Doggrell Sheila A
Department of Physiology and Pharmacology, School of Biomedical Sciences, The University of Queensland, Brisbane, QLD 4072, Australia.
Expert Opin Pharmacother. 2002 Nov;3(11):1543-56. doi: 10.1517/14656566.3.11.1543.
Both angiotensin-converting enzyme (ACE) inhibitors and AT-1 receptor antagonists reduce the effects of angiotensin II, however they may have different clinical effects. This is because the ACE inhibitors, but not the AT-1 receptor antagonists, increase the levels of substance P, bradykinin and tissue plasminogen activator. The AT-1 receptor antagonists, but not the ACE inhibitors, are capable of inhibiting the effects of angiotensin II produced by enzymes other than ACE. On the basis of the present clinical trial evidence, AT-1 receptor antagonists, rather than the ACE inhibitors, should be used to treat hypertension associated with left ventricular (LV) hypertrophy. Both groups of drugs are useful when hypertension is not complicated by LV hypertrophy, and in diabetes. In the treatment of diabetes with or without hypertension, there is good clinical support for the use of either an ACE inhibitor or an AT-1 receptor antagonist. ACE inhibitors are recommended in the treatment of renal disease that is not associated with diabetes, after myocardial infarction when left ventricular dysfunction is present, and in heart failure. As the incidence of cough is much lower with the AT-1 receptor antagonists, these can be substituted for ACE inhibitors in patients with hypertension or heart failure who have persistent cough. Preliminary studies suggest that combining an AT-1 receptor antagonist with an ACE inhibitor may be more effective than an ACE inhibitor alone in the treatment of hypertension, diabetes with hypertension, renal disease without diabetes and heart failure. However, further trials are required before combination therapy can be recommended in these conditions.
血管紧张素转换酶（ACE）抑制剂和AT-1受体拮抗剂均可降低血管紧张素II的作用，但它们可能具有不同的临床效果。这是因为ACE抑制剂会升高P物质、缓激肽和组织纤溶酶原激活剂的水平，而AT-1受体拮抗剂则不会。AT-1受体拮抗剂能够抑制ACE以外的酶产生的血管紧张素II的作用，而ACE抑制剂则不能。根据目前的临床试验证据，治疗与左心室（LV）肥厚相关的高血压时，应使用AT-1受体拮抗剂而非ACE抑制剂。当高血压不伴有LV肥厚以及在糖尿病患者中，这两类药物均有用。在治疗伴有或不伴有高血压的糖尿病时，使用ACE抑制剂或AT-1受体拮抗剂均有充分的临床依据。ACE抑制剂被推荐用于治疗与糖尿病无关的肾脏疾病、存在左心室功能障碍的心肌梗死后患者以及心力衰竭患者。由于AT-1受体拮抗剂引起咳嗽的发生率要低得多，因此对于患有持续性咳嗽的高血压或心力衰竭患者，可以用它们替代ACE抑制剂。初步研究表明，在治疗高血压、高血压合并糖尿病、非糖尿病性肾脏疾病和心力衰竭时，将AT-1受体拮抗剂与ACE抑制剂联合使用可能比单独使用ACE抑制剂更有效。然而，在这些情况下推荐联合治疗之前，还需要进一步的试验。
