Effect of fluconazole on the pharmacokinetics of halofantrine in healthy volunteers
| Autor: | Gerhard K. E. Scriba, A. Adedapo, Ajibola A. Olaniyi, Yetunde T. Kolade, Chinedum P. Babalola |
|---|---|
| Rok vydání: | 2009 |
| Předmět: |
Adult
Male Pharmacology Antifungal Agents Cross-Over Studies Metabolite Cmax Phenanthrenes Biology Drug interaction Crossover study Antimalarials chemistry.chemical_compound Pharmacokinetics Halofantrine chemistry medicine Humans Drug Interactions Pharmacology (medical) Fluconazole Active metabolite medicine.drug |
| Zdroj: | Journal of Clinical Pharmacy and Therapeutics. 34:677-682 |
| ISSN: | 1365-2710 0269-4727 |
| Popis: | Summary Background: Halofantrine, an antimalarial drug used in endemic areas such as the tropics is mainly metabolized by CYP3A4 to the active metabolite N-desbutylhalofantrine. Fluconazole, an antifungal agent and an inhibitor of CYP3A4 is an established part of the therapy in HIV patients, who in turn are prone to malaria in the tropics. This study investigated the effect of fluconazole on the pharmacokinetics of halofantrine after concurrent administration of the two drugs. Methods: The effect of fluconazole on the pharmacokinetics of the antimalarial drug halofantrine was evaluated in 15 healthy volunteers in a Latin Square crossover design. The subjects received a single oral dose of 500 mg halofantrine hydrochloride alone or with 50 mg fluconazole after an overnight fast. Venous blood samples were collected during the next 336 h and analysed by HPLC for halofantrine and its active metabolite N-desbutylhalofantrine. Results: Co-administration of fluconazole did not alter the pharmacokinetics of halofantrine significantly with the exception of elimination t1/2 that was significantly increased by 25% (P |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|