Diphenoxylate - Related Drugs

Related Drugs

Diphenoxylate is metabolised in the body to yield difenoxin. Difenoxin is another centrally acting antidiarrhoeal that is 250 to 400 per cent the strength of diphenoxylate via the oral route and is also able to be manufactured and is distributed as Motofen, (1 mg difenoxin/25 µg atropine), which was introduced in the United States in the late 1990s after being discovered in 1970 at Janssen.

The Diphenoxylate-Loperamide subfamily of gastrointestinal drugs works directly on opioid receptors, which can be found in the intestine, brain, and spinal cord. Diphenoxylate itself crosses the blood–brain barrier. This being the case, this medication is potentially habit-forming and can generate significant tolerance if taken continuously for a protracted period. Physical dependence is most common particularly with high doses and/or long-term use. The CNS penetration of diphenoxylate makes it an agent that can cause euphoria and other psychoactive effects, which could over time lead to habituation and dependency on the drug in the user. As with other medicinal opioids, iatrogenic addiction is uncommon although physical dependence secondary to treatment of a functional bowel disorder with diphenoxylate for more than 45–90 days may very well occur; it typically requires the use of high doses to impart a morbid seek orientation for the drug in the user. Because of this, diphenoxylate is manufactured and marketed as a combination drug with atropine (Lomotil, Pfizer) as an abuse deterrent. Lomotil was used during the Apollo program, as was pethidine.

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