PHARMACOKINETICS OF CARVEDILOL IN
CHILDREN WITH CONGESTIVE HEART FAILURE.
SORIN E. LEUCUŢA1, ANGELA BUTNARIU2, LAURIAN VLASE1,
DANIELA IACOB2, DANA MUNTEAN1
1University of Medicine and Pharmacy “Iuliu Haţieganu”, Cluj-Napoca,
Faculty of Pharmacy, Department of Pharmaceutical Technology and
Biopharmaceutics, 12, I.Creangă RO-400010
2University of Medicine and Pharmacy “Iuliu Haţieganu”, Cluj-Napoca,
Faculty of Medicine, Department of Pediatrics, 18, Victor Babeş, RO-400012
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Abstract:
In order to study the pharmacokinetics of carvedilol (CVD) in children with congestive heart failure, multiple per os doses of 0.05-0.1-0.2-0.4-0.8 mg/kg body weight were administered to 5 children, with at least one week wash-out time among doses. Plasma concentrations of CVD were determined during a 24 hours period following drug administration. Pharmacokinetic parameters of CVD were calculated using non-compartmental analysis. Following administration of CVD doses between 0.05-0.8 mg/kg bw, the mean normalized peak plasma level (Cmax) was 5.13±2.89 ng/mL. The time taken to reach Cmax, tmax, was 0.93±0.39 h and the total area under the curve (AUC0-∞) normalized to dose was 20.4±12.89 (ng/mL)·h. The mean half-life of CVD was 3.12±1.37 h. Although there is a large inter- and intra-subject variability, the pharmacokinetics of CVD in children with congestive heart failure is linear and some pharmacokinetic parameters (half-life, mean residence time) have different values in comparison with those registered in healthy adult population.
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