Description of the active substance:
This information is a reference and it is not enough that the drug has been prescribed by a doctor ..
PHARMACHOLOGIC EFFECT
Antiulcer, H + -K + -ATPase inhibitor (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.
PHARMACOKINETICS
After oral intake absorbed from the digestive tract. At a dose of 20 mg C max is achieved after 3.5 hours. Changes in C max and AUC are linear in the dose range of 10 to 40 mg. Absolute bioavailability is about 52% due to the effect of "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 exposed to the effect of "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.
In healthy volunteers, T 1/2 is about 1 hour, the total clearance is about 283. About 90% is excreted in the urine mainly in the form of two metabolites: a mercaptopuric acid conjugate and a carboxylic acid. In toxicological studies, 2 unidentified metabolites were found in laboratory animals. The rest is excreted with feces.
In patients with stable terminal stage of chronic renal failure requiring hemodialysis (CK less than 5 ml / min / 1.73 m 2 ), AUC and C max were 35% lower than in healthy volunteers. On average, T 1/2 rabeprazole was 0.82 h in healthy volunteers, 0.95 h in patients during hemodialysis and 3.6 h after hemodialysis. In kidney diseases, the clearance of rabeprazole in patients on hemodialysis was approximately 2 times higher than in healthy volunteers.
In patients with chronic hepatic insufficiency of mild or moderate degree after a single dose of rabeprazole, an increase in C max , T 1/2 , AUC was observed.
In the case of delayed metabolism of CYP2C19 after taking rabeprazole 20 mg / day for 7 days, AUC and T 1/2 were 1.9 and 1.6, respectively, with extensive metabolism, while C max increased by only 40%.
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.
DOSING MODE
Is taken internally. Single dose - 10-20 mg. Frequency and duration of use depend on the indications and treatment regimen.
SIDE EFFECT
From the digestive system: diarrhea, nausea, abdominal pain, vomiting, flatulence, constipation; rarely - dry mouth, dyspepsia, belching; in isolated cases - anorexia, gastritis, stomatitis, increased activity of hepatic transaminases.
From the central nervous system and peripheral nervous system: headache, asthenia, dizziness, insomnia; rarely - nervousness, drowsiness; in isolated cases - depression, visual impairment and taste sensations.
From the respiratory system: possible - rhinitis, pharyngitis, cough; rarely - sinusitis, bronchitis.
Allergic reactions: rarely - skin rash; in isolated cases - itching.
Other: back pain, flu-like syndrome; rarely - myalgia, chest pain, chills, calf muscle cramps, urinary tract infection, arthralgia, fever; in isolated cases - an increase in body weight, increased sweating, leukocytosis.
CONTRAINDICATIONS
Pregnancy, lactation (breastfeeding), hypersensitivity to rabeprazole sodium or substituted benzimidazoles.
PREGNANCY AND LACTATION
Rabeprazole is contraindicated in pregnancy and lactation.
In experimental studies it was found that rabeprazole penetrates insignificantly through the placental barrier, but there were no violations of fertility or fetal development defects; is excreted with the milk of lactating rats.
Clinical experience of using rabeprazole in children is not available, therefore, the use is not recommended.
APPLICATION FOR FUNCTIONS OF THE LIVER
Patients with impaired renal function are not required to adjust the dose.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Patients with impaired liver function are not required to adjust the dose, however, in patients with severe liver function abnormalities, rabeprazole is recommended for use with caution.
SPECIAL INSTRUCTIONS
Before the beginning of therapy it is necessary to exclude malignant neoplasms of the stomach, tk. The use of rabeprazole can mask symptoms and delay proper diagnosis.
Patients with hepatic or renal dysfunction are not required to adjust the dose, however, in patients with severe hepatic impairment, it is recommended that rabeprazole be used with caution.
When used simultaneously with rabeprazole, the dosages of ketoconazole and digoxin should be adjusted.
In experimental studies , carcinogenic effects of rabeprazole have not been established, however, in the study of mutagenicity, ambiguous results were obtained. Tests on lymphoma cells in mice were positive, with a micronuclear in vivo test and a DNA restoration test in vivo and in vitro negative.
DRUG INTERACTION
With simultaneous use with digoxin, an increase (from small to moderate) of digoxin concentration in the blood plasma is possible.
With simultaneous application with ketoconazole, its bioavailability decreases.
