Gabapentin. A Review of Its Pharmacological Properties and Clinical Potential in Epilepsy

普瑞巴林 麻醉 药物治疗 拉莫三嗪 卡马西平 神经病理性疼痛 神经学 临床试验
作者
Karen L. Goa,Eugene M. Sorkin
出处
期刊:Drugs [Adis, Springer Healthcare]
卷期号:46 (3): 409-427 被引量:285
标识
DOI:10.2165/00003495-199346030-00007
摘要

Gabapentin is an antiepileptic drug with an unknown mechanism of action apparently dissimilar to that of other antiepileptic agents, and possessing some desirable pharmacokinetic traits. The drug is not protein bound, is not metabolised and does not induce liver enzymes, diminishing the likelihood of drug interactions with other antiepileptic agents and drugs such as oral contraceptives. Although gabapentin is a structural analogue of the neurotransmitter gamma-aminobutyric acid (GABA), which does not cross the blood-brain barrier, gabapentin penetrates into the CNS and its activity is seemingly distinct from GABA-related effects. Present clinical evaluation is largely restricted to proof of efficacy trials of gabapentin as add-on therapy in patients with partial epilepsy resistant to conventional treatment. Gabapentin (usually 600 to 1800 mg/day) provides notable benefit, reducing seizure frequency by > or = 50% in 18 to 28% of patients with refractory partial seizures, as shown in 3 double-blind, placebo-controlled trials. Overall, seizure frequency decreased by 18 to 32% during 3-month treatment periods. Patients with complex partial seizures, and partial seizures secondarily generalised, are particularly likely to respond to gabapentin. Current experience with the drug in other seizure types, and as monotherapy, is limited. Mild adverse events, commonly somnolence, fatigue, ataxia and dizziness, have been reported in about 75% of gabapentin recipients. While the drug has been well tolerated when administered to a few patients for periods of up to 5 years, its long term tolerability profile has yet to be fully expounded. Thus, with its favourable pharmacokinetic profile, and efficacy in some refractory patients, gabapentin is poised to fill a niche as an adjunct to the treatment of partial epilepsy. Promising results obtained thus far warrant further work to clarify its long term tolerability, its possible efficacy in other seizure types, its position relative to other agents and its use as monotherapy. In the meantime, gabapentin is likely to provide a much-needed option in a therapeutic area requiring complex management.
最长约 10秒,即可获得该文献文件

科研通智能强力驱动
Strongly Powered by AbleSci AI
更新
PDF的下载单位、IP信息已删除 (2025-6-4)

科研通是完全免费的文献互助平台,具备全网最快的应助速度,最高的求助完成率。 对每一个文献求助,科研通都将尽心尽力,给求助人一个满意的交代。
实时播报
ccchengzi完成签到,获得积分10
刚刚
乐乐应助wcy采纳,获得10
1秒前
2秒前
hahahaweiwei完成签到,获得积分10
2秒前
chengzi202发布了新的文献求助10
2秒前
鹿丫丫发布了新的文献求助10
3秒前
Nougat发布了新的文献求助10
3秒前
害羞大碗完成签到,获得积分10
3秒前
3秒前
大美女发布了新的文献求助10
3秒前
香蕉觅云应助刚刚好采纳,获得10
4秒前
4秒前
所所应助科研通管家采纳,获得10
4秒前
4秒前
我是老大应助科研通管家采纳,获得10
4秒前
4秒前
Lucas应助科研通管家采纳,获得10
4秒前
4秒前
wanwan应助科研通管家采纳,获得10
4秒前
小牧鱼发布了新的文献求助10
4秒前
4秒前
王球球完成签到,获得积分10
4秒前
4秒前
4秒前
小蘑菇应助科研通管家采纳,获得10
5秒前
5秒前
5秒前
5秒前
羊羊羊发布了新的文献求助10
5秒前
5秒前
yiyi131发布了新的文献求助10
5秒前
Johnpick应助纳斯达克采纳,获得10
5秒前
5秒前
5秒前
5秒前
5秒前
5秒前
临河盗龙完成签到,获得积分10
7秒前
饱满的尔云完成签到,获得积分10
7秒前
8秒前
高分求助中
The Mother of All Tableaux: Order, Equivalence, and Geometry in the Large-scale Structure of Optimality Theory 3000
Social Research Methods (4th Edition) by Maggie Walter (2019) 2390
A new approach to the extrapolation of accelerated life test data 1000
北师大毕业论文 基于可调谐半导体激光吸收光谱技术泄漏气体检测系统的研究 390
Phylogenetic study of the order Polydesmida (Myriapoda: Diplopoda) 370
Robot-supported joining of reinforcement textiles with one-sided sewing heads 360
Atlas of Interventional Pain Management 300
热门求助领域 (近24小时)
化学 材料科学 医学 生物 工程类 有机化学 生物化学 物理 内科学 纳米技术 计算机科学 化学工程 复合材料 遗传学 基因 物理化学 催化作用 冶金 细胞生物学 免疫学
热门帖子
关注 科研通微信公众号,转发送积分 4004302
求助须知:如何正确求助?哪些是违规求助? 3543838
关于积分的说明 11288580
捐赠科研通 3280550
什么是DOI,文献DOI怎么找? 1809210
邀请新用户注册赠送积分活动 885098
科研通“疑难数据库(出版商)”最低求助积分说明 810708