Sullivan P A, Dineen M, Cervenka J, O'Connor D T
Mallow and Cork Regional Hospital, County Cork, Ireland.
Am J Hypertens. 1988 Jul;1(3 Pt 3):280S-283S. doi: 10.1093/ajh/1.3.280s.
Fosenopril, a new angiotensin-converting enzyme (ACE) inhibitor, is a prodrug that is converted to its active diacid metabolite after intestinal absorption. Its excretion is equally divided between hepatic and renal routes. This study details the efficacy of fosenopril at rest and during exercise on blood pressure, plasma potassium, plasma renin activity, and plasma aldosterone in 11 hypertensive males, mean age 55 years. Individual subjects underwent an identical exercise protocol (bicycle ergometry) on placebo and on active treatment. Supine mean blood pressure fell from 116 to 100 mm Hg, P less than 0.005, and at 9 minutes of exercise mean blood pressure fell from 137 to 125 mm Hg, P less than 0.01 on fosenopril. Plasma potassium fell slightly at rest from 4.27 to 3.96 mmol/L and during exercise from 5.23 to 4.93 mmol/L, both P less than 0.025. Plasma renin activity (ng/mL/hr) rose on fosenopril, at rest 0.94 to 4.72, and during exercise 2.06 to 10.39, both P less than 0.005. Aldosterone changes on treatment were marginal and nonsignificant. The compound was well tolerated and free of subjective and routine laboratory side effects. Its antihypertensive action is broadly similar to the other ACE inhibitors currently available.
福辛普利是一种新型血管紧张素转换酶(ACE)抑制剂,为前体药物,经肠道吸收后转化为其活性二酸代谢物。其排泄在肝脏和肾脏途径之间平均分配。本研究详细阐述了福辛普利在11名平均年龄55岁的男性高血压患者静息和运动时对血压、血钾、血浆肾素活性及血浆醛固酮的影响。个体受试者在服用安慰剂和活性药物治疗时接受相同的运动方案(自行车测力计运动)。服用福辛普利时,仰卧位平均血压从116毫米汞柱降至100毫米汞柱,P<0.005;运动9分钟时,平均血压从137毫米汞柱降至125毫米汞柱,P<0.01。血钾在静息时从4.27毫摩尔/升略有下降至3.96毫摩尔/升,运动时从5.23毫摩尔/升降至4.93毫摩尔/升,两者P均<0.025。服用福辛普利时血浆肾素活性(纳克/毫升/小时)升高,静息时从0.94升至4.72,运动时从2.06升至10.39,两者P均<0.005。治疗期间醛固酮变化轻微且无统计学意义。该化合物耐受性良好,无主观及常规实验室副作用。其降压作用与目前可用的其他ACE抑制剂大致相似。