Composition, form of production and packaging
Capsules hard gelatinous, size 3, turquoise (bluish-green) color, with a MICRO / MICRO imprint; the contents of the capsules are pellets of white or almost white color.
1 caps.
lansoprazole 15 mg
Excipients: mannitol - 129.7 mg, lactose monohydrate - 13 mg, sucrose - 16.6 mg, povidone - 3.5 mg, hypromellose phthalate - 18.2 mg, cetyl alcohol - 2 mg.
The composition of the capsule body: gelatin - 24.7626 mg, sodium lauryl sulfate - 0.024 mg, propyl parahydroxybenzoate 0.24 mg, methyl parahydroxybenzoate 0.06 mg, titanium dioxide 0.5557 mg, brilliant blue dye 0.0034 mg, quinoline yellow 0.0042 mg, water 4.35 mg.
The capsule capsule composition: gelatine - 16.5084 mg, sodium lauryl sulfate 0.016 mg, propyl parahydroxybenzoate 0.04 mg, methyl parahydroxybenzoate 0.16 mg, titanium dioxide 0.3705 mg, brilliant blue colorant 0.0022 mg, quinoline yellow color 0.0028 mg, water 2.9 mg.
10 pieces. - blisters (3) - packs of cardboard.
Hard gelatin capsules, size 1, pink, with MICRO / MICRO imprint; the contents of the capsules are pellets of white or almost white color.
1 caps.
lansoprazole 30 mg
Excipients: mannitol - 189 mg, lactose monohydrate - 26 mg, sucrose - 52 mg, povidone - 14.9 mg, hypromellose phthalate - 34.3 mg, cetyl alcohol 3.8 mg.
The composition of the capsule body: gelatin 38.9575 mg, sodium lauryl sulfate 0.0376, propyl parahydroxybenzoate 0.376 mg, methyl parahydroxybenzoate 0.094 mg, titanium dioxide 0.712 mg, crimson (Ponso 4R) 0.0078 mg, water 6.815 mg.
The capsule capsule composition: gelatin - 24.0376 mg, sodium lauryl sulfate - 0.0232 mg, propyl parahydroxybenzoate 0.058 mg, methylparahydroxybenzoate 0.232 mg, titanium dioxide 0.4393 mg, crimson (Ponso 4R) 0.0048 mg, water 4.205 mg.
10 pieces. - blisters (3) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2012.
PHARMACHOLOGIC EFFECT
Specific proton pump inhibitor (H + -K + -ATPase); is metabolized in parietal cells of the stomach to active sulfonamide derivatives that inactivate H + -K + -ATPase. It blocks the final stage of hydrochloric acid secretion, reducing basal and stimulated secretion, regardless of the nature of the stimulus. Possessing high lipophilicity, it easily penetrates into the parietal cells of the stomach, concentrates in them and has a cytoprotective effect, increasing oxygenation of the gastric mucosa and increasing the secretion of bicarbonate.
The rate and extent of inhibition of basal and stimulated hydrochloric acid secretion are dose-dependent: the pH begins to increase after 1-2 hours and 2-3 hours after administration of 15 and 30 mg, respectively; inhibition of production of hydrochloric acid at a dose of 30 mg is 80-97%. Does not affect the motility of the gastrointestinal tract. Inhibitory effect increases in the first 4 days of admission. After stopping the intake, the acidity for 39 hours remains below 50% basal level, the "ricochet" increase in secretion is not noted. Secretory activity is normalized 3-4 days after the end of the drug intake.
In patients with Zollinger-Ellison syndrome, it is more prolonged. It promotes the formation in the gastric mucosa of specific IgA to Helicobacter pylori, suppressing their growth, increases the anti-Helicobacter pylori activity of other drugs. Increases the concentration of pepsinogen in the blood serum and inhibits the production of pepsin. Oppression of secretion is accompanied by an increase in the number of nitrosobacteria and an increase in the concentration of nitrates in the gastric secretion.Effective in the treatment of peptic ulcer of the stomach and duodenum, resistant to blockers of histamine H 2 -receptors. Provides faster healing of ulcerative defects in the duodenum (85% of duodenal ulcers heal after 4 weeks of treatment at a dose of 30 mg / day).
After the first dose of lansoprazole at a dose of 30 mg, the pH of the gastric juice increases after 1-2 hours. When taking the drug several times a day (30 mg each), the pH of the gastric juice is increased in the first hour after administration. The duration of action is more than 24 hours. There was no risk of increased gastric acidity after discontinuation of lansoprazole. Restoration of the level of secretion of hydrochloric acid to normal occurs gradually in the period from 2 to 4 days after taking several doses of the drug.
PHARMACOKINETICS
Suction
Absorption of lansoprazole begins as soon as the drug leaves the stomach. The rate of absorption is high and C max in plasma is achieved in 1.7 h, which is combined with a high degree of bioavailability of more than 80%. Eating lowers absorption and bioavailability (by 50%), but the inhibitory effect on gastric secretion remains the same, regardless of food intake. Such indicators of the pharmacokinetics of lansoprazole as Cmax and AUC are approximately proportional. If the drug is taken 30 minutes after eating, both pharmacokinetic indicators are reduced by 50%. Food does not have any significant effect if the drug is taken before meals.
Distribution
Binding to plasma proteins - 97.7-99.4%. Lansoprazole penetrates well into tissues, incl. in the lining of the stomach. V d - 0.5 l / kg.
Metabolism
Lansoprazole is metabolized in the liver. In significant amounts in the plasma, two metabolites (sulfinyl hydroxide and sulfone derivative) are found which are inactive. In the acidic environment of the tubules of parietal cells, lansoprazole is transformed into 2 active substances not detectable in the systemic bloodstream.
Excretion
T 1/2 of lansoprazole is less than 2 hours, which does not affect the duration of suppression of gastric secretion. It is excreted from the body in the form of lansoprazole sulfone and hydroxylansoprazole with bile (2/3), with urine - 14-23%.
Pharmacokinetics in special clinical cases
With cirrhosis of the liver, absorption may be delayed.
Renal insufficiency does not significantly affect the rate and amount of excretion. In patients with impaired renal function, binding to proteins can be reduced by 1-1.5%.
INDICATIONS
- Stomach ulcer and duodenal ulcer (in the phase of exacerbation);
- erosive-ulcerative esophagitis;
- reflux esophagitis;
- Zollinger-Ellison syndrome;
- Stress ulcers of the gastrointestinal tract;
- non-ulcer dyspepsia.
DOSING MODE
Is taken internally. Capsules should be swallowed without chewing.
With duodenal ulcer and stress ulcers - 30 mg / day for 1 reception, preferably in the morning, before eating for 2-4 weeks.
With gastric ulcer and erosive-ulcerative esophagitis - 30 mg / day for 4-8 weeks; if necessary, 60 mg / day.
With reflux esophagitis - 30 mg / day for 4 weeks.
With Zollinger-Ellison syndrome, the dose is selected individually, until basal acid production is less than 10 mmol / h.
To eradicate Helicobacter pylori - 30 mg 2 times / day, in combination with antibiotics (clarithromycin and amoxicillin), for at least 7 days.
With non-ulcer dyspepsia: 15-30 mg / day for 2-4 weeks.
With liver failure and in elderly patients, treatment starts with half the doses, gradually increasing them to the recommended, but not more than 30 mg / day.
SIDE EFFECT
On the part of the digestive system: less often - increased or decreased appetite, nausea, abdominal pain; rarely diarrhea or constipation; in some cases - nonspecific ulcerative colitis, candidiasis of the gastrointestinal tract, increase activity of hepatic transaminases (ALT, AST), GGT, APF and LDH, hyperbilirubinemia.
From the side of the nervous system: headache; rarely - malaise, dizziness, drowsiness, depression, anxiety.
On the part of the respiratory system: rarely - cough, pharyngitis, rhinitis, upper respiratory tract infection, flu-like syndrome.
On the part of the organs of hematopoiesis: rarely - thrombocytopenia (with hemorrhagic manifestations); in some cases - anemia.
Allergic reactions: skin rash; in some cases - photosensitivity, multiforme exudative erythema.
Other: rarely - myalgia, alopecia.
CONTRAINDICATIONS
- malignant neoplasms of the gastrointestinal tract;
- I trimester of pregnancy;
- lactation period;
- Hypersensitivity to the components of the drug.
With caution should prescribe the drug for liver failure, in the II-III trimesters of pregnancy, elderly patients and patients under the age of 18 years.
PREGNANCY AND LACTATION
Group B. Adequate and controlled studies of the use of the drug in pregnancy have not been conducted.
Contraindicated in the first trimester of pregnancy.
With caution should prescribe the drug in the II-III trimesters of pregnancy.
The use of the drug during lactation is contraindicated.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
With liver failure, treatment starts with half the doses, gradually increasing them to the recommended, but not more than 30 mg / day.
APPLICATION FOR CHILDREN
Caution should be given to patients under the age of 18 years.
APPLICATION IN ELDERLY PATIENTS
Caution should be given to elderly patients.
In elderly patients, treatment starts with half doses, gradually increasing them to the recommended, but not more than 30 mg / day.
SPECIAL INSTRUCTIONS
Before and after treatment, endoscopic control is necessary to exclude malignant neoplasm, because treatment can mask the symptoms and delay correct diagnosis.
OVERDOSE
There are no data on the drug overdose at the present time.
DRUG INTERACTION
With the simultaneous use of lansoprazole slows down the elimination of drugs metabolized in the liver by microsomal oxidation (including diazepam, phenytoin, indirect anticoagulants).
Lansoprazole reduces the clearance of theophylline by 10%.
Lansoprazole, when used concomitantly, slows down the pH-dependent absorption of drugs belonging to weak acid groups and accelerates the absorption of drugs belonging to the groups of bases. Prevents the absorption of ketoconazole, ampicillin, iron salts, digoxin.
Lansoprazole is compatible with ibuprofen, indomethacin, diazepam, propranolol, warfarin, oral contraceptives, phenytoin, prednisolone.
Sucralfate reduces the bioavailability of lansoprazole by 30%, so it is necessary to observe the interval between taking medicines 30-40 minutes.
Antacids should be prescribed 1 hour before or 1-2 hours after taking lansoprazole, as they slow down and reduce their absorption.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored in a dry, protected from light, out of reach of children at a temperature of no higher than 25 В° C. Shelf life - 3 years.
