Description

Simple

A medication used to treat certain types of seizures and nerve pain.

Clinical

An anticonvulsant medication used in the management of peripheral neuropathic pains, postherpetic neuralgia, and partial-onset seizures.

Overview

Gabapentin is a structural analogue of the inhibitory neurotransmitter gamma-aminobutyric acid ([GABA]) that was first approved for use in the United States in 1993.[16] It was originally developed as a novel anti-epileptic for the treatment of certain types of seizures[14,5] - today it is also widely used to treat neuropathic pain.[8,10] Gabapentin has some stark advantages as compared with... Read more

Pharmacology

Indication

In the United States, gabapentin is officially indicated for the treatment of postherpetic neuralgia in adults and for the adjunctive treatment of partial-onset seizures, with or without secondary generalization, in patients 3 years of age and older.[ Read more

Pharmacodynamic

Gabapentin is an anti-convulsant medication that inhibits the release of excitatory neurotransmitters, allowing for its use against pathologic neurotransmission such as that seen in neuropathic pain and seizure disorders.[ Read more

Mechanism of action

The precise mechanism through which gabapentin exerts its therapeutic effects is unclear.[16,17] The primary mode of... Read more

Absorption

Absorption of gabapentin is thought to occur solely via facilitated transport by the LAT1 transporter within the intestines.[ Read more

Protein binding

Less than 3% of an orally administered dose of gabapentin is bound to plasma proteins.[16,17]

Volume of distribution

The apparent volume of distribution of gabapentin after IV administration is 58±6 L.[16,17] The drug is found in the... Read more

Clearance

Both the plasma clearance and renal clearance of gabapentin are directly proportional to the patient's creatinine clearance due to its primarily renal elimination.[16, Read more

Half life

The elimination t1/2 of gabapentin in patients with normal renal function is 5-7 hours.[16,17, Read more

Route of elimination

Gabapentin is eliminated solely in the urine as unchanged drug.[16,17] Cimetidine, an inhibitor of renal tubular sec... Read more

Toxicity

The oral TDLo of gabapentin in humans is 2.86 mg/kg and the LD50 in rats has been found to be >8000 mg/kg.[21] Symptoms of overdose are consistent with the drug's adverse effect profile and involve CN... Read more

Adverse Effects

Contraindications

  • Hypersensitivity:
    • true
  • Regions: US

Food Interactions

  • Avoid alcohol.
  • Take without regard to meals.

Interactions

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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
2,5-Dimethoxy-4-ethylthioamphetamine
The risk or severity of adverse effects can be increased when Gabapentin is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
3-isobutyl-1-methyl-7H-xanthine
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.
4-Bromo-2,5-dimethoxyamphetamine
The risk or severity of adverse effects can be increased when Gabapentin is combined with 4-Bromo-2,5-dimethoxyamphetamine.
4-Methoxyamphetamine
The risk or severity of adverse effects can be increased when Gabapentin is combined with 4-Methoxyamphetamine.
5-methoxy-N,N-dimethyltryptamine
The risk or severity of adverse effects can be increased when Gabapentin is combined with 5-methoxy-N,N-dimethyltryptamine.
6-O-benzylguanine
Gabapentin may increase the excretion rate of 6-O-benzylguanine which could result in a lower serum level and potentially a reduction in efficacy.
7-Deazaguanine
Gabapentin may increase the excretion rate of 7-Deazaguanine which could result in a lower serum level and potentially a reduction in efficacy.
7-Nitroindazole
The risk or severity of adverse effects can be increased when Gabapentin is combined with 7-Nitroindazole.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline
The risk or severity of adverse effects can be increased when Gabapentin is combined with 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline.
7,9-Dimethylguanine
Gabapentin may increase the excretion rate of 7,9-Dimethylguanine which could result in a lower serum level and potentially a reduction in efficacy.
8-azaguanine
Gabapentin may increase the excretion rate of 8-azaguanine which could result in a lower serum level and potentially a reduction in efficacy.
8-chlorotheophylline
Gabapentin may increase the excretion rate of 8-chlorotheophylline which could result in a lower serum level and potentially a reduction in efficacy.
9-Deazaguanine
Gabapentin may increase the excretion rate of 9-Deazaguanine which could result in a lower serum level and potentially a reduction in efficacy.
9-Methylguanine
Gabapentin may increase the excretion rate of 9-Methylguanine which could result in a lower serum level and potentially a reduction in efficacy.
Acefylline
Gabapentin may increase the excretion rate of Acefylline which could result in a lower serum level and potentially a reduction in efficacy.
Acepromazine
The risk or severity of adverse effects can be increased when Gabapentin is combined with Acepromazine.
Aceprometazine
The risk or severity of adverse effects can be increased when Gabapentin is combined with Aceprometazine.
Acetazolamide
The risk or severity of adverse effects can be increased when Acetazolamide is combined with Gabapentin.
Acetophenazine
The risk or severity of adverse effects can be increased when Gabapentin is combined with Acetophenazine.
Acetylglycinamide chloral hydrate
The risk or severity of adverse effects can be increased when Gabapentin is combined with Acetylglycinamide chloral hydrate.
21 References
  1. 1 . Yagi T, Naito T, Mino Y, Umemura K, Kawakami J: Impact of concomitant antacid administration on gabapentin plasma exposure and oral bioavailability in healthy adult subjects. Drug Metab Pharmacokinet. 2012;27(2):248-54. Epub 2012 Jan 13.PubMed: 22240839
  2. 2 . Czapinski P, Blaszczyk B, Czuczwar SJ: Mechanisms of action of antiepileptic drugs. Curr Top Med Chem. 2005;5(1):3-14. doi: 10.2174/1568026053386962.PubMed: 15638774
  3. 3 . Patsalos PN, Berry DJ, Bourgeois BF, Cloyd JC, Glauser TA, Johannessen SI, Leppik IE, Tomson T, Perucca E: Antiepileptic drugs--best practice guidelines for therapeutic drug monitoring: a position paper by the subcommission on therapeutic drug monitoring, ILAE Commission on Therapeutic Strategies. Epilepsia. 2008 Jul;49(7):1239-76. doi: 10.1111/j.1528-1167.2008.01561.x.PubMed: 18397299
  4. 4 . Abou-Khalil BW: Antiepileptic Drugs. Continuum (Minneap Minn). 2016 Feb;22(1 Epilepsy):132-56. doi: 10.1212/CON.0000000000000289.PubMed: 26844734
  5. 5 . Bockbrader HN, Wesche D, Miller R, Chapel S, Janiczek N, Burger P: A comparison of the pharmacokinetics and pharmacodynamics of pregabalin and gabapentin. Clin Pharmacokinet. 2010 Oct;49(10):661-9. doi: 10.2165/11536200-000000000-00000.PubMed: 20818832
  6. 6 . Goto M, Miyahara I, Hirotsu K, Conway M, Yennawar N, Islam MM, Hutson SM: Structural determinants for branched-chain aminotransferase isozyme-specific inhibition by the anticonvulsant drug gabapentin. J Biol Chem. 2005 Nov 4;280(44):37246-56. Epub 2005 Sep 1.PubMed: 16141215
  7. 7 . Dickens D, Webb SD, Antonyuk S, Giannoudis A, Owen A, Radisch S, Hasnain SS, Pirmohamed M: Transport of gabapentin by LAT1 (SLC7A5). Biochem Pharmacol. 2013 Jun 1;85(11):1672-83. doi: 10.1016/j.bcp.2013.03.022. Epub 2013 Apr 6.PubMed: 23567998
  8. 8 . Maneuf YP, Luo ZD, Lee K: alpha2delta and the mechanism of action of gabapentin in the treatment of pain. Semin Cell Dev Biol. 2006 Oct;17(5):565-70. Epub 2006 Sep 24.PubMed: 17067834
  9. 9 . Hendrich J, Van Minh AT, Heblich F, Nieto-Rostro M, Watschinger K, Striessnig J, Wratten J, Davies A, Dolphin AC: Pharmacological disruption of calcium channel trafficking by the alpha2delta ligand gabapentin. Proc Natl Acad Sci U S A. 2008 Mar 4;105(9):3628-33. doi: 10.1073/pnas.0708930105. Epub 2008 Feb 25.PubMed: 18299583
  10. 10 . Kukkar A, Bali A, Singh N, Jaggi AS: Implications and mechanism of action of gabapentin in neuropathic pain. Arch Pharm Res. 2013 Mar;36(3):237-51. doi: 10.1007/s12272-013-0057-y. Epub 2013 Feb 24.PubMed: 23435945
  11. 11 . Cheng JK, Chen CC, Yang JR, Chiou LC: The antiallodynic action target of intrathecal gabapentin: Ca2+ channels, KATP channels or N-methyl-d-aspartic acid receptors? Anesth Analg. 2006 Jan;102(1):182-7.PubMed: 16368827
  12. 12 . Martins DF, Prado MR, Daruge-Neto E, Batisti AP, Emer AA, Mazzardo-Martins L, Santos AR, Piovezan AP: Caffeine prevents antihyperalgesic effect of gabapentin in an animal model of CRPS-I: evidence for the involvement of spinal adenosine A1 receptor. J Peripher Nerv Syst. 2015 Dec;20(4):403-9. doi: 10.1111/jns.12149.PubMed: 26456872
  13. 13 . Manville RW, Abbott GW: Gabapentin Is a Potent Activator of KCNQ3 and KCNQ5 Potassium Channels. Mol Pharmacol. 2018 Oct;94(4):1155-1163. doi: 10.1124/mol.118.112953. Epub 2018 Jul 18.PubMed: 30021858
  14. 14 . Sills GJ: The mechanisms of action of gabapentin and pregabalin. Curr Opin Pharmacol. 2006 Feb;6(1):108-13. doi: 10.1016/j.coph.2005.11.003. Epub 2005 Dec 22.PubMed: 16376147
  15. 15 . Zuchora B, Wielosz M, Urbanska EM: Adenosine A1 receptors and the anticonvulsant potential of drugs effective in the model of 3-nitropropionic acid-induced seizures in mice. Eur Neuropsychopharmacol. 2005 Jan;15(1):85-93.PubMed: 15572277
  16. 16 . FDA Approved Drugs: Gabapentin Link
  17. 17 . DPD Approved Drugs: Gabapentin Link
  18. 18 . MedSafe NZ: Gabapentin Link
  19. 19 . EMA Approved Drugs: Gabapentin Link
  20. 20 . FDA Approved Drugs: Gabapentin XR Link
  21. 21 . CaymenChem: Gabapentin MSDS Link