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赖诺普利:一种新型血管紧张素转换酶抑制剂。

Lisinopril: a new angiotensin-converting enzyme inhibitor.

作者信息

Chase S L, Sutton J D

机构信息

Department of Pharmacy, Thomas Jefferson University Hospital, Camden, NJ.

出版信息

Pharmacotherapy. 1989;9(3):120-8; discussion 128-30. doi: 10.1002/j.1875-9114.1989.tb04117.x.

Abstract

Lisinopril is a synthetic, nonsulfhydryl, angiotensin-converting enzyme inhibitor. Its bioavailability is approximately 25% and is not affected by food. Hepatic metabolism is not required for pharmacologic effect, which occurs 1 hour after administration. Peak serum concentration and effect are delayed, occurring 6-8 hours after a single dose and lasting for at least 24 hours. The drug is eliminated primarily by the kidneys. The elimination half-life is 12.6 hours and is prolonged in renal impairment. Lisinopril 10-80 mg once a day is effective in lowering blood pressure in all grades of essential and renovascular hypertension. It is as effective as hydrochlorothiazide, atenolol, metoprolol, and nifedipine. Combining lisinopril with hydrochlorothiazide produces a greater degree of blood pressure reduction. Patients with congestive heart failure have demonstrated immediate and prolonged beneficial hemodynamic effects and increased exercise tolerance. Lisinopril is well tolerated. Clinically significant drug interactions have not been reported, but caution should be used when lisinopril is administered with diuretics, nifedipine, or agents that may increase concentrations of potassium. The usual initial oral dosage of lisinopril is 10 mg once a day (range 20-40 mg/day). Lower dosages may be necessary in patients with renal impairment or congestive heart failure, elderly persons, and those receiving diuretics.

摘要

赖诺普利是一种合成的、非巯基的血管紧张素转换酶抑制剂。其生物利用度约为25%,不受食物影响。药理作用无需肝代谢,服药后1小时起效。单次给药后6 - 8小时出现血清峰值浓度和效应延迟,且持续至少24小时。该药主要经肾脏排泄。消除半衰期为12.6小时,肾功能损害时半衰期延长。赖诺普利每日一次,剂量为10 - 80毫克,对各级原发性高血压和肾血管性高血压均有降压效果。其效果与氢氯噻嗪、阿替洛尔、美托洛尔和硝苯地平相当。赖诺普利与氢氯噻嗪联用可产生更大程度的血压降低。充血性心力衰竭患者已显示出即刻和持久的有益血流动力学效应以及运动耐量增加。赖诺普利耐受性良好。尚未报道有临床显著的药物相互作用,但赖诺普利与利尿剂、硝苯地平或可能增加钾浓度的药物合用时应谨慎。赖诺普利通常的初始口服剂量为每日一次10毫克(范围为20 - 40毫克/天)。肾功能损害或充血性心力衰竭患者、老年人以及接受利尿剂治疗的患者可能需要较低剂量。

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