Spigset O, Granberg K, Hägg S, Norström A, Dahlqvist R
Division of Clinical Pharmacology, Norrland University Hospital, Umeä, Sweden.
Eur J Clin Pharmacol. 1997;52(2):129-33. doi: 10.1007/s002280050261.
The purpose of this study was to investigate whether the disposition of fluvoxamine is associated with the CYP2D6 and CYP2C19 phenotype polymorphisms.
The serum concentration of fluvoxamine was followed for 48 h after oral administration of a single dose of 50 mg fluvoxamine to five poor metabolizers of the CYP2D6 test drug dextromethorphan, five poor metabolizers of the CYP2C19 test drug mephenytoin, and five extensive metabolizers of both test drugs.
Poor metabolizers of dextromethorphan had significantly higher areas under the serum concentration-time curve than extensive metabolizers of dextromethorphan (mean 1.31 vs 1.00 mumol.h.l-1). There were no differences between poor and extensive metabolizers of mephenytoin (mean, 1.00 vs 1.15 mumol.h.l-1).
The results are consistent with a possible minor to moderate role of CYP2D6, but not CYP2C19, in fluvoxamine metabolism.
本研究旨在调查氟伏沙明的处置是否与CYP2D6和CYP2C19表型多态性相关。
对5名CYP2D6测试药物右美沙芬的代谢不良者、5名CYP2C19测试药物美芬妥因的代谢不良者以及5名两种测试药物的广泛代谢者口服单剂量50mg氟伏沙明后，监测其血清中氟伏沙明浓度48小时。
右美沙芬代谢不良者的血清浓度-时间曲线下面积显著高于右美沙芬广泛代谢者（平均分别为1.31和1.00μmol·h·l-1）。美芬妥因代谢不良者与广泛代谢者之间无差异（平均分别为1.00和1.15μmol·h·l-1）。
结果表明CYP2D6可能在氟伏沙明代谢中起轻微至中度作用，而CYP2C19则不然。
