The influence of food on the pharmacokinetics and ACE inhibition of cilazapril.

Abstract

1 The influence of food on the pharmacokinetics and angiotensin-converting enzyme (ACE) inhibitory effects of oral 5 mg doses of cilazapril was investigated in a two-way crossover study in 16 volunteers. 2 Plasma and urine concentrations of cilazaprilat, the active diacid metabolite of cilazapril, and plasma ACE activity were determined by a radio-enzymatic method.3 Cmax decreased by 30% (P < 0.05) with a delay in tmax of 1 h (P < 0.05) and area under curve (AUC) was decreased by 14% (P < 0.05). The elimination rate was unaltered.4 Onset of ACE inhibition was delayed by 30 min but degree and duration were unaffected.5 The effect of food on the bioavailability of cilazapril at this dose would not be expected to be clinically significant.

Pharmacology and Clinical Use of the New ACE‐Inhibitor Moexipril

“…This effect was not considered to be clinically relevant, however, since the degree of ACE inhibition by moexipril 24 hours after administration did not differ significantly between postprandial and fasting conditions (79% vs. 80.5%) (32). Reduced bioavailability after coadministration with food has also been reported for captopril (14) and cilazapril (25).…”

Food- and gender-dependent pharmacokinetics of paeoniflorin after oral administration with Samul-tang in rats

“…The peak plasma drug concentration (C max ) and the time to reach C max (T max ) were directly obtained from plasma data. The relative bioavailability of paeoniflorin (F rel ) for gender and food was determined from the ratio of AUC female /AUC male or AUC fed /AUC fasted (Massarella et al, 1989;Nadulski et al, 2005).…”

Pharmacological and Clinical Profile of Moexipril: A Concise Review

“…Also, moexipril should never be administered to pregnant women because of the danger of fetal injury or to patients with hypertension secondary to bilateral renal artery stenosis because of the danger of severe azotemia due to a decrease of the filtration pressure in the glomerulus 70 . Other side effects seen with the administration of moexipril include coughing (7%), vertigo (5%), diarrhea (4%), fatigue (3%), hyperkalemia (0.8%), azotemia (0.4%), and angioedema (0.1%) 15 . These side effects are not different compared to other ACE inhibitors 67 …”

“…12 Decreased bioavailability after food administration has also been reported for captopril 14 and cilazapril. 15…”