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[Δ⁹-四氢大麻酚的药代动力学]

[Delta-9-tetrahydrocannabinol pharmacokinetics].

作者信息

Goullé J-P, Saussereau E, Lacroix C

机构信息

Laboratoire de pharmacocinétique et de toxicologie cliniques, groupe hospitalier du Havre, BP 24, 76083 Le Havre cedex, France.

出版信息

Ann Pharm Fr. 2008 Aug;66(4):232-44. doi: 10.1016/j.pharma.2008.07.006. Epub 2008 Aug 29.

Abstract

Delta-9-tetrahydrocannabinol (Delta-9-THC) is the main psychoactive ingredient of cannabis. Smoking is currently most common use of cannabis. The present review focuses on the pharmacokinetics of THC. The variability of THC in plant material which has significantly increased in recent years leads to variability in tissue THC levels from smoking, which is, in itself, a highly individual process. This variability of THC content has an important impact on drug pharmacokinetics and pharmacology. After smoking THC bioavailability averages 30%. With a 3.55% THC cigarette, a peak plasma level near 160 ng/mL occurs approximately 10 min after inhalation. THC is eliminated quickly from plasma in a multiphasic manner and is widely distributed to tissues, which is responsible for its pharmacologic effects. Body fat then serves as a long-term storage site. This particular pharmacokinetics explains the noncorrelation between THC blood level and clinical effects as is observed for ethanol. A major active 11-hydroxy metabolite is formed after both inhalation and oral dosing (20 and 100% of parent, respectively). The elimination of THC and its many metabolites, mainly THC-COOH, occurs via the feces and urine for several weeks. Thus, to confirm abstinence, urine THC-COOH analysis would be a useful tool. A positive result could be checked by gas chromatography-mass spectrometry THC blood analysis, indicative of a recent cannabis exposure.

摘要

Δ-9-四氢大麻酚(Δ-9-THC)是大麻的主要精神活性成分。吸烟是目前最常见的使用大麻的方式。本综述聚焦于THC的药代动力学。近年来,植物材料中THC的变异性显著增加,这导致吸烟后组织中THC水平存在变异性,而吸烟本身就是一个高度个体化的过程。THC含量的这种变异性对药物的药代动力学和药理学有重要影响。吸烟后THC的生物利用度平均为30%。使用含3.55%THC的香烟时,吸入后约10分钟血浆峰值水平接近160 ng/mL。THC以多相方式从血浆中快速消除,并广泛分布于组织中,这与其药理作用有关。身体脂肪随后成为长期储存部位。这种特殊的药代动力学解释了THC血药水平与临床效应之间不存在相关性,正如乙醇的情况。吸入和口服给药后均会形成一种主要的活性11-羟基代谢物(分别为母体的20%和100%)。THC及其多种代谢物(主要是THC-COOH)通过粪便和尿液排出体外,持续数周。因此,为确认戒断情况,尿液THC-COOH分析将是一种有用的工具。阳性结果可通过气相色谱-质谱法进行THC血液分析来验证,这表明近期接触过大麻。

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