Wiseman L R, McTavish D
Adis International Limited, Auckland, New Zealand.
Drugs. 1994 Jul;48(1):71-90. doi: 10.2165/00003495-199448010-00007.
Trandolapril is a non-sulfhydryl prodrug which, after oral administration, is hydrolysed in the liver to its active diacid, trandolaprilat. Trandolaprilat inhibits the angiotensin converting enzyme (ACE) and displays similar pharmacodynamic properties to other ACE inhibitors, improving haemodynamic and cardiac parameters in patients with essential hypertension. Trandolapril 2 to 4mg once daily effectively controls blood pressure for at least 24 hours in patients with mild to moderate hypertension. In a small number of double-blind comparative trials, trandolapril had similar antihypertensive efficacy to that of atenolol, enalapril, hydrochlorothiazide, lisinopril and sustained release nifedipine, but was more effective than captopril. Combined therapy with trandolapril and hydrochlorothiazide or sustained release nifedipine had a significantly greater antihypertensive effect than either drug treatment alone. Further comparative trials are warranted to confirm these preliminary findings. The tolerability profile of trandolapril is similar to that of other ACE inhibitors, most adverse events being generally mild and transient in nature, and trandolapril lacks adverse effects on carbohydrate and lipid metabolism. Thus, trandolapril, with its favourable pharmacological profile and antihypertensive activity similar to that of agents currently used to treat patients with mild to moderate hypertension, is likely to provide a well tolerated option for the treatment of this disease. The results of ongoing and future clinical trials will determine its potential as a cardioprotective agent in patients following myocardial infarction.
群多普利是一种非巯基前体药物,口服后在肝脏中水解为其活性二酸群多普利拉。群多普利拉抑制血管紧张素转换酶(ACE),并表现出与其他ACE抑制剂相似的药效学特性,可改善原发性高血压患者的血流动力学和心脏参数。对于轻度至中度高血压患者,每日一次服用2至4毫克群多普利可有效控制血压至少24小时。在少数双盲对照试验中,群多普利的降压疗效与阿替洛尔、依那普利、氢氯噻嗪、赖诺普利和缓释硝苯地平相似,但比卡托普利更有效。群多普利与氢氯噻嗪或缓释硝苯地平联合治疗的降压效果明显大于单独使用任何一种药物治疗。有必要进行进一步的对照试验以证实这些初步发现。群多普利的耐受性与其他ACE抑制剂相似,大多数不良事件通常性质轻微且短暂,并且群多普利对碳水化合物和脂质代谢无不良影响。因此,群多普利具有良好的药理学特性,其降压活性与目前用于治疗轻度至中度高血压患者的药物相似,可能为该疾病的治疗提供一种耐受性良好的选择。正在进行的和未来的临床试验结果将决定其作为心肌梗死后患者心脏保护剂的潜力。