血管紧张素转换酶抑制剂的概述。
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Piepho RW
血管紧张素转换酶抑制剂的概述。
是J卫生系统制药。2000年10月1日,57增刊1:S3-7。
- PubMed ID
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11030016 (在PubMed]
- 文摘
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药理学的血管紧张素转换酶(ACE)抑制剂在肾素-血管紧张素系统(RAS)和他们的作用是描述,和药代动力学特性和常见的不良事件。血管紧张素转换酶抑制剂发挥至关重要的作用在RAS规范有效的血管收缩的血管紧张素ⅱ。血管紧张素转换酶抑制剂共享相同的基本结构;然而,他们可以被分离的基础上功能(绑定)组:羧基,巯基或phosphinyl。这些官能团,部分负责的差异这些药物的药代动力学和安全配置文件。卡托普利和赖诺普利是唯一不高活性化合物需要激活血管紧张素转换酶抑制剂通过肝生物转化。亲油性的ACE抑制剂是描述之间的差异;fosinopril最大的亲油性,赖诺普利。ACE是发现在许多组织中,有越来越多的证据表明差异ACE抑制剂抑制的能力组织王牌。大多数血管紧张素转换酶抑制剂消除主要通过肾脏和一定程度上的肝脏。 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.