![]() ![]() Atropine is added in a fixed dose of 0.025 mg it is a competitive inhibitor of acetylcholine receptors to prevent patients from misusing diphenoxylate. Atropine produces anticholinergic side effects like nausea/bloating/tachycardia/dryness of mouth/eyes when ingested at higher doses. It does not have analgesic effects of morphine at standard doses, but it can lead to CNS effects, like euphoria, at higher doses. The drug can have misuse potential if used for a prolonged time and classified as a Schedule II drug under the Food and Drug Administration when used alone. Diphenoxylate reduces the epithelial secretion of fluid and electrolytes and enhances active absorption by mild action on delta receptors. This action leads to a decrease in segmental contractions and prolongation of gastrointestinal transit time. By acting on the presynaptic opioid receptors, it blocks the release of acetylcholine in the synaptic cleft and hence inhibits the motility and secretory action of the enteric nervous system. The submucosal plexus controls the secretions of fluid and electrolytes in the lumen of the intestine. The myenteric plexus lies between the circular and longitudinal smooth muscles of the bowel wall and controls segmental contractions, i.e., peristaltic movements of the gut. Diphenoxylate is an opioid agonist that acts on the presynaptic opioid receptors (predominantly mu receptors) in the enteric nervous system. The enteric nervous system is comprised of two components: the myenteric plexus and submucosal plexus.
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