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多沙唑嗪(DOX)存在一定心脏毒性作用,已非一线降压药物,但是作为治疗良性前列腺增生症合并下尿路症状(BPH/LUTS)的一线药物仍广泛应用于临床。同时,它可以轻度降低总胆固醇(TC)和甘油三脂(TG)水平。为减轻DOX心血管的不良反应,对其进行了手性拆分,发现DOX的分子中存在一个手性中心和一对光学异构体,即右旋多沙唑嗪((+)DOX)和左旋多沙唑嗪((-)DOX)。发现(-)DOX可能成为心血管不良反应较小的治疗BPH/LUTS药物。现就(±)DOX及其光学异构体对血脂代谢的作用的研究进展作一综述。
Doxazosin (DOX) has some cardiotoxic effect and is not a front-line antihypertensive drug. However, DOX is widely used as a first-line drug in the treatment of benign prostatic hyperplasia with lower urinary tract symptoms (BPH / LUTS). At the same time, it can slightly reduce total cholesterol (TC) and triglyceride (TG) levels. In order to reduce the cardiovascular adverse reactions of DOX, it was chirally resolved and found that there is a chiral center and a pair of optical isomers in DOX molecule, ie, doxazosin ((+) DOX) and L-Doxazosin ((-) DOX). Discovery of (-) DOX may be a treatment of BPH / LUTS with less adverse cardiovascular events. The research progress on the effect of (±) DOX and its optical isomers on lipid metabolism is reviewed.