基因多态性对普罗帕酮峰浓度的影响：无显著影响。

Effect of genetic polymorphism on peak propafenone concentration: no significant effect of .

机构信息

Department of Pharmaceutical Sciences, Faculty of Medicine, University of Tsukuba, Tennodai 1-1-1, Tsukuba, Ibaraki, 305 8575, Japan.

Department of Internal Medicine, Faculty of Medicine, University of Tsukuba, Tennodai 1-1-1, Tsukuba, Ibaraki, 305 8575, Japan.

出版信息

Pharmacogenomics. 2020 Dec;21(18):1279-1288. doi: 10.2217/pgs-2020-0105. Epub 2020 Nov 18.

DOI:10.2217/pgs-2020-0105

PMID:33203295

Abstract

The study aims to investigate the clinical implication of nonfunctional poor metabolizer (PM) alleles and intermediate metabolizer (IM) alleles of , including the allele which shows substrate-dependent decrease in enzymatic activity, in antiarrhythmic therapy using propafenone. We examined serum propafenone concentrations and metabolic ratio, which was expressed as serum concentrations of propafenone to 5-hydroxypropafenone, in 66 Japanese patients with tachyarrhythmias. The peak propafenone concentration and metabolic ratio in PM allele carriers were higher than those in extensive metabolizer (EM)/EM, EM/IM and IM/IM genotype groups. Results suggest that PM alleles affect peak propafenone concentration, but the IM allele has no clinical implication in propafenone dosing.

摘要

本研究旨在探讨非功能性弱代谢者（PM）等位基因和中间代谢者（IM）等位基因，包括表现出底物依赖性酶活性降低的等位基因，在普罗帕酮抗心律失常治疗中的临床意义。我们检测了 66 例心动过速患者的普罗帕酮血清浓度和代谢比，即普罗帕酮与 5-羟普罗帕酮的血清浓度比值。PM 等位基因携带者的普罗帕酮峰浓度和代谢比均高于广泛代谢者（EM）/EM、EM/IM 和 IM/IM 基因型组。结果表明，PM 等位基因影响普罗帕酮峰浓度，但 IM 等位基因对普罗帕酮剂量无临床意义。