Literature DB >> 8681309

Gabapentin: pharmacokinetics, efficacy, and safety.

A Beydoun1, B M Uthman, J C Sackellares.   

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 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 trails. 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.

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Year:  1995        PMID: 8681309

Source DB:  PubMed          Journal:  Clin Neuropharmacol        ISSN: 0362-5664            Impact factor:   1.592


  14 in total

Review 1.  Calcium channel alpha2delta subunits: differential expression, function, and drug binding.

Authors:  Norbert Klugbauer; Else Marais; Franz Hofmann
Journal:  J Bioenerg Biomembr       Date:  2003-12       Impact factor: 2.945

2.  Pilot trial of gabapentin for the treatment of benzodiazepine abuse or dependence in methadone maintenance patients.

Authors:  John J Mariani; Robert J Malcolm; Agnieszka K Mamczur; Jean C Choi; Ronald Brady; Edward Nunes; Frances R Levin
Journal:  Am J Drug Alcohol Abuse       Date:  2016-03-10       Impact factor: 3.829

3.  A randomized double-blind pilot trial of gabapentin versus placebo to treat alcohol dependence and comorbid insomnia.

Authors:  Kirk J Brower; Hyungjin Myra Kim; Stephen Strobbe; Maher A Karam-Hage; Flavia Consens; Robert A Zucker
Journal:  Alcohol Clin Exp Res       Date:  2008-06-06       Impact factor: 3.455

4.  Effect of mushroom diet on pharmacokinetics of gabapentin in healthy Chinese subjects.

Authors:  Dorothy Su Lin Toh; Lie Michael George Limenta; Jie Yin Yee; Ling-Zhi Wang; Boon-Cher Goh; Michael Murray; Edmund Jon Deoon Lee
Journal:  Br J Clin Pharmacol       Date:  2014-07       Impact factor: 4.335

5.  Pharmacokinetics and metabolism of 14C-levetiracetam, a new antiepileptic agent, in healthy volunteers.

Authors:  Margherita Strolin Benedetti; Rhys Whomsley; Jean-Marie Nicolas; Colin Young; Eugène Baltes
Journal:  Eur J Clin Pharmacol       Date:  2003-10-07       Impact factor: 2.953

Review 6.  New and emerging prophylactic agents for migraine.

Authors:  Abouch V Krymchantowski; Marcelo E Bigal; Pedro F Moreira
Journal:  CNS Drugs       Date:  2002       Impact factor: 5.749

7.  Preventive agents for migraine: focus on the antiepileptic drugs.

Authors:  R Shahien; K Beiruti
Journal:  J Cent Nerv Syst Dis       Date:  2012-02-26

8.  Attenuation of the pressor response to direct laryngoscopy and tracheal Intubation: oral clonidine vs. oral gabapentin premedication.

Authors:  Kamran Montazeri; Parviz Kashefi; Azim Honarmand; Mohammadreza Safavi; Anahita Hirmanpour
Journal:  J Res Med Sci       Date:  2011-03       Impact factor: 1.852

9.  Pharmacokinetic effects of simultaneous administration of single-dose gabapentin 500 mg and zolpidem tartrate 10 mg in healthy volunteers: a randomized, open-label, crossover trial.

Authors:  Lawrence A Galitz; Shyamalie Jayawardena; Sandy A Furey
Journal:  Drugs R D       Date:  2015-03

10.  Mixed effects modeling of weight change associated with placebo and pregabalin administration.

Authors:  Bill Frame; Stuart L Beal; Raymond Miller; Jeannette Barrett; Paula Burger
Journal:  J Pharmacokinet Pharmacodyn       Date:  2007-08-10       Impact factor: 2.410

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