Hyrabezol, 20 mg 30 pcs.

A gastric gland secretion reducing agent – proton pump inhibitor.

Pharmacodynamics

. An antiulcer agent from the group of proton pump inhibitors (H+/K+-ATPase), metabolized in the parietal cells of the stomach to active sulfonamide derivatives, which inactivate the sulfhydryl groups of H+/K+-ATPase.

Blocks the final stage of hydrochloric acid secretion, reducing basal and stimulated secretion, regardless of the nature of the stimulus.

It has high lipophilicity, easily penetrates into the parietal cells of the stomach and concentrates in them with cytoprotective effect.

The antisecretory effect after oral administration of 20 mg occurs within 1 hour and reaches its maximum after 2-4 hours; inhibition of basal and food stimulated acid secretion after 23 hours after the first dose is 62% and 82%, respectively; duration of action is 48 hours. After the end of the intake, secretory activity normalizes within 2-3 days.

In the first 2-8 weeks of therapy, serum gastrin concentration increases and returns to baseline levels within 1-2 weeks after discontinuation of the drug. It does not affect the central nervous system, cardiovascular and respiratory systems.

Pharmacokinetics

Absorption occurs in the small intestine (due to the presence of acid-resistant enteric coating) is high, time to reach maximum concentration – 3.5 hours. Values of maximum concentration (Cmax) and area under the curve “concentration of active substance – time” (AUC) are linear in the dose range from 10 to 40 mg. Metabolized in the liver with the participation of cytochrome P-450 CYP2C19 and CYP3A4 isoenzymes. Bioavailability is 52% and does not increase with repeated administration. Period of semi-elimination (T1/2) – 0.7-1.5 hour, clearance – 283 ± 98 ml/min.

In patients with chronic hepatic insufficiency of mild or moderate degree after a single use AUC is increased by 2 times, T1/2 – 2-3 times. After rabeprazole administration during 7 days the AUC is increased 1.5 times, T1/2 – 1.2 times.

In patients with stable terminal renal failure requiring hemodialysis (creatinine clearance less than 5 ml/min/1.73 m2) the distribution of rabeprazole sodium is close to that of healthy persons.

In elderly patients after rabeprazole administration for 7 days the AUC is 2 times higher, Cmax is 60% higher than in young patients.
Binding to plasma proteins is 97%.

Excreted by the kidneys – 90% as two metabolites: mercapturic acid conjugate (M5) and carbolic acid (M6); by the intestine – 10%. In patients with delayed CYP2C19 metabolism after 7 days of taking rabeprazole at the dose of 20 mg per day AUC is increased 1.9 times and half-life 1.6 times as compared with the same parameters in “fast metabolizers”, while Cmax is increased by 40%.

Indications

Active ingredient

Interaction

Directions for use

Special Instructions

Contraindications

Side effects

Overdose

Pregnancy use

Similarities