甲氟喹在人体内的药代动力学：甲氟喹对安替比林代谢无影响。
The pharmacokinetics of mefloquine in man: lack of effect of mefloquine on antipyrine metabolism.
作者信息
Rivière J H, Back D J, Breckenridge A M, Howells R E
出版信息
Br J Clin Pharmacol. 1985 Nov;20(5):469-74. doi: 10.1111/j.1365-2125.1985.tb05099.x.
Abstract
A method is described for the determination of the new antimalarial agent, mefloquine, in plasma and urine. After oral administration of 750 mg mefloquine to six volunteers, absorption, was apparently slow, with plasma mefloquine concentrations at 24 h (559 +/- 181 ng ml-1; mean +/- s.d.) higher than at 6 h (459 +/- 166 ng ml-1). The elimination half-life was 373 +/- 249 h, oral clearance was 5.09 +/- 2.7 1 h-1, and apparent volume of distribution was 35.7 +/- 30.7 l kg-1 (assuming 100% bioavailability). Mefloquine (750 mg) had no significant effect on salivary kinetics of antipyrine or on the metabolic clearance of antipyrine to its three main metabolites, 3-hydroxymethylantipyrine, 4-hydroxyantipyrine and norantipyrine, when antipyrine was administered either 2 h or 2 weeks after dosing with mefloquine.
摘要
本文描述了一种测定血浆和尿液中新型抗疟药甲氟喹的方法。给6名志愿者口服750mg甲氟喹后，吸收明显缓慢，24小时时血浆中甲氟喹浓度（559±181ng/ml；平均值±标准差）高于6小时时（459±166ng/ml）。消除半衰期为373±249小时，口服清除率为5.09±2.7l/h，表观分布容积为35.7±30.7l/kg（假设生物利用度为100%）。当在给予甲氟喹后2小时或2周给予安替比林时，甲氟喹（750mg）对安替比林的唾液动力学或安替比林代谢为其三种主要代谢物3-羟甲基安替比林、4-羟基安替比林和去甲安替比林的代谢清除率均无显著影响。
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