Disposition of monodesethylamodiaquine after a single oral dose of amodiaquine and three regimens for prophylaxis against Plasmodium falciparum malaria
| Autor: | F. Faurisson, M.C. Blayo, J. Le Bras, J. M. Scherrmann, Eric Pussard, F. Verdier |
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| Rok vydání: | 1987 |
| Předmět: |
Adult
Male medicine.medical_treatment Plasmodium falciparum Amiodarone Amodiaquine Pharmacology Single oral dose Pharmacokinetics Oral administration medicine Animals Humans Pharmacology (medical) Chemotherapy biology business.industry General Medicine Disposition Middle Aged biology.organism_classification medicine.disease Malaria Female business medicine.drug Half-Life |
| Zdroj: | European journal of clinical pharmacology. 33(4) |
| ISSN: | 0031-6970 |
| Popis: | The disposition of monodesethylamodiaquine was studied in four healthy subjects after a single oral dose of 10 mg/kg amodiaquine base. Amodiaquine was not found in any sample, but the major metabolite monodesethylamodiaquine was detected and was assumed to be the sole derivative that contributed significantly to antimalarial activity in the blood. The best fit for the decay of the metabolite was obtained with a three-compartment model. The half-lives of the first two phases were 3.2 to 11.4 h for t1/2 alpha 1 and 22.7 to 50.3 h for t1/2 alpha 2 in plasma. The half-life of the terminal phase (t1/2 beta) was between 9 and 18.2 days. The concentration in whole blood was 4- to 6-times higher than in plasma. Three schedules (alternate days, weekly, daily) of the conventional prophylactic dose of 10 mg/kg per week were compared in six other healthy subjects. There were significant differences in the plasma monodesethylamodiaquine levels between the three schedules. |
| Databáze: | OpenAIRE |
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