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Benazepril盐酸盐口服后水解为活性代谢产物Benazeprilat,后者对ACE具有选择性抑制作用。本品对ACE实际上无抑制作用,代谢产物则口服吸收差。口服80分钟后,血浆原形浓度达峰值;1.5小时后活性代谢产物达血浆峰浓度,主要是在肝内水解。血浆原形在4小时后完全消失;代谢产物最初半减期3小时,终末半减期约22小时。原形主要经肝廓清,代谢产物则主要由肾廓清。老年人药动学 15例65~80岁男性口服本品单剂10mg后发现,血浆原形峰值和廓清率无明显变化,4小时后完全清除。但代谢产物消除半减期比年轻人长20~40%,肾
Benazepril hydrochloride is hydrolyzed orally to the active metabolite Benazeprilat, which selectively inhibits ACE. This product does not actually inhibit the role of ACE, metabolites are poor oral absorption. After 80 minutes of oral administration, the peak plasma concentration reached its peak. After 1.5 hours, the active metabolites reached peak plasma concentrations, mainly in the liver. Plasma prototype completely disappeared after 4 hours; metabolites were initially reduced by 3 hours, with a final half-life of about 22 hours. Prototype by the liver clearance, metabolites mainly by the renal clearance. Pharmacokinetics in the elderly 15 cases of 65 to 80-year-old male oral single dose of 10mg found no significant change in plasma peak and clearance rate, 4 hours after the complete removal. However, half of the elimination of metabolites longer than the young 20 to 40%, kidney