Less rapid systemic absorption as compared to loperamide. Possibly low systemic exposure. Probably CYP-metabolized. No data pointing to CYP-induction. Two references consider the substance (loperamide) generated in the intestines safe.

Prodrug till loperamide, used in diarrhoea, 1 mg after each instance of defeacation. Converted to loperamide in the intestines through bacterial action. Systemic absorbtion of loperamide formed from loperamideoxide is 50% slower than that of the substance given perorally. Metabolized by oxidative demethylation. No data given on CYP-interaction, loperamide:Use/safe