Effect of CYP2D6 genetic polymorphism on peak propafenone concentration: no significant effect of CYP2D6*10

被引：2

作者：

Doki, Kosuke ^{[1
]}

Shirayama, Yuki ^{[1
]}

Sekiguchi, Yukio ^{[2
]}

Aonuma, Kazutaka ^{[2
]}

Kohda, Yukinao ^{[1
]}

Ieda, Masaki ^{[2
]}

Homma, Masato ^{[1
]}

机构：

[1] Univ Tsukuba, Dept Pharmaceut Sci, Fac Med, Tennodai 1-1-1, Tsukuba, Ibaraki 3058575, Japan

[2] Univ Tsukuba, Dept Internal Med, Fac Med, Tennodai 1-1-1, Tsukuba, Ibaraki 3058575, Japan

来源：

PHARMACOGENOMICS | 2020年 / 21卷 / 18期

关键词：

intermediate metabolizer; metabolic ratio; poor metabolizer; propafenone; PHARMACOKINETICS; GENOTYPE; METABOLISM; ALLELE; PHARMACOLOGY; ENANTIOMERS;

D O I：

10.2217/pgs-2020-0105

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Aim: The study aims to investigate the clinical implication of nonfunctional poor metabolizer (PM) alleles and intermediate metabolizer (IM) alleles of CYP2D6, including the CYP2D6*10 allele which shows substrate-dependent decrease in enzymatic activity, in antiarrhythmic therapy using propafenone. Materials & methods: 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. Results: The peak propafenone concentration and metabolic ratio in CYP2D6 PM allele carriers were higher than those in extensive metabolizer (EM)/EM, EM/IM and IM/IM genotype groups. Conclusion: Results suggest that CYP2D6 PM alleles affect peak propafenone concentration, but the CYP2D6 IM allele CYP2D6*10 has no clinical implication in propafenone dosing.

引用

页码：1279 / 1288

页数：10

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