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多沙唑嗪(doxazosin,简称DOX)是一种新的长效选择性突触后α_1受体阻滞剂,其结构类似哌唑嗪,为第二代选择性α_1受体阻滞剂。与哌唑嗪相比,本品具有降压作用强、半减期长、给药次数少等优点。本文综述DOX的药动学、药理作用和临床评价。一、药动学 DOX口服吸收迅速完全,给药2.4±0.7小时后血药浓度达峰值,5.7±0.1小时后达最大降压作用,一次给药后其降压作用可维持12～24小时。本品主要在肝脏经O-脱甲基(23%)和C-羟基化(12%)作用后在
Doxazosin (DOX) is a new long-acting selective post-synaptic alpha 1 receptor blocker with prazosin-like structure and is the second-generation selective alpha-1 blocker. Compared with prazosin, this product has the advantages of strong antihypertensive effect, long half-term delay, fewer administration times and so on. This article reviews DOX pharmacokinetics, pharmacological effects and clinical evaluation. First, pharmacokinetics DOX oral absorption quickly and completely, after administration of 2.4 ± 0.7 hours peak plasma concentration, 5.7 ± 0.1 hours after the maximum antihypertensive effect, after a dose of antihypertensive effect can be maintained for 12 to 24 hours. This product is mainly in the liver by O-demethylation (23%) and C-hydroxylation (12%) after the role