Perez-Reyes M, Jeffcoat A R, Myers M, Sihler K, Cook C E
Department of Psychiatry, University of North Carolina, Chapel Hill 27599-7175.
Psychopharmacology (Berl). 1994 Dec;116(4):428-32. doi: 10.1007/BF02247473.
Cocaethylene (the ethyl ester of benzoylecgonine) is a product of the interaction between ethanol and cocaine. The results of preclinical studies and of a pilot clinical study have shown cocaethylene to produce pharmacologic effects similar to those of cocaine. However, no information is available concerning the potency and pharmacokinetics of cocaethylene in comparison to those of cocaine in humans. We report the results of a single-blind, crossover study in which six male, healthy, paid volunteers, who were moderate users of cocaine, were intravenously injected with the water soluble fumarate salt of cocaethylene (0.25 mg/kg cocaethylene base) or an equivalent dose of the water soluble hydrochloride salt of cocaine (0.25 mg/kg cocaine base). Each dose was dissolved in normal saline and injected over a 1-min interval. Test sessions were separated by a 1-week interval. The variables measured were: cocaine and cocaethylene plasma concentrations, subjective and cardiovascular effects. The results indicate, that in comparison to cocaine, cocaethylene had a significant smaller elimination rate constant (0.42 versus 0.67 l/h), had a longer elimination half-life (1.68 versus 1.07 h), and induced ratings of "high" and changes in heart rate that were of lower magnitude (65%, and 43%, respectively). During the period of time that pharmacologic effects were present the plasma concentrations of cocaine and cocaethylene were statistically indistinguishable. This finding supports the conclusion that in humans cocaethylene is less potent than cocaine.
可卡因乙酯（苯甲酰芽子碱的乙酯）是乙醇与可卡因相互作用的产物。临床前研究及一项初步临床研究的结果表明，可卡因乙酯产生的药理作用与可卡因相似。然而，关于可卡因乙酯与可卡因在人体内的效价及药代动力学的比较尚无相关信息。我们报告了一项单盲交叉研究的结果，该研究中，六名有偿参与的健康男性可卡因中度使用者被静脉注射可卡因乙酯的水溶性富马酸盐（0.25mg/kg可卡因乙酯碱）或等效剂量的可卡因水溶性盐酸盐（0.25mg/kg可卡因碱）。每种剂量均溶解于生理盐水中，并在1分钟内注射完毕。各测试阶段间隔1周。所测量的变量包括：可卡因和可卡因乙酯的血浆浓度、主观效应和心血管效应。结果表明，与可卡因相比，可卡因乙酯的消除速率常数显著更小（分别为0.42和0.67l/h），消除半衰期更长（分别为1.68和1.07h），且诱发的“兴奋”评分及心率变化幅度更低（分别为65%和43%）。在药理效应出现期间，可卡因和可卡因乙酯的血浆浓度在统计学上无显著差异。这一发现支持了可卡因乙酯在人体内效价比可卡因低的结论。
