Description

Itopride HCl is a prokinetic agent and a substituted benzamide derivative. It is not available in all countries (for example, it is not available in the U.S. or U.K.) but is used in many parts of the world. It is known for its dual action, which improves gastrointestinal motility without the significant central nervous system side effects of some other prokinetics, such as metoclopramide.

Indications

Itopride HCl is primarily indicated for the treatment of gastrointestinal symptoms caused by reduced gastrointestinal motility and delayed gastric emptying. Its main uses include:

• Functional Dyspepsia: It is used to relieve symptoms of non-ulcer dyspepsia, often called chronic gastritis. This includes symptoms such as a sensation of bloating, early satiety (feeling full after eating very little), post-meal fullness, upper abdominal discomfort or pain, nausea, and vomiting.

• Gastroesophageal Reflux Disease (GERD): It can be used to treat symptoms of GERD, such as heartburn, by improving the function of the lower esophageal sphincter and accelerating gastric emptying.

• Other motility disorders: It can be used to treat other conditions where delayed gastric emptying is a problem, such as gastroparesis.

Mechanism of Action

Itopride has a unique dual mechanism of action that enhances gastrointestinal motility:

1. Dopamine D2 Receptor Antagonism: Dopamine, a neurotransmitter, has an inhibitory effect on gastrointestinal motility when it binds to D2 receptors in the gut. By blocking these D2 receptors, itopride prevents dopamine from exerting its inhibitory effects. This removal of the “brake” on gastrointestinal muscle contractions allows for increased and more coordinated movement of food through the digestive tract.
2. Acetylcholinesterase Inhibition: Acetylcholine is a neurotransmitter that promotes muscle contraction in the gastrointestinal tract. The enzyme acetylcholinesterase is responsible for breaking down and inactivating acetylcholine. Itopride inhibits this enzyme, which leads to an increase in the concentration of acetylcholine in the synaptic clefts of the gut. Elevated levels of acetylcholine then stimulate muscarinic receptors on smooth muscle cells, leading to stronger and more frequent contractions and enhancing peristalsis.

The combination of these two actions—D2 receptor antagonism and acetylcholinesterase inhibition—results in a significant increase in acetylcholine and an overall enhancement of gastrointestinal motility, leading to accelerated gastric emptying and symptom relief. Because itopride does not readily cross the blood-brain barrier, it has a lower risk of causing central nervous system side effects, such as extrapyramidal symptoms, compared to drugs like metoclopramide.