Benowitz N L
Division of Clinical Pharmacology and Experimental Therapeutics, University of California, San Francisco.
Pharmacol Toxicol. 1993 Jan;72(1):3-12. doi: 10.1111/j.1600-0773.1993.tb01331.x.
Cocaine abuse has produced a major epidemic health problem in North America in the 1980s. The abuse of cocaine is maintained by the drug's effects on brain reward systems, mediated at least in part by its dopaminergic action. The patterns and consequences of use are best understood by considering the pharmacokinetics (rapid absorption and delivery to the brain, relatively short half-life) and the pharmacodynamics (intense central and peripheral neural stimulation). Cocaine is used therapeutically as a topical and local anaesthetic. Toxicity occurs primarily in cocaine abusers, but also occasionally after therapeutic dosing. Medical complications reflect primarily excessive central nervous system stimulation and excessive vasoconstriction, the latter resulting in severe hypertension and/or organ ischaemia with associated organ injury. Most deaths that result from medical complications of cocaine intoxication are sudden and occur before medical intervention is possible. Other complications of cocaine abuse with severe personal and social consequences include traumatic deaths and injuries, and reproductive disturbances, as well as transmission of infectious diseases, especially AIDS. Cocaine addiction is clearly a problem, although the number of addicts is unknown. Pharmacologic treatment of cocaine addiction has as yet been unsuccessful. Psychosocial approaches remain the mainstay of therapy.
20世纪80年代,可卡因滥用在北美引发了一场重大的流行性健康问题。可卡因的滥用是由该药物对大脑奖赏系统的作用维持的,这至少部分是由其多巴胺能作用介导的。通过考虑药代动力学(快速吸收并输送到大脑,半衰期相对较短)和药效学(强烈的中枢和外周神经刺激),可以最好地理解使用模式及其后果。可卡因在治疗上用作局部麻醉剂。毒性主要发生在可卡因滥用者身上,但在治疗用药后也偶尔会出现。医学并发症主要反映为中枢神经系统过度刺激和过度血管收缩,后者会导致严重高血压和/或器官缺血以及相关的器官损伤。可卡因中毒的医学并发症导致的大多数死亡都是突然发生的,且在进行医疗干预之前就已出现。可卡因滥用的其他并发症会带来严重的个人和社会后果,包括创伤性死亡和伤害、生殖紊乱以及传染病传播,尤其是艾滋病。尽管成瘾者的数量未知,但可卡因成瘾显然是一个问题。可卡因成瘾的药物治疗迄今尚未成功。心理社会方法仍然是治疗的主要手段。