Kaye C M, Kumana C R, Franklin D A, Baker L R
Int J Clin Pharmacol Biopharm. 1975 Jul;12(1-2):83-8.
Plasma and renal elimination of practolol have been studied in 12 patients with varying degrees of stable chronic renal failure and 14 normal volunteers. Each individual received 200 mg of oral practolol. The mean time to peak plasma level in the group of patients with renal failure was later than in the normal group, the difference between the two being significant. There were significant correlations between plasma practolol clearance and creatinine clearance, and also between renal practolol clearance and creatinine clearance. Total clearance of practolol from plasma was slightly higher than its renal clearance, the difference being significant, which suggested a small non-renal component to elimination. Renal practolol clearances tended to exceed creatinine clearances, the difference being significant, suggesting some renal tubular secretion of the drug. It is suggested that--in patients with chronic renal failure--the maintenance dose of practolol be reduced roughly in proportion to the reduction in creatinine clearance from normal. If effective plasma practolol concentrations are required quickly, the need for giving a loading dose becomes important under such circumstances.
对12例不同程度稳定期慢性肾衰竭患者和14名正常志愿者研究了醋氨心安的血浆及肾脏清除情况。每位受试者口服200mg醋氨心安。肾衰竭组达到血浆峰值水平的平均时间比正常组晚，两组间差异有显著性。血浆醋氨心安清除率与肌酐清除率之间以及肾脏醋氨心安清除率与肌酐清除率之间均有显著相关性。醋氨心安从血浆中的总清除率略高于其肾脏清除率，差异有显著性，这提示存在少量非肾脏清除成分。肾脏醋氨心安清除率往往超过肌酐清除率，差异有显著性，提示该药有一定的肾小管分泌。建议在慢性肾衰竭患者中，醋氨心安维持剂量应大致与肌酐清除率相对于正常时的降低程度成比例减少。如果需要迅速达到有效的血浆醋氨心安浓度，在这种情况下给予负荷剂量就很重要。
