Hedner T
Department of Clinical Pharmacology, Sahlgrenska University Hospital, Gothenburg, Sweden.
J Hypertens Suppl. 1999 Jun;17(2):S21-5.
Angiotensin-converting enzyme (ACE) inhibitors and angiotensin II type 1 (AT1) receptor antagonists have received increased therapeutic recognition in the treatment of hypertension. Although the overall effects of the ACE inhibitors and AT1 receptor antagonists may seem superficially similar, there are important differences between the two classes in terms of neurohumoral activation, concomitant bradykinin potentiation, and inhibition of angiotensin II, derived not only from the classical ACE pathway, but also from alternative pathways. The AT1 receptor antagonist eprosartan has been shown to lower blood pressure effectively in hypertensive patients. When taken in the recommended dose range, 600-800 mg once daily, eprosartan is effective in patients with all grades of hypertension, regardless of age, sex or race. In several clinical studies, the blood-pressure-lowering effect of eprosartan has been shown to be at least as great as that of the ACE inhibitor enalapril. With respect to tolerability, eprosartan is superior to ACE inhibitor therapy and comparable to placebo. The pharmacological and therapeutic profiles of the expanding array of AT1 receptor antagonists differ in a number of respects. Most of these agents are biphenyl tetrazole, non-competitive antagonists, and some have active metabolites. Eprosartan differs from other AT1 receptor antagonists in that it is a non-biphenyl, non-tetrazole competitive antagonist without active metabolites. Several large-scale, ongoing clinical research programmes (e.g. LIFE, SCOPE and VALUE) are expected to provide information on the extent to which AT1 receptor antagonists, in comparison with other therapeutic regimens, reduce cardiovascular morbidity and mortality in different groups of hypertensive subjects. Meanwhile, current evidence suggests that the AT1 receptor antagonists provide a new approach to the management of hypertension and that they merit a fuller assessment in other cardiovascular diseases.
血管紧张素转换酶（ACE）抑制剂和血管紧张素II 1型（AT1）受体拮抗剂在高血压治疗中获得了越来越多的治疗认可。尽管ACE抑制剂和AT1受体拮抗剂的总体效果表面上可能相似，但这两类药物在神经体液激活、伴随的缓激肽增强以及对血管紧张素II的抑制方面存在重要差异，这些差异不仅源于经典的ACE途径，还源于替代途径。已证明AT1受体拮抗剂依普罗沙坦能有效降低高血压患者的血压。当按推荐剂量范围（每日一次600 - 800毫克）服用时，依普罗沙坦对所有高血压分级的患者均有效，无论年龄、性别或种族。在多项临床研究中，依普罗沙坦的降压效果已被证明至少与ACE抑制剂依那普利相当。在耐受性方面，依普罗沙坦优于ACE抑制剂治疗，与安慰剂相当。不断增加的一系列AT1受体拮抗剂的药理和治疗特性在许多方面存在差异。这些药物大多数是联苯四唑类非竞争性拮抗剂，有些还有活性代谢物。依普罗沙坦与其他AT1受体拮抗剂不同，它是一种非联苯、非四唑类竞争性拮抗剂，没有活性代谢物。几个正在进行的大规模临床研究项目（如LIFE、SCOPE和VALUE）预计将提供有关与其他治疗方案相比，AT1受体拮抗剂在不同高血压患者群体中降低心血管发病率和死亡率程度的信息。同时，目前的证据表明，AT1受体拮抗剂为高血压管理提供了一种新方法，并且它们在其他心血管疾病中值得进行更全面的评估。
