Heel R C, Brogden R N, Speight T M, Avery G S
Drugs. 1980 Dec;20(6):409-52. doi: 10.2165/00003495-198020060-00001.
Captopril is the first orally active inhibitor of angiotensin-converting enzyme to become available. It has been studied primarily in hypertension. In mild to moderate essential hypertension captopril is about as effective as usual doses of hydrochlorothiazide or propranolol, about one-half of such patients needing the addition of a diuretic to achieve satisfactory control of blood pressure. In severe hypertension captopril plus a diuretic (and in some patients a beta-blocker) usually reduced blood pressure significantly more than could be achieved with 'standard triple therapy' in patients not responding adequately to such a regimen, and often resulted in an improved feeling of well-being in severely hypertensive patients previously receiving intensive multiple drug therapy. Indeed, at the present stage of the drug's development, patients not responding to or not tolerating 'traditional' antihypertensive therapy represent the most suitable candidates for captopril treatment. While captopril has been well tolerated in most patients, some troublesome or potentially serious side effects have been reported, including agranulocytosis, dysgeusia and reduced renal function; although a clear causal relationship with captopril was not always established, it would appear that the final place of captopril in the treatment of hypertension may ultimately depend on further clarification of its adverse effects profile. In addition to studies in hypertension, captopril has produced encouraging improvement in a small number of patients with severe congestive heart failure resistant to conventional therapy. Captopril must be considered an exciting addition to the therapeutic armamentarium; it, and pharmacologically related compounds of the future, will continue to generate much interest as their final place in therapy becomes better defined through additional well designed studies and wider clinical experience.
卡托普利是首个上市的口服活性血管紧张素转换酶抑制剂。它主要用于高血压的研究。在轻度至中度原发性高血压中，卡托普利的疗效与常规剂量的氢氯噻嗪或普萘洛尔相当，约一半的此类患者需要加用利尿剂才能使血压得到满意控制。在重度高血压中，卡托普利加利尿剂（部分患者还加用β受体阻滞剂）通常比未对“标准三联疗法”充分反应的患者采用该疗法能更显著地降低血压，并且常常能使先前接受强化多种药物治疗的重度高血压患者的幸福感得到改善。实际上，在该药物研发的现阶段，对“传统”抗高血压治疗无反应或不耐受的患者是卡托普利治疗的最合适人选。虽然大多数患者对卡托普利耐受性良好，但也有一些令人烦恼或潜在严重的副作用报道，包括粒细胞缺乏症、味觉障碍和肾功能减退；尽管与卡托普利的明确因果关系并非总能确立，但卡托普利在高血压治疗中的最终地位可能最终取决于对其不良反应谱的进一步明确。除了高血压研究外，卡托普利还使少数对传统治疗耐药的重度充血性心力衰竭患者有了令人鼓舞的改善。卡托普利必须被视为治疗药物库中令人兴奋的新增药物；随着通过更多精心设计的研究和更广泛的临床经验其在治疗中的最终地位得到更明确的界定，它以及未来的药理相关化合物将继续引发极大的兴趣。
