Sassano P, Pedrinelli R, Magagna A, Abdel-Haq B, Salvetti A
Am J Cardiol. 1982 Apr 21;49(6):1574-6. doi: 10.1016/0002-9149(82)90395-2.
To compare the hemodynamic and humoral effects of increasing doses of captopril, blood pressure, heart rate, plasma renin activity, plasma aldosterone and angiotensin-converting enzyme activity were measured in 10 patients with mild uncomplicated essential hypertension before and after captopril given in an increasing dose of 25, 50 and 100 mg twice a day, with each dose given for 3 days. The maximal decrease in blood pressure, which was predicted both by basal plasma renin activity values and by the hypotensive response to the first dose, was found after the lowest (25 mg) dose; this effect was detectable for 12 hours independently of the dose administered. Similarly, plasma renin activity was already maximally increased and plasma aldosterone maximally decreased at the lowest dose, while angiotensin-converting enzyme activity showed a dose-dependent inhibition. These data suggest that (1) neither the magnitude nor the duration of the hypotensive effect nor the resin-stimulating and aldosterone-inhibiting actions of captopril are enhanced by drug doses above 25 mg (at least up to 100 mg), and (2) there was no apparent correlation between the degree of angiotensin-converting enzyme inhibition with increasing doses of captopril and the hypotensive effects of the drug.
为比较递增剂量卡托普利的血流动力学和体液效应，对10例轻度单纯原发性高血压患者，在每日两次给予递增剂量25mg、50mg和100mg卡托普利，且每个剂量给药3天前后，测量其血压、心率、血浆肾素活性、血浆醛固酮和血管紧张素转换酶活性。最低剂量（25mg）给药后，血压出现最大降幅，这由基础血浆肾素活性值及对首剂的降压反应所预测；该效应在给药12小时内均可检测到，且与给药剂量无关。同样，最低剂量时血浆肾素活性已最大程度升高，血浆醛固酮已最大程度降低，而血管紧张素转换酶活性呈剂量依赖性抑制。这些数据表明：（1）卡托普利剂量超过25mg（至少达100mg）时，其降压效应的幅度、持续时间以及刺激肾素和抑制醛固酮的作用均未增强；（2）卡托普利剂量增加时，血管紧张素转换酶的抑制程度与该药的降压效应之间无明显相关性。
