Kawamura M, Imanishi M, Matsushima Y, Akabane S, Kuramochi M, Ito K, Omae T
Division of Hypertension and Nephrology, National Cardiovascular Center, Osaka, Japan.
Jpn J Pharmacol. 1990 Oct;54(2):143-9. doi: 10.1254/jjp.54.143.
The present study was designed to examine and compare the acute effects of lisinopril (20 mg) and enalapril (10 mg) after a single oral administration on the inhibition of the renin-angiotensin system (RAS) in eight normal subjects. Serum concentration of lisinopril and enalaprilat, an active metabolite of enalapril, reached the respective maximal levels at 6 and 4 hr after administration of the drugs. At 24 hr, the serum concentration of lisinopril was higher than that of enalapril; thus the rate of disappearance of lisinopril was retarded, in comparison to that of enalapril. The reduction of serum angiotensin I converting enzyme (ACE) activity was consistent with the pattern of increase of concentration of the drugs in the serum. However, with these two drugs, the concentration of plasma ANG II was decreased in a similar manner, and it returned to the pretreatment level within 24 hr. Thus, there was no significant difference in ANG II levels throughout the 24 hr-study between the lisinopril and enalapril treatment. The results indicate that a single administration of 20 mg lisinopril and 10 mg enalapril show similar potency for lowering the circulating ANG II level, although lisinopril exerts a more sustained inhibition of serum ACE activity. The measurement of ANG II provides useful informations for evaluating the efficacy of ACE inhibitors for the inhibition of circulatory RAS.
本研究旨在检测并比较8名正常受试者单次口服赖诺普利（20毫克）和依那普利（10毫克）后对肾素 - 血管紧张素系统（RAS）抑制的急性效应。赖诺普利及其活性代谢产物依那普利拉的血清浓度在给药后6小时和4小时分别达到各自的最高水平。24小时时，赖诺普利的血清浓度高于依那普利；因此，与依那普利相比，赖诺普利的消失速率较慢。血清血管紧张素I转换酶（ACE）活性的降低与血清中药物浓度升高的模式一致。然而，使用这两种药物时，血浆血管紧张素II（ANG II）的浓度以相似的方式降低，并在24小时内恢复到治疗前水平。因此，在整个24小时的研究中，赖诺普利和依那普利治疗之间的ANG II水平没有显著差异。结果表明，单次服用20毫克赖诺普利和10毫克依那普利在降低循环ANG II水平方面显示出相似的效力，尽管赖诺普利对血清ACE活性的抑制作用更持久。ANG II的测量为评估ACE抑制剂对循环RAS的抑制效果提供了有用的信息。
