Noble T A, Murray K M
Drug Information Service, College of Pharmacy, University of South Carolina, Columbia 29208.
Clin Pharm. 1988 Sep;7(9):659-69.
The chemistry, pharmacology, pharmacokinetics, clinical use, adverse effects, and dosage of lisinopril are reviewed. Lisinopril, a new nonsulfhydryl angiotensin-converting-enzyme (ACE) inhibitor, is absorbed in its active form. Like the other ACE inhibitors, it lowers peripheral vascular resistance, with a resultant decrease in blood pressure. Approximately 29% of lisinopril is absorbed after oral administration. No measurable metabolism occurs, and excretion is primarily renal. Accumulation of lisinopril occurs in patients with renal dysfunction; however, dosage adjustment is necessary only when the creatinine clearance is less than 30 mL/min. Lisinopril has been shown to be an effective antihypertensive agent at doses of 10 to 80 mg given once daily in patients with essential and secondary hypertension caused by renal artery stenosis. The effectiveness of lisinopril is comparable to that with diuretics, beta blockers, and calcium-channel antagonists. In patients who are unresponsive to maximal doses of lisinopril alone, addition of another antihypertensive agent may be beneficial. Limited information suggests that lisinopril may be comparable to captopril for the treatment of congestive heart failure. Adverse effects associated with lisinopril are relatively minor and are comparable to those associated with enalapril. Hematological abnormalities have not been reported with lisinopril. Class-related adverse effects include cough, azotemia, angioedema, hypotension, and hyperkalemia. Lisinopril appears to be comparable to other ACE inhibitors for the treatment of hypertension and may be as effective as its predecessors for the treatment of congestive heart failure. Further study is needed to better define a therapeutic niche for lisinopril.
对赖诺普利的化学性质、药理学、药代动力学、临床应用、不良反应及剂量进行了综述。赖诺普利是一种新型非巯基血管紧张素转换酶（ACE）抑制剂，以活性形式被吸收。与其他ACE抑制剂一样，它可降低外周血管阻力，从而使血压下降。口服给药后，约29%的赖诺普利被吸收。无明显代谢发生，排泄主要通过肾脏。肾功能不全患者会出现赖诺普利蓄积；然而，只有当肌酐清除率低于30 mL/min时才需要调整剂量。在因肾动脉狭窄导致的原发性和继发性高血压患者中，已证明赖诺普利每日一次给予10至80 mg的剂量是一种有效的抗高血压药物。赖诺普利的有效性与利尿剂、β受体阻滞剂和钙通道拮抗剂相当。对于单独使用最大剂量赖诺普利无反应的患者，加用另一种抗高血压药物可能有益。有限的信息表明，赖诺普利在治疗充血性心力衰竭方面可能与卡托普利相当。与赖诺普利相关的不良反应相对较轻，与依那普利相关的不良反应相当。赖诺普利未报告血液学异常。类相关不良反应包括咳嗽、氮质血症、血管性水肿、低血压和高钾血症。赖诺普利在治疗高血压方面似乎与其他ACE抑制剂相当，在治疗充血性心力衰竭方面可能与其前代药物一样有效。需要进一步研究以更好地确定赖诺普利的治疗定位。
