Difenoxin

Mechanism of action:
Difenoxin is an opioid. It binds to μ-opioid receptors in the intestine and in the enteric plexus of the intestinal wall, inhibiting neurons from releasing neurotransmitters such as acetylcholine and thereby reducing smooth muscle contraction and peristaltic activity. The result is prolonged intestinal transit time, increased reabsorption of water and electrolytes, and firmer stools with less diarrhea. At therapeutic doses, its central nervous system effects are usually relatively weak, although overdose may still produce reactions related to central nervous system depression.
Reference(s):
1. De Luca A et al. (1993). Difenoxin and loperamide: studies on possible mechanisms of intestinal antisecretory action. Naunyn Schmiedebergs Arch Pharmacol.
2. Innocenti P et al. (1983). Clinical effectiveness of difenoxine in patients with acute and chronic diarrhea. Boll Chim Farm.
