PHARMACOKINETICS OF COCAETHYLENE

可卡因是一种具有药理活性的可卡因同系物，由可卡因在酒精存在下酯交换形成。本研究采用随机、安慰剂对照、双盲方法，以可卡因为对照物，研究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。依赖可卡因的参与者在每个实验阶段随机接受一种研究药物或安慰剂，这些实验在不同的日子进行。对完成这项研究的前6名受试者进行的中期分析表明，虽然同等剂量的可卡因和可卡因的血浆浓度没有差异，但可卡因提高心率的能力似乎较弱。主观测量（“可卡因兴奋”、“兴奋”、“刺激”和“良好的药物效果”）也发现了类似的结果。与安慰剂相比，所有有效药物条件下的收缩压均显著升高，但迄今未观察到对舒张压的显著影响。可卡因似乎比可卡因有更长的半衰期。迄今为止，这项研究的结果证实了以前的研究结果，即可卡因对人体的作用不如可卡因。这项研究继续招募受试者，并将完成按性别对可卡因和可卡因反应差异的第二次分析。

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.