Pharmacokinetics of imidapril and its active metabolite imidaprilat following single dose and during steady state in patients with impaired liver function

Hoogkamer, J. F. W.; Kleinbloesem, C. H.; Nokhodian, A.; Ouwerkerk, M.; Lankhaar, G; Ungethüm, W.; Kirch, Wilhelm

doi:10.1007/s002280050236

Cited by 7 publications

(3 citation statements)

References 6 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The authors concluded that minimum clinically effective doses should be given to patients with a creatinine clearance of <25 ml/min. open study in 16 subjects given once-daily single and multiple (seven) doses of oral imidapril 10 mg. 16 Eight subjects (mean age 43 years) had normal liver function and eight subjects (mean age 55 years) had impaired liver function (fatty liver disease in six cases and grade A Child-Pugh classification cirrhosis in two cases). There were no significant differences in C max , time to maximum plasma concentration, AUC or plasma beta-half-life between the two groups after one or seven doses, with the exception of imidaprilat C max on day 1, which was two-fold lower in the subjects with impaired hepatic function (p<0.05).…”

Section: Special Populationsmentioning

confidence: 97%

See 1 more Smart Citation

Review: Imidapril in Heart Failure

Doležal

2006

J Renin Angiotensin Aldosterone Syst

View full text Add to dashboard Cite

Angiotensin-converting enzyme (ACE) inhibitors improve the prognosis in mild, moderate and severe heart failure, as well as preventing the onset of heart failure in patients with chronic asymptomatic left-ventricular dysfunction and in those with reduced ejection fraction after myocardial infarction (MI). Imidapril is a longacting ACE inhibitor that is rapidly converted in the liver to its active metabolite, imidaprilat. Maximum plasma concentrations of imidapril and imidaprilat are achieved after 2 and 5-6 hours, respectively, with corresponding elimination half-lives of 1.1-2.5 and 10-19 hours. Imidapril is used in the treatment of hypertension, chronic heart failure, acute MI and diabetic nephropathy. In patients with mild-tomoderate chronic heart failure, imidapril 10 mg once-daily increased exercise time and physical working capacity, decreased plasma atrial natriuretic peptide and brain natriuretic peptide levels and reduced blood pressure. It also improved left ventricular ejection fraction, being significantly more effective than bisoprolol, in patients with acute MI. Imidapril is well tolerated and preliminary studies suggest it has an advantage over captopril and enalapril in terms of a lower incidence of cough. In conclusion, imidapril is a well-investigated versatile ACE inhibitor for the treatment of a range of cardiovascular diseases. BackgroundAlthough data on the incidence of heart failure are limited, it appears to range from one to five cases per 1,000 population each year in the general population, increasing steeply with age to more than 30 cases per 1,000 population each year among people aged 75 years or older.

show abstract

Section: Special Populationsmentioning

confidence: 97%

“…15 In eight healthy volunteers given imidapril 10 mg once-daily for seven days, the elimination half-life of imidapril ranged from 1.1 to 2.5 hours and that of imidaprilat from 10.1 to 14.7 hours; others have reported values of 18 to 19 hours for the half-life of imidaprilat. [14][15][16]…”

Section: Excretionmentioning

confidence: 99%

Review: Imidapril in Heart Failure

Doležal

2006

J Renin Angiotensin Aldosterone Syst

View full text Add to dashboard Cite

show abstract

“…Accumulation of imidaprilat is increased in patients with chronic renal failure (creatinine clearance <25 mL/min) (41). Although the conversion of imidapril to imidaprilat in the liver is delayed in patients with impaired liver function, no accumulation of either imidapril or imidaprilat occurred after repeated dosing (42).…”

Section: Pharmacokineticsmentioning

confidence: 99%

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

Hosoya

Ishimitsu

2002

Cardiovascular Drug Reviews

View full text Add to dashboard Cite

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

show abstract

Pharmacokinetics of imidapril and its active metabolite imidaprilat following single dose and during steady state in patients with chronic renal failure

Hoogkamer

Kleinbloesem

Nokhodian

et al. 1998

European Journal of Clinical Pharmacology

View full text Add to dashboard Cite

show abstract

Pharmacokinetics of imidapril and its active metabolite imidaprilat following single dose and during steady state in patients with impaired liver function

Abstract: Imidapril is regarded as an ACE inhibitor of which the pharmacokinetic disposition is only slightly affected in patients with impaired liver function.

Cited by 7 publications

References 6 publications

Review: Imidapril in Heart Failure

Review: Imidapril in Heart Failure

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

Pharmacokinetics of imidapril and its active metabolite imidaprilat following single dose and during steady state in patients with chronic renal failure

Contact Info

Product

Resources

About