Reeves Roy R, Burke Randy S
Mental Health Service, G.V. (Sonny) Montgomery VA Medical Center, 1500 E. Woodrow Wilson Drive, Jackson, MS 29216, USA.
Curr Drug Abuse Rev. 2010 Mar;3(1):33-8. doi: 10.2174/1874473711003010033.
Carisoprodol (N-isopropyl-2 methyl-2-propyl-1,3-propanediol dicarbamate; N-isopropylmeprobamate) is a centrally acting skeletal muscle relaxant whose primary active metabolite is meprobamate, a substance with well established abuse potential similar to that of benzodiazepines. A number of reports show that carisoprodol has been abused for its sedative and relaxant effects, to augment or alter the effects of other drugs, and by the intentional combination of carisoprodol and other noncontrolled medications because of the relative ease (as compared to controlled substances) of obtaining prescriptions. The diversion and abuse of carisoprodol and its adverse health effects appear to have dramatically increased over the last several years. Clinicians have begun to see a withdrawal syndrome consisting of insomnia, vomiting, tremors, muscle twitching, anxiety, and ataxia in patients who abruptly cease intake of large doses of carisoprodol. Hallucinations and delusions may also occur. The withdrawal symptoms are very similar to those previously described for meprobamate withdrawal, suggesting that what may actually be occurring is withdrawal from meprobamate accumulated as a result of intake of excessive amounts of carisoprodol. However carisoprodol itself is capable of modulating GABA(A) function, and this may contribute both to the drugs abuse potential and to the occurrence of a withdrawal syndrome with abrupt cessation of intake. Carisoprodol has been classified as a controlled substance in several states in the US and restrictions on the use of the drug have been imposed in some European countries. Carisoprodol is metabolized to a controlled substance, has clear evidence of abuse potential and increasing incidence of abuse, and has shown evidence of a withdrawal syndrome with abrupt cessation from intake. This article will discuss the abuse potential of carisoprodol and the associated withdrawal syndrome, and consider implications for future use of the drug.
卡立普多(N-异丙基-2-甲基-2-丙基-1,3-丙二醇二氨基甲酸酯;N-异丙基眠尔通)是一种中枢性骨骼肌松弛剂,其主要活性代谢产物是眠尔通,这是一种具有与苯二氮䓬类药物类似的、已被充分证实的滥用潜力的物质。一些报告显示,卡立普多因其镇静和松弛作用而被滥用,用于增强或改变其他药物的效果,以及由于获取处方相对容易(与管制药物相比)而被故意将卡立普多与其他非管制药物合用。在过去几年中,卡立普多的转移和滥用及其对健康的不良影响似乎急剧增加。临床医生开始在突然停止大量服用卡立普多的患者中看到一种戒断综合征,包括失眠、呕吐、震颤、肌肉抽搐、焦虑和共济失调。还可能出现幻觉和妄想。这些戒断症状与先前描述的眠尔通戒断症状非常相似,这表明实际发生的可能是由于摄入过量卡立普多而积累的眠尔通的戒断。然而,卡立普多本身能够调节GABA(A)功能,这可能既导致了该药物的滥用潜力,也导致了突然停药时出现戒断综合征。在美国的几个州,卡立普多已被列为管制物质,在一些欧洲国家也对该药物的使用施加了限制。卡立普多可代谢为一种管制物质,有明确的滥用潜力证据且滥用发生率不断增加,并且已显示出突然停药会出现戒断综合征的证据。本文将讨论卡立普多的滥用潜力和相关的戒断综合征,并考虑该药物未来使用的影响。