Mayersohn M, Perrier D
Res Commun Chem Pathol Pharmacol. 1978 Dec;22(3):465-74.
Cocaine plasma concentration-response-time data obtained from the literature were analyzed by pharmacokinetic methods. The plasma concentration-time data yield an elimination half-life of approximately 1 hour and the data suggest that only about 20% of an oral dose of cocaine is absorbed intact into the systemic circulation. Response, as assessed by means of a relative "high" rating scale, declined linearly with time as predicted by theory. The rate of decline of response was found to be 0.0221 "high"/min. The rate of decline of response is a function of the apparent first-order elimination rate constant (K) of the drug and the slope of the response-log plasma concentration curve (m). A value for m of 4.2 "high" was calculated from the response-time data which agreed well with a value of 3.9 "high" for m determined from the slope of the response-log plasma concentration curve.
通过药代动力学方法分析了从文献中获取的可卡因血浆浓度-反应-时间数据。血浆浓度-时间数据得出消除半衰期约为1小时，数据表明口服剂量的可卡因只有约20%完整吸收进入体循环。通过相对“高”评分量表评估的反应，如理论预测的那样随时间呈线性下降。发现反应下降速率为0.0221“高”/分钟。反应下降速率是药物表观一级消除速率常数（K）和反应-对数血浆浓度曲线斜率（m）的函数。根据反应-时间数据计算出m值为4.2“高”，与根据反应-对数血浆浓度曲线斜率确定的m值3.9“高”非常吻合。
