title: Pharmacokinetic interactions of artemether and pyrimethamine in healthy male Thais.
abstract: The pharmacokinetics of a single oral dose of artemether (300 mg) and pyrimethamine (100 mg) given as each individual drug alone or as a drug combination (artemether 300 mg plus pyrimethamine 100 mg), were investigated in 8 healthy male Thai volunteers. Both artemether and pyrimethamine were rapidly absorbed after oral administration. Elimination of pyrimethamine was however, a relatively slow process compared with artemether, and thus resulted in a long terminal phase elimination half-life (50-106 hours). Pharmacokinetics of artemether and dihydroartemisinin following a single oral dose of artemether alone or in combination with pyrimethamine were similar. In contrast, coadministration of artemether resulted in significantly increased Cmax (medians of 818 vs 1,180 ng/ml) and contracted the apparent volume of distribution (medians of 3 vs 2.56 l/kg) of pyrimethamine.
authors.affiliation: Department of Microbiology, Faculty of Science, Mahidol University, Bangkok, Thailand.
authors.forename: P
authors.initials: P
authors.lastname: Tan-ariya
authors.forename: K
authors.initials: K
authors.lastname: Na-Bangchang
authors.forename: R
authors.initials: R
authors.lastname: Ubalee
authors.forename: A
authors.initials: A
authors.lastname: Thanavibul
authors.forename: P
authors.initials: P
authors.lastname: Thipawangkosol
authors.forename: J
authors.initials: J
authors.lastname: Karbwang
mesh_terms: D000328:Adult; D000962:Antimalarials / Q000097:blood / Q000493:pharmacokinetics*; D000077549:Artemether; D037621:Artemisinins; D018592:Cross-Over Studies; D004347:Drug Interactions; D006801:Humans; D008297:Male; D011739:Pyrimethamine / Q000097:blood / Q000493:pharmacokinetics*; D012717:Sesquiterpenes / Q000097:blood / Q000493:pharmacokinetics*; D013785:Thailand
chemical_list: D000962:Antimalarials; D037621:Artemisinins; D012717:Sesquiterpenes; D000077549:Artemether; D011739:Pyrimethamine