Description

Cinitapride is a substituted benzamide drug that acts as a gastroprokinetic agent. It is a dual-action compound that works by stimulating gastrointestinal motility and is used to treat disorders related to slow gastric emptying. Cinitapride is not available in all countries, with its use being more common in Europe and Latin America.

Indications

Cinitapride is primarily indicated for the treatment of gastrointestinal motility disorders. Its main uses include:

• Symptomatic treatment of dyspepsia: It is used to relieve symptoms like discomfort, fullness, and bloating in functional dyspepsia (non-ulcer dyspepsia), which is not caused by an ulcer or other obvious disease.

• Delayed gastric emptying: It is used to improve gastric emptying and reduce symptoms associated with slow stomach emptying.

• Gastroesophageal Reflux Disease (GERD): It can be used as an adjunct treatment for GERD by improving esophageal clearance and gastric emptying, thereby reducing reflux episodes.

Mechanism of Action

Cinitapride’s mechanism of action is based on its dual agonist and antagonist effects on two key neurotransmitter receptors in the gastrointestinal tract: serotonin and dopamine. This dual action makes it a highly effective prokinetic agent.

1. Serotonin 5-HT4​ Receptor Agonism:
   • Cinitapride is a partial agonist of the serotonin 5-HT4​ receptors, which are located on the smooth muscle cells and enteric neurons of the GI tract.
   • When cinitapride binds to and activates these receptors, it stimulates the release of acetylcholine (ACh).

1. • Acetylcholine is a major neurotransmitter in the enteric nervous system that promotes muscle contraction. The increased release of ACh enhances the peristaltic contractions of the stomach and intestines, leading to improved gastric emptying and faster transit of food through the GI tract.
2. Dopamine D2 Receptor Antagonism:
   • Cinitapride also acts as an antagonist of the dopamine D2 receptors.

• • Dopamine typically has an inhibitory effect on gastrointestinal motility. By blocking these D2 receptors, cinitapride removes this inhibitory influence.
  • This action further enhances the prokinetic effect by allowing acetylcholine to exert its full contractile effect on the smooth muscles of the GI tract.

In summary, the combined effect of stimulating pro-motility receptors (5-HT4​) and blocking inhibitory receptors (D2) results in a potent and coordinated increase in GI motility, which helps to alleviate symptoms of dyspepsia and other motility disorders.