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Pharmacokinetics of Chlorproguanil in Man after a Single Oral Dose of Lapudrine®
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1988
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Whole BloodPharmacotherapyMolecular PharmacologyGas ChromatographyHealthy Male VolunteersBioanalysisAnalytical ChemistryToxicologyLiquid ChromatographyClinical ChemistryChromatographyTherapeutic Drug MonitoringPharmacokinetic ModelingPharmacokinetic ParametersChromatographic AnalysisPharmacologyPhysiologyClinical PharmacologyMedicineSingle Oral DosePharmacokineticsDrug Analysis
The pharmacokinetic parameters of chlorproguanil (Lapudrine) and its active metabolite, chlorcycloguanil, were determined in 6 healthy male volunteers after a single oral dose of 4 Lapudrine tables (80 mg). The mean maximum plasma chlorproguanil concentration was 36.7 +/- (SD) 7.9 ng/ml and was reached at 3.8 +/- 1.3 h. The chlorproguanil elimination half-life was 17.5 +/- 6.7 h and its plasma clearance was 1.28 +/- 0.12 l/h/kg. The mean whole blood to plasma ratio was 3.1 at 4 h after dosing. Chlorcycloguanil could not be quantified in plasma and whole blood at the detection limit of 10 ng/ml using a high-performance liquid chromatographic method. An excretion rate-time plot from urine data shows a rapid (t1/2 = 20 h) and a slow phase (t1/2 = 51 h) in the elimination of chlorcycloguanil. Our findings suggest that the current prophylactic regimen of chlorproguanil hydrochloride (20 mg weekly) may not be optimal in preventing infections with chloroquine-resistant falciparum malaria.