Sullivan J M, Ginsburg B A, Ratts T E, Johnson J G, Barton B R, Kraus D H, McKinstry D N, Muirhead E E
Hypertension. 1979 Jul-Aug;1(4):397-401. doi: 10.1161/01.hyp.1.4.397.
Captopril inhibits angiotensin II formation and bradykinin degradation in vivo. Eleven patients with essential hypertension (EH) and four patients with renovascular hypertension (RVH) were treated with captopril for periods ranging from 3 days to 12 months. All patients had a diastolic blood pressure (DBP) over 95 mm Hg after receiving a placebo for 3 days. Captopril given in ascending doses (10-1000 mg/day) caused normalization of blood pressure in all but three patients, one with severe RVH whose pressure fell 11%, one patient with severe EH, whose pressure fell 27%, and one with EH whose blood pressure fell 8.5%. The average control DBP in patients with EH was 113.7 +/- 5.5 (SE) mm Hg and fell to 89.9 +/- 3.6 mm Hg (p less than 0.001), while DBP in patients with RVH fell from 110.7 +/- 7.6 mm Hg to 94.5 +/- 8.2 (p less than 0.005). All patients were studied in balance on a 100 mEq sodium (Na) diet. Plasma renin activity (PRA) versus 24-hour urinary Na excretion increased sevenfold during therapy while converting enzyme activity fell by about one half. The magnitude of the blood pressure response was not related to control PRA. Cardiac output was estimated by echocardiography during placebo administration and during maintenance therapy with captopril. A significant change was not observed. Total peripheral resistance fell an average of 18.9% (p less than 0.05) in 11 of the 13 patients in whom the measurement could be made. It is concluded that captopril effectively lowers blood pressure in patients with EH or RHV by reducing total peripheral resistance.
卡托普利在体内可抑制血管紧张素II的形成并阻止缓激肽降解。11例原发性高血压（EH）患者和4例肾血管性高血压（RVH）患者接受了为期3天至12个月的卡托普利治疗。所有患者在接受3天安慰剂治疗后舒张压（DBP）均超过95 mmHg。给予递增剂量（10 - 1000 mg/天）的卡托普利后，除3例患者外，其余患者血压均恢复正常，这3例患者分别为：1例严重RVH患者，血压下降11%；1例严重EH患者，血压下降27%；1例EH患者，血压下降8.5%。EH患者的平均对照DBP为113.7±5.5（SE）mmHg，降至89.9±3.6 mmHg（p＜0.001），而RVH患者的DBP从110.7±7.6 mmHg降至94.5±8.2（p＜0.005）。所有患者均采用100 mEq钠（Na）饮食进行平衡研究。治疗期间，血浆肾素活性（PRA）与24小时尿钠排泄量增加了7倍，而转换酶活性下降了约一半。血压反应的幅度与对照PRA无关。在给予安慰剂期间和卡托普利维持治疗期间，通过超声心动图估计心输出量。未观察到显著变化。在13例可进行测量的患者中，有11例总外周阻力平均下降了18.9%（p＜0.05）。结论是，卡托普利通过降低总外周阻力有效降低EH或RVH患者的血压。
