Disposition of atovaquone in humans | Zendy

P. Rolan | Zendy; AJ Mercer | Zendy; Edward W. Tate | Zendy; Ivor Benjamin | Zendy; John Posner | Zendy

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Disposition of atovaquone in humans

Author(s) -

P. Rolan,

AJ Mercer,

Edward W. Tate,

Ivor Benjamin,

John Posner

Publication year - 1997

Publication title -

antimicrobial agents and chemotherapy

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 2.07

H-Index - 259

eISSN - 1070-6283

pISSN - 0066-4804

DOI - 10.1128/aac.41.6.1319

Subject(s) - atovaquone , feces , pharmacokinetics , urine , chemistry , pharmacology , metabolism , medicine , physiology , biology , microbiology and biotechnology , immunology , plasmodium falciparum , malaria

Atovaquone is an antiprotozoal compound with good in vitro stability against metabolic inactivation. Previous human studies which did not involve radiolabelling had not accounted for a substantial proportion of the dose. The possible metabolism of atovaquone in men was examined in a radiolabelling study involving four healthy male volunteers. Radioactivity was eliminated almost exclusively via the feces. All radioactivity in plasma, urine, and feces was accounted for by atovaquone, with no evidence of metabolites. Radiolabelled atovaquone was administered to a patient with an indwelling biliary tube after surgery. Biliary radioactivity was approximately 10- to 40-fold higher than that in plasma and was accounted for by atovaquone. Atovaquone is not significantly metabolized in humans but is excreted into bile against a high concentration gradient.

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