Gotoh M, Mizuno K, Hashimoto S, Kunii N, Fukuchi S
Nihon Naibunpi Gakkai Zasshi. 1985 May 20;61(5):619-29. doi: 10.1507/endocrine1927.61.5_619.
The acute antihypertensive effect of a new long-acting oral angiotensin I-converting enzyme (ACE) inhibitor, enalapril maleate, was assessed in 20 hypertensive patients, of whom 14 had essential hypertension, 4 had renovascular hypertension, one had hypertension associated with chronic renal failure, and one had primary aldosteronism. Enalapril maleate significantly lowered the blood pressure in either low-renin or normal- and high-renin hypertensives. There was a significant correlation for all patients as a group between the pretreatment levels of serum ACE activity and the reduction in mean blood pressure (r = -0.454, p less than 0.05, n = 20) 2 h after drug administration. The serum ACE activity decreased maximally 3 to 4 hours after drug administration and did not return to baseline levels within 24 h. There was a significant correlation between the reduction in mean blood pressure and changes in ACE activity 90 min and 2 h after drug administration, respectively, for all patients as a group (r = 0.495, p less than 0.05, n = 20, at 90 min; r = 0.508, p less than 0.05, n = 20, at 2 h). The plasma renin activity (PRA) significantly increased in normal- and high-renin hypertensives but not in low-renin hypertensives. There was a close correlation between the reduction in mean blood pressure and the PRA 8 h after drug administration in normal- and high-renin patients (r = -0.623, p less than 0.05, n = 13), while no such relationship was observed in low-renin patients. The plasma aldosterone concentration (PAC) significantly decreased within 3 h, the lowest values occurring at 8 h after drug administration, and it returned to baseline levels within 24 h in all patients. No relationship was found between the reduction in mean blood pressure and changes in PAC after drug administration in either low-renin or normal- and high-renin hypertensives. The plasma bradykinin concentration (PBC) increased within 1 h, the highest values occurring at 3 h after drug administration, and returned to baseline levels within 24 h in low-renin hypertensives, while the PBC was significantly increased at 4 h and had not returned to baseline levels within 24 h in normal- and high-renin hypertensives. There was a significant correlation between percentage changes in mean blood pressure and those in PBC 90 min after drug administration in normal- and high-renin hypertensives (r = -0.556, p less than 0.05, n = 13), while no relationship was observed between them in low-renin hypertensives.(ABSTRACT TRUNCATED AT 400 WORDS)
对一种新型长效口服血管紧张素I转换酶（ACE）抑制剂马来酸依那普利的急性降压作用进行了评估，研究对象为20例高血压患者，其中14例为原发性高血压，4例为肾血管性高血压，1例为伴有慢性肾衰竭的高血压，1例为原发性醛固酮增多症。马来酸依那普利可显著降低低肾素型或正常肾素及高肾素型高血压患者的血压。作为一个整体，所有患者给药2小时后，血清ACE活性的预处理水平与平均血压降低之间存在显著相关性（r = -0.454，p < 0.05，n = 20）。给药后3至4小时血清ACE活性最大程度降低，且24小时内未恢复至基线水平。作为一个整体，所有患者给药90分钟和2小时后，平均血压降低与ACE活性变化之间分别存在显著相关性（给药90分钟时，r = 0.495，p < 0.05，n = 20；给药2小时时，r = 0.508，p < 0.05，n = 20）。正常肾素及高肾素型高血压患者的血浆肾素活性（PRA）显著升高，而低肾素型高血压患者则无此变化。正常肾素及高肾素型患者给药8小时后，平均血压降低与PRA之间存在密切相关性（r = -0.623，p < 0.05，n = 13），而低肾素型患者未观察到这种关系。血浆醛固酮浓度（PAC）在3小时内显著降低，给药8小时时降至最低值，所有患者在24小时内均恢复至基线水平。低肾素型或正常肾素及高肾素型高血压患者给药后，平均血压降低与PAC变化之间均未发现相关性。血浆缓激肽浓度（PBC）在1小时内升高，给药3小时时达到最高值，低肾素型高血压患者在24小时内恢复至基线水平，而正常肾素及高肾素型高血压患者在4小时时PBC显著升高，24小时内未恢复至基线水平。正常肾素及高肾素型高血压患者给药90分钟后，平均血压变化百分比与PBC变化百分比之间存在显著相关性（r = -0.556，p < 0.05，n = 13），而低肾素型高血压患者两者之间未观察到相关性。（摘要截选至400字）
