Rabiril

Rabiril is a medicine for the treatment of diseases of the gastrointestinal tract. Let's consider the features of therapy with this drug and the nuances of its use.

Pharmacotherapeutic group of the drug - means for the treatment of gastroesophageal reflux disease and peptic ulcer. Tablets are included in the category of H2 receptor antagonists. Rabiril affects metabolism and the digestive system, is suitable for the treatment of acid-dependent diseases.

Rabiril is used to treat and prevent gastrointestinal tract lesions. The drug is effective in the treatment of gastroesophageal reflux disease and peptic ulcers, but can only be used as prescribed by a doctor.

Indications Rabiril

Indications for use of Rabiriil are based on the activity of its active components. Tablets are used to treat and prevent the following diseases:

• Gastroesophageal reflux disease
• Dyspepsia
• Nonerosive reflux disease
• Symptomatic treatment of GERD
• Bloating
• Belching and flatulence
• Nausea and vomiting
• Acid peptic disorders
• Feeling of fullness in the epigastrium
• Postoperative nausea and vomiting

Pain in the upper abdomen.

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Release form

Release form – combined packaging with a blister of 10 tablet capsules. Each capsule is a tablet with an enteric coating, which contains 20 mg of rabeprazole and 20 mg of domperidone maleate.

The tablets are available only with a doctor's prescription.

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Pharmacodynamics

Pharmacodynamics of Rabiril are the processes that occur with its active substances. Let's consider in more detail the activity of the components of the drug.

• Rabeprazole has antiulcer properties. Its mechanism of action is based on inhibition of the enzyme H+/K+-ATPase. The enzyme system refers to acid pumps, since the active substance is an inhibitor of the proton pump of the stomach, blocking the formation of hydrochloric acid at the final stage. Dose-dependent action inhibits basal and stimulated secretion of hydrochloric acid, the nature of the irritant is not important.
• Domperidone – stimulates gastrointestinal motility. This substance is an antagonist of dopamine (D2) receptors, eliminating the inhibitory effect of dopamine on the motor functions of the stomach. The component prolongs peristaltic contractions in the antrum of the stomach and duodenum. This increases the tone of the lower esophageal sphincter and accelerates the release of the stomach, but does not affect gastric secretion. The antiemetic effect is due to a combination of antagonism and gastrokinetic effect on dopamine receptors in the trigger zone of chemoreceptors. The substance eliminates nausea and hiccups.

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Pharmacokinetics

Pharmacokinetics of Rabiril allows to learn about the processes of absorption, metabolism and distribution. That is, the actions that occur with the drug after administration.

1. Rabeprazole

• The antisecretory effect lasts for 60 minutes after taking 20 mg of the drug. The pH of the gastric environment decreases to the maximum level 3-4 hours after taking. Three days after treatment, a stable antisecretory effect occurs.
• The active substance is completely and quickly absorbed in the digestive tract, but is destroyed by hydrochloric acid. The enteric-coated dosage form is destroyed by hydrochloric acid.
• Bioavailability is 52% and does not increase with repeated administration. Food intake and time of administration do not affect its absorption. Plasma protein binding is 97%.
• The substance is metabolized in the liver with the active participation of the cytochrome P450 enzyme system. 90% of the substance is excreted in the urine as metabolites, the remainder is excreted in the feces.

2. Domperidone

• When taken orally on an empty stomach, it is quickly and completely absorbed in the digestive tract. It is intensively metabolized in the intestinal walls and liver. Bioavailability is at the level of 15%. The maximum concentration in the blood plasma is achieved 60 minutes after administration. Food intake and a decrease in the acidity of gastric juice slow down the absorption process.
• Plasma protein binding is 90%. The substance does not penetrate the BBB, but penetrates into breast milk. Biotransformation occurs by hydroxylation and N-dealkylation. 66% of the drug is excreted in feces, 33% in urine and about 10% unchanged.

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Dosing and administration

The method of administration and dosage are individual for each patient. Usually the drug is prescribed in a dosage of 1 tablet per day (preferably in the morning) 10-20 minutes before meals. The maximum duration of treatment is 14 days.

If the drug is prescribed to patients with malignant neoplasm of the stomach, it leads to a decrease in the severity of drug symptoms. Before treatment, such pathologies must be excluded. With special caution, the drug is prescribed to patients with moderate or mild liver and kidney dysfunction. Cross-hypersensitivity with other substituted benzimidazoles or proton pump inhibitors is not excluded.

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Use Rabiril during pregnancy

The use of Rabiriil during pregnancy is prohibited. The use of the drug is possible when the potential benefit to the mother is more important than the risk to the health of the fetus. The active substances are excreted in breast milk and penetrate the placental barrier.

Rabiriil is not prescribed to pediatric patients. As of today there is not enough information about the safety of its use in this age group.

Contraindications

Rabiril is prohibited to take in case of individual intolerance to the components of the drug and benzimidazole derivatives. The drug is not taken in case of gastrointestinal bleeding, mechanical intestinal obstruction, intestinal and stomach perforation. Severe renal and hepatic dysfunction, hyperprolactinemia and prolactinoma also refer to the prohibition on the use of tablets.

The use of the drug simultaneously with ketoconazole, potent CYP 3A4 inhibitors, erythromycin and drugs that prolong the QT interval (clarithromycin, fluconazole, amiodarone, telithromycin, voriconazole) is strictly contraindicated.

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Side effects Rabiril

Side effects of Rabiriil occur when the instructions for the drug are not followed. To date, there is a specific assessment of the frequency of adverse reactions (including isolated data):

• Very common – ≥1/10
• Often – ≥1/100 to <1/10
• Uncommon – ≥1/1000 to <1/100
• Rare – ≥1/10,000, <1/1000
• Very rare - <1/10,000

If all recommendations regarding dosage and duration of therapy are followed, the drug is well tolerated and side effects are rare.

Most often, patients complain of allergic reactions, various disorders of the endocrine system, nervousness, irritability and anxiety. The drug provokes side symptoms from the nervous and cardiovascular systems. From the gastrointestinal tract, gastrointestinal disorders, hepatitis, jaundice, intestinal spasms and diarrhea are possible. In rare cases, galactorrhea, pain in the lower extremities and back, increased prolactin levels occur. All symptoms completely disappear after stopping the course of treatment.

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Overdose

Symptoms of overdose:

• Increased sleepiness
• Extrapyramidal disorders (motor activity disorders)
• Disorientation

To treat side effects, the drug should be discontinued. Patients are prescribed absorbents (activated carbon) and symptomatic therapy is administered. The active substances bind well to blood proteins, so dialysis is ineffective. There is no specific antidote.

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Interactions with other drugs

Interaction of Rabiri with other drugs is possible only on medical advice. Thus, anticholinergic drugs neutralize the antidyspeptic effect of domperidone. The drug is not taken with antisecretory and antacid drugs, since they reduce the bioavailability of domperidone.

Concomitant oral administration of erythromycin and ketoconazole inhibits presystemic metabolism of domperidone. CYP 3A4 inhibitors such as azole antifungals, macrolide antibiotics, HIV protease inhibitors, and calcium antagonists should not be used with domperidone.

The drug causes a long-term and strong decrease in the production of hydrochloric acid. That is, the active substance can work without side effects with agents whose absorption depends on the pH of the stomach contents. Rabiril does not interact with antacids in liquid form and is not used in combination with atazanavir.

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Storage conditions

Storage conditions for Rabirill are similar to the rules for storing any other tablet preparations. The temperature should not exceed 30°C, the medicine is stored in a dry place, protected from sunlight and out of the reach of children.

If the above recommendations are not followed, the medicine loses its properties and is prohibited for use. If the tablets have changed color or acquired a smell, they are also prohibited for use and must be disposed of.

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Shelf life

The shelf life is 36 months from the date of manufacture. After its expiration, the drug is prohibited for use and must be disposed of. Failure to comply with storage rules affects the suitability of the drug.

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