Solimon M, Massry S G, Campese V M
Am J Cardiol. 1986 Nov 26;58(12):21E-24E. doi: 10.1016/0002-9149(86)90593-x.
The effects of bevantolol on renal blood flow and glomerular filtration rate and the drug's pharmacokinetics were studied for 7 days in 18 patients (mean age 50 years) with varying degrees of renal dysfunction. Patients were divided into 3 groups: group 1 had a creatinine clearance of 50 to 80 ml/min, group 2, 20 to 49 ml/min and group 3, less than 20 ml/min. After baseline inulin and paraaminohippuric acid clearance values were obtained, patients were given a single, 150-mg "priming" administration of bevantolol. The kinetics of the drug (including plasma drug levels, plasma half-life and plasma clearance) and its effects on renal function were observed for 24 hours. On days 4 to 6 of the study, patients received 150 mg of bevantolol twice daily, with only a single dose given on day 7. Bevantolol did not significantly affect either inulin or paraaminohippuric acid clearance in patients with differing degrees of renal function. In 50% of patients with a creatinine clearance of less than or equal to 50 ml/min, both the half-life and maximum trough serum levels were higher than the ranges seen in healthy subjects. However, neither value appears to be clinically relevant because bevantolol has a wide therapeutic range. Renal impairment did not change the percentages of the bevantolol dosage excreted unchanged or as conjugated drug in the urine, and no toxic or active drug metabolites accumulated in the blood. From these results, it appears that bevantolol may be used safely in short-term therapy of patients with renal impairment.
在18例（平均年龄50岁）不同程度肾功能不全的患者中，研究了贝凡洛尔对肾血流量和肾小球滤过率的影响以及该药物的药代动力学，为期7天。患者被分为3组：第1组肌酐清除率为50至80 ml/分钟，第2组为20至49 ml/分钟，第3组小于20 ml/分钟。在获得基础菊粉和对氨基马尿酸清除率值后，给患者单次静脉注射150 mg贝凡洛尔进行“起始”给药。观察该药物的动力学（包括血浆药物水平、血浆半衰期和血浆清除率）及其对肾功能的影响24小时。在研究的第4至6天，患者每日两次接受150 mg贝凡洛尔，第7天仅给予单剂量。贝凡洛尔对不同程度肾功能的患者的菊粉或对氨基马尿酸清除率均无显著影响。在50%肌酐清除率小于或等于50 ml/分钟的患者中，半衰期和最低谷血清水平均高于健康受试者所见范围。然而，由于贝凡洛尔有较宽的治疗范围，这两个值似乎均无临床意义。肾功能损害并未改变贝凡洛尔以原形或结合药物形式经尿液排泄的剂量百分比，且血液中未累积有毒或活性药物代谢产物。从这些结果来看，贝凡洛尔似乎可安全用于肾功能损害患者的短期治疗。
