Difenoxilato

Difenoxilato is a pharmaceutical drug classified as an antidiarrheal agent. It functions by slowing down intestinal motility, thereby reducing the frequency of bowel movements and the liquidity of stool. Difenoxilato is structurally related to the opioid analgesic meperidine, and it exerts its effects through opioid receptors in the myenteric plexus of the intestine.

It is typically formulated in combination with atropine sulfate, a combination product often marketed under brand names such as Lomotil. The inclusion of atropine serves a dual purpose: it acts as a mild anticholinergic and is intended to discourage intentional abuse of the difenoxilato component. When taken in excessive doses, difenoxilato can produce opioid-like central nervous system effects, and the atropine component can cause unpleasant anticholinergic side effects, such as blurred vision, dry mouth, and urinary retention, which may deter overdose.

Difenoxilato is prescribed for the symptomatic treatment of diarrhea. It is not intended to treat the underlying cause of diarrhea, but rather to alleviate the distressing symptoms. Its use is generally reserved for cases where diarrhea is not severe enough to warrant hospitalization and when other treatments have not been effective.

The drug is administered orally and is absorbed from the gastrointestinal tract. It is metabolized in the liver and excreted in the urine and feces. Due to its opioid-like properties, difenoxilato is a controlled substance in many countries, including the United States, where it is classified as a Schedule V controlled substance. This means it has a relatively low potential for abuse compared to other schedules, but still requires careful regulation and prescription. Potential side effects include constipation, dizziness, drowsiness, and abdominal cramping. In rare cases, more serious adverse effects may occur.