Antiulcer agent. A specific primobolan results inhibitor of proton pump metabolised in the gastric parietal cells to active sulfonamide derivatives that inactivate the sulfhydryl groups. Blocks the synthesis final stage of hydrochloric acid to decrease both basal and stimulated secretion regardless of the nature of the stimulus. Inhibition of production of hydrochloric acid at a dose of 30 mg – 80-97%. No effect on the motility of the gastrointestinal tract. The inhibitory effect of increases in the first four days of admission. After discontinuation of acidity for 39 hours is less than 50% of basal level, “rebound” increase the secretion is not marked. The secretory activity is restored in 3-4 days after ingestion. In patients with Zollinger-Ellison syndrome acts more lasting.
Absorption – high (eating reduces the absorption and bioavailability, but the inhibitory effect on gastric secretion remains the same, regardless of the meal). Occurrence of a maximum concentration (Cmax) after oral administration of 30 mg – 1.5-2.2 hours C max -0,75-1,15 mg / l. Relationship to plasma proteins – 97,799,4%. Extensively metabolized during the initial passage through the liver. Half-life of 1.3-1.7 h excretion by the kidneys (in the form of metabolites.) – 14-23%, and through the intestines. In hepatic insufficiency and in the elderly is slowing down.
- Gastric ulcer and duodenal ulcer.
- Reflux esophagitis, erosive and ulcerative esophagitis.
- Erosive-ulcerative lesions of gastric and duodenal ulcers associated with nonsteroidal anti-inflammatory drugs (NSAIDs), stress ulcers.
- Erosive-ulcerative lesions of gastric and duodenal ulcers associated with Helicobacter pylori (in the complex therapy).
- Ellison – Syndrome Zollinger.Contraindications : Hypersensitivity to the drug, gastrointestinal malignant tumors, pregnancy (I trimester), lactation, age 18 years.
liver and / or kidney failure, pregnancy (II-III trimester), advanced age.
Dosing and Administration
Inside. The capsules should be swallowed whole without chewing. Duodenal ulcer in the acute phase of the disease – by 30 mg daily for 2-4 weeks (in resistant cases up to 60 mg per day). Peptic ulcer exacerbation and erosive and ulcerative esophagitis – on 30 -. 60 mg daily for 4 weeks, -8 Erosive and ulcerative lesions of the gastrointestinal tract caused by NSAID – 30 mg daily for 4-8 weeks. Eradication primobolan results of Helicobacter pylori – on 30 mg 2 times a day for 10 14 days in combination with antibacterial agents. anti-treatment of gastric ulcer and 12 duodenal ulcer -. at 3O mg per day of anti-treatment of reflux esophagitis – 30 mg per day for a long time (up to 6 months). Zollinger-Ellison syndrome – the dose is adjusted individually to achieve the level of basal secretion less than 10 mmol / h.
Side effect From the digestive system: the increase or decrease of appetite, nausea, stomach pain; rarely – diarrhea or constipation; in some cases – ulcerative colitis, candidiasis gastrointestinal, increased activity of “liver” enzymes, increased bilirubin in the blood. From the nervous system: headache; rarely – discomfort, dizziness, drowsiness, depression, anxiety. Respiratory system: rare cough, pharyngitis, rhinitis, upper respiratory tract infection, flu-like symptoms. From the side of hematopoiesis: rarely – thrombocytopenia (with hemorrhagic manifestations); in some cases – anemia. Allergic reactions: skin rash; in some cases – photosensitivity, erythema multiforme. Other: rarely – myalgia, alopecia.
Before treatment to rule out malignancy in the upper gastrointestinal tract, ie. To. The drug can “mask” symptoms and complicate diagnosis.
Interaction with other drugs
Slows elimination of drugs metabolized in the liver by microsomal oxidation (in Vol. H. Of diazepam, phenytoin, anticoagulants). Reduces 10% of theophylline clearance.
Changes of pH-dependent absorption of drugs belonging to the group of weak acids (slowing) and foundations (acceleration).
Sucralfate reduces the bioavailability of lansoprazole by 30% (observe the interval between administration of these preparations 30-40 minutes)
Antacids slow down and reduce primobolan results the absorption of lansoprazole (they should be administered for 1 hour or 1-2 hours after receiving lansoprazole).