PHARMACOKINETICS OF COCAETHYLENE

可卡因乙烯是可卡因的一种具有药理活性的同系物，由可卡因在酒精存在下进行酯交换而形成。这项随机、安慰剂对照、双盲研究以可卡因为参照物，研究了静脉注射可卡因对人体的生理和主观影响以及药代动力学。可卡因依赖的参与者在每个实验过程中随机接受一种研究药物或安慰剂，实验过程发生在不同的几天。对完成这项研究的前6名受试者进行的中期分析表明，虽然等量可卡因和可可乙烯的药物血浆浓度没有差异，但可卡因似乎没有那么强的提高心率的能力。主观指标(“可卡因兴奋”、“冲动”、“刺激”和“良好的药物效果”)也检测到了类似的结果。与安慰剂相比，所有活性药物条件都能显著提高收缩压，但到目前为止还没有观察到对舒张压的显著影响。可卡因的消除半衰期似乎比可卡因要长。到目前为止，这项研究的发现证实了之前的研究，这些研究表明可卡因对人类的效力低于可卡因。这项研究继续招募受试者，并将完成对可卡因和可卡因反应的性别差异的第二次分析。

Cocaethylene is a pharmacologically active homolog of cocaine, formed by transesterification of cocaine in the presence of alcohol. This randomized, placebo-controlled, double-blind study has been undertaken to examine the physiological and subjective effects and pharmacokinetics of intravenously administered cocaethylene in humans using cocaine as a comparator. Cocaine-dependent participants randomly receive one study drug or placebo, during each experimental session which occurs on separate days. Interim analysis of the first 6 subjects to complete the study shows that while drug plasma concentrations for equivalent doses of cocaine and cocaethlyene do not differ, cocaethylene appears to be less potent in its ability to elevate heart rate. Similar results were detected for subjective measures ("cocaine high", "rush", "stimulated" and "good drug effects"). All active drug conditions produce significant increases in systolic blood pressure relative to placebo, but no significant effect on diastolic blood pressure has been observed thus far. Cocaethylene appears to have a longer elimination half-life than cocaine. The findings from this study to date confirm those of previous studies which show that cocaethylene is less potent that cocaine in humans. This study continues to enroll subjects and a second analysis of differences in responses to cocaine and cocaethylene by gender will be completed.