Lowenthal D T, Irvin J D, Merrill D, Saris S, Ulm E, Goldstein S, Hichens M, Klein L, Till A, Harris K
Clin Pharmacol Ther. 1985 Dec;38(6):661-6. doi: 10.1038/clpt.1985.242.
Enalapril maleate (MK-421), a nonmercapto-containing angiotensin converting enzyme (ACE) inhibitor, is converted in vivo to enalaprilat (MK-422), the active diacid. We evaluated serum profiles and urinary excretion of oral enalapril maleate in patients with renal disease (group I, creatinine clearance less than 3 ml/min, patients undergoing dialysis, n = 10; group II, creatinine clearance 10 to 79 ml/min, n = 9) compared with healthy subjects (group III, creatinine clearance greater than 80 ml/min, n = 10). Group I received a 10 mg dose during a day while not receiving dialysis and a 10 mg dose 1 hour before dialysis 2 weeks later. Groups II and III received a single 10 mg dose. Blood samples and urine were collected for 48 hours. Impaired renal function resulted in elevated serum and plasma concentrations of enalapril maleate and decreased excretion rates and urinary recovery of enalapril maleate and enalaprilat. The data suggest an apparent increase in the extent of metabolism of enalapril maleate to enalaprilat or an increase in nonrenal elimination of unchanged enalapril maleate in renal disease compared with normal health. Enalaprilat was dialyzable.
马来酸依那普利（MK - 421）是一种不含巯基的血管紧张素转换酶（ACE）抑制剂，在体内可转化为活性二酸依那普利拉（MK - 422）。我们评估了肾病患者（第一组，肌酐清除率低于3 ml/min，正在接受透析的患者，n = 10；第二组，肌酐清除率为10至79 ml/min，n = 9）与健康受试者（第三组，肌酐清除率大于80 ml/min，n = 10）口服马来酸依那普利后的血清情况和尿排泄情况。第一组在未接受透析时一天服用10 mg剂量，两周后在透析前1小时服用10 mg剂量。第二组和第三组均单次服用10 mg剂量。采集血样和尿液48小时。肾功能受损导致马来酸依那普利的血清和血浆浓度升高，马来酸依那普利和依那普利拉的排泄率及尿回收率降低。数据表明，与正常健康状态相比，肾病患者中马来酸依那普利向依那普利拉的代谢程度明显增加，或未改变的马来酸依那普利的非肾清除增加。依那普利拉可被透析清除。
