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Diphenoxylate is a centrally active opioid drug of the phenylpiperidine series primarily used as an antidiarrheal agent. It functions by acting as an opioid agonist, predominantly on mu receptors within the enteric nervous system, which slows intestinal contractions and prolongs gastrointestinal transit time. This action also reduces epithelial secretion of fluid and electrolytes and enhances active absorption. While chemically related to narcotic analgesics, diphenoxylate exhibits minimal to no analgesic activity at standard therapeutic doses. It is rapidly metabolized in the body to difenoxin, an active metabolite. Diphenoxylate is frequently formulated in combination with atropine to deter abuse due to its opioid properties.
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