Rabiril

Rabil - a remedy for the treatment of diseases of the organs of the gastrointestinal tract. Let's consider features of therapy by the given preparation and nuances of its application.

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

Razoril is used to treat and prevent lesions of the gastrointestinal tract. The drug is effective in the therapy of gastroesophageal reflux disease and peptic ulcer, but can only be used for medical purposes.

Indications Rabiril

Indications for the use of Rabilil are based on the activity of its active ingredients. Tablets are used to treat and prevent such diseases:

• Gastroesophageal reflux disease
• Dyspepsia
• Non-erosive reflux disease
• Symptomatic treatment of GERD
• Bloating
• Belching and flatulence
• Nausea and vomiting
• Acidic peptic disorders
• Feeling of overfilling in epigastrium
• Postoperative nausea and vomiting

Pain in the upper abdomen.
 

[1], [2], [3]

Release form

The form of production is a combined package with a blister for 10 tableted capsules. Each capsule is an enteric-coated tablet that contains 20 mg of rabeprazole and 20 mg of domperidone maleate.

Tablets are released only on the prescription.

[4], [5], [6]

Pharmacodynamics

Pharmacodynamics Rabilil are processes occurring with its active substances. Let's consider the activity of the medicament components in more detail.

• Rabeprazole - has antiulcer properties. The mechanism of its action is based on the 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 in the final stage. The dose-dependent effect inhibits the basal and stimulated secretion of hydrochloric acid, the nature of the stimulus does not matter.
• Domperidone - stimulates the motility of the gastrointestinal tract. This substance is an antagonist of dopamine (D2) receptors, which eliminate the inhibitory effect of dopamine on the motor functions of the stomach. The component prolongs peristaltic contractions in the antrum part of the stomach and duodenum. This increases the tone of the lower sphincter of the esophagus and accelerates the release of the stomach, but does not affect gastric secretion. Antiemetic effect is caused by a combination of antagonism and gastrokinetic effect to dopamine receptors in the trigger zone of chemoreceptors. The substance eliminates nausea and hiccups.

[7], [8], [9], [10], [11], [12]

Pharmacokinetics

Pharmacokinetics Rabilil allows you to learn about the processes of absorption, metabolism and distribution. That is, the actions taking place with the drug after taking.

1. Rabeprazole

• The antisecretory effect lasts for 60 minutes after taking 20 mg of the drug. Reduction of the pH of the gastric environment to the maximum level occurs 3-4 hours after admission. Three days after treatment, there is a stable antisecretory effect.
• The active substance is completely and rapidly absorbed in the digestive tract, but is destroyed by the action of hydrochloric acid. The enteric dosage form is destroyed by hydrochloric acid.
• Bioavailability is 52% and does not increase with multiple admission. The use of food and the time of taking the medicine does not affect its absorption. Binding to blood plasma proteins 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 in the form of metabolites, the residue is excreted with feces.

2. Domperidone

• When taken orally on an empty stomach, it is quickly and completely absorbed in the digestive tract. Intensively metabolized in the walls of the intestine and liver. Bioavailability at the level of 15%. The maximum concentration in the blood plasma is reached after 60 minutes after administration. Eating and lowering the acidity of gastric juice slows down the absorption process.
• Binding to blood plasma proteins 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 with feces, 33% with urine and about 10% unchanged.

[13], [14], [15]

Dosing and administration

The method of administration and dose 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 for patients with a malignant neoplasm of the stomach, this leads to a decrease in the severity of the drug symptomatology. Before treatment it is necessary to exclude similar pathologies. With special care, the drug is prescribed for patients with moderate or mild impairment of liver and kidney function. Do not exclude cross-hypersensitivity with other substituted benzimidazoles or proton pump inhibitors.

[21], [22], [23], [24], [25]

Use Rabiril during pregnancy

Use of Rabilil during pregnancy is prohibited. The use of the drug is possible if 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.

The rabies are not prescribed to children of childhood. Since to date there is insufficient information about the safety of its use in this age group.

Contraindications

It is forbidden to take Rabiril for individual intolerance of the components of the drug and the benzimidazole derivative. Medication is not taken with gastrointestinal bleeding, mechanical intestinal obstruction, perforation of the intestine and stomach. Severe violations of kidney and liver function, hyperprolactinaemia and prolactinoma, also apply to the ban on the use of tablets.

Categorically contraindicated use of the drug simultaneously with ketoconazole, potent CYP 3A4 inhibitors, erythromycin and QT prolonging drugs (clarithromycin, fluconazole, amiodarone, telithromycin, voriconazole).

[16], [17], [18]

Side effects Rabiril

Side effects of the drug arise when the conditions of the drug are not observed. To date, there is a specific assessment of the incidence of adverse reactions (including isolated data):

• Very often - ≥1 / 10
• Frequently - ≥1 / 100 to <1/10
• Infrequently - ≥1 / 1000 to <1/100
• Rarely ≥1 / 10,000, <1/1000
• Very rarely - <1/10 000

If all recommendations regarding the dosage and duration of therapy are observed, then the medication 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 medication provokes side symptoms from the nervous and cardiovascular system. From the gastrointestinal tract, gastrointestinal disorders, hepatitis, jaundice, intestinal spasms and diarrhea are possible. In rare cases, there is a galactorrhea, pain in the lower extremities and back, an increase in the level of prolactin. All symptoms disappear completely after the cessation of treatment.

[19], [20]

Overdose

Symptoms of overdose:

• Increased drowsiness
• Extrapyramidal disorders (impaired motor activity)
• Disorientation

As a treatment for side symptoms it is necessary to cancel the drug. Patients are prescribed absorption of absorbents (activated charcoal) and conduct symptomatic therapy. The active substances bind well to blood proteins, so dialysis is ineffective. There is no specific antidote.

[26], [27], [28], [29]

Interactions with other drugs

Interaction of Rabilil with other drugs is possible only on medical recommendations. Thus, anticholinergic drugs neutralize the antispecific effect of domperidone. The drug is not taken with antisecretory and antacid agents, as they reduce the bioavailability of domperidone.

With simultaneous oral administration of erythromycin and ketoconazole, pre-systemic domperidone metabolism is suppressed. Such CYP 3A4 inhibitors as: azole antifungal agents, macrolide antibiotics, HIV protease inhibitors and calcium antagonists are not used with domperidone.

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

[30], [31], [32], [33]

Storage conditions

The storage conditions of Rabilil are similar to the rules for storage of any other tablet preparations. The temperature should not exceed 30 ° C, the medicine should be stored in a dry place, protected from sunlight and inaccessible to children.

If the above recommendations are not observed, the medicament loses its properties and is prohibited for use. If the tablets have changed color or got a smell, they are also forbidden to use and must be disposed of.

[34], [35], [36],

Shelf life

Shelf life is 36 months from the date of production. At the expiration of the drug is prohibited to take and must be disposed of. Failure to comply with storage rules affects the suitability of the drug.

[37], [38]