Lansoprazole

Brand Micro Labs Limited

In stock 1852 Items

Available since: 2019-09-19

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Clinical Pharmacology

Pharmaceutical group: a means of reducing the secretion of gastric glands - a proton pump inhibitor.
Pharmacological action: Lancid - specific inhibitor of the proton pump (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.
The rate and degree of inhibition of basal and stimulated secretion of hydrochloric acid are dose-dependent: the pH begins to increase after 1-2 hours and 2-3 hours after taking 15 and 30 mg, respectively; Inhibition of hydrochloric acid production when taken in a dose of 30 mg is 80-97%. Does not affect gastrointestinal motility. 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 is more prolonged. 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 faster 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 in 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 increases 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
The absorption of lansoprazole 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 is 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, lansoprazole is transformed into 2 active substances that are not detectable in the systemic circulation.
Removal
T1 / 2 lansoprazol is less than 2 hours, which does not affect the duration of the 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 situations
With liver cirrhosis, absorption may be delayed.
Renal failure does not significantly affect the rate and magnitude of elimination. 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.

Composition

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 body of the capsule: 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, dye brilliant blue - 0.0034 mg, dye quinoline yellow - 0.0042 mg, water - 4.36 water, 5.56 mg, water - 4.36 dye, dye blue diamond - 0.0034 mg;
The composition of the capsule cap: gelatin - 16.5084 mg, sodium lauryl sulfate - 0.016 mg, propyl parahydroxybenzoate - 0.04 mg, methyl parahydroxybenzoate - 0.16 mg, titanium dioxide - 0.3705 mg, dye brilliant blue - 0.0022 mg, dye quinoline yellow - 0.0028 mg, water - 2), dye brilliant blue - 0.0022 mg, dye quinoline yellow - 0.0028 mg, water - 2), dye blue diamond - 0.0022 mg, dye quinoline yellow - 0.0028 mg, water - 2)

Lansoprazole is marketed under different brands and generic names, and comes in different dosage forms:

Brand name	Manufacturer	Country	Dosage form
Lancid®	Micro Labs Limited	India	capsules
Epicurus	Obolensky OP	Russia	capsules

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Dosage and Administration

For oral use. Lancid capsules should be swallowed without chewing.
With duodenal ulcer and stress ulcers - 30 mg / day. 1 dose, preferably in the morning, before meals for 2-4 weeks.
In case of gastric ulcer and erosive and ulcerative esophagitis, 30 mg / day. within 4-8 weeks; if necessary - 60 mg / day.
With reflux esophagitis - 30 mg / day. within 4 weeks.
With Zollinger-Ellison syndrome, the dose of Lancid is adjusted individually, until the basal acid production is less than 10 mmol / h.
For eradication of Helicobacter pylori - 30 mg 2 times / day, in combination with antibiotics (clarithromycin and amoxicillin), for at least 7 days.
When non-ulcer dyspepsia: 15-30 mg / day. within 2-4 weeks.
With liver failure and in elderly patients, treatment begins with half the dose of Lancid, gradually increasing them to the recommended, but not more than 30 mg / day.

Adverse reactions

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, gastrointestinal candidiasis, increased activity of hepatic transaminases (ALT, AST), GGT, ALP and LDH, hyperbilirubinemia.
On the part 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.
From the side of 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.

Contraindications

- Malignant neoplasm of the digestive tract;
- I trimester of pregnancy;
- lactation period;
- Hypersensitivity to the components of the drug Lancid.
Precautions should be prescribed the drug for liver failure, in the II-III trimesters of pregnancy, elderly patients and patients under the age of 18 years.

Drug interactions

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 theophylline clearance by 10%.
Lansoprazole with simultaneous use slows down the pH-dependent absorption of drugs 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.
Lansoprazol is compatible with ibuprofen, indomethacin, diazepam, propranolol, warfarin, oral contraceptives, phenytoin, prednisolone.
Sucralfate reduces the bioavailability of lansoprazole by 30%, therefore it is necessary to observe the interval between taking the medication 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.

Special instructions

Endoscopic control is required before and after treatment to exclude a malignant neoplasm, since treatment may mask the symptoms and delay the correct diagnosis.