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Pharmacokinetics of intramuscular ceforanide in infants, children, and adolescents
Insights
This study on ceforanide pharmacokinetics in pediatric patients found that a 20 mg/kg dose every 12 hours is generally safe and effective. However, 1- to 2-year-olds require specific dosage adjustments due to shorter half-lives.
Area of Science:
- Pharmacology
- Pediatric Therapeutics
- Drug Metabolism
Background:
- Understanding the pharmacokinetics of antibiotics in pediatric populations is crucial for optimizing treatment efficacy and safety.
- Ceforanide is an antibiotic used to treat various bacterial infections.
- Pediatric patients exhibit diverse physiological characteristics that can influence drug disposition.
Purpose of the Study:
- To investigate the pharmacokinetic profile of intramuscular ceforanide in infants, children, and adolescents.
- To determine appropriate ceforanide dosing regimens for different pediatric age groups.
- To assess potential drug accumulation with repeated dosing.
Main Methods:
- Pharmacokinetic analysis of intramuscular ceforanide in 46 pediatric subjects (1 month to 17 years).
- Administration of 20 mg/kg ceforanide doses, with plasma concentration monitoring at various time points.
- Urine sample analysis to determine drug excretion rates.
Main Results:
- Mean peak plasma concentration of 56.3 microgram/ml, with mean 8-h and 12-h levels of 5.9 and 1.5 microgram/ml, respectively.
- Shorter ceforanide half-life (1.5 h) and lower plasma concentrations at 8 and 12 h observed in 1- to 2-year-old children.
- High urinary excretion (77.5% within 6 h, 93.9% within 12 h) with no drug accumulation at 12-h intervals.
Conclusions:
- A recommended intramuscular ceforanide dose of 20 mg/kg every 12 hours is suitable for most pediatric patients.
- Specific dosage recommendations are necessary for 1- to 2-year-old children due to altered pharmacokinetics.
- Ceforanide demonstrates predictable excretion and minimal accumulation in pediatric patients when administered every 12 hours.
Abstract:
We studied the pharmacokinetics of intramuscular ceforanide in 46 infants, children, and adolescents, ranging in age from 1 month to 17 years. After the subjects were given 20-mg doses of ceforanide per kg, the mean peak plasma concentration was 56.3 microgram/ml (range, 27.0 to 95.0), the mean 8-h level was 5.9 microgram/ml (range, 1.5 to 13.5), and the mean 12-h level was 1.5 microgram/ml (range, 0.2 to 4.2). Ceforanide half-life varied with the ages of the patients: in 1- to 2-year-old children, in half-life was significantly shorter (1.5 h) than in younger or older children. Plasma concentrations at 8 and 12 h after a dose were lowest in 1- to 2-year-old children. There was no relationship between the area under the curve, the volume of distribution, or the body clearance of ceforanide to the ages of the patients. Within 6 h of administration of the drug, a mean of 77.5% of a dose was excreted in urine, and at the end of 12 h, virtually all (93.9%) of the administered dose was recovered in urine samples. The administration of ceforanide every 12 h did not result in drug accumulation. A dose of 20 mg of ceforanide per kg every 12 h is recommended for most pediatric patients. Dosage recommendations for 1- to 2 year-old children are presented.