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Pharmacokinetics of intravenous chlorpheniramine in children
Insights
This study on chlorpheniramine disposition in children found that drug clearance generally decreased with age. The elimination half-life in children was shorter than in adults, likely due to higher clearance rates.
Area of Science:
- Pharmacokinetics
- Pediatric Pharmacology
- Drug Metabolism
Background:
- Chlorpheniramine is a commonly used antihistamine.
- Understanding its pharmacokinetic profile in children is crucial for safe and effective dosing.
Purpose of the Study:
- To characterize the disposition of chlorpheniramine in pediatric subjects.
- To evaluate age-related changes in chlorpheniramine pharmacokinetics.
Main Methods:
- Seven children aged 6-14 years received a 0.1 mg/kg intravenous dose of chlorpheniramine.
- Serum chlorpheniramine levels were monitored over time.
- Pharmacokinetic parameters including volume of distribution, clearance, and half-life were calculated.
Main Results:
- Serum chlorpheniramine levels declined biexponentially.
- Volume of distribution at steady state varied significantly (1.20–5.46 L/kg).
- Chlorpheniramine clearance showed approximately twofold variation (234–470 mL/hr/kg) and decreased with age.
- Mean elimination half-life in children was 9.6 hours, shorter than in adults.
Conclusions:
- Pediatric chlorpheniramine pharmacokinetics exhibit significant intersubject variability, particularly in the distribution phase.
- Age influences chlorpheniramine clearance, with higher rates observed in younger children.
- The shorter elimination half-life in children is attributed to higher clearance compared to adults.
Abstract:
The disposition of chlorpheniramine was examined in seven children, 6-14 years of age, following a 0.1 mg/kg iv dose. Postinjection serum chlorpheniramine levels in each subject declined biexponentially, with the greatest intersubject variability occurring in the initial distribution of the drug. The volume of distribution at steady state ranged from 1.20 to 5.46 liters/kg. The chlorpheniramine serum clearance varied approximately twofold (234-470 ml/hr/kg) and generally decreased with age. The chlorpheniramine elimination half-life in children (mean of 9.6 hr) appeared shorter than that in adults, probably due to higher chlorpheniramine serum clearance in children.