difenoxin

Ligand id: 7592

Name: difenoxin

Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 4
Hydrogen bond donors 1
Rotatable bonds 7
Topological polar surface area 64.33
Molecular weight 424.22
XLogP 9.4
No. Lipinski's rules broken 1

Molecular properties generated using the CDK

No information available.
Summary of Clinical Use
Approved for the treatment of acute and chronic diarrhea. The 1978 FDA approval was for a a brand mixture containing difenoxin hydrochloride and atropine sulphate (Motofen). The atropine is added to decrease deliberate opioid misuse.
Mechanism Of Action and Pharmacodynamic Effects
Although difenoxin is capable of crossing the blood brain barrier and produces weak sedative and analgesic effects, its most significant and clinically useful effects are via activation of peripheral opioid receptors in the intestine. Activation of intestinal opioid receptors inhibits peristalsis, therby increasing intestinal transit time.