Hyrabezol, 10 mg 15 pcs

Pharmgroup:

A gastric gland secretion reducing agent – proton pump inhibitor.

Pharmic action:

Hairabezol is an anti-ulcer drug from the group of proton pump inhibitors (H+/K+-ATPase) and is metabolized in gastric parietal cells 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 is 62% and 82% respectively 23 hours after the first dose; 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 CNS, cardiovascular and respiratory systems.

Pharmacokinetics:

Absorption and distribution

Absorbed from the small intestine (due to the presence of acid-resistant enteric coating). Absorption is high, time to reach Cmax – 3.5 h. Values of Cmax and AUC are linear in the dose range from 10 to 40 mg. Bioavailability is 52%, it does not increase with multiple administration.

The binding to plasma proteins is 97%.

Metabolism and excretion

Metabolized in liver with participation of cytochrome Р450 isoenzymes (CYP 2C19 and CYP 3A4).

T1/2 – 0.7-1.5 h, clearance – 283 ± 98 ml/min. Excreted by the kidneys – 90% as two metabolites: mercapturic acid conjugate (M5) and carboxylic acid (M6); by the intestines – 10%.

Pharmacokinetics in special clinical cases

In patients with mild to moderate chronic hepatic impairment after a single dose the AUC increases 2-fold, T1/2 – 2-3 times. After administration of 20 mg of rabeprazole during 7 days AUC is increased 1.5 times, T1/2 – 1.2 times. In patients with stable terminal renal failure requiring hemodialysis (CK less than 5 ml/min/1.73 m2), distribution of rabeprazole sodium is close to that in healthy subjects.

In elderly patients after administration of rabeprazole for 7 days the AUC is 2 times higher, Cmax is 60% higher than in young patients.
In patients with delayed CYP2C19 metabolism after 7 days of taking rabeprazole at the dose of 20 mg per day the AUC is 1.9 times higher and T1/2 is 1.6 times higher compared to the same parameters in “fast metabolizers”, while Cmax is increased by 40%.

Indications

peptic ulcer of the stomach and duodenum in the acute stage;
gastroesophageal reflux disease;
hypersecretory conditions, including Zollinger-Ellison syndrome;
stress ulcers of the gastrointestinal tract.
As part of complex therapy:
eradication of Helicobacter pylori in patients with gastric and duodenal ulcers or chronic gastritis;
treatment and prevention of relapse of peptic ulcer associated with Helicobacter pylori.

Pharmacological effect

Pharmaceutical group:

a drug that reduces the secretion of gastric glands – a proton pump inhibitor.

Pharmaceutical action:

Khairabezol is an antiulcer drug from the group of proton pump inhibitors (H+/K+-ATPase), metabolized in the parietal cells of the stomach to active sulfonamide derivatives that inactivate the sulfhydryl groups of H+/K+-ATPase.
Blocks the final stage of hydrochloric acid secretion, reducing the content of basal and stimulated secretion, regardless of the nature of the stimulus.

It is highly lipophilic, easily penetrates into the parietal cells of the stomach and concentrates in them, exerting a cytoprotective effect.

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

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

Pharmacokinetics:

Suction and distribution

Absorbed from the small intestine (due to the presence of an acid-resistant enteric coating). Absorption is high, time to reach Cmax is 3.5 hours. Cmax and AUC values ​​are linear in the dose range from 10 to 40 mg. Bioavailability – 52%, does not increase with repeated doses.

Communication with plasma proteins – 97%.

Metabolism and excretion

Metabolized in the liver with the participation of cytochrome P450 isoenzymes (CYP 2C19 and CYP 3A4).

T1/2 – 0.7-1.5 hours, clearance – 283 ± 98 ml/min. Excreted by the kidneys – 90% in the form of two metabolites: a conjugate of mercapturic acid (M5) and carboxylic acid (M6); intestines – 10%.

Pharmacokinetics in special clinical situations

In patients with mild or moderate chronic liver failure, after a single dose, AUC increases by 2 times, T1/2 by 2-3 times. After taking 20 mg of rabeprazole for 7 days, AUC increases by 1.5 times, T1/2 – by 1.2 times. In patients with stable end-stage renal failure requiring hemodialysis (creatinine clearance less than 5 ml/min/1.73 m2), the distribution of rabeprazole sodium is close to that in healthy individuals.

In elderly patients, after taking rabeprazole for 7 days, AUC is 2 times greater, Cmax is 60% greater than in young patients.
In patients with slow metabolism of CYP2C19, after 7 days of taking rabeprazole at a dose of 20 mg per day, AUC increases by 1.9 times and T1/2 by 1.6 times compared with the same parameters in “rapid metabolizers,” while Cmax increases by 40%.

Special instructions

The patient’s response to rabeprazole therapy does not exclude the presence of malignant neoplasms in the stomach. Khairabezol tablets should not be chewed or crushed. The tablets should be swallowed whole. It has been established that neither time of day nor food intake affects the activity of rabeprazole.

In a special study in patients with mild or moderate hepatic impairment, the incidence of side effects of rabeprazole was not found to be significantly different from that in age- and sex-matched healthy individuals, but despite this, caution is recommended when first prescribing rabeprazole to patients with severe hepatic impairment.

In patients with impaired renal or hepatic function, no dosage adjustment of Khairabezol is required. The AUC of rabeprazole in patients with severe hepatic impairment is approximately 2 times higher than in healthy patients.

Hypomagnesemia. When treated with proton pump inhibitors for at least 3 months, cases of symptomatic or asymptomatic hypomagnesemia have been reported in rare cases. In most cases, these reports were received one year after therapy. Serious adverse events included tetany, arrhythmia, and seizures. Most patients required treatment for hypomagnesemia, including magnesium replacement and discontinuation of proton pump inhibitor therapy. In patients who will be receiving long-term treatment or who are taking proton pump inhibitors with drugs such as digoxin or drugs that can cause hypomagnesemia (eg, diuretics), healthcare providers should monitor magnesium levels before starting treatment with proton pump inhibitors and during treatment.

Fractures. Observational studies suggest that treatment with proton pump inhibitors may increase the risk of osteoporosis-related fractures of the hip, wrist, and spine. The risk of fractures was increased in patients taking high doses of proton pump inhibitors for a year or more.

Active ingredient

Rabeprazole

Composition

1 tablet contains:

Active substance:

rabeprazole sodium 10 mg;

Excipients:

magnesium oxide;

mannitol;

corn starch;

povidone K30;

low-substituted hyprolose;

sodium stearyl fumarate;

Enteric coating:

cellacephate; titanium dioxide; red iron oxide dye.

Pregnancy

Rabeprazole should not be prescribed to pregnant women (there are no data on the safety of rabeprazole during pregnancy).

Breastfeeding should be stopped during treatment.

It is not known whether rabeprazole is excreted in breast milk.

Appropriate studies have not been conducted in lactating women.

Contraindications

pregnancy;
breast-feeding;
children and adolescents up to 18 years of age;
hypersensitivity to rabeprazole, benzimidazoles or other components of the drug.

The drug should be prescribed with caution in cases of severe liver failure and severe renal failure.

Side Effects

abdominal pain, nausea, loose stools or constipation
headache, dizziness
runny nose, cough
decrease in the number of leukocytes, blood platelets
allergic reactions.

Interaction

The drug Khairabezol does not interact with liquid antacids.

If drowsiness occurs, you should avoid driving and other activities that require increased concentration.

When taken together, the drug Khairabezol reduces the effect.

Overdose

Symptoms: There is minimal evidence of intentional or accidental overdose. There have been no cases of severe overdose of rabeprazole.

Treatment: A specific antidote for rabeprazole is unknown. Rabeprazole binds well to plasma proteins and is therefore poorly excreted during dialysis. In case of overdose, symptomatic and supportive treatment should be provided.

Storage conditions

In a dry place, protected from light, at a temperature of 8–25 °C

Shelf life

2 years

Manufacturer

Highglans Laboratories Pvt. Ltd, India