Primaquine metabolism by human liver microsomes: effect of other antimalarial drugs.

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Bangchang KN, Karbwang J, Back DJ

Primaquine metabolism by human liver microsomes: effect of other antimalarial drugs.

Biochem Pharmacol. 1992 Aug 4;44(3):587-90.

PubMed ID

1510705 [ View in PubMed

]

Abstract

A number of drugs have been studied for their effect on the metabolism of the antimalarial drug primaquine by human liver microsomes (N = 4) in vitro. The only metabolite generated was identified as carboxyprimaquine by co-chromatography with the authentic standard. Ketoconazole, a known inhibitor of cytochrome P450 isozymes, caused marked inhibition of carboxyprimaquine formation with IC50 and K(i) values of 15 and 6.7 microM, respectively. This finding and the dependency of metabolite formation on NADPH indicates that cytochrome P450 isozyme(s) catalysed metabolite production. Of compounds actually or likely to be coadministered with primaquine to malaria patients, only mefloquine produced any inhibition (K(i) = 52.5 microM). Quinine, artemether, artesunate, halofantrine and chloroquine did not significantly inhibit metabolite formation. It seems unlikely that the concurrent administration of mefloquine, or other antimalarials, with primaquine will lead to appreciably altered disposition.

DrugBank Data that Cites this Article

Drug Enzymes

Drug	Enzyme	Kind	Organism	Pharmacological Action	Actions
Mefloquine	Cytochrome P450 3A4	Protein	Humans	Unknown	Substrate Inhibitor	Details
Primaquine	Cytochrome P450 3A4	Protein	Humans	Unknown	Substrate Inhibitor	Details