Johnson Matthew W, MacLean Katherine A, Caspers Michael J, Prisinzano Thomas E, Griffiths Roland R
Behavioral Pharmacology Research Unit, Department of Psychiatry and Behavioral Sciences, Johns Hopkins University School of Medicine, Baltimore, MD, USA
Behavioral Pharmacology Research Unit, Department of Psychiatry and Behavioral Sciences, Johns Hopkins University School of Medicine, Baltimore, MD, USA.
J Psychopharmacol. 2016 Apr;30(4):323-9. doi: 10.1177/0269881116629125. Epub 2016 Feb 15.
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.
萨尔维诺林A是一种κ阿片受体激动剂，也是鼠尾草植物的主要精神活性成分，该植物一直被用于产生致幻效果。先前关于萨尔维诺林A药代动力学的研究可能低估了通常因给药剂量而产生的血浆水平，这是由于汽化效率低下且未在药物效果峰值期间采集样本所致。六名健康成年人吸入了单次高剂量的汽化萨尔维诺林A（n = 4，21微克/千克；n = 2，18微克/千克）。吸入后60分钟内，每2分钟评估一次参与者和监测者评定的效果。在吸入后长达90分钟的13个时间点采集血样。药物水平在2分钟时达到峰值，然后迅速下降。药物水平与参与者和监测者的药物效果评定显著正相关。吸入后5分钟开始观察到催乳素显著升高，并在吸入后15分钟达到峰值。皮质醇在各参与者中呈现出不一致的升高。激素反应与药物水平相关性不佳。这是第一项证明人类血浆中萨尔维诺林A水平变化与药物效果之间存在直接关系的研究。结果证实了吸入技术对萨尔维诺林A的有效性。
