School of Pharmaceutical Sciences of Ribeirão Preto, University of São Paulo, Ribeirão Preto, São Paulo, Brazil.
J Pharm Pharmacol. 2013 Sep;65(9):1347-53. doi: 10.1111/jphp.12109. Epub 2013 Jul 21.
The purpose of this study was to phenotype the CYP2D6 in elderly with heart disease classified as extensive metabolizer or poor metabolizers (PM) of metoprolol, develop and validate the method of analysis of metoprolol tartrate and its metabolite in urine using HPLC, and identify potential correlations between anthropometric factors with metabolic ratios of metoprolol/α-OH metoprolol in urine.
The sample was composed of 130 elderly individuals with a previously identified type of heart condition, with normal renal and hepatic functions. The urine of all the patients were collected 0-8 h after the administration of a pill of 100 mg of metoprolol to determine concentrations of metoprolol and α-hydroxymetoprolol. Those patients presenting a metabolic ratio greater than 12.6 were phenotyped as PM.
The median age of patients was 71.0 years, with a minimum of 60 and maximum of 93 years old. Three patients (2.3%) were phenotyped as PM of metoprolol different from the rate (7-10%) of PM existing in the Caucasian population.
Most of the studied individuals were women, and the proportion of elderly with heart disease classified as PM was smaller than what is usually found among Caucasian populations.
本研究旨在对患有心脏病的老年人进行 CYP2D6 表型分析，这些老年人被分类为美托洛尔的广泛代谢者或弱代谢者（PM），开发并验证使用 HPLC 分析酒石酸美托洛尔及其代谢物在尿液中的方法，并确定人体测量因素与尿液中美托洛尔/α-OH 美托洛尔代谢比值之间的潜在相关性。
该样本由 130 名先前确诊患有某种心脏病的老年人组成，他们的肾功能和肝功能均正常。所有患者在服用 100mg 美托洛尔片后 0-8 小时内收集尿液，以测定美托洛尔和 α-羟美托洛尔的浓度。代谢比值大于 12.6 的患者被表型为 PM。
患者的中位年龄为 71.0 岁，最小年龄为 60 岁，最大年龄为 93 岁。有 3 名（2.3%）患者被表型为 PM，与白种人群中 PM 的发生率（7-10%）不同。
大多数研究对象为女性，而被分类为 PM 的心脏病老年患者的比例小于白种人群中的常见比例。
