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2024-09-03
Domperidone is a benzimidazole derivative that acts as a peripheral dopamine receptor antagonist. It is commonly used as an antiemetic and prokinetic agent to treat various gastrointestinal disorders.
**Pharmacodynamics:**
Domperidone primarily works by blocking dopamine D2 receptors located in the gastrointestinal tract. This action enhances gastrointestinal motility by increasing the tone and amplitude of contractions in the stomach and small intestine. It promotes gastric emptying and coordinates the movement of the stomach and intestines, preventing food reflux and aiding in the relief of symptoms such as nausea and vomiting.
Key points of its pharmacodynamics include:
1. **Anti-emetic Effect:** By blocking dopamine receptors in the chemoreceptor trigger zone (CTZ) of the brain, domperidone helps prevent nausea and vomiting.
2. **Prokinetic Activity:** It enhances gastrointestinal motility, which is beneficial in conditions like delayed gastric emptying and gastroesophageal reflux disease (GERD).
3. **No Central Nervous System Effects:** Due to its poor penetration into the blood-brain barrier, domperidone does not significantly affect the central nervous system, making it less likely to cause side effects such as drowsiness or extrapyramidal symptoms.
4. **Increased Serum Prolactin Levels:** Domperidone can increase serum prolactin levels, which may promote lactation in postpartum women but is not effective in patients with prolactin-secreting tumors.
**Pharmacokinetics:**
- **Absorption:** Domperidone is rapidly absorbed after oral administration, with peak plasma concentrations occurring within 15-30 minutes.
- **Distribution:** It has a low volume of distribution and does not significantly penetrate the brain.
- **Metabolism:** Domperidone is metabolized in the liver, mainly by the cytochrome P450 enzyme system.
- **Elimination:** It has a half-life of approximately 7 hours and is excreted primarily in the feces.
**Indications:**
- **Gastrointestinal Disorders:** Used to treat symptoms of gastrointestinal motility disorders, including delayed gastric emptying, gastroesophageal reflux disease, and functional dyspepsia.
- **Nausea and Vomiting:** Effective in preventing nausea and vomiting associated with various causes, including chemotherapy, radiation therapy, and the use of dopamine receptor agonists.
**Adverse Effects:**
Common adverse effects include transient abdominal cramps and occasional increases in serum prolactin levels, which may lead to side effects such as galactorrhea and menstrual irregularities. Rarely, it may cause allergic reactions or extrapyramidal symptoms, especially in high doses or in susceptible individuals.
**Contraindications:**
- Hypersensitivity to domperidone.
- Patients with conditions such as pheochromocytoma, breast cancer, mechanical bowel obstruction, or gastrointestinal bleeding.
- caution in patients with heart disease (especially arrhythmias) and those undergoing chemotherapy.
**Drug Interactions:**
- Avoid concurrent use with antifungal agents like ketoconazole and itraconazole, macrolide antibiotics like erythromycin, HIV protease inhibitors, and nefazodone.
- Anticholinergic drugs may decrease the effectiveness of domperidone.
- Antacids and drugs that reduce stomach acid secretion can lower domperidone's bioavailability.
**Conclusion:**
Domperidone is an effective medication for managing gastrointestinal motility disorders and nausea/vomiting, with a relatively favorable safety profile due to its peripheral selectivity and low central nervous system penetration. However, it should be used with caution in certain patient populations and in combination with other medications.
Add:Room 310-312, Building 11, Maiduo Plaza, 1500 Lianhua South Road
Tel:(0086)021-51083888
Email:dingkangpharma@dingkang.com.cn