Gabapentin: Pharmacokinetics, efficacy, and safety

A. Beydoun, B. M. Uthman, J. C. Sackellares

Research output: Contribution to journalArticlepeer-review

102 Scopus citations

Abstract

Gabapentin is a new antiepileptic drug (AED) with an attractive pharmacokinetic profile. It is absorbed by an active and saturable transport system, and has a high volume of distribution. Gabapentin is not bound to plasma proteins, does not induce hepatic enzymes and is not metabolized. At steady state, it has a half-life of 6-8 h, and is eliminated unchanged by the renal route with a plasma clearance proportional to the creatinine clearance. It is devoid of significant drug-drug interactions when administered with the established AEDs or with oral contraceptives. Gabapentin used as an add-on AED significantly reduced the frequency of partial seizures and secondarily generalized tonic-clonic seizures in three large double-blind, placebo- controlled, parallel-group clinical trials. It is well tolerated, with transient somnolence and dizziness being the most frequent adverse effects. Although the mechanism of action of gabapentin is not fully established, there is strong evidence to suggest a novel mechanism of action. Gabapentin is a unique and promising drug that could improve the quality of life of patients with epilepsy and is a welcome addition to the armamentarium of currently available AEDs for the treatment of patients with seizures of partial onset.

Original languageEnglish (US)
Pages (from-to)469-481
Number of pages13
JournalClinical neuropharmacology
Volume18
Issue number6
DOIs
StatePublished - 1995
Externally publishedYes

Keywords

  • Efficacy
  • Gabapentin
  • Pharmacokinetics
  • Review
  • Safety

ASJC Scopus subject areas

  • Pharmacology
  • Clinical Neurology
  • Pharmacology (medical)

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