Loperamide

Loperamide (Imodium, Janssen-Cilag; Gastro-Stop, Rhone-Poulenc Rorer) is the author's preferred drug for the symptomatic treatment of diarrhea. It binds to peripheral opioid receptors in the gastrointestinal tract and inhibits release of secretory neurotransmitters such as acetylcholine. It also has calmodulin-binding and calcium-channel-blocking effects which may have additional antisecretory and motility-altering actions. In therapeutic doses loperamide has no central effects and approximately 80 per cent remains in the gut wall where it is taken up by the myenteric plexus and longitudinal muscle. Some is also found in the mucosa, probably bound to p- and d-opioid receptors (AW0U\§IS...eLaí 1993).

The effects of loperamide on the gastrointestinal tract are summarized in Ta.b!e.J... Its effect on the mucosal transport of water and electrolytes in the non-stimulated state is minimal, but when secretion is stimulated its action on the p- and d-opioid receptors decreases secretion of sodium, potassium, and chloride, with this effect being maximal in the jejunum and less marked in the colon. Slowing of intestinal transit increases mucosal contact time and promotes reabsorption of water.

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