Zacopride

Zacopride is a benzamide derivative that functions primarily as a 5-HT3 receptor antagonist and, to a lesser extent, as a 5-HT4 receptor agonist. It has been investigated for various therapeutic applications, including the treatment of irritable bowel syndrome (IBS), chemotherapy-induced nausea and vomiting (CINV), and cognitive impairment.

As a 5-HT3 antagonist, zacopride blocks the action of serotonin at the 5-HT3 receptor, which is involved in the emetic reflex and gastrointestinal motility. This action can alleviate nausea and vomiting, and regulate bowel function.

As a 5-HT4 agonist, zacopride stimulates the 5-HT4 receptor, which promotes the release of acetylcholine in the gastrointestinal tract, thereby increasing gut motility. This effect can potentially benefit patients with constipation-predominant IBS.

While showing promise in clinical trials, zacopride has not been widely adopted as a first-line treatment due to concerns regarding potential cardiovascular side effects and the availability of alternative medications with similar efficacy and a better safety profile. Research into its potential applications continues, particularly in areas where its dual mechanism of action may offer a therapeutic advantage. The drug is not currently approved for use in all countries.