Impact of the CYP2D6 Genotype on the Clinical Effects of Metoprolol: A Prospective Longitudinal Study
Impact of the CYP2D6 Genotype on the Clinical Effects of Metoprolol: A Prospective Longitudinal Study
复制标题
DOI：
10.1038/clpt.2008.218
复制
发表时间：
2009-03-01
影响因子：
6.7
通讯作者：
Eschenhagen, T.
中科院分区：
文献类型：
--
作者：
Rau, T.;Wuttke, H.;Eschenhagen, T.
美托洛尔给药后，CYP2D6弱代谢者（PM）的血浆药物浓度明显高于非PM。在一项为期3个月的前瞻性双盲研究中，我们调查了这是否会转化为治疗开始后美托洛尔效果的差异。尽管给予相同剂量的PM和非PM，PM组的美托洛尔血浆浓度高4.9倍。美托洛尔诱发PM患者的心率、舒张压和平均动脉压显著且持续降低，高于非PM患者。因此，CYP2D6基因型似乎有助于美托洛尔反应的个体间差异。
After administration of metoprolol, plasma concentrations of the drug are markedly higher in CYP2D6 poor metabolizers (PMs) than in non-PMs. In a prospective double-blind 3-month study, we investigated whether this translates into differences in metoprolol's effects after initiation of therapy. Despite administering equal doses to PMs and non-PMs, metoprolol plasma concentrations were 4.9-fold higher in the PM group. Metoprolol evoked significantly and persistently greater reductions in heart rate, diastolic blood pressure, and mean arterial pressure in PMs than in non-PMs. It appears, therefore, that the CYP2D6 genotype contributes to interindividual differences in metoprolol response.