1. Clinical Overview
Rebamipide is a gastroprotective agent with a unique mechanism of action, distinct from proton pump inhibitors (PPIs) and H2-receptor antagonists. It is a quinolinone derivative that promotes gastric mucosal defense and healing by increasing prostaglandin synthesis, scavenging free radicals, and stimulating mucus secretion. It is a cornerstone in the management of gastritis and gastric ulcers in the Indian context, where dietary and lifestyle factors are prevalent.
| Onset | Duration | Bioavailability |
|---|---|---|
| Symptomatic relief may begin within 1-2 weeks of therapy, but full mucosal healing effects are typically observed after 4-8 weeks of continuous use. | The therapeutic effect is dependent on continued administration; it does not have a prolonged anti-secretory effect like PPIs. | Approximately 70-80% following oral administration in fasting state. |
2. Mechanism of Action
Rebamipide enhances the natural defense mechanisms of the gastric mucosa. It does not inhibit gastric acid secretion. Its primary actions include: 1) Induction of endogenous prostaglandins (PGE2 and PGI2) synthesis in the gastric mucosa, which promotes mucus and bicarbonate secretion and mucosal blood flow. 2) Scavenging of hydroxyl radicals, providing antioxidant protection against reactive oxygen species (ROS) generated during inflammation or by NSAIDs. 3) Upregulation of growth factors like EGF and TGF-α, promoting epithelial cell proliferation and repair. 4) Inhibition of neutrophil activation and adhesion, reducing inflammatory cytokine release (e.g., IL-8).
3. Indications & Uses
- Gastric ulcer
- Acute gastritis
- Chronic gastritis
- Exacerbation of gastric mucosal lesions (erosions, bleeding, redness, edema)
4. Dosage & Administration
Adult Dosage: 100 mg orally three times daily (after meals).
Administration: Administer after meals to improve tolerability and potentially enhance mucosal contact. Tablet should be swallowed whole with a glass of water. Do not crush or chew.
5. Side Effects
Common side effects may include:
- Diarrhea
- Constipation
- Nausea
- Abdominal discomfort/pain
- Flatulence
- Rash
- Pruritus
6. Drug Interactions
| Drug | Effect | Severity |
|---|---|---|
| Warfarin | Theoretical risk of increased anticoagulant effect due to protein binding displacement. Monitor INR closely. | Moderate |
| NSAIDs (e.g., Diclofenac, Ibuprofen) | Rebamipide is used to protect against NSAID-induced gastropathy. No significant PK interaction. | Minor |
| Proton Pump Inhibitors (e.g., Omeprazole, Pantoprazole) | Additive or synergistic mucosal healing effect. No significant PK interaction. | Minor |
| Antacids/Aluminum hydroxide | May decrease the absorption of rebamipide. Administer rebamipide at least 2 hours before or after antacids. | Moderate |
| Sucralfate | May interfere with absorption of rebamipide. Administer rebamipide at least 2 hours before sucralfate. | Moderate |
7. Patient Counselling
- DO take the medicine exactly as prescribed, three times a day after meals.
- DO complete the full course of treatment (usually 4-8 weeks) even if you feel better.
- DO inform your doctor about all other medicines you are taking, including over-the-counter drugs and supplements.
- DONT take antacids or sucralfate within 2 hours of taking Rebamipide.
- DONT crush, break, or chew the tablet.
8. Toxicology & Storage
Overdose: No specific reports of acute overdose in humans. Based on pharmacology, symptoms may include exacerbation of known side effects: severe diarrhea, nausea, abdominal pain, and possibly dizziness.
Storage: Store below 30°C. Protect from light and moisture. Keep out of reach of children. Do not use after the expiry date printed on the pack.