Studies on angiotensin I converting enzyme (ACE): Inhibitory effect of imidapril, a novel ACE inhibitor (II). Inhibition of various tissue ACEs ex vivo.

Hashimoto, Yoshikatsu; Kubo, Masami; Sugaya, Takeshi; Minobe, Satoshi; Watanabe, Taizo; Yamamura, Masatoshi; Matsuoka, Yoshiki

doi:10.1254/fpj.104.51

Cited by 5 publications

(4 citation statements)

References 8 publications

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“…It is interesting to know whether the difference in the affinities correlates with the difference in the degree of augmentation of BK-induced vascular leakage and with the incidence of dry cough induction after treatment with ACE inhibitors. Because imidapril has lower activities in these two responses than enalapril and captopril in spite of its compatible or higher inhibitory activity of ACE (17)(18)(19)(20). Okamura et al (33) studied the activity of ACE inhibitors from the viewpoint of substrate specificity using the isolated dog mesenteric artery and vein.…”

Section: Discussionmentioning

confidence: 99%

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Difference among Angiotensin-Converting Enzyme Inhibitors in Potentiating Effects on Bradykinin-Induced Microvascular Leakage in Guinea Pig Airways

Murata

Matsumoto

Kashida

et al. 1995

Japanese Journal of Pharmacology

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ABSTRACT-We investigated the effect of imidapril, a novel angiotensin-converting enzyme (ACE) inhibitor, on augmentation of airway microvascular leakage induced by bradykinin (BK) and substance P (SP) in guinea pigs and compared it with those of enalapril and captopril. The three ACE inhibitors significantly potentiated BK-and SP-induced airway microvascular leakage in a dose-dependent manner. In spite of the compatible or higher ACE inhibitory activity of imidapril, its potentiating activity in BK-induced leakage was lower than those of enalapril and captopril both by single administration (0.3-30 mg/kg, p.o.) and repeated administration for eight days (0.1-10 mg/kg/day, p.o.). The potentiating activities of the three ACE inhibitors were suppressed by pretreatment with a BK2-receptor antagonist, but not by neurokinin 1 and neurokinin 2 antagonists, suggesting that neurokinins may not be involved in BK-induced leakage under the conditions used. On the other hand, the potentiating effect of imidapril in SP-induced leakage was weaker than those of enalapril and captopril only after single high doses. The present study shows that the ACE inhibitors have different activity in potentiation of the airway microvascular leakage induced by BK, which may be ascribable to the difference in their inhibition of BK hydrolysis. This evidence may partly explain the smaller incidence of dry cough induced by imidapril compared with other ACE inhibitors when clinically used as antihypertensive drugs.

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Section: Discussionmentioning

confidence: 99%

“…Imidapril is a novel ACE inhibitor of the non-sulfhydryl type (16) that possesses potent ACE inhibitory activity (17,18) and antihypertensive activity in various animal models (19) and in patients (20,21). In clinical trials, the episode of cough induced by imidapril is reported to be less than those induced by enalapril and captopril (20,21).…”

mentioning

confidence: 99%

Difference among Angiotensin-Converting Enzyme Inhibitors in Potentiating Effects on Bradykinin-Induced Microvascular Leakage in Guinea Pig Airways

Murata

Matsumoto

Kashida

et al. 1995

Japanese Journal of Pharmacology

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“…Imidapril, like other ACE inhibitors, alleviates renal lesions in rat models of various types of nephropathy (1,25,29,119). Imidapril has been shown to inhibit renal ACE activity more potently than captopril or enalapril (35,50,100). In addition, it has been reported that imidapril increases renal NO production in rats (38,110) and improves insulin sensitivity in diabetic rats (68).…”

Section: Renal Insufficiencymentioning

confidence: 99%

“…First, the incidence of cough with imidapril is lower than with other ACE inhibitors (47,84,85), which is expected to improve patients' compliance. Second, imidapril potently suppresses ACE activity not only in the blood but also in the heart and vascular tissue (35,50,55,100), which may lead to an advantage over older ACE inhibitors by preventing tissue damage and cardiovascular diseases.…”

Section: Introductionmentioning

confidence: 99%

Protection of the Cardiovascular System by Imidapril, a Versatile Angiotensin‐Converting Enzyme Inhibitor

Hosoya

Ishimitsu

2002

Cardiovascular Drug Reviews

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Imidapril hydrochloride (imidapril) is a long-acting, non-sulfhydryl angiotensin-converting enzyme (ACE) inhibitor, which has been used clinically in the treatment of hypertension, chronic congestive heart failure (CHF), acute myocardial infarction (AMI), and diabetic nephropathy. It has the unique advantage over other ACE inhibitors in causing a lower incidence of dry cough. After oral administration, imidapril is rapidly converted in the liver to its active metabolite imidaprilat. The plasma levels of imidaprilat gradually increase in proportion to the dose, and decline slowly. The time to reach the maximum plasma concentration (T max ) is 2.0 h for imidapril and 9.3 h for imidaprilat. The elimination half-lives (t 1/2 ) of imidapril and imidaprilat is 1.7 and 14.8 h, respectively. Imidapril and its metabolites are excreted chiefly in the urine. As an ACE inhibitor, imidaprilat is as potent as enalaprilat, an active metabolite of enalapril, and about twice as potent as captopril. In patients with hypertension, blood pressure was still decreased at 24 h after imidapril administration. The antihypertensive effect of imidapril was dose-dependent. The maximal reduction of blood pressure and plasma ACE was achieved with imidapril, 10 mg once daily, and the additional effect was not prominent with higher doses. When administered to patients with AMI, imidapril improved left ventricular ejection fraction and reduced plasma brain natriuretic peptide (BNP) levels. In patients with mild-to-moderate CHF [New York Heart Association (NYHA) functional class II-III], imidapril increased exercise time and physical working capacity and decreased plasma atrial natriuretic peptide (ANP) and BNP levels in a dose-related manner. In patients with diabetic nephropathy, imidapril decreased urinary albumin excretion. Interestingly, imidapril improved asymptomatic dysphagia in patients with a history of stroke. In the same patients it 93

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A twelve-week, multicenter, randomized, double-blind, parallel-group, noninferiority trial of the antihypertensive efficacy and tolerability of imidapril and candesartan in adult patients with mild to moderate essential hypertension: The Iberian Multicenter Imidapril study on hypertension (IMISH)

Gámiz

Pêgo

Contreras

et al. 2006

Clinical Therapeutics

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Studies on angiotensin I converting enzyme (ACE): Inhibitory effect of imidapril, a novel ACE inhibitor (II). Inhibition of various tissue ACEs ex vivo.

Cited by 5 publications

References 8 publications

Difference among Angiotensin-Converting Enzyme Inhibitors in Potentiating Effects on Bradykinin-Induced Microvascular Leakage in Guinea Pig Airways

Difference among Angiotensin-Converting Enzyme Inhibitors in Potentiating Effects on Bradykinin-Induced Microvascular Leakage in Guinea Pig Airways

Protection of the Cardiovascular System by Imidapril, a Versatile Angiotensin‐Converting Enzyme Inhibitor

A twelve-week, multicenter, randomized, double-blind, parallel-group, noninferiority trial of the antihypertensive efficacy and tolerability of imidapril and candesartan in adult patients with mild to moderate essential hypertension: The Iberian Multicenter Imidapril study on hypertension (IMISH)

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