Rebamipide for Gastritis and Ulcers
Rebamipide 100 mg three times daily is the recommended dosage for treating gastric ulcers and chronic gastritis, typically continued for 4-8 weeks until mucosal healing is achieved. 1, 2
Standard Dosing and Administration
- Administer rebamipide 100 mg orally three times daily for gastric ulcers, chronic gastritis with hyperacidity in the acute stage, and erosive gastritis 1
- Peak gastric mucosal concentrations occur 30-60 minutes after oral administration and remain elevated for approximately 120 minutes, with therapeutic levels maintained for about 5 hours 3
- Continue treatment for 4-8 weeks to achieve complete mucosal healing and improve the quality of ulcer healing 4
Specific Clinical Indications
- Use rebamipide for prevention of NSAID-induced gastrointestinal mucosal damage in patients requiring chronic NSAID therapy who cannot discontinue these medications 1, 2
- Consider rebamipide as adjunctive therapy during H. pylori eradication to reduce inflammatory changes and potentially enhance eradication rates 1, 4
- Rebamipide is particularly valuable in Asian populations where glandular atrophy and low acid output are more prevalent, as it improves mucosal protection independent of acid suppression 2
Mechanisms Supporting Clinical Use
- Rebamipide increases gastric blood flow, stimulates prostaglandin biosynthesis, and scavenges oxygen free radicals, providing multiple protective mechanisms beyond simple acid suppression 2, 4
- The drug improves both the speed and quality of ulcer healing by increasing gastric mucus glycoprotein components, stimulating epithelial cell migration and proliferation, and increasing epidermal growth factor expression 4
- Rebamipide is the only mucosal-protective drug proven to improve histological gastritis in vivo, reducing inflammatory markers like iNOS expression in gastric mucosa 2
Special Populations and Contraindications
Active Gastrointestinal Bleeding
- In patients with active bleeding peptic ulcers, initiate high-dose PPI therapy first: 80 mg bolus followed by 8 mg/hour continuous infusion for 72 hours after endoscopic hemostasis 5, 6
- Rebamipide can be added after bleeding is controlled to enhance mucosal healing quality and reduce recurrence risk 4
- Never delay urgent endoscopy for medication administration in patients with hematemesis, melena, or hemodynamic instability 6, 7
Liver Disease
- No specific dose adjustments are documented for hepatic impairment, as rebamipide achieves therapeutic concentrations primarily through local gastric mucosal penetration rather than systemic distribution 3
- Serum concentrations remain low (0.25 ± 0.23 μg/ml) even at therapeutic doses, suggesting minimal hepatic metabolism concerns 3
Kidney Disease
- Limited data exist on dosing in renal impairment, but the predominantly local mechanism of action suggests standard dosing may be appropriate 3
- Monitor for accumulation if severe renal dysfunction is present, though systemic absorption is minimal 3
Integration with Standard Ulcer Therapy
- Combine rebamipide with PPI therapy rather than using it as monotherapy for optimal outcomes in peptic ulcer disease 6, 7
- Standard PPI dosing remains: omeprazole 20 mg, lansoprazole 30 mg, or pantoprazole 40 mg once daily for 6-8 weeks 6
- Always test for H. pylori and eradicate if present, as failure to do so leads to 40-50% recurrence rates over 10 years regardless of other therapies 6, 7
NSAID-Related Ulcers: Critical Algorithm
- First priority: Discontinue NSAID therapy if clinically feasible, as this heals 95% of ulcers and reduces recurrence from 40% to 9% 5, 6
- If NSAIDs cannot be stopped: Switch to selective COX-2 inhibitor (celecoxib) PLUS maintain long-term PPI therapy PLUS add rebamipide 100 mg three times daily 5, 1, 2
- Rebamipide provides additional protection against NSAID-induced injury through mechanisms independent of COX inhibition, including free radical scavenging and enhanced mucosal blood flow 2, 4
Common Pitfalls to Avoid
- Do not use rebamipide as a substitute for H. pylori eradication therapy—always test and treat H. pylori infection, as this is the single most important intervention to prevent recurrence 6, 7
- Do not rely on rebamipide alone for active bleeding ulcers—these patients require urgent endoscopy and high-dose PPI therapy as first-line management 5, 6
- Do not assume mucosal protection equals acid suppression—rebamipide works through distinct mechanisms and should complement, not replace, PPI therapy in most cases 2, 4
- Rebamipide's benefits are most evident in improving healing quality and preventing recurrence, not just speed of initial healing 4
Emerging Evidence and Future Directions
- Rebamipide may reduce gastric cancer risk by improving histological gastritis and reducing inflammatory markers, though long-term studies are needed 2
- The drug shows promise in reducing inflammatory changes in the oral mucosa after chemoradiotherapy in oncology patients 1
- Current trials are investigating efficacy in inflammatory conditions including rheumatoid arthritis, Sjögren's syndrome, and ulcerative colitis 1, 8