Hasenfuss G, Schäfer-Korting M, Knauf H, Mutschler E, Just H
Eur J Clin Pharmacol. 1985;29(4):461-5. doi: 10.1007/BF00613462.
The plasma levels and urinary excretion of carteolol and its main metabolites 8-hydroxycarteolol and carteolol glucuronide were investigated in 6 healthy subjects and 9 patients with varying degrees of renal impairment following a single oral dose of 30 mg carteolol hydrochloride. In healthy subjects the half-life of carteolol was 7.1 h. 63% of the administered dose was recovered unchanged in urine, and in all 84% was excreted by the kidneys. The renal clearance of carteolol was 255 ml/min. In chronic renal failure (CRF) the terminal half-life was increased to a maximum of 41 h. Both the elimination rate constant and renal clearance were closely related to the creatinine clearance. In CRF the recovery of carteolol and its metabolites from urine was considerably reduced, suggesting that another pathway of drug elimination becomes relevant in renal disease. To avoid an increase in side-effects due to drug accumulation, the dosage of carteolol should be adjusted in relation to the reduction in creatinine clearance. The maintenance dose should be reduced to a half in patients with a creatinine clearance below 40 ml/min and above 10 ml/min. In those with a creatinine clearance of 10 ml/min or less, the dose should be reduced to 1/4.
对6名健康受试者和9名不同程度肾功能损害的患者单次口服30mg盐酸卡替洛尔后，研究了卡替洛尔及其主要代谢产物8 - 羟基卡替洛尔和卡替洛尔葡萄糖醛酸苷的血浆水平和尿排泄情况。在健康受试者中，卡替洛尔的半衰期为7.1小时。给药剂量的63%以原形从尿液中回收，总计84%经肾脏排泄。卡替洛尔的肾清除率为255ml/分钟。在慢性肾衰竭（CRF）中，终末半衰期延长至最长41小时。消除速率常数和肾清除率均与肌酐清除率密切相关。在CRF中，卡替洛尔及其代谢产物从尿液中的回收率显著降低，提示在肾脏疾病中药物消除的另一条途径变得重要。为避免因药物蓄积导致副作用增加，卡替洛尔的剂量应根据肌酐清除率的降低进行调整。肌酐清除率低于40ml/分钟且高于10ml/分钟的患者，维持剂量应减半。肌酐清除率为10ml/分钟或更低的患者，剂量应减至1/4。
