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Oxamniquine


ACCESSION NB: DB01096 (APRD01150)


TYPE: small molecule


GROUP: approved


DESCRIPTION:
An anthelmintic with schistosomicidal activity against Schistosoma mansoni, but not against other Schistosoma spp. Oxamniquine causes worms to shift from the mesenteric veins to the liver where the male worms are retained; the female worms return to the mesentery, but can no longer release eggs. (From Martidale, The Extra Pharmacopoeia, 31st ed, p121)

VOLUME OF DISTRIBUTION: Not Available

CATEGORIES:
Schistosomicides

ABSORPTION: Well absorbed orally

INDICATION:
For treatment of Schistosomiasis caused by Schistosoma mansoni

PHARMACODYNAMICS:
Oxamniquine is an anthelmintic with schistosomicidal activity against Schistosoma mansoni, but not against other Schistosoma spp. Oxamniquine causes worms to shift from the mesenteric veins to the liver where the male worms are retained; the female worms return to the mesentery, but can no longer release egg.

MECHANISM OF ACTION:
Oxamniquine may associate with an irreversible inhibition of the nucleic acid metabolism of the parasites. A hypothesis has been put forth that the drug is activated by a single step, in which a schistosome sulfotransferase enzyme converts oxamniquine into an ester (probably acetate, phosphate, or sulfate). Subsequently, the ester spontaneously dissociates, the resulting electrophilic reactant is capable of alkylation of schistosome DNA.

PROTEIN BINDING:
Not Available

METABOLISM:
Probably hepatic

TOXICITY:
Not Available

AFECTED ORGANISMS:
Schistosoma mansoni