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甲巯丙脯酸(captopril,SQ14225)首次合成于1976年。目前国产甲疏丙脯酸已问世,并投入临床使用。甲巯丙脯酸是血管紧张素转换酶抑制剂,通过抑制血管紧张素转换酶,降低肾素—血管紧张素(R—A)系统的活性,减少血管紧张素Ⅱ(AⅡ)的形成,从而抑制R—A系统的效应。AⅡ是强有力的缩血管物质,当AⅡ减少时,血管壁的张力降低,血管扩张,血压降低。此药还抑制激肽释放酶—激肽(K—K)系统中的激肽酶Ⅱ,减少激肽的灭活,增加激肽的舒血管效应。近来研究还提示,此药还会间接导致前列腺素(PG_(E2))合成增加,降压作用增强。
Captopril (SQ14225) was first synthesized in 1976. At present, China made Jia Pinjian acid has come out and put into clinical use. Captopril is an angiotensin-converting enzyme inhibitor that decreases the activity of the renin-angiotensin (R-A) system and reduces the formation of angiotensin II (AII) by inhibiting angiotensin-converting enzyme Inhibit the effects of R-A system. A Ⅱ is a strong vasoconstrictor substance, when A Ⅱ decreases, the vessel wall tension decreases, vasodilation, lower blood pressure. The drug also inhibits kallikrein II in the kallikrein-kinin system, reducing kinin inactivation and increasing the vasodilator effect of kinins. Recent studies also suggest that this drug will indirectly lead to prostaglandin (PG_ (E2)) synthesis increased antihypertensive effect.