血管紧张素转换酶抑制剂综述。
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Piepho RW
血管紧张素转换酶抑制剂综述。
美国健康系统制药。2000年10月1日;57增刊1:S3-7。
- PubMed ID
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11030016 (PubMed视图］
- 摘要
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描述了血管紧张素转换酶(ACE)抑制剂的药理学及其在肾素-血管紧张素系统(RAS)中的作用，并介绍了药代动力学特性和常见的不良事件。ACE抑制剂通过调节有效的血管收缩素II在RAS中发挥重要作用。所有ACE抑制剂都有相同的基本结构;然而，它们可以根据它们的官能团(结合)分开:羧基、巯基或磷酸基。这些官能团在一定程度上是造成这些药物药代动力学和安全性差异的原因。卡托普利和赖诺普利是仅有的不需要通过肝脏生物转化激活的前药的ACE抑制剂。ACE抑制剂在亲脂性方面的差异被描述;福辛普利的亲脂性最强，赖诺普利的亲脂性最低。ACE存在于许多组织中，越来越多的证据表明，ACE抑制剂在抑制组织ACE能力方面存在差异。大多数ACE抑制剂主要由肾脏排出，少量通过肝脏排出。 Lisinopril is the only ACE inhibitor that does not require hepatic metabolism. In the selection of an ACE inhibitor for once-daily use to treat hypertension, differences in trough-peak ratios are clinically relevant. Fosinopril, ramipril, and trandolapril have minimum trough-peak ratios of 50% or greater. ACE inhibitors are generally well tolerated, with hypotension, cough, and hyperkalemia being the most frequently reported adverse effects for the entire class. Drug interactions across the ACE inhibitor class as well as agent-specific interactions are described. Factors to be considered in the selection of an ACE inhibitor include differences in potency, affinity for ACE, pharmacokinetics, and toxicity that are related to structural properties of the drug; whether the trough-peak ratio enables use of a once-daily dose; and potential adverse effects related to a drug's functional (binding) group.