rebamipide

Action and Spectrum

Actions and Spectrum: 

rebamipide is a medication used primarily to treat gastrointestinal conditions, particularly mucosal damage or inflammation. It is available in several forms, including tablets, suspension, and eye drops.  

• Mucosal Protection: rebamipide is known for its mucosal protective properties. It helps to enhance the protective mechanisms of the mucous membrane lining the gastrointestinal tract, particularly in the stomach and small intestine. This action mainly benefits individuals with conditions like gastritis, peptic ulcers, or gastritis induced by nonsteroidal anti-inflammatory drugs (NSAIDs). rebamipide promotes the secretion of mucus and bicarbonate, which can help protect the mucosal lining from damage caused by stomach acid or other irritants. 
• Anti-Inflammatory: rebamipide also exhibits anti-inflammatory properties. It can help diminish inflammation in the gastrointestinal tract, which is especially important in conditions like gastritis and peptic ulcers, where inflammation can exacerbate symptoms and delay healing. 
• Cytoprotective Effects: rebamipide’s cytoprotective effects extend beyond the gastrointestinal tract. It has been used in ophthalmology as eye drops to promote the healing of corneal and conjunctival epithelial tissues. This is particularly useful in dry eye syndrome and corneal ulcers. 

Drug Interaction

Adverse Reaction

Frequency not defined 

shock 

dizziness 

heartburn 

leucopenia 

thrombocytopenia 

hypersensitivity 

constipation 

dry mouth 

belching 

rare liver dysfunction 

anaphylactoid reactions 

jaundice 

taste abnormality 

drowsiness 

abdominal pain 

diarrhoea 

nausea 

vomiting 

Black Box Warning

Black Box Warning: 

None 

Contraindication / Caution

Contraindication/Caution: 

Contraindication 

• Hypersensitivity: Individuals with a known hypersensitivity or allergic reaction to rebamipide or its components should not use this medication. Allergic reactions can range from mild-severe anaphylaxis, a life-threatening condition. 
• Children: rebamipide’s safety and effectiveness in pediatric populations have not been well established, so it is typically not recommended for use in children under a certain age. Specific age restrictions may vary by region and medical guidelines. 
• Pregnancy and Breastfeeding: The safety of rebamipide during pregnancy condition and breastfeeding has not been adequately studied. Therefore, pregnant or breastfeeding women should consult with their healthcare provider before using this medication. In such cases, the potential benefits and risks should be carefully weighed. 
• Severe Liver or Kidney Dysfunction: rebamipide is primarily metabolized by the liver and also eliminated through the kidneys. Individuals with severe liver or kidney dysfunction may experience altered drug metabolism and elimination, potentially leading to adverse effects. In such cases, rebamipide should be closely monitored or avoided altogether. 
• Gastrointestinal Perforation or Bleeding: rebamipide is unsuitable for treating active gastrointestinal bleeding or perforation because it may interfere with hemostasis (the body’s ability to stop bleeding) or worsen existing bleeding. 
• Concurrent Use of Nonsteroidal Anti-Inflammatory Drugs (NSAIDs): rebamipide is often prescribed to protect the gastrointestinal mucosa in individuals taking NSAIDs, which can cause gastric irritation and ulcers. However, its use should be carefully monitored in these cases, and the patient should follow their healthcare provider’s recommendations. 

Caution 

• Allergic Reactions: Although rare, allergic reactions to rebamipide can occur. If you experience symptoms such as rash, itching, swelling, severe dizziness, or difficulty breathing, discontinue the medication and seek immediate medical attention. 
• Pregnancy and Breastfeeding: As previously mentioned, the safety of rebamipide during pregnancy and breastfeeding is not well-established. Consult with your healthcare provider if you are pregnant, planning to become pregnant, or breastfeeding. They will help weigh the potential risks and benefits and determine if rebamipide suits your situation. 
• Pediatric Use: rebamipide’s safety and effectiveness in children have not been adequately studied. Its use in pediatric populations may be limited, and it should only be prescribed to children if deemed necessary by a healthcare provider. 
• Renal and Hepatic Impairment: Patients with significant renal (kidney) or hepatic (liver) impairment may require dosage adjustments or closer monitoring when taking rebamipide. The drug is metabolized in the liver and also excreted via the kidneys so that impaired organ function may affect drug clearance. 
• Drug Interactions: Some medications may interact with rebamipide, potentially altering its effects or increasing the risk of side effects. Inform the healthcare provider about all the drugs, supplements, and herbal products you are taking to assess potential interactions. 
• Gastrointestinal Perforation or Bleeding: If you have a history of gastrointestinal perforation or bleeding, use rebamipide cautiously. It is generally used to protect the gastrointestinal mucosa, but its use should be monitored in individuals with a history of these conditions. 
• Ophthalmic Use: If you use rebamipide ophthalmic solutions (eye drops), use them as your eye care professional directs. Be cautious while driving or performing tasks requiring clear vision immediately after using these drops, as they may cause temporary blurred vision. 
• Alcohol: Avoid excessive alcohol consumption while taking rebamipide, as it may increase the risk of side effects or interact with the medication. 

Pregnancy / Lactation

Pregnancy consideration:  

US FDA pregnancy category: Not assigned. 

Lactation:   

Excreted into human milk: Not known. 

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 
• Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    
• Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence, these categories of drugs need to be avoided by pregnant women.    
• Category N: There is no data available for the drug under this category. 

Pharmacology

Pharmacology: 

rebamipide is a medication with pharmacological actions primarily focused on gastrointestinal and ocular tissues. It exerts its effects by enhancing the protective mechanisms of mucous membranes, particularly in the stomach and small intestine, where it stimulates the secretion of mucus and bicarbonate, thus promoting mucosal protection and reducing inflammation.

rebamipide’s mucosal protective properties make it valuable in treating conditions like gastric and duodenal ulcers, gastritis, and gastric erosions, often in conjunction with nonsteroidal anti-inflammatory drugs (NSAIDs). Additionally, in ophthalmology, rebamipide is used as an eye drop to increase tear production and stabilize the tear film, making it an effective treatment for dry eye syndrome and also other ocular surface disorders. 

Pharmacodynamics: 

Mechanism of action: The action of rebamipide is not fully understood. However, it is believed to involve several pharmacological effects that collectively contribute to its therapeutic actions, particularly in gastrointestinal and ocular conditions.  

• Mucosal Protection: rebamipide enhances the protective mechanisms of the mucous membrane lining the gastrointestinal tract, particularly in the stomach and small intestine. It stimulates mucus and bicarbonate secretion, which help create a physical barrier against stomach acid and other irritants. This mucosal protection is essential for preventing and healing mucosal damage, such as in gastric and duodenal ulcers. 
• Anti-Inflammatory Properties: rebamipide has anti-inflammatory properties, which can help reduce inflammation in the gastrointestinal mucosa. In conditions like gastritis or gastritis induced by nonsteroidal anti-inflammatory drugs (NSAIDs), this anti-inflammatory effect can help alleviate symptoms and promote healing. 
• Increased Blood Flow: rebamipide has been shown to increase blood flow to the mucosal tissues of the stomach and small intestine. Improved blood flow can enhance the delivery of nutrients and oxygen to these tissues, aiding healing. 
• Stimulation of Prostaglandin Production: rebamipide may stimulate the production of prostaglandins, which are the natural substances in the body with various physiological functions, including promoting mucosal protection and blood flow. This stimulation of prostaglandin production can contribute to the drug’s protective effects. 

Pharmacokinetics: 

Absorption 

rebamipide is typically administered orally in tablet or suspension form. 

It is well-absorbed from the gastrointestinal tract after oral administration. 

The absorption of rebamipide is not significantly affected by food so that it can be taken with or without meals. 

Distribution 

rebamipide is distributed throughout the body via the bloodstream. 

It has a relatively low binding affinity to plasma proteins, which means it is mainly present in its free form in the blood. 

When administered orally or as an ophthalmic solution, the drug is distributed to various tissues, including the gastrointestinal mucosa and the eye. 

Metabolism 

rebamipide undergoes minimal hepatic (liver) metabolism. 

The drug is primarily excreted in its unchanged form in the urine, suggesting that it does not undergo extensive metabolic transformation in the liver. 

Due to its limited hepatic metabolism, the risk of drug interactions related to hepatic enzymes is relatively low. 

Elimination and Excretion 

rebamipide is primarily excreted through the renal (kidney) route. 

It is eliminated in the urine in its unchanged form, with a relatively short elimination half-life. 

Patients with impaired renal function might require dosage adjustments, as the clearance of the drug can be affected in these individuals. 

Adminstartion

Administration: 

The administration of rebamipide can vary depending on the specific formulation and the treated condition. rebamipide is available in different forms, including oral tablets, oral suspension, and ophthalmic (eye) solutions.  

Oral Tablets: 

Take rebamipide tablets by mouth as directed by your healthcare provider. 

Swallow the tablets whole with a glass of water, usually with or without food, depending on your provider’s instructions. 

Follow the prescribed dosage and dosing schedule. Do not exceed the recommended dose. 

Oral Suspension: 

If prescribed the oral suspension form of rebamipide, shake the bottle well before use. 

Use the provided measuring device (dosing spoon or syringe) to measure the correct dose. 

Administer the suspension orally, either with or without food, as instructed by your healthcare provider. 

After use, clean the measuring device and recap the bottle. 

Ophthalmic Solution (Eye Drops): 

If using rebamipide ophthalmic solution, wash your hands before handling the eye drops. 

Tilt your head back/lie down and look up at the ceiling. 

Gently pull down lower eyelid to create a small pocket. 

Hold the dropper tip close to your eye without touching it, and instill the prescribed number of drops into the eye. 

Close your eye gently for a few moments to allow the solution to spread over the eye’s surface. 

If using other eye drops, wait at least 5 minutes between each drug to prevent interactions. 

Avoid touching your eye with the dropper tip to prevent contamination. 

Dosage and Frequency: 

The healthcare provider will generally determine the dosage and frequency of rebamipide based on your medical condition and needs. 

Always follow your provider’s instructions regarding when and how to take the medication. 

Do not adjust the dosage or frequency without consulting your healthcare provider. 

Duration of Treatment: 

Continue taking or using rebamipide for the entire duration your healthcare provider prescribes, even if you start to feel better. Stopping prematurely may result in the return of symptoms. 

Special Instructions: 

If a dose is missed, taking it as soon as possible is generally recommended. However, if the next scheduled dose is missed, it should be skipped and the following dose should be taken at the appropriate time. It is key to avoid taking a double dose of the drug in order to compensate for the missed dose. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: rebamipide 

Why do we use rebamipide? 

rebamipide is a medication used for various therapeutic purposes, primarily treating gastrointestinal conditions and ophthalmic (eye) disorders.  

• Gastric and Duodenal Ulcers: rebamipide treats and promotes the healing of gastric (stomach) and duodenal (small intestine) ulcers. It helps protect the mucosal lining of the gastrointestinal tract from the harmful effects of stomach acid and other irritants. 
• Gastritis: This medication is prescribed to manage and relieve symptoms of gastritis and stomach lining inflammation. rebamipide’s anti-inflammatory properties can help reduce gastric inflammation and alleviate discomfort. 
• Gastrointestinal Disorders Associated with NSAID Use: Nonsteroidal anti-inflammatory drugs (NSAIDs) may irritate the stomach lining, leading to gastritis or ulcers. rebamipide is often used as a mucosal protective agent in individuals taking NSAIDs to prevent or mitigate these side effects. 
• Chronic Gastric Erosions: It is used to treat chronic gastric erosions, which are small areas of damage to the stomach lining. rebamipide helps in the repair and protection of these erosions. 
• Dry Eye Syndrome: rebamipide is available in ophthalmic (eye) formulations as eye drops. rebamipide eye drops help promote tear production and reduce eye discomfort. 
• Ocular Surface Disorders: Besides dry eye syndrome, rebamipide eye drops may be used to manage other ocular surface disorders, such as conjunctivitis and keratoconjunctivitis, characterized by inflammation and irritation of the eye’s surface. 
• Corneal Ulcers: rebamipide eye drops can be an adjunctive therapy for treating corneal ulcers. They help in the healing process of corneal epithelial tissues. 
• Mucosal Protection: rebamipide’s mucosal protective properties make it useful when protecting the mucous membranes of the gastrointestinal tract or the ocular surface is necessary.