Overview:
Rebamipide, an analog of 2 (1H) - quinolone, was introduced in the year 1980 for treating gastritis, an inflammation of the stomach. The FDA has not approved the drug in the United States. However, many studies have proven the drug protects against the damaging effects of nonsteroidal anti-inflammatory drugs on the gastrointestinal mucosa. The drug belongs to a medication called antacids or anti-reflux agents, which are effective against duodenal ulcers.
The drug improves the defense mechanism of the gastric mucus by increasing the prostaglandin section, thereby acting as an antiulcer drug. It is primarily involved in reducing the free radicals that have great potential to cause damage to the gastrointestinal mucosa.
How Does Rebamipide Work?
The mechanism of action of Rebamipide generates by targeting the oxygen radicals and reducing the number of molecules by acting as a mucosal protective agent. The mucosa is the inner lining of cells found in the esophagus and stomach. The drug acts by increasing the synthesis of a chemical messenger called prostaglandins. Prostaglandins are the lipid molecules that generally act on tissue injury or infection sites. They control the inflammatory process and blood flow, thereby aiding in healing. Hence the drug is a mucosal safeguarded.
What Are the Uses of Rebamipide?
Rebamipide is prescribed for specific medical conditions involving gastric or intestinal mucosa ulceration. The drug acts on the mucosa and inhibits the exaggeration of the inflammatory process by blocking the COX pathway. COX refers to cyclo-oxygenase, which helps to mediate the inflammatory process as a defense mechanism to protect and fight the infiltration of infection. The most prominent usage of the drug is in healing ulcers and sores of the mouth and esophageal tract. Some of the most common conditions requiring Rebamipide are mentioned below:
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Gastritis: Gastritis is a condition that causes inflamed gastric mucosal lining, which can be a constant irritation and affect the stomach. It results in symptoms like acidity and heartburn.
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Recurrent Aphthous Ulcer: A recurrent aphthous ulcer occurs in the oral cavity (mouth). They can occur in the inner lining of cheeks and lips. They are painful and make food consumption difficult.
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Behcet's Syndrome: It is a disorder of a kind that affects the entire body. It is a rare condition that causes blood vessel inflammation, resulting in initially irrelevant symptoms. The symptoms include eye inflammation, mouth sores, and skin rashes.
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Peptic Ulcer: A sore in the lining of the stomach, esophagus, and small intestine is known as a peptic ulcer. It causes nausea, vomiting, heartburn, and stomach bloating. Complications of this disease can be life-threatening and can cause mucosal bleeding.
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GERD: Gastroesophageal reflux disorder (GERD) is a condition that causes acid regurgitation. This is because of improper and untimely food intake that causes increased acid secretion due to starvation. It erodes the gastric lining and tooth surfaces and is extremely harmful.
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Gastric Atrophy: Atrophy is generally considered thinning out of tissues. Gastric atrophy is a condition characterized by thinning of the stomach lining. It affects the digestion process. Severe cases may result in a lifetime risk of gastric cancer development. It is usually caused by Helicobacter pylori infection.
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Intestinal Metaplasia: Metaplasia is the differentiation of a specific cell into different types. For example, in intestinal metaplasia, the cells of the upper digestive tract transform. It is a precancerous condition.
Dosage and Administration
Rebamipide is a 100 mg tablet and can be administered thrice daily in the morning, evening, and before bedtime in three divided doses. The route of administration of Rebamipide is oral and has to be stored at a temperature below 25 degrees Celsius for better efficacy. The other variant of the drug is an ophthalmic solution that is used to prevent dry eyes.
Drug Interactions
Rebamipide can interact with painkillers like Diclofenac and Celecoxib. In addition, heavy smokers or alcohol consumers may have increased secretion of stomach acids, which causes acidity and heart burns. So the effects of Rebamipide may diminish with alcohol intake. However, the interaction of the drug in patients taking NSAIDs (non-steroidal anti-inflammatory drugs) has been of utmost benefit by preventing complications and healing the ulcerated mucosa, thereby ensuring less damage to the gastric lining and recurring inflammatory response.
Warnings
The drug may cause adverse effects when consumed with other drugs. Hence, giving a good medical and drug history is essential so the doctor can prescribe medications accordingly.
Warning for Special Population
Pregnancy
The drug should be avoided in pregnant women unless extremely necessary. Therefore, it is essential to understand the risks and benefits of the drug before administration.
Breastfeeding
Breastfeeding women are generally advised to discontinue the consumption of drugs unless completely necessary. Therefore, the drug is usually not recommended for breastfeeding.
General Warnings
Elderly People
The drug may cause adverse effects in older adults. Hence, the dosage and method of drug administration have to be altered so they do not suffer any side effects.
Use in Liver Disorders
The drug may cause severe effects in liver diseases as it is metabolized in the liver. So, regular drug monitoring is done to rule out unnecessary complications. In addition, the doctor may advise a liver function test to determine the liver's health and function and adjust the dosage accordingly.
Driving
The drug may cause side effects like dizziness and visual disturbances. Hence, avoiding the drug when performing activities requiring mental alertness is important. For example, people working in the heavy machinery industry and using industrial equipment may require mental alertness. Therefore, they may have to avoid medication for better focus during work.
For Patients
What Is Gastritis?
Gastritis is an inflammatory disorder of the gastric mucosa that can be classified as acute or chronic, depending on the duration of inflammation. This condition has a higher prevalence in women than in men. Also, gastritis is frequently found in heavy drinkers and smokers. The etiology usually stems from the congestion of corrosive and erosive substances that affect the mucosa lining. However, it could also be due to infections affecting the gastric lining. In addition, particular drugs may cause side effects that increase acid production, and acute alcoholism and food poisoning are common causes.
The stomach mucosa is extremely tender and can be affected by spicy food substances. In addition, foods that have a rough texture and are consumed at hot temperatures can damage the gastric lining. Acute gastritis is generally of shorter duration unless the gastric lining is damaged to a greater extent.
What Is Rebamipide?
Rebamipide is an antacid that limits the excess production of gastric acid to a level that starts damaging the tissues and the lining of mucosa, causing constant irritation and inflammation.
Why Is Rebamipide Prescribed?
Rebamipide is given explicitly in conditions like gastritis (inflammation of the gastric mucosa) and conditions like gastroesophageal reflux disorders and recurrent ulcers of the mouth caused due to acid reflux.
How Should Rebamipide Be Used?
Rebamipide is taken orally for two weeks to a month, depending on the severity of the damage in the gastrointestinal lining. After that, it is taken in divided doses thrice daily, usually before food. Consuming the drug half an hour before the food intake can help form a protective barrier on the gastric lining that helps during food consumption.
What Special Precautions Should Be Taken Before Administering Rebamipide?
There is no sufficient evidence to support the effects of the drug on pregnant and breastfeeding mothers. However, informing the doctor and taking proper advice before using the drug is crucial. The drug actions in an unborn child are yet to be manifested. As the drug can be excreted in human milk, it could lead to health issues in infants.
Rebamipide should be avoided in individuals with previous history or family history of allergic reactions to the drug and its components. In addition, individuals with severe liver or kidney disorders can inform the doctor before drug intake, so they can frequently monitor and assess the functioning of those organs.
What Are the Side Effects of Rebamipide?
Although Rebamipide is a safe drug, there are chances of a few major and minor side effects exhibited by individuals during the drug intake. Any such encounter should be informed to the doctor immediately. Some of the side effects are mentioned below.
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Itching.
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Nausea.
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Vomiting.
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Irritation of the eyes.
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Eye discharge.
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Constipation.
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Bitter taste.
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Dizziness.
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Loss of appetite.
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Xerostomia (dry mouth).
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Heartburn.
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Breathing difficulties.
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Abdominal pain.
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Belching.
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Eczema.
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Pruritus.
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Stomach upset.
Dietary Alterations
No specific diet is recommended unless suggested by the healthcare professional. Consuming a balanced diet could be sufficient.
For Doctors
Taxonomy
Kingdom: Organic compounds.
Superclass: Benzoids.
Class: Benzene and derivatives.
Subclass: Aniline.
Alternative Parent: Toluene.
Pharmacology
Rebamipide is an amino acid analog that alters the free oxygen radicals. When in abundance, these radicals cause ill effects on the mucosal lining of the gastrointestinal tract. It helps in the replacement of tissue that has been lost. It also increases the expression of epidermal growth factor (EGF), which causes angiogenesis, and increases the production of granulation tissue. This ultimately leads to the epithelization of the ulcer and aids with the healing process. It is also a cytoprotective agent with superior healing properties on large-sized ulcers measuring about 20 to 40 millimeters.
Pharmacodynamics
Rebamipide is a novel anti-ulcer agent with low aqueous solubility and permeability in the human body. Hence, many supporting studies and research have proved the bioavailability of the drug to be less than 10 percent in humans. In addition, the unique properties of the drug exhibit convincingly increased gastric mucus glycoprotein components, which act as a scavenger to free radicals.
Pharmacokinetics
The drug interactions between Rebamipide and nonsteroidal anti-inflammatory drugs (NSAID) cause severe effects on the gastrointestinal tract and kidneys. In addition, Rebamipide, being a neuroprotective agent, causes side effects when simultaneously administered with NSAIDs. The main purpose of the drug is to provide quality healing of ulcers and recurrence of ulcers. The drug attenuates the neutrophil activity and stimulates cytokines by Helicobacter pylori. Limiting such immunoinflammatory responses in infections helps to fasten the healing process.
Other Specifications:-
Rebamipide in Pregnant Women:
The use of the drug in pregnant women requires careful consideration. Limited data on the drug's safety in pregnant women has been established. The use of drugs in pregnant women has resulted in gastrointestinal disorders like gastric ulcers. Hence extra care should be taken before drug administration.
Rebamipide in Lactating Women:
Studies are yet to prove the transfer of the drug into breast milk. There is a theoretical risk of adverse effects on the child. An alternative method or drug should be considered during breastfeeding.
Rebamipide in Pediatric Patients:
Careful consideration is required before administering the drug to pediatric patients. Due to limited data, there is a lack of dosage guidelines for this drug. If prescribed to pediatric patients, close monitoring is required. Also, the dosage has to rely on the age and weight of the patient.
Rebamipide in Geriatric Patients:
The use of drugs in elderly individuals should be approached with caution due to age-related changes in drug metabolism. Also, there is an increased risk of drug adversities due to existing comorbidities.
Rebamipide in Renal Impairment Patients:
The use of the drug could require dose adjustments or cautions to reduce the risk of potential changes in drug clearance. Minimal data concerning the use of drugs in renal-impaired patients has been recovered.
Rebamipide in Hepatic Impairment Patients:
The drug use could require caution and dose adjustments to reduce the risk in hepatic-impaired patients potentially. Additionally, individualized assessment and monitoring are mandatory to prevent adverse effects of the drug.
Involvement of the Healthcare Team
The healthcare team plays a pivotal role in monitoring the drug dosage and making specific alterations to support the needs and requirements of each individual. Extra care has to be taken in individuals suffering from pre-existing liver and kidney disorders to prevent any consequences that may lead to comorbidities. Also, pregnant and breastfeeding mothers should be considered for special care in prescribing this medication to prevent the side effects on the newborn child. For better outcomes of the drug, frequent follow-up and dosage alteration can aid in the success of the treatment.
