Wanwimolruk S, Chalcroft S
School of Pharmacy, University of Otago, Dunedin, New Zealand.
Br J Clin Pharmacol. 1991 Nov;32(5):617-20. doi: 10.1111/j.1365-2125.1991.tb03961.x.
The relationship between debrisoquine oxidation phenotype and the pharmacokinetics of quinine after a single dose (600 mg) of quinine sulphate was studied in eight extensive metabolizers (EM) and five poor metabolizers (PM). The mean elimination half-life of quinine in the PMs (10.2 +/- 1.6 (s.d.)h) was similar to that in the EMs (10.9 +/- 1.7 h). The oral clearance of quinine in the PM subjects was 0.092 +/- 0.021 l h-1 kg-1 and was not significantly different (P greater than 0.05) from that observed in the EM subjects (0.073 +/- 0.019 l h-1 kg-1). This suggests that even though quinine is extensively metabolized by oxidative biotransformation, this is carried out largely by P450 isoenzymes different from P450IID6 which oxidizes debrisoquine.
在8名快代谢者(EM)和5名慢代谢者(PM)中研究了异喹胍氧化表型与单次服用600毫克硫酸奎宁后奎宁药代动力学之间的关系。慢代谢者中奎宁的平均消除半衰期(10.2±1.6(标准差)小时)与快代谢者中的(10.9±1.7小时)相似。慢代谢受试者中奎宁的口服清除率为0.092±0.021升·小时⁻¹·千克⁻¹,与快代谢受试者中观察到的清除率(0.073±0.019升·小时⁻¹·千克⁻¹)相比无显著差异(P>0.05)。这表明,尽管奎宁通过氧化生物转化被广泛代谢,但这主要是由不同于氧化异喹胍的P450IID6的P450同工酶进行的。