Langtry H D, Markham A
Adis International Limited, Auckland, New Zealand.
Drugs Aging. 1997 Feb;10(2):131-66. doi: 10.2165/00002512-199710020-00006.
Lisinopril, the lysine analogue of enalaprilat, is a long-acting angiotensin converting enzyme (ACE) inhibitor which is administered once daily by mouth. The efficacy of lisinopril in reducing blood pressure is well established in younger populations, and many trials now show it to be effective in lowering blood pressure in elderly patients with hypertension. In comparative and non-comparative clinical trials, 68.2 to 89.1% of elderly patients responded (diastolic pressure < or = 90 mm Hg) to > or = 8 weeks' lisinopril treatment. Age-related differences in antihypertensive efficacy do not appear to be clinically significant, and dosages effective in elderly patients tend to range from 2.5 to 40 mg/day. Dosages usually need to be lower in patients with significant renal impairment. In congestive heart failure, lisinopril 2.5 to 20 mg/day increases exercise duration, improves left ventricular ejection fraction and has no significant effect on ventricular ectopic beats. It is similar in efficacy to enalapril and digoxin and similar or superior to captopril on most end-points. Data from the GISSI-3 post-myocardial infarction trial show that lisinopril reduced mortality and left ventricular dysfunction when given for 42 days starting within 24 hours of the onset of infarction symptoms. Results at 6 weeks and 6 months were similar in elderly and younger patients. Elderly patients, however, among other subgroups, exhibited a strong reduction in risk of low ejection fraction after treatment (-25.5%). Economic studies suggest that lisinopril is cost saving compared with other ACE inhibitors in some markets. When given according to the GISSI-3 protocol, lisinopril appears to be one of the less expensive of the successful ACE inhibitor regimens for acute myocardial infarction. In other trials, patients with diabetic nephropathy and hypertension improved or did not deteriorate during lisinopril treatment. Blood pressure was controlled and reductions or trends towards reductions in albuminuria were observed. These reductions were similar to those in diltiazem, nifedipine and verapamil recipients, and greater than those in patients receiving atenolol. Lisinopril appears to reduce mortality in diabetic patients after myocardial infarction and may also improve neuropathy associated with diabetes. Lisinopril is well tolerated and the profile of adverse events seen is typical of ACE inhibitors as a class. There is a tendency for more elderly than younger patients to discontinue treatment, but this trend is not clearly related to the incidence of adverse events in these age groups. Drug interactions occur with few other agents and are usually clinically significant only between lisinopril and either diuretics or lithium. Lisinopril is, thus, an effective treatment for elderly patients with hypertension, congestive heart failure and acute myocardial infarction and has shown promising benefits in patients with diabetic nephropathy.
赖诺普利是依那普利拉的赖氨酸类似物，是一种长效血管紧张素转换酶（ACE）抑制剂，每日口服一次。赖诺普利在年轻人群中降低血压的疗效已得到充分证实，现在许多试验表明它对老年高血压患者降低血压也有效。在比较性和非比较性临床试验中，68.2%至89.1%的老年患者在接受≥8周的赖诺普利治疗后有反应（舒张压≤90mmHg）。抗高血压疗效的年龄相关差异在临床上似乎并不显著，老年患者有效的剂量范围往往为2.5至40mg/天。肾功能严重受损的患者剂量通常需要降低。在充血性心力衰竭中，赖诺普利2.5至20mg/天可增加运动持续时间，改善左心室射血分数，对室性早搏无显著影响。其疗效与依那普利和地高辛相似，在大多数终点方面与卡托普利相似或更优。GISSI-3心肌梗死后试验的数据表明，在梗死症状发作后24小时内开始给予赖诺普利42天，可降低死亡率和左心室功能障碍。6周和6个月时老年患者和年轻患者的结果相似。然而，老年患者在其他亚组中，治疗后低射血分数风险显著降低（-25.5%）。经济学研究表明，在某些市场中，与其他ACE抑制剂相比，赖诺普利具有成本效益。按照GISSI-3方案给药时，赖诺普利似乎是急性心肌梗死成功的ACE抑制剂治疗方案中成本较低的药物之一。在其他试验中，糖尿病肾病和高血压患者在赖诺普利治疗期间病情改善或未恶化。血压得到控制，观察到蛋白尿减少或有减少趋势。这些减少与地尔硫卓、硝苯地平和维拉帕米治疗的患者相似，且大于阿替洛尔治疗的患者。赖诺普利似乎可降低糖尿病患者心肌梗死后的死亡率，还可能改善与糖尿病相关的神经病变。赖诺普利耐受性良好，所观察到的不良事件情况是ACE抑制剂这一类药物的典型情况。老年患者比年轻患者更倾向于停药，但这种趋势与这些年龄组中不良事件的发生率并无明显关联。与其他药物很少发生药物相互作用，通常仅在赖诺普利与利尿剂或锂之间具有临床显著意义。因此，赖诺普利是老年高血压、充血性心力衰竭和急性心肌梗死患者的有效治疗药物，并且在糖尿病肾病患者中已显示出有前景的益处。
