Anavekar S N, Jarrott B, Toscano M, Louis W J
Eur J Clin Pharmacol. 1982;23(1):1-5. doi: 10.1007/BF01061368.
The pharmacokinetics of clonidine and its relation to blood pressure response and side effects were studied after single oral doses of 75 micrograms, 150 micrograms and 250 micrograms in normotensive subjects. Following oral administration, the drug was absorbed rapidly after an initial lag time of 19-22 min and peak levels were reached between 2.4 and 2.9 h. Sampling over 48 h was necessary for accurate estimation of pharmacokinetic parameters. Post-peak plasma concentration declined in a monoexponential manner and the half-life of the elimination phase ranged from 9.0 to 15.1 h. Maximum plasma concentration (Cmax) and area under curve (AUC) increased proportionally with increasing doses. Clonidine produced significant reductions in the pulse rate and a dose dependent decrease in blood pressure. Clonidine (150 micrograms) also produced significant reductions in plasma catecholamine levels.
在血压正常的受试者中，研究了单次口服75微克、150微克和250微克可乐定后的药代动力学及其与血压反应和副作用的关系。口服给药后，药物在初始滞后时间19 - 22分钟后迅速吸收，在2.4至2.9小时之间达到峰值水平。为准确估计药代动力学参数，有必要在48小时内进行采样。峰后血浆浓度以单指数方式下降，消除相半衰期为9.0至15.1小时。最大血浆浓度（Cmax）和曲线下面积（AUC）随剂量增加而成比例增加。可乐定可使脉搏率显著降低，并使血压呈剂量依赖性下降。可乐定（150微克）还可使血浆儿茶酚胺水平显著降低。
