PMID- 12177688
OWN - NLM
STAT- MEDLINE
DCOM- 20021105
LR  - 20191106
IS  - 0897-5957 (Print)
IS  - 0897-5957 (Linking)
VI  - 20
IP  - 2
DP  - 2002 Summer
TI  - Protection of the cardiovascular system by imidapril, a versatile 
      angiotensin-converting enzyme inhibitor.
PG  - 93-110
AB  - 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 increased serum substance P levels, while the angiotensin 
      II receptor antagonist losartan was ineffective. These studies indicate that 
      imidapril is a versatile ACE inhibitor. In addition to its effectiveness in the 
      treatment of hypertension, CHF, and AMI, imidapril has beneficial effects in the 
      treatment of diabetic nephropathy and asymptomatic dysphagia. Good tissue 
      penetration and inhibition of tissue ACE by imidapril contributes to its 
      effectiveness in preventing cardiovascular complications of hypertension. The 
      major advantages of imidapril are its activity in the treatment of various 
      cardiovascular diseases and lower incidence of cough compared with some of the 
      older ACE inhibitors.
FAU - Hosoya, Kazuyoshi
AU  - Hosoya K
AD  - Department of Hypertension and Cardiorenal Medicine, Dokkyo University School of 
      Medicine, Mibu, Tochigi, Japan.
FAU - Ishimitsu, Toshihiko
AU  - Ishimitsu T
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PT  - Review
PL  - United States
TA  - Cardiovasc Drug Rev
JT  - Cardiovascular drug reviews
JID - 9006912
RN  - 0 (Angiotensin-Converting Enzyme Inhibitors)
RN  - 0 (Imidazoles)
RN  - 0 (Imidazolidines)
RN  - BW7H1TJS22 (imidapril)
SB  - IM
MH  - Angiotensin-Converting Enzyme 
      Inhibitors/pharmacokinetics/pharmacology/*therapeutic use
MH  - Arrhythmias, Cardiac/drug therapy
MH  - Cardiomegaly/drug therapy
MH  - Cardiovascular Diseases/*drug therapy
MH  - Clinical Trials as Topic
MH  - Deglutition Disorders/drug therapy
MH  - Heart Failure/drug therapy
MH  - Humans
MH  - Hypertension/drug therapy
MH  - Imidazoles/pharmacokinetics/pharmacology/*therapeutic use
MH  - *Imidazolidines
MH  - Kidney Failure, Chronic/drug therapy
MH  - Myocardial Ischemia/drug therapy
RF  - 119
EDAT- 2002/08/15 10:00
MHDA- 2002/11/26 04:00
CRDT- 2002/08/15 10:00
PHST- 2002/08/15 10:00 [pubmed]
PHST- 2002/11/26 04:00 [medline]
PHST- 2002/08/15 10:00 [entrez]
AID - 10.1111/j.1527-3466.2002.tb00185.x [doi]
PST - ppublish
SO  - Cardiovasc Drug Rev. 2002 Summer;20(2):93-110. doi: 
      10.1111/j.1527-3466.2002.tb00185.x.