Hearn W L, Rose S, Wagner J, Ciarleglio A, Mash D C
Dade County Medical Examiner Department, Miami, FL 33136-1133.
Pharmacol Biochem Behav. 1991 Jun;39(2):531-3. doi: 10.1016/0091-3057(91)90222-n.
Cocaethylene is a pharmacologically active cocaine metabolite that is formed in the presence of ethanol by the activity of liver enzymes. The pharmacology of cocaethylene has not been extensively investigated and its acute toxicity is unknown. The acute toxicity of cocaethylene was compared to cocaine in Swiss-Webster mice. The LD50 of cocaethylene was 60.7 mg/kg and 63.8 mg/kg in female and male mice, respectively. In comparison, the LD50 of cocaine was 93.0 mg/kg in both female and male mice. These studies demonstrate that the cocaine-alcohol metabolite, cocathylene, is more potent in mediating lethality than the parent drug.
可卡乙碱是一种具有药理活性的可卡因代谢产物，它在乙醇存在的情况下由肝脏酶的活性形成。可卡乙碱的药理学尚未得到广泛研究，其急性毒性也未知。在瑞士韦伯斯特小鼠中比较了可卡乙碱与可卡因的急性毒性。可卡乙碱在雌性和雄性小鼠中的半数致死量分别为60.7毫克/千克和63.8毫克/千克。相比之下，可卡因在雌性和雄性小鼠中的半数致死量均为93.0毫克/千克。这些研究表明，可卡因 - 酒精代谢产物可卡乙碱在介导致死性方面比母体药物更具效力。
