β1肾上腺素能受体和CYP2D6基因多态性对美托洛尔治疗效果的影响。
Effects of polymorphism of the beta(1) adrenoreceptor and CYP2D6 on the therapeutic effects of metoprolol.
作者信息
Yuan H, Huang Z, Yang G, Lv H, Sang H, Yao Y
机构信息
Centre of Clinical Pharmacology, The Third Xiangya Hospital, Central South University, Changsha, China.
出版信息
J Int Med Res. 2008 Nov-Dec;36(6):1354-62. doi: 10.1177/147323000803600624.
Metoprolol is a lipophilic beta(1) selective adrenergic receptor antagonist used in antihypertensive therapy. It is metabolized by the protein product of the cytochrome P450 2D6 (CYP2D6) gene. Few studies have been performed on the association between the beta(1) adrenoreceptor, CYP2D6 polymorphism and blood pressure. The one reported here is a prospective, observational, clinical study in Chinese Han hypertensive patients on the combined influences of CYP2D6 and beta(1) adrenoreceptor polymorphisms on the therapeutic effects of metoprolol in 300 out-patients with essential hypertension. The same dose of metoprolol achieved different therapeutic effects in patients with different CYP2D6 and beta(1) adrenoreceptor polymorphisms. Additionally, different doses of metoprolol could achieve the same therapeutic effects in patients with different CYP2D6 and beta(1) adrenoreceptor polymorphisms. Knowledge of the combination of CYP2D6 and beta(1) adrenoreceptor polymorphisms may be used to guide antihypertensive therapy using beta(1) adrenoreceptor antagonists.
美托洛尔是一种亲脂性β₁选择性肾上腺素能受体拮抗剂，用于抗高血压治疗。它由细胞色素P450 2D6（CYP2D6）基因的蛋白质产物代谢。关于β₁肾上腺素能受体、CYP2D6多态性与血压之间的关联，所做的研究较少。本文报告的是一项针对中国汉族高血压患者的前瞻性、观察性临床研究，研究了CYP2D6和β₁肾上腺素能受体多态性对300例原发性高血压门诊患者美托洛尔治疗效果的联合影响。相同剂量的美托洛尔在具有不同CYP2D6和β₁肾上腺素能受体多态性的患者中产生不同的治疗效果。此外，不同剂量的美托洛尔在具有不同CYP2D6和β₁肾上腺素能受体多态性的患者中可产生相同的治疗效果。了解CYP2D6和β₁肾上腺素能受体多态性的组合情况，可用于指导使用β₁肾上腺素能受体拮抗剂的抗高血压治疗。
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