Oxamniquine (Vansil) is a tetrahydroquinoline that stimulates parasite muscular activity at low concentrations but causes paralysis at higher concentrations. The drug may act by esterification and binding of DNA, leading to the death of the schistosome by interruption of its nucleic acid and protein synthesis. The fluke may esterify oxamniquine to produce a reactive metabolite that alkylates parasite DNA. Resistance results from absent or defective esterifying activity of the drug. Oxamniquine has a restricted range of efficacy, being active only against S. mansoni infections.
Oxamniquine is given orally and is readily absorbed from the intestinal tract. Peak concentrations in plasma are obtained in about 3 hours. The drug is excreted in urine mostly as a 6-carboxyl derivative.
Side effects include CNS toxicity with unsteadiness and occasionally seizures, especially in patients with a history of seizures. It is contraindicated in pregnancy.
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