Loperamide is an antidiarrheal used for general diarrhea and chronic diarrhea. Loperamide is taken orally as a pill. It is transported from the intestine into the intestinal epithelial cell possibly via solute carrier family 15 member 1, one of 3 drug transporters into epithelial cells. It is then transported into blood vessels via ATP-binding cassette sub-family C member 3. In the blood it travels to the target cells via the loperamide pathway as well as to the liver where it is transported into the liver hepatic cell vis P-glycoprotein. On the endoplasmic reticulum membrane loperamide is metabolized by Cytochrome P450 3A4, Cytochrome P450 2D6, Cytochrome P450 2C8, or Cytochrome P450 2B6 into N-Desmethyloperamide. The majority of loperamide is metabolized, but some leaves the liver with the metabolite N-Desmethyloperamide. They are transported into the bile ducts through the P-glycoprotein transporter. In the bile ducts they are then transported to the intestines where they are both excreted through the feces.

Loperamide Metabolism References