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Arpraziquantel ((R)-praziquantel) is the eutomer (the biologically active enantiomer) of praziquantel, and is a medication which is currently under investigation for the treatment of schistosomiasis in young children since it has less side effects than the usual racemic mixture formulation of praziquantel.
Praziquantel is well absorbed (about 80%) from the gastrointestinal tract. However, due to extensive first-pass metabolism, only a relatively small amount enters systemic circulation. Praziquantel has a serum half-life of 0.8 to 1.5 hours in adults with normal renal and liver function. Metabolites have a half-life of 4 to 5 hours.
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Oxamniquine acts mainly on male worms, but also induces small changes on a small proportion of females. Like praziquantel, it promotes more severe damage of the dorsal tegument than of the ventral surface. The drug causes the male worms to shift from the mesenteric circulation to the liver, where the cellular host response causes its final ...