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Time course of pharmacokinetic and hormonal effects of inhaled high-dose salvinorin A in humans

机译:吸入大剂量萨尔维诺林A在人体中的药代动力学和激素作用的时程

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摘要

Salvinorin A is a kappa opioid agonist and the principal psychoactive constituent of the Salvia divinorum plant, which has been used for hallucinogenic effects. Previous research on salvinorin A pharmacokinetics likely underestimated plasma levels typically resulting from the doses administered due to inefficient vaporization and not collecting samples during peak drug effects. Six healthy adults inhaled a single high dose of vaporized salvinorin A (n=4, 21 mcg/kg; n=2, 18 mcg/kg). Participant- and monitor-rated effects were assessed every 2 min for 60 min post-inhalation. Blood samples were collected at 13 time points up to 90 min post-inhalation. Drug levels peaked at 2 min and then rapidly decreased. Drug levels were significantly, positively correlated with participant and monitor drug effect ratings. Significant elevations in prolactin were observed beginning 5 min post-inhalation and peaking at 15 min post-inhalation. Cortisol showed inconsistent increases across participants. Hormonal responses were not well correlated with drug levels. This is the first study to demonstrate a direct relationship between changes in plasma levels of salvinorin A and drug effects in humans. The results confirm the efficacy of an inhalation technique for salvinorin A.
机译:Salvinorin A是κ阿片类激动剂,是鼠尾草(Salvia divinorum)植物的主要精神活性成分,已被用于产生致幻作用。先前对salvinorin A的药代动力学研究可能低估了血浆水平,这通常是由于无效的蒸发导致的给药剂量导致的,并且在药物作用高峰期未收集样品。六名健康成年人吸入单次高剂量的汽化Salvinorin A(n = 4,21 mcg / kg; n = 2,18 mcg / kg)。吸入后60分钟,每2分钟评估一次参与者和监测者评估的效果。在吸入后直至90分钟的13个时间点采集血样。药物水平在2分钟达到峰值,然后迅速下降。药物水平与参与者显着正相关,并监测药物效果评分。吸入后5分钟开始观察到催乳素的显着升高,并在吸入后15分钟达到峰值。皮质醇显示参与者之间不一致的增加。激素反应与药物水平没有很好的相关性。这是第一项证明Salvinorin A血浆水平变化与人类药物作用之间直接关系的研究。该结果证实了沙维诺林A吸入技术的功效。

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