Domperidone NEW

Domperidone Cas 57808-66-9

Specification

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Domperidone is a medication that belongs to a class of drugs known as dopamine antagonists. Its primary action is to block dopamine receptors in the brain and, more importantly, in the digestive tract. This action leads to two main effects: it acts as an anti-emetic (preventing nausea and vomiting) and it stimulates stomach emptying and intestinal movement (a prokinetic effect).

How Does It Work?

Dopamine is a neurotransmitter that, among its many roles, can suppress stomach contractions and slow the movement of food from the stomach into the intestines (a process called gastric emptying). By blocking dopamine receptors:

1. In the Gut: It releases this "brake," allowing the natural muscles of the stomach and upper intestine to contract more forcefully. This accelerates gastric emptying and reduces backward flow of stomach contents.

2. In the Chemoreceptor Trigger Zone (CTZ): The CTZ is an area of the brain that detects toxins in the blood and induces vomiting. Blocking dopamine receptors here helps to prevent nausea and vomiting signals from being sent.

A key feature of domperidone is that it does not readily cross the blood-brain barrier. This means it has fewer neurological side effects (like drowsiness or involuntary movements) compared to older, similar medications like metoclopramide.

What Is It Used For?

• Primary Medical Use: Treatment of nausea and vomiting.

  Gastrointestinal Motility Disorders: It is used to relieve symptoms like fullness, bloating, and discomfort in conditions where delayed gastric emptying is a problem (e.g., gastroparesis, functional dyspepsia).

  Off-Label Use for Lactation: Domperidone is commonly used off-label to stimulate breast milk production. This is because the blockade of dopamine receptors in the brain can lead to an increase in prolactin, the hormone responsible for lactation. This use is often a primary reason for patient inquiries, though it is not the officially approved indication in many countries.

Important Side Effects and Warnings

The most significant risk associated with domperidone is its potential effect on the heart. It can prolong the QT interval on an electrocardiogram (ECG), which can lead to serious, potentially fatal, abnormal heart rhythms (arrhythmias), such as Torsades de Pointes.

Serious Side Effects:

• Cardiac Arrhythmias: Irregular heartbeats, palpitations, dizziness, fainting.

  Sudden Cardiac Death: Risk is increased with higher doses, prolonged use, or in patients with pre-existing heart conditions.

Common Side Effects:

• Dry mouth

  Headache

  Abdominal cramps

  Diarrhea

  Due to its effect on prolactin, it can sometimes cause breast tenderness, swelling, or galactorrhea (milk secretion) in men and non-lactating women.

Regulatory Status and Controversy

Due to the cardiac risks, the regulatory status of domperidone is strict and varies globally:

• In the European Union and Canada: It remains available but with significant restrictions. Its use is typically recommended at the lowest effective dose for the shortest possible duration (usually less than one week) and is contraindicated in patients with known heart conditions or those taking other QT-prolonging drugs.

  In the United States: The FDA has not approved domperidone for any therapeutic use. It is banned from being marketed as a drug. However, the FDA has a policy that allows for limited personal importation and compounding for specific clinical needs (e.g., GI motility disorders under strict supervision), though it is not readily available in pharmacies.

Disclaimer: This information is for educational purposes only. Domperidone is a drug with serious risks and must only be used under the direct supervision and prescription of a qualified healthcare professional who can evaluate your individual health status.

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