McCance E F, Price L H, Kosten T R, Jatlow P I
Yale Psychiatric Institute, Connecticut Mental Health Center, Haven, USA.
J Pharmacol Exp Ther. 1995 Jul;274(1):215-23.
Comorbid abuse of cocaine and alcohol is a common occurrence. Cocaethylene, the ethyl ester of benzoylecgonine, is an active metabolite formed as a result of simultaneous use of these substances. In humans, the concurrent ingestion of cocaine and alcohol, with resulting cocaethylene formation, has been associated with enhanced subjective euphoria, increased heart rate and increased plasma cocaine concentration. These findings suggest that cocaethylene may play a role in the morbidity and mortality associated with concurrent cocaine/alcohol abuse. This placebo-controlled, double-blinded study examined the behavioral and physiological effects and pharmacokinetics of intranasal cocaethylene administration in humans (n = 8), using cocaine as a comparator. Cocaethylene administration resulted in a euphoria similar to that produced by cocaine, although the effects differed significantly over time. Subjects were unable to distinguish between equimolar doses of cocaine and cocaethylene, although cocaethylene appeared to be eliminated more slowly than cocaine. Cardiovascular effects of cocaethylene and cocaine were similar. These findings are considered in light of the epidemiology and possible consequences of cocaine and alcohol abuse.
可卡因与酒精的合并滥用很常见。可卡因乙酯，即苯甲酰爱康宁的乙酯，是同时使用这些物质时形成的一种活性代谢产物。在人类中，同时摄入可卡因和酒精并形成可卡因乙酯，与主观欣快感增强、心率加快以及血浆可卡因浓度升高有关。这些发现表明，可卡因乙酯可能在与可卡因/酒精合并滥用相关的发病率和死亡率中起作用。这项安慰剂对照、双盲研究以可卡因作为对照，研究了鼻内给予可卡因乙酯对8名人类受试者的行为、生理影响及药代动力学。给予可卡因乙酯产生的欣快感与可卡因相似，尽管随着时间推移效果有显著差异。受试者无法区分等摩尔剂量的可卡因和可卡因乙酯，尽管可卡因乙酯的消除似乎比可卡因更慢。可卡因乙酯和可卡因对心血管的影响相似。根据可卡因和酒精滥用的流行病学及可能后果对这些发现进行了考量。
