An Investigation into the Effects of Ivermectin and Praziquantel on the Intestinal Transport and Metabolism of Albendazole

Abstract

Preliminary investigation into the effects of ivermectin and praziquantel on the intestinal transport and biotransformation of albendazole was carried out on the rat using the in-vitro gut-sac method. Drug detection was carried out by high performance liquid chromatography. Ivermectin caused a 3-5-fold (P<0.01) increase in serosal concentrations of albendazole over the control at both the 60 and 120-minute study while the two higher concentrations of ivermectin resulted in a 3-fold (P<0.0001) increase in albendazole biotransformation campared to the control at all time points. Praziquantel had no effect on albendazole or albendazole sulphoxide.
As both albendazole and ivermectin are substrates of cytochrome 3A4 (CYP3A4) and P-glycoprotein transporter protein, the data is suggestive of a strong interaction between albendazole and ivermectin at P-glycoprotein level that results in an increased absorption albendazole as well as the transformation of albendazole sulfoxide.