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Active ingredients
Lansoprazole
Release form
Capsules
Composition
Lansoprazol 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; 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 dye (Ponzo 4R) - 0.0078 mg, water - 6.815 mg.; , propyl parahydroxybenzoate - 0.058 mg, methyl parahydroxybenzoate - 0.232 mg, titanium dioxide - 0.4393 mg, dye Crimson powder (Ponso 4R) - 0.0048 mg, water - 4.205 mg.
Pharmacological effect
Specific proton pump inhibitor (H + -K + -ATP-ase); metabolized in the parietal cells of the stomach to active sulfonamide derivatives, which inactivate H + -K + -ATP-azu. Blocks the final stage of secretion of hydrochloric acid, 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 the oxygenation of the gastric mucosa and increasing the secretion of bicarbonate; and 2-3 hours after taking 15 and 30 mg, respectively; inhibition of the production of hydrochloric acid when taken at a dose of 30 mg is 80-97%. Does not affect the motility of the digestive tract. Inhibitory effect increases in the first 4 days of admission. After the cessation of intake, the acidity for 39 hours remains below 50% of the basal level, and there is no "rebound" increase in secretion. Secretory activity is normalized 3-4 days after the end of the drug.; In patients with Zollinger-Ellison syndrome, it has a longer duration. It promotes the formation of specific IgA to Helicobacter pylori in the gastric mucosa, inhibiting their growth, increases the anti-helicobacter activity of other drugs. Increases the concentration of pepsinogen in the serum and inhibits the production of pepsin. Inhibition 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 gastric ulcer and duodenal ulcer resistant to histamine H2 receptor blockers.Provides more rapid healing of ulcers 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. once a day (30 mg) there is an increase in the pH of the gastric juice in the first hour after administration. Duration of action - more than 24 hours. No risk of an increase in gastric acidity after cessation of the use of lansoprazole was noted. 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
Absorption; Lansoprazole absorption begins as soon as the drug leaves the stomach. The absorption rate is high and Cmax in plasma is reached after 1.7 h, which is combined with a high degree of bioavailability of more than 80%. Food intake reduces absorption and bioavailability (by 50%), but the inhibitory effect on gastric secretion remains the same, regardless of the meal. Such pharmacokinetics of lansoprazole as Cmax and AUC are approximately proportional. If the drug is taken 30 minutes after a meal, both pharmacokinetic indicators are reduced by 50%. Food does not have any pronounced effect if the drug is taken before meals.; Distribution; Plasma protein binding - 97.7-99.4%. Lansoprazol penetrates well into tissues, incl. in the occipital cells of the stomach. Vd - 0.5 l / kg.; Metabolism; Lansoprazole is metabolized in the liver. In significant quantities, two metabolites are detected in plasma (sulfinyl hydroxylate and sulfon derivative), which are inactive. In the acidic environment of the tubules of the parietal cells, lansoprazol is transformed into 2 active substances that are not detectable in the systemic circulation.; Elimination; T1 / 2 lansoprazole is less than 2 hours, which does not affect the duration of suppression of gastric secretion. 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 liver cirrhosis, absorption may be delayed.; Renal failure for the rate and magnitude of elimination is not significantly affects. In patients with impaired renal function, protein binding can be reduced by 1–1.5%.
Indications
- peptic ulcer of the stomach and duodenum (in the acute phase); - erosive and ulcerative esophagitis; - reflux esophagitis; - Zollinger-Ellison syndrome; - stressful ulcers of the digestive tract; - nonulcer dyspepsia.
Contraindications
- Malignant neoplasm of the digestive tract; - I trimester of pregnancy; - lactation period; - Hypersensitivity to the components of the drug.; The drug should be prescribed with caution in case of liver failure, in II-III trimesters of pregnancy, elderly patients and patients under the age of 18 years.
Use during pregnancy and lactation
Group B. Adequate and well-controlled studies of the use of the drug during pregnancy have not been conducted.; It is contraindicated in the first trimester of pregnancy.; The drug should be prescribed with caution in the second and third trimesters of pregnancy.
Dosage and administration
Is ingested. The capsules should be swallowed without chewing. For duodenal ulcers and stressful ulcers, 30 mg / day for 1 dose, preferably in the morning, before meals for 2-4 weeks. For ulcers of the stomach and erosive and 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 adjusted individually until basal acid production is less than 10 mmol / h; For Helicobacter pylori eradication, 30 mg 2 times / day, in combination with antibiotics (clarithromycin and amoxicillin), for at least 7 days.; For non-ulcer dyspepsia: 15-30 mg / day for 2-4 weeks; For liver failure and in elderly patients begin treatment with half doses, gradually increasing them to the recommended, but not Over 30 mg / day.
Side effects
On the part of the digestive system: less often - increased or decreased appetite, nausea, abdominal pain; rarely diarrhea or constipation; in some cases - ulcerative colitis, gastrointestinal candidiasis, increased activity of hepatic transaminases (ALT, AST), GGT, alkaline phosphatase and LDH, hyperbilirubinemia. From the nervous system: headache; rarely - malaise, dizziness, drowsiness, depression, anxiety.; On the part of the respiratory system: rarely - cough, pharyngitis, rhinitis, an infection of the upper respiratory tract,flu-like syndrome. From the blood-forming organs: rarely - thrombocytopenia (with hemorrhagic manifestations); in some cases - anemia.; Allergic reactions: skin rash; in some cases - photosensitization, erythema multiforme exudative.; Other: rarely - myalgia, alopecia.
Overdose
Data on overdose of the drug at present is not available.
Interaction with other drugs
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%. belonging to the groups of weak acids, and accelerates the absorption of drugs belonging to the groups of bases. Interferes with the absorption of ketoconazole, ampicillin, iron salts, digoxin -40 min; Antacids should be prescribed 1 hour before or 1-2 hours after taking lansoprazole, as they slow down and reduce their absorption.
special instructions
Before and after treatment, endoscopic control is required to exclude a malignant neoplasm, since treatment can mask the symptoms and delay the correct diagnosis.