Widler P, Mathys K, Brenneisen R, Kalix P, Fisch H U
Department of Psychiatry, University of Berne, Switzerland.
Clin Pharmacol Ther. 1994 May;55(5):556-62. doi: 10.1038/clpt.1994.69.
To show the subjective and cardiovascular effects of khat leaves having a standardized content of cathinone.
The main effect of khat is an increase of energy and alertness. This effect is thought to be attributable to the phenylalkylamine cathinone, but no controlled clinical trials have been published.
The design was balanced and double blind. Six drug-naïve volunteers received a single dose of khat corresponding to 0.8 mg/kg body weight, as well as alkaloid-free khat as a placebo. Psychologic effects were evaluated by the Addiction Research Center Inventory (ARCI) and visual analog scales. Physiologic measures were systolic blood pressure, diastolic blood pressure, and heart rate. Plasma concentrations of cathinone and its metabolites norephedrine and R,R-(-)norpseudoephedrine were determined by HPLC.
Maximal plasma concentrations of cathinone (127 +/- 53 [SD] ng/ml) were attained after 127 +/- 30 minutes. The area under the plasma concentration-time curve from 0 to 9 hours was 415 +/- 207 ng/ml.hr, and the terminal elimination half-life was 260 +/- 102 minutes. An effect of khat was observed in the ARCI scales Abuse Potential (p < 0.01), Motor Stimulation (p < 0.02), Amphetamine-Like Effect (p < 0.005), and Stimulation-Euphoria (p < 0.005), as well as in the visual analog scales Excited-Calm (p < 0.001) and Energetic-Lethargic (p < 0.001).
Our results provide objective evidence for the amphetamine-like stimulatory effects of khat leaves. These effects were closely similar to those observed after cathinone, 0.5 mg/kg body weight, although peak plasma concentrations of cathinone after khat were delayed.
研究具有标准化卡西酮含量的巧茶树叶的主观及心血管效应。
巧茶的主要作用是提高精力和警觉性。这种作用被认为归因于苯烷基胺类卡西酮，但尚未发表对照临床试验。
设计为平衡双盲。6名未使用过药物的志愿者接受了相当于0.8毫克/千克体重的单剂量巧茶，以及不含生物碱的巧茶作为安慰剂。通过成瘾研究中心量表（ARCI）和视觉模拟量表评估心理效应。生理指标为收缩压、舒张压和心率。通过高效液相色谱法测定卡西酮及其代谢产物去甲麻黄碱和R,R-(-)-去甲伪麻黄碱的血浆浓度。
卡西酮的最大血浆浓度（127±53[标准差]纳克/毫升）在127±30分钟后达到。0至9小时血浆浓度-时间曲线下面积为415±207纳克/毫升·小时，终末消除半衰期为260±102分钟。在ARCI量表的滥用潜力（p<0.01）、运动刺激（p<0.02）、苯丙胺样效应（p<0.005）和刺激-欣快感（p<0.005）以及视觉模拟量表的兴奋-平静（p<0.001）和精力充沛-无精打采（p<0.001）方面观察到了巧茶的效应。
我们的结果为巧茶树叶的苯丙胺样刺激作用提供了客观证据。这些效应与给予0.5毫克/千克体重卡西酮后观察到的效应非常相似，尽管巧茶后卡西酮的血浆峰值浓度出现延迟。
