Amemiya M, Tabei K, Furuya H, Sakairi Y, Asano Y
Department of Medicine, Jichi Medical School, Tochigi, Japan.
Eur J Clin Pharmacol. 1992;43(4):417-21. doi: 10.1007/BF02220619.
In order to determine the appropriate dosage of carteolol in renal dysfunction, the pharmacokinetics of carteolol has been examined in appropriate patients. The plasma concentrations and urinary excretion of carteolol were investigated in 15 patients with varying degrees of renal impairment during the administration of 5-20 mg carteolol hydrochloride (5 mg/tablet) for 2-45 months. Plasma carteolol levels were linearly correlated with the serum creatinine concentration (r = 0.87) and reciprocally with the creatinine clearance (r = 0.82). The urinary carteolol concentration was correlated with the urinary creatinine concentration (r = 0.69) and the urinary carteolol excretion was also correlated with the creatinine clearance (r = 0.79). These relationships become even closer when the plasma carteolol concentrations and urinary excretion rate of carteolol were factored by the administered tablets. The fractional renal excretion of carteolol was virtually constant at various degrees of renal function, and it always exceeded 100%, which indicates that carteolol was actively secreted, even in patients with renal failure. The estimated tubular secretion rate of carteolol was logarithmically correlated with the fractional renal excretion of carteolol (r = 0.93). The results indicate that the dose of carteolol should be determined according to the degree of renal impairment.
为了确定卡替洛尔在肾功能不全患者中的合适剂量，已对合适的患者进行了卡替洛尔的药代动力学研究。在15例不同程度肾功能损害的患者中，给予5 - 20 mg盐酸卡替洛尔（5 mg/片），给药2 - 45个月，研究卡替洛尔的血药浓度和尿排泄情况。血浆卡替洛尔水平与血清肌酐浓度呈线性相关（r = 0.87），与肌酐清除率呈负相关（r = 0.82）。尿卡替洛尔浓度与尿肌酐浓度相关（r = 0.69），尿卡替洛尔排泄也与肌酐清除率相关（r = 0.79）。当将血浆卡替洛尔浓度和卡替洛尔尿排泄率按给药片数进行校正后，这些关系变得更加密切。卡替洛尔的肾脏排泄分数在不同程度的肾功能下基本恒定，且始终超过100%，这表明即使在肾衰竭患者中，卡替洛尔也是主动分泌的。卡替洛尔的估计肾小管分泌率与卡替洛尔的肾脏排泄分数呈对数相关（r = 0.93）。结果表明，卡替洛尔的剂量应根据肾功能损害程度来确定。
