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

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