Giudicelli J F
Presse Med. 1985 Dec 19;14(44):2209-11.
Enalapril is an inhibitor of the converting enzyme which transforms angiotensin I into angiotensin II, an octapeptide with pharmacological properties uniformly tending to increase blood pressure. The enalapril molecule is not active until it has been hydrolyzed into enalaprilic acid in the liver. This acid induces a very strong (85-95%), very early (maximum at 2 hours) and long lasting (20% at 72 hours) blockade of the angiotensin-converting enzyme, resulting in a paralleled fall in systolic and diastolic blood pressure. The fall begins with a 2.5 mg dose of the drug, is maximum with 10 mg and is not increased by higher doses. No tachyphylaxis has been observed with prolonged administration. The fall in blood pressure is due to reduction of peripheral resistance, without changes in heart rate and cardiac output. There is no sodium retention. The two main pharmacokinetic features of the drug are its very long half-life and the 100% urinary excretion of the active metabolite. The drug can be taken as a single dose at any moment of the day. The only known interaction is with propranolol, which reduces by one-third the bioavailability of enalapril. Side-effects are uncommon and mild.
依那普利是一种转化酶抑制剂，该转化酶可将血管紧张素I转化为血管紧张素II，血管紧张素II是一种八肽，其药理特性通常会导致血压升高。依那普利分子在肝脏中水解为依那普利酸之前是没有活性的。这种酸会引起血管紧张素转换酶非常强烈（85%-95%）、非常早期（2小时时达到最大值）且持久（72小时时为20%）的抑制，导致收缩压和舒张压同时下降。血压下降从2.5毫克剂量的药物开始，10毫克时达到最大值，更高剂量不会使其进一步升高。长期给药未观察到快速耐受性。血压下降是由于外周阻力降低，心率和心输出量无变化。不存在钠潴留。该药物的两个主要药代动力学特征是其半衰期非常长以及活性代谢产物100%经尿液排泄。该药物可在一天中的任何时刻单次服用。唯一已知的相互作用是与普萘洛尔，普萘洛尔会使依那普利的生物利用度降低三分之一。副作用不常见且轻微。
