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Stereoselective pharmacokinetics of mefloquine in young children
A Bourahla1, C Martin, F Gimenez
1Hôpital Pitie Salpetriere Service Pharmacie 47, Paris, France.
Insights
Mefloquine pharmacokinetics in children show stereoselectivity, with differences in enantiomer levels and clearance similar to adults. This study investigated mefloquine enantiomer behavior in young children treated for malaria.
Area of Science:
- Pharmacology
- Clinical Pharmacy
- Pediatric Infectious Diseases
Background:
- Mefloquine is a key antimalarial drug.
- Understanding its pharmacokinetics in children is crucial for effective treatment.
- Stereospecificity may influence drug efficacy and safety.
Purpose of the Study:
- To investigate the stereospecificity of mefloquine pharmacokinetics in children.
- To compare mefloquine enantiomer behavior in pediatric patients with adult data.
Main Methods:
- Twelve children (6-24 months) received a single oral dose of racemic mefloquine with sulfadoxine and pyrimethamine.
- Mefloquine enantiomer concentrations were measured using chiral chromatography.
- Pharmacokinetic parameters were determined via model-independent analysis.
Main Results:
- The (-) mefloquine enantiomer exhibited higher plasma concentrations and longer half-lives.
- The (+) mefloquine enantiomer showed greater volume of distribution and total clearance.
- Significant stereoselectivity in mefloquine pharmacokinetics was observed.
Conclusions:
- Mefloquine pharmacokinetics in children demonstrate stereoselectivity.
- The observed stereoselectivity in children is comparable to that found in adults.
- These findings support consistent dosing strategies across age groups.
Objective:
the stereospecificity of mefloquine pharmacokinetics in children has been investigated.
Patients:
Twelve children aged 6 to 24 months were treated for uncomplicated falciparum malaria with a single oral dose of 25 mg.kg-1 racemic mefloquine in combination with sulfadoxine and pyrimethamine.
Methods:
concentrations of mefloquine enantiomers were determined using a coupled achiral-chiral chromatographic system. Pharmacokinetic parameters were calculated using model-independent analysis.
Results:
Maximum plasma concentrations, areas under the curve and apparent plasma elimination half-lives were higher for the (-) enantiomer than its antipode. In contrast, the apparent volume of distribution (V/f) and total clearance (Cl/f) values were higher for the (+) enantiomer.
Conclusion:
the stereoselectivity of mefloquine pharmacokinetics is similar to that observed in adults.