Rabeprazole - instructions for use, dose, side effects, contraindications

Antiulcer. Is a prodrug - in the acidic environment of parietal cells it is converted into an active sulfenamide form interacting with cysteine H+-K+-ATPase (proton pump). The mechanism of action is associated with inhibition of the enzyme H + -K + -ATPase in parietal cells of the stomach, which leads to blocking the final stage of the formation of hydrochloric acid. This action is dose-dependent and leads to inhibition of both basal and stimulated secretion of hydrochloric acid regardless of the nature of the stimulus.

Has anti-Helicobacter activity: minimum inhibitory concentration (MIC) 4-16 μg / ml. Accelerates the manifestation of anti-Helicobacter pylori activity of a number of antibiotics.

Pharmacokinetics:

After oral intake absorbed from the digestive tract. At a dose of 20 mg, the maximum concentration is achieved after 3.5 hours. Changes in the maximum concentration and AUC are linear in the dose range of 10 to 40 mg. Absolute bioavailability is about 52% due to the effect of the first passage through the liver. Bioavailability of rabeprazole does not increase with multiple admission.

The intake of food and time of reception during the day does not affect the absorption of rabeprazole.

Binding to plasma proteins is 97%.

Rabeprazole sodium is subjected to the effect of the first passage. Metabolized in the liver with the participation of isoenzymes of the CYP system.

The main metabolites (thioester and carboxylic acid) and minor metabolites (sulfone, dimethyl thioester and mercaptopuric acid conjugate) are present in low concentrations.

Approximately 90% is excreted in the urine mainly in the form of two metabolites: a conjugate of mercaptopuric acid and a carboxylic acid.

In elderly patients the excretion of rabeprazole is somewhat slowed down.

Indications:Stomach ulcer and duodenal ulcer in the phase of exacerbation; peptic ulcer of the stomach and duodenum, associated with Helicobacter pylori (in combination with antibiotics); gastroesophageal reflux. FROMConditions characterized by pathological hypersecretion, including the Zollinger-Ellison syndrome. Treatment and prevention of recurrent ulcers in patients with peptic ulcer associated with Helicobacter pylori.

ICD-10

XI.K20-K31.K21.0 Gastroesophageal reflux with esophagitis

XI.K20-K31.K21 Gastroesophageal reflux

XI.K20-K31.K25 Stomach ulcer

XI.K20-K31.K26 Duodenal ulcer

XI.K20-K31.K28 Gastroejunal ulcer

Contraindications:Hypersensitivityincluding substituted benzimidazoles, pregnancy, breast-feeding.

Carefully:Childhood age, severe renal failure, tsevere hepatic impairment.

Pregnancy and lactation:

Rabeprazole should not be given to pregnant women (there is no safety data for the use of rabeprazole during pregnancy).

Action category for the fetus by FDA - C.

For the duration of treatment, breastfeeding should be discontinued. It is not known whether rabeprazole with breast milk; corresponding studies in lactating women were not conducted.

Dosing and Administration:Inside in the morning before meals, without chewing or grinding, 20 mg once a day; with peptic ulcer and duodenal ulcerat the stage of exacerbation - within 4-6 weeks, if necessary - up to 12 weeks; with reflux esophagitise - 4-8 weeks, later maintenance therapy is possible: 10-20 mg once a day; with Zollinger-Ellis syndromeshe selects a dose individually. With H. pylori infection as part of eradication therapy with the appropriate combinations of antibiotics for 7 days.

Side effects:

From the side organs of the digestive tract: diarrhea, nausea, vomiting, abdominal pain, constipation, flatulence, increased activity of hepatic transaminases, dryness of the oral mucosa; rarely - a decrease in appetite, stomatitis.

From the side nervous system and sense organs: headache, dizziness, drowsiness, asthenia; rarely - depression, visual impairment or taste sensations.

From the side cardiovascular system and blood (hematopoiesis, hemostasis): thrombocytopenia, and leukopenia.

From the side musculoskeletal system: myalgia, calf muscle cramps, arthralgia.

From the side respiratory system: pharyngitis, rhinitis; rarely - cough, sinusitis.

Allergic reactions: skin rash.

Other: back pain, flu-like syndrome, fever; rarely - weight gain, excessive sweating

Overdose:

Symptoms: not described.

Treatment: Supportive and symptomatic therapy is recommended for suspected overdose. The specific antidote is unknown. Dialysis is ineffective (rabeprazole binds well to plasma proteins).

Interaction:

Digoxin. Against the background of rabeprazole, the concentration of digoxin in the blood increases (with combined use, a dose adjustment of digoxin is necessary).

Itraconazole. Reduces plasma concentration.

Ketoconazole. Against the background of rabeprazole, the concentration of ketoconazole in the blood decreases (in case of combined use, a dose adjustment of ketoconazole is necessary).

Clarithromycin increases (mutually) the concentration in the blood and the effect rabeprazole.

Rilpivirin. Do not use rilpivirine in combination with rabeprazole, since this can lead to a significant decrease in rilpivirin level in the blood plasma (increase in the pH level) and in turn cause a loss of therapeutic effect of rilpivirin.

Special instructions:

Before the start of treatment, it is necessary to exclude the malignant neoplasm of the stomach (symptomatic improvement against the background of treatment with rabeprazole may make it difficult to timely diagnose). It is advisable to use caution in the first appointment of rabeprazole to patients with severe impairment of liver function. Patients concomitantly receiving rabeprazole ketoconazole or digoxin, require additional monitoring (may require adjustment of the dose of these drugs).

Impact on the ability to drive vehicles and manage mechanisms

In case of occurrence of drowsiness it is necessary to refuse driving of the car and other kinds of the activity demanding the raised concentration of attention.

Instructions

Rabeprazole (Rabeprazolum)