Rebamipide

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Rebamipide

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Medically reviewed

Laura Arias

Last updated on 22/12/2025

This page provides general, reference-level information compiled from official medical sources. It is not a substitute for professional medical advice, diagnosis, or treatment. For decisions about your health, please consult a qualified healthcare professional.

Overview of Rebamipide

Property Description
Active ingredient Rebamipide (INN)
Form Oral Tablet, Ophthalmic Drops
Pharmacological class Mucosal Protective Agent
General purpose Enhancing defense and promoting repair of mucosal linings
Origin Synthetic Quinolone Derivative

What is Rebamipide and What Type of Medicine is it?

Rebamipide is the designated International Nonproprietary Name (INN) for a synthetic pharmaceutical compound that functions as a Gastrointestinal Agent. It is specifically categorized as a Mucosal Protective Agent. Chemically defined as a quinolinone derivative, its structure differentiates it from medications that primarily target acid suppression. The compound is widely utilized across Asia, and it carries the Anatomical Therapeutic Chemical (ATC) code A02BX14, which groups it with other non-acid-reducing drugs used for peptic conditions.

Composition and Available Forms of Rebamipide

The compound’s precise composition is represented by the molecular formula C19H15ClN2O4. Rebamipide is generally available as a single active ingredient product. It is manufactured in two primary dosage forms: the standard oral tablet, intended for the oral route of administration, and a specialized ophthalmic form (eye drops) for topical administration to the eyes. The availability of an ophthalmic solution highlights a key differentiating feature, underscoring the compound’s clinically recognized epithelial protective action beyond the stomach lining.

General Purpose and Action of this Mucosal Agent

The general purpose of this medicine is to promote the integrity and defensive function of the body's mucosal linings. Rebamipide achieves this primarily by acting as a Prostaglandin E2 Stimulant, which aids the body's natural healing and protective processes. This mechanism supports the body's mucosal defense by enhancing mucus production and improving blood flow to the digestive lining. Furthermore, Rebamipide exhibits established free radical scavenging (antioxidant) activity. This comprehensive, multifaceted approach is clinically recognized for supporting a robust mucosal defense system against various stressors.

Regulatory References

  1. NIH PubMed Study

What side effects are possible with Rebamipide?

Possible Side Effects and Safety Information

The safety profile of Rebamipide is defined by adverse reactions and limitations documented in official government regulatory information, categorized by frequency and the body system affected.

Adverse Reactions by Frequency and System-Organ Class

Adverse reactions are classified by incidence rates (e.g., less than 0.1%) or as having an Incidence Unknown (typically from post-marketing reports).

  • Gastrointestinal Disorders (Incidence < 0.1%): Constipation, diarrhea, nausea, vomiting, abdominal pain, and taste abnormality are documented.
  • Hepatobiliary Disorders (Incidence < 0.1%): Hepatic dysfunction, indicated by an increase in liver enzymes (AST, ALT, alkaline phosphatase), is listed.
  • Blood and Lymphatic System Disorders (Incidence < 0.1%): Leukopenia (decrease in white blood cells) has been observed.
  • Hypersensitivity/Skin (Incidence < 0.1%): Reactions such as rash and pruritus (itching) are documented.

Clinically Significant Adverse Reactions

The official labeling notes that certain severe reactions are clinically significant and require close monitoring:

  • Shock and Anaphylactoid Reactions
  • Severe Hepatic Dysfunction and Jaundice
  • Thrombocytopenia and Leukopenia

Safety Considerations for Specific Populations

Official documents define specific cautions for certain groups:

  • Elderly Patients: Close monitoring is advised, as this population may be more sensitive, particularly concerning gastrointestinal effects.
  • Pregnancy and Lactation: The safety of use during human pregnancy has not been established. For nursing mothers, nursing should be interrupted, as the compound has been shown to be distributed into breast milk.
  • Pediatric Patients: Safety in children has not been established; the medication is not to be used in this population.

Safety Restrictions and Limitations

Rebamipide is contraindicated in individuals with a history of hypersensitivity to the drug. Furthermore, regulatory labeling mandates immediate discontinuation of the medicine if signs of hypersensitivity or clinically significant adverse reactions, such as markedly increased liver enzyme levels, occur.

Overdose and Emergency Response

The official regulatory documentation for Rebamipide defines its overdose profile by the required emergency response rather than a comprehensive list of clinical manifestations. Due to the limited clinical experience with massive acute over-ingestion, official prescribing information does not define a specific, expected symptom profile in overdose scenarios. Likewise, regulatory summaries do not list explicit severe or life-threatening organ-systemic outcomes, as specific data in this context is constrained.

Overdose Management Requirement Regulatory Statement
Symptom Profile No specific expected symptom profile is documented due to limited data on massive acute overdose.
Specific Antidote No specific antidote is known for Rebamipide overdose.

In the event of any suspected over-ingestion, the regulator-mandated action is to seek immediate medical attention or contact emergency services immediately. This instruction must be followed immediately to initiate professional medical management, as there is no specific reversal agent available. Consequently, the management of overdose consists exclusively of providing symptomatic and supportive treatment. This supportive care, which includes observation and clinical monitoring as deemed necessary by medical staff, is the defined standard regulatory procedure. Official labels do not provide explicit details regarding population-specific overdose severity or risk factors.

Therapeutic Uses of Rebamipide

What Rebamipide Treats: Main Uses and Benefits

Rebamipide is generally used to provide supportive relief for the gastrointestinal tract, especially in situations involving certain distressing symptoms. Its therapeutic profile focuses on easing symptomatic discomfort and promoting internal stability.

It is commonly used across conditions presenting with acute episodes, such as gastric ulcers, acute or chronic gastritis, and issues involving the inner lining of the stomach. This medication is considered relevant in contexts marked by increased discomfort or tension, helping with symptom clusters that interfere with daily comfort. It is often used when symptoms intensify and supportive relief is needed, as it offers symptomatic relief that helps ease the overall symptom burden.

Quick Fact: Support for Symptoms Related to Irritative States

Rebamipide is generally applied across domains where additional symptomatic support is needed to help with symptoms related to inflammatory or irritative states.

Regulatory References

  1. Philippine Food and Drug Administration's product information

Eligibility and Restrictions for Use

This section summarizes the official eligibility and non-eligibility information for Rebamipide, based strictly on government regulatory documents. The use of this medicine is defined by absolute prohibitions and restrictions for certain patient groups.

Contraindications and Exclusions

Population Category Eligibility Status (Regulatory Label)
Hypersensitivity Contraindicated (Must not be used due to a history of allergy to Rebamipide or any component).
Pediatric Patients Not Recommended (Safety and effectiveness have not been established).
Nursing/Breastfeeding Not Recommended (Nursing should be interrupted, as studies show excretion into breast milk).

Populations Requiring Special Caution

Official labeling mandates that Rebamipide be used with special care in certain populations due to altered physiological response or pharmacokinetics:

  • Pregnant or Possibly Pregnant Women: Use is permitted only if the anticipated therapeutic benefit is judged to outweigh any potential risk, as the safety of the drug in human pregnancy has not been established.
  • Elderly Patients: Requires special care/caution due to potential physiological sensitivity and an increased risk of adverse effects, particularly gastrointestinal disturbances.
  • Hepatic or Renal Impairment: Requires caution due to the risk of altered drug clearance, which may lead to higher plasma concentrations.

What should I know about interactions with other medicines?

Interactions with other medicines and products

Official regulatory documents from regions where Rebamipide is licensed generally indicate that clinically significant drug-drug interactions are not documented. The primary interaction profile is notable for the absence of specific warnings or restrictions regarding co-administration with other medicines.


Summary of Official Interaction Status

Interaction Domain Official Regulatory Statement
Interacting Medicinal Products No specific medicinal products or product classes are explicitly listed as having clinically significant interactions that necessitate dosage adjustments or avoidance.
Interaction Mechanism No specific mechanistic basis (e.g., enzyme inhibition or induction) for clinically relevant interactions with co-administered drugs is stated in official labeling.
Food and Beverages Clinical study data shows that the co-administration of food does not significantly affect the systemic availability (bioavailability) of Rebamipide.

The established regulatory context for this product is characterized by a favorable interaction profile. This means that government regulatory documentation does not outline restrictive procedural constraints, such as required spacing of administration or specialized monitoring, when Rebamipide is used alongside other prescription or over-the-counter medicines. Patients should always inform a healthcare provider of all products being taken, including herbal and dietary supplements, prior to beginning treatment.

Mechanism of Action

How Rebamipide Works

Rebamipide exerts its pharmacologic effect through multiple, interconnected mechanisms targeted at the gastric mucosa. The primary action involves the induction of prostaglandin synthesis and secretion ( PGE2 and PGI2). This intracellular signaling cascade increases the production of protective gastric mucus and bicarbonate, which elevates the physical and chemical resistance of the mucosal barrier.

Simultaneously, the drug functions as a hydroxyl radical scavenger, directly mitigating local oxidative stress in the tissue. This domain of activity includes the modulation of the inflammatory cascade by inhibiting the activation of neutrophils and suppressing the release of pro-inflammatory mediators.

A third key pathway involves the promotion of epithelial integrity. Rebamipide engages mechanisms that enhance cellular proliferation and migration of damaged epithelial cells. This is mediated by increasing the expression of Epidermal Growth Factor (EGF) and its receptor, leading to accelerated epithelial restitution and the maintenance of mucosal function.

Dosage and Administration Information

Rebamipide is administered via two official routes: orally, as a 100 mg film-coated tablet, and topically, as a 2% ophthalmic suspension. The established usage guidelines define distinct protocols and administration conditions for each form.


Oral Administration Protocol

The standard regimen for the 100 mg oral tablet is one tablet taken three times daily (TID). For gastric ulcers, the administration times are in the morning, in the evening, and before going to bed. The tablet may be taken with or without food, as meal consumption does not significantly alter the drug’s bioavailability. If a dose is missed, instructions advise skipping the missed dose and continuing the regular schedule if the next dose time is near, without taking two doses at once.


Ophthalmic Administration Protocol

The 2% ophthalmic suspension is administered as one drop per eye four times daily (QID). Prior to use, the suspension bottle must be shaken well to ensure the proper dispersion of the active ingredient. A key procedural condition requires that if other eye drop products are used, they must be instilled first, followed by a minimum waiting period of more than five minutes before applying the rebamipide suspension. Use in the pediatric population is generally not established, and while careful monitoring is standard, no specific mandatory dose adjustment is defined for older adults in the core regimen.

Recent Clinical Evidence

Research Evidence / Overview of Studies for Rebamipide


Evidence for Use in Healing Gastric Ulcers

Research has explored the use of the medicine in conditions characterized by fluctuating or episodic manifestations, specifically in the context of research involving gastric ulcers. This involved Randomized Controlled Trials (RCTs) and subsequent analyses that summarized the findings from these trials. These studies were evaluated in adults diagnosed with gastric ulcers, including those linked to the continuous use of pain and inflammation medications (NSAIDs). The primary focus was on measuring the endoscopic confirmation of changes in ulcer status, and tracking patient-reported outcomes describing perceived discomfort.

Evidence for Use in Treating Gastritis

Research has explored the use of the medicine in conditions involving periods of heightened symptoms, specifically acute and chronic inflammation of the stomach lining (gastritis). Studies have included Randomized Controlled Trials (RCTs) and observational research examining patterns in daily-life experiences. The populations included adults with endoscopically confirmed or symptomatic gastritis. The outcomes related to outcomes linked to inflammatory or irritative states and patient-reported outcomes describing perceived discomfort.

Evidence for Preventing Mucosal Damage Caused by NSAIDs

The medicine was evaluated in research exploring short-term symptom changes in research scenarios involving NSAID use and mucosal outcomes. This research utilized Randomized Controlled Trials (RCTs) comparing the medicine against placebo or other protective agents. The endpoints were studied for the occurrence rate of gastric ulcers and the presence of mucosal breaks in the small intestine, which are outcomes related to physical discomfort observed in research.


What Research Gaps and Uncertainty Remain

The current body of research provides context but presents several areas of uncertainty. Evidence quality varies across studies, and the majority of high-quality data originates from specific geographical regions (e.g., East Asia), meaning results apply only to the populations studied. Furthermore, the medicine was observed in many trials as an added treatment rather than a standalone option; due to the design, the independent effect of the medicine is sometimes less clearly characterized. Critically, there is limited information for long-term outcomes, and comparative evidence is lacking for certain study types.

Key Studies & References

  1. THE EFFECTIVENESS OF REBAMIPIDE WITH PPI IN POST ENDOSCOPIC SUBMUCOSAL DISSECTION INDUCED ULCER: A META ANALYSIS
  2. Healing Effect of Rebamipide in Addition to Omeprazole for Gastric Ulcer: Preliminary Results of a Randomized

Frequently Asked Questions (FAQ)

Common questions about Rebamipide (FAQ)


Q: What is Rebamipide primarily used for besides stomach ulcers?

According to official product information, Rebamipide is primarily licensed for the improvement of gastric mucosal lesions (such as bleeding, erosion, or redness) often associated with acute or worsening chronic gastritis. Official documentation also lists its use for oral mucositis (inflammation of the mouth lining) in some regions.

Q: What is the main difference between Rebamipide and a proton pump inhibitor (PPI)?

Rebamipide is categorized as a Mucosal Protective Agent, and its mechanism focuses on enhancing the body’s natural defenses, such as increasing protective mucus and repairing the stomach lining. In contrast, Proton Pump Inhibitors (PPIs) are a different class of medicine whose primary action is to reduce the amount of acid the stomach produces. The focus on mucosal protection rather than acid reduction is reflected in its official classification.

Q: Can Rebamipide be taken for a long period of time?

While the duration of use is determined by a healthcare provider, research summaries accessible through authoritative sources note that there is limited information available regarding long-term outcomes (use extending beyond the typical treatment period).

Q: Are there any major diet restrictions while taking Rebamipide?

Regulatory documents indicate that taking Rebamipide with food does not significantly affect how the medicine is absorbed by the body. However, common patient advisories suggest avoiding or limiting alcohol and caffeine, as these substances can stimulate acid production, which may counteract the medicine's protective action.

Q: What are the most commonly reported mild side effects of Rebamipide?

Official safety documents list adverse reactions by their reported frequency, though they do not typically categorize them as strictly 'mild' for the public. The documented side effects with low incidence rates include common gastrointestinal issues such as constipation, diarrhea, nausea, and taste abnormality.

Q: Can Rebamipide cause tiredness or dizziness?

Official safety information indicates that Rebamipide can, in some cases, cause adverse reactions that include dizziness and drowsiness.

Q: Does Rebamipide interact with caffeine or alcohol?

Official regulatory summaries generally report no clinically significant drug-drug interactions with this medicine. However, common patient advisories note that avoiding or limiting alcohol is often suggested because it stimulates stomach acid production, which can counteract the medicine's protective action.

Q: Is Rebamipide considered safe for use in older adults?

Official regulatory labeling advises that special care and close monitoring are required when Rebamipide is used by older adults, as this population may be more susceptible to adverse effects, particularly gastrointestinal disturbances.

Q: What kind of research has been done on Rebamipide outside of Asia?

Research overviews confirm that authoritative sources note that the majority of high-quality clinical data is concentrated in East Asia, meaning the results may not be fully generalizable to other populations.

Q: Is Rebamipide effective for all types of stomach discomfort?

The official indications for this medicine restrict its use to specific diagnoses like gastric ulcers, gastritis, and certain mucosal lesions. Its efficacy has not been officially established or proven for the entire spectrum of general or unspecified 'stomach discomfort.'

Q: Why do some people take Rebamipide for mouth sores?

Rebamipide is officially documented for use in conditions that require mucosal protection and healing. In certain regions, its licensed indications include the treatment of oral mucositis, which involves inflammation and sores in the lining of the mouth.

Q: What happens if I stop taking Rebamipide suddenly?

Patient information sheets in regions where the drug is licensed often note that patients are generally advised to not stop taking the medicine unless instructed to do so by a healthcare provider.

Q: Can Rebamipide affect sleep patterns?

Yes, official safety information lists drowsiness as a possible adverse reaction. Since drowsiness can impact wakefulness, it can indirectly affect a patient's normal sleep patterns.

Q: Does Rebamipide interact with herbal supplements?

While regulatory documents typically focus on drug-drug interactions and report no clinically significant medicinal interactions, patient advisories emphasize the need to inform a healthcare provider of all products being taken, including herbal supplements. This is a cautionary measure due to the potential for unstudied co-administration effects.

Q: Can Rebamipide affect fertility or reproductive health?

The core regulatory label focuses on safety during pregnancy and lactation. However, clinical studies accessible via official medical resources have investigated the medicine's effect in infertile males, with some research observing improved seminal parameters and decreased oxidative stress.

Q: Do any official warnings exist about operating machinery while taking Rebamipide?

Yes, official regulatory warnings advise that individuals who experience effects like dizziness, drowsiness, or tremors should avoid activities such as operating machinery or driving.

Q: Are there different brand names for Rebamipide?

Yes, Rebamipide is the active ingredient's International Nonproprietary Name (INN). Official substance listings and regulatory resources confirm that the medicine is marketed under various brand names in different countries, such as MUCOSTA and REBATOR.

Q: Are there common user complaints about the taste or size of Rebamipide tablets?

Official safety documents do include taste disturbances (listed as taste abnormality) among the possible adverse reactions reported in a small number of patients. Information regarding common complaints about the physical size of the tablets is not typically included in official safety labeling.

How should Rebamipide be stored and disposed of?

How to Store and Dispose of Rebamipide?

The storage and disposal of rebamipide are defined by official regulatory requirements to ensure its stability and safety. The medicine must be stored away from excessive heat, moisture, and direct sunlight. Maintaining these conditions is crucial for protecting the integrity of the product.

Official Storage and Disposal Rules

Storage Component Requirement
Environmental Protection Store away from direct sunlight, heat, and moisture.
Child Safety Keep the medicine out of the reach of children.
Handling Discard the remainder of the medicine; do not store it.
Disposal Guidance If uncertain about disposal procedures, consult a medical institution or pharmacy for advice.

Patients are officially instructed not to keep leftover or unused medicine after its intended use. Furthermore, it is specified that unused medicine must not be given to other individuals.

Attention! Always consult to a doctor or pharmacist before using pills or medicines.

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