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Rebamipide – Uses, Mechanism & Dosage

Rebamipide is a gastroprotective drug used to protect and heal the gastric mucosa in conditions such as peptic ulcers and gastritis. It stimulates mucus production and promotes mucosal regeneration.

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Things worth knowing about "Rebamipide"

Rebamipide is a gastroprotective drug used to protect and heal the gastric mucosa in conditions such as peptic ulcers and gastritis. It stimulates mucus production and promotes mucosal regeneration.

What is Rebamipide?

Rebamipide is a gastroprotective agent – a compound that protects and supports the regeneration of the gastric mucosal lining. It belongs to the class of mucosal protective substances and has been used clinically for decades, primarily in Asian countries such as Japan, South Korea, and China. Scientific interest in rebamipide is also growing in Western countries.

Indications

Rebamipide is used in the treatment of:

Peptic ulcers (gastric and duodenal ulcers)
Gastritis, including Helicobacter pylori-associated gastritis
NSAID-induced gastropathy – mucosal damage caused by non-steroidal anti-inflammatory drugs (e.g., ibuprofen, diclofenac)
Oral mucositis related to chemotherapy
As adjunctive therapy during Helicobacter pylori eradication treatment

Mechanism of Action

Rebamipide exerts its protective effects through several complementary mechanisms:

Stimulation of prostaglandin synthesis: Rebamipide increases the production of prostaglandins E2 and I2 in the gastric mucosa, which promote mucus secretion and mucosal blood flow.
Enhancement of mucus production: The compound stimulates goblet cells to produce greater quantities of mucins, the primary components of the protective gastric mucus layer.
Antioxidant activity: Rebamipide scavenges free radicals and reduces oxidative stress within mucosal cells.
Inhibition of pro-inflammatory cytokines: It reduces the release of inflammatory mediators such as interleukin-8 (IL-8) and TNF-alpha, thereby attenuating the inflammatory effects of Helicobacter pylori.
Promotion of mucosal cell regeneration: Rebamipide supports the proliferation and migration of epithelial cells, accelerating the healing of mucosal lesions.

Dosage and Administration

The standard dosage for peptic ulcers and gastritis is 100 mg three times daily (morning, noon, and evening), typically administered as an oral tablet. The duration of treatment depends on the clinical indication and individual response, commonly ranging from 4 to 8 weeks. In cases of NSAID-induced gastropathy, rebamipide is administered concurrently with NSAID therapy as a protective measure.

Side Effects

Rebamipide is generally well tolerated. Possible side effects include:

Abdominal pain or gastrointestinal discomfort
Constipation or diarrhea
Nausea
Elevated liver enzymes (rare)
Skin reactions such as pruritus or rash (rare)

Serious adverse events are uncommon. The drug is contraindicated in patients with known hypersensitivity to rebamipide.

Special Considerations

The safety of rebamipide during pregnancy and breastfeeding has not been fully established. Use in these situations should only be considered after careful assessment of the benefit-risk ratio by the treating physician. Rebamipide is not officially approved in many European countries but may be used on an individual case basis.

References

Haruma K. et al. – Rebamipide, a mucosal protective drug, in combination with Helicobacter pylori eradication therapy. Journal of Gastroenterology, 2014.
Tarnawski A.S., Ahluwalia A. – Molecular mechanisms of epithelial regeneration and neovascularization during healing of gastric ulcers. Current Medicinal Chemistry, 2012.
Yoshikawa T. et al. – Rebamipide: overview of its mechanisms of action and efficacy in mucosal protection and ulcer healing. Digestive Diseases and Sciences, 1998.

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