ATC Group: A07DA Antipropulsives

Diphenoxylate is a synthetic opioid derivative with selective effects on gastrointestinal smooth muscle. It is essentially devoid of “morphine type subjective effects” at therapeutic doses.

Eluxadoline is a locally acting, mixed mu opioid receptor (μOR) agonist and delta opioid receptor (δOR) antagonist. Eluxadoline is also an agonist at the kappa opioid receptor (κOR). Eluxadoline has demonstrated efficacy in normalizing GI transit and defecation in several models of stress induced or post GI inflammation-altered GI function in animals.

By binding to opiate receptors in the gut wall, loperamide hydrochloride reduces propulsive peristalsis, increases intestinal transit time and enhances resorption of water and electrolytes. Loperamide increases the tone of the anal sphincter, which helps reduce faecal incontinence and urgency.

Opium alkaloids (opioids and isoquinoline derivatives) induce constipation, euphoria, analgesia and sedation dependent on the dose and derivative. The constipating effect is caused by inhibition of the intestines' peristalsis.