, ptosis, sedation, hypoactivity, and excitati... Read more


Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Dizziness US
  • Kind: experimental
    • Percent: 28%
  • Kind: placebo
    • Percent: 7.5%
  • Clinical Trial
    Somnolence US
  • Kind: experimental
    • Percent: 21.4%
  • Kind: placebo
    • Percent: 5.3%
  • Clinical Trial
    Somnolence US
  • Kind: experimental
    • Percent: 19.3%
  • Kind: placebo
    • Percent: 8.7%
  • Clinical Trial
    Dizziness US
  • Kind: experimental
    • Percent: 17.1%
  • Kind: placebo
    • Percent: 6.9%
  • Clinical Trial
    Ataxia US
  • Kind: experimental
    • Percent: 12.5%
  • Kind: placebo
    • Percent: 5.6%
  • Clinical Trial
    Fatigue US
  • Kind: experimental
    • Percent: 11%
  • Kind: placebo
    • Percent: 5%
  • Clinical Trial
    Viral Infection US
  • Kind: experimental
    • Percent: 10.9%
  • Kind: placebo
    • Percent: 3.1%
  • Clinical Trial
    Fever US
  • Kind: experimental
    • Percent: 10.1%
  • Kind: placebo
    • Percent: 3.1%
  • Clinical Trial
    Somnolence US
  • Kind: experimental
    • Percent: 8.4%
  • Kind: placebo
    • Percent: 4.7%
  • Clinical Trial
    Vomiting US
  • Kind: experimental
    • Percent: 8.4%
  • Kind: placebo
    • Percent: 7%
  • Clinical Trial
    Nausea US
  • Kind: experimental
    • Percent: 8.4%
  • Kind: placebo
    • Percent: 7%
  • Clinical Trial
    Peripheral Edema US
  • Kind: experimental
    • Percent: 8.3%
  • Kind: placebo
    • Percent: 2.2%
  • Clinical Trial
    Nystagmus US
  • Kind: experimental
    • Percent: 8.3%
  • Kind: placebo
    • Percent: 4%
  • Clinical Trial
    Hostility US
  • Kind: experimental
    • Percent: 7.6%
  • Kind: placebo
    • Percent: 2.3%
  • Clinical Trial
    Tremor US
  • Kind: experimental
    • Percent: 6.8%
  • Kind: placebo
    • Percent: 3.2%
  • Clinical Trial
    Diplopia US
  • Kind: experimental
    • Percent: 5.9%
  • Kind: placebo
    • Percent: 1.9%
  • Clinical Trial
    Athenia US
  • Kind: experimental
    • Percent: 5.7%
  • Kind: placebo
    • Percent: 4.8%
  • Clinical Trial
    Diarrhea US
  • Kind: experimental
    • Percent: 5.7%
  • Kind: placebo
    • Percent: 3.1%
  • Clinical Trial
    Infection US
  • Kind: experimental
    • Percent: 5.1%
  • Kind: placebo
    • Percent: 3.5%
  • Clinical Trial
    Dry Mouth US
  • Kind: experimental
    • Percent: 4.8%
  • Kind: placebo
    • Percent: 1.3%
  • Clinical Trial
    Amblyopia US
  • Kind: experimental
    • Percent: 4.2%
  • Kind: placebo
    • Percent: 1.1%
  • Clinical Trial
    Emotional Lability US
  • Kind: experimental
    • Percent: 4.2%
  • Kind: placebo
    • Percent: 1.6%
  • Clinical Trial
    Rhinitis US
  • Kind: experimental
    • Percent: 4.1%
  • Kind: placebo
    • Percent: 3.7%
  • Clinical Trial
    Nausea US
  • Kind: experimental
    • Percent: 3.9%
  • Kind: placebo
    • Percent: 3.1%
  • Clinical Trial
    Constipation US
  • Kind: experimental
    • Percent: 3.9%
  • Kind: placebo
    • Percent: 1.8%
  • Clinical Trial
    Weight increase US
  • Kind: experimental
    • Percent: 3.4%
  • Kind: placebo
    • Percent: 0.8%
  • Clinical Trial
    Bronchitis US
  • Kind: experimental
    • Percent: 3.4%
  • Kind: placebo
    • Percent: 0.8%
  • Clinical Trial
    Fatigue US
  • Kind: experimental
    • Percent: 3.4%
  • Kind: placebo
    • Percent: 1.6%
  • Clinical Trial
    Ataxia US
  • Kind: experimental
    • Percent: 3.3%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Vomiting US
  • Kind: experimental
    • Percent: 3.3%
  • Kind: placebo
    • Percent: 1.8%
  • Clinical Trial
    Headache US
  • Kind: experimental
    • Percent: 3.3%
  • Kind: placebo
    • Percent: 3.1%
  • Clinical Trial
    Accidental injury US
  • Kind: experimental
    • Percent: 3.3%
  • Kind: placebo
    • Percent: 1.3%
  • Clinical Trial
    Weight increase US
  • Kind: experimental
    • Percent: 2.9%
  • Kind: placebo
    • Percent: 1.6%
  • Clinical Trial
    Pharyngitis US
  • Kind: experimental
    • Percent: 2.8%
  • Kind: placebo
    • Percent: 1.6%
  • Clinical Trial
    Thinking abnormal US
  • Kind: experimental
    • Percent: 2.7%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Amblyopia US
  • Kind: experimental
    • Percent: 2.7%
  • Kind: placebo
    • Percent: 0.9%
  • Clinical Trial
    Abdominal Pain US
  • Kind: experimental
    • Percent: 2.7%
  • Kind: placebo
    • Percent: 2.6%
  • Clinical Trial
    Respiratory Infection US
  • Kind: experimental
    • Percent: 2.5%
  • Kind: placebo
    • Percent: 0.8%
  • Clinical Trial
    Hyperkinesia US
  • Kind: experimental
    • Percent: 2.5%
  • Kind: placebo
    • Percent: 0.8%
  • Clinical Trial
    Dizziness US
  • Kind: experimental
    • Percent: 2.5%
  • Kind: placebo
    • Percent: 1.6%
  • Clinical Trial
    Nervousness US
  • Kind: experimental
    • Percent: 2.4%
  • Kind: placebo
    • Percent: 1.9%
  • Clinical Trial
    Dysarthria US
  • Kind: experimental
    • Percent: 2.4%
  • Kind: placebo
    • Percent: 0.5%
  • Clinical Trial
    Dyspepsia US
  • Kind: experimental
    • Percent: 2.2%
  • Kind: placebo
    • Percent: 0.5%
  • Clinical Trial
    Amnesia US
  • Kind: experimental
    • Percent: 2.2%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Flatulence US
  • Kind: experimental
    • Percent: 2.1%
  • Kind: placebo
    • Percent: 1.8%
  • Clinical Trial
    Myalgia US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 1.9%
  • Clinical Trial
    Otitis Media US
  • Kind: experimental
    • Value: >0.05%
  • Kind: experimental
    • Percent: >2%
    • Value: >0.05%
  • Clinical Trial
    Anorexia US
  • Kind: experimental
    • Value: >0.05%
  • Kind: experimental
    • Percent: >2%
    • Value: >0.05%
  • Clinical Trial
    Coughing US
  • Kind: experimental
    • Value: >0.05%
  • Kind: experimental
    • Percent: >2%
    • Value: >0.05%
  • Clinical Trial
    Rhinitis US
  • Kind: experimental
    • Percent: >2%
    • Value: >0.05%
  • Kind: experimental
    • Value: >0.05%
  • Clinical Trial

    Contraindications

    Information currently not available.

    Food Interactions

    • Avoid alcohol.
    • Take without regard to meals.

    Interactions

    Type in a drug name to check for interaction with Gabapentin

    The metabolism of (R)-warfarin can be decreased when combined with Gabapentin.
    The metabolism of (S)-Warfarin can be decreased when combined with Gabapentin.
    The risk or severity of hypoglycemia can be increased when Gabapentin is combined with 2,4-thiazolidinedione.
    The risk or severity of adverse effects can be increased when Gabapentin is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
    Gabapentin may increase the excretion rate of 3-isobutyl-1-methyl-7H-xanthine which could result in a lower serum level and potentially a reduction in efficacy.
    The metabolism of 3,5-diiodothyropropionic acid can be decreased when combined with Gabapentin.
    The risk or severity of adverse effects can be increased when Gabapentin is combined with 4-Bromo-2,5-dimethoxyamphetamine.
    The risk or severity of adverse effects can be increased when Gabapentin is combined with 4-Bromo-2,5-dimethoxyphenethylamine.
    The metabolism of 4-hydroxycoumarin can be decreased when combined with Gabapentin.
    The risk or severity of adverse effects can be increased when Gabapentin is combined with 4-Methoxyamphetamine.
    The metabolism of 5-androstenedione can be decreased when combined with Gabapentin.
    The risk or severity of adverse effects can be increased when Gabapentin is combined with 5-methoxy-N,N-dimethyltryptamine.
    The metabolism of Gabapentin can be decreased when combined with 6-Deoxyerythronolide B.
    Gabapentin may increase the excretion rate of 6-O-benzylguanine which could result in a lower serum level and potentially a reduction in efficacy.
    Gabapentin may increase the excretion rate of 7-Deazaguanine which could result in a lower serum level and potentially a reduction in efficacy.
    The metabolism of Gabapentin can be decreased when combined with 7-ethyl-10-hydroxycamptothecin.
    The risk or severity of adverse effects can be increased when Gabapentin is combined with 7-Nitroindazole.
    The risk or severity of adverse effects can be increased when Gabapentin is combined with 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline.
    Gabapentin may increase the excretion rate of 7,9-Dimethylguanine which could result in a lower serum level and potentially a reduction in efficacy.
    Gabapentin may increase the excretion rate of 8-azaguanine which could result in a lower serum level and potentially a reduction in efficacy.

    References

    • 1 . Mathew NT, Rapoport A, Saper J, Magnus L, Klapper J, Ramadan N, Stacey B, Tepper S: Efficacy of gabapentin in migraine prophylaxis. Headache. 2001 Feb;41(2):119-28. [PubMed: 11251695]
    • 2 . Backonja MM, Serra J: Pharmacologic management part 1: better-studied neuropathic pain diseases. Pain Med. 2004 Mar;5 Suppl 1:S28-47. [PubMed: 14996228]
    • 3 . Choudhuri I, Sarvananthan N, Gottlob I: Survey of management of acquired nystagmus in the United Kingdom. Eye (Lond). 2007 Sep;21(9):1194-7. Epub 2006 May 26. [PubMed: 16732211]
    • 4 . Pande AC, Crockatt JG, Janney CA, Werth JL, Tsaroucha G: Gabapentin in bipolar disorder: a placebo-controlled trial of adjunctive therapy. Gabapentin Bipolar Disorder Study Group. Bipolar Disord. 2000 Sep;2(3 Pt 2):249-55. [PubMed: 11249802]
    • 5 . Su TZ, Feng MR, Weber ML: Mediation of highly concentrative uptake of pregabalin by L-type amino acid transport in Chinese hamster ovary and Caco-2 cells. J Pharmacol Exp Ther. 2005 Jun;313(3):1406-15. Epub 2005 Mar 15. [PubMed: 15769862]

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