PLASMA DELTA-9-TETRAHYDROCANNABINOL CONCENTRATIONS AND CLINICAL EFFECTS AFTER ORAL AND INTRAVENOUS ADMINISTRATION AND SMOKING
PLASMA DELTA-9-TETRAHYDROCANNABINOL CONCENTRATIONS AND CLINICAL EFFECTS AFTER ORAL AND INTRAVENOUS ADMINISTRATION AND SMOKING
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DOI：
10.1038/clpt.1980.181
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发表时间：
1980-01-01
影响因子：
6.7
通讯作者：
GILLESPIE, HK
中科院分区：
文献类型：
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作者：
OHLSSON, A;LINDGREN, JE;GILLESPIE, HK
β-9-四氢大麻酚(THC)静脉注射、吸烟和口服给11名健康受试者。吸烟和静脉注射后THC的血浆谱。注射用药相似，但口服后血药浓度低且不规则，表明吸收缓慢且不稳定。根据AUC[浓度下的面积：时间曲线]，估计吸烟后0-360min的THC的系统利用度为18.+-。6%。巧克力饼干中的口服THC提供了6.+-的系统利用度。3%。在大麻中毒的两个主要临床症状中，只要THC水平为5 ng/ml，结膜发红就会持续，而心动过速是THC水平或高水平的较不可靠的衡量标准。静脉注射的血药浓度和临床高剂量的时间进程是相同量级的。注射和吸烟，起效迅速，在4h内稳定下降。高浓度的出现滞后于血浆浓度的上升，表明脑内浓度随着血浆浓度的下降而增加。口服THC后，临床效应起效较慢，持续时间较长，但在较低的血药浓度下起效，远低于其他两种给药方法。
.delta.-9-Tetrahydrocannabinol (THC) was given i.v., by smoking and by mouth to 11 healthy subjects. Plasma profiles of THC after smoking and i.v. injection were similar, but plasma levels after oral doses were low and irregular, indicating slow and erratic absorption. Based on AUC[area under the concentration: time curve]0-360 min systemic availability of THC after smoking was estimated to be 18 .+-. 6%. Oral THC in a chocolate cookie provided systemic availability of 6 .+-. 3%. Of the 2 major clinical signs of cannabis intoxication, reddened conjunctivae persisted for as long as THC levels were > 5 ng/ml and tachycardia was a less reliable measurement of prevailing THC levels or high. The time courses of plasma concentrations and clinical high were of the same order for i.v. injection and smoking, with prompt onset and steady decline over 4 h. The appearance of high lagged behind the increase in plasma concentrations, suggesting that brain concentrations were increasing as plasma concentrations decreased. After oral THC, the onset of clinical effects was much slower and lasted longer, but effects occurred at much lower plasma concentrations than after the other 2 methods of administration.