Dosage form:
Hard gelatin capsules No. 2. The capsule cap is opaque yellow, the body is opaque white. The contents of the capsules - white or almost white pellets
Structure:
Each capsule contains an omeprazole pallet - 235.00 mg in terms of 20.00 mg of omeprazole. Pellet composition: Active substance: omeprazole - 19.975 mg; Excipients: mannitop - 39.95 mg; sucrose - 64.2255 mg; sodium hydrogen phosphate (sodium phosphate disubstituted) - 2.9845 mg; sodium laurylsulfate - 0.799 mg; lactose - 7.99 mp calcium carbonate - 7.99 mg; Shell: hypromellose (hydroxypropyl methylcellulose) - 20.5625 mg; methacrylic acid and ethyl acrylate copolymer (methacrylic acid copolymer L30D) - 58.75 mg; propylene glycol - 1.9035 mg; diethyl phthalate - 5.875 mg; cetyl alcohol
- 1.7625 mg; sodium hydroxide (sodium hydroxide)
- 0.3525 mg; polysorbate-80 (tween-80)
- 0.705 mg; povidone (polyvinylpyrrolidone)
- 0.611 mg; titanium dioxide
- 0.423 mg; talc
- 0.141 mg.
Capsule composition:
Capsule body: titanium dioxide (E 171)
- 2%; gelatin - up to 100%;
Capsule lid: quinoline yellow dye (E104)
- 0.75%; dye yellow sunny sunset (E 110)
- 0.0059%, titanium dioxide (E 171) - 2%; gelatin
- up to 100%.
Pharmacodynamics:
Omeprazole inhibits the H7K + -ATPase enzyme (“proton pump”) in the parietal cells of the stomach and thereby blocks the final stage of hydrochloric acid synthesis. This leads to a decrease in the level of basal and stimulated secretion, regardless of the nature of the stimulus. After a single oral administration, the action of omeprazole occurs within the first hour and lasts for 24 hours, the maximum effect is achieved after 2 hours. In patients with peptic ulcer of the duodenum, taking 20 mg of omeprazole maintains an intragastric pH of 3.0 for 17 hours.
After discontinuation of the drug, secretory activity is fully restored after 3-5 days.
Indications:
- Peptic ulcer of the stomach and duodenum; - Reflux esophagitis;
- Erosive-ulcerative lesions of the stomach and duodenum associated with the use of non-steroidal anti-inflammatory drugs (NSAIDs), stress ulcers. - Erosive-ulcerative lesions of the stomach and duodenum associated with Helicobacter pylori (as part of complex therapy); - Zollinger-Ellison syndrome.
Pharmacokinetics:
Omeprazole is rapidly absorbed from the gastrointestinal tract, the maximum plasma concentration is reached after 0.5-1 hours. Bioavailability is 30-40%. Communication with plasma proteins - about 90%. Omeprazole is almost completely metabolized in the liver. The elimination half-life is 0.5-1 hours. It is excreted mainly by the kidneys in the form of metabolites. In chronic renal failure, excretion decreases in proportion to a decrease in creatinine clearance. In elderly patients, excretion decreases, bioavailability increases. With liver failure, bioavailability is 100%, the half-life is 3 hours.
Side effects:
In rare cases, the following, usually reversible, side effects may occur: From the digestive system: diarrhea or constipation, nausea, vomiting, flatulence, abdominal pain, dry mucous membrane of the oral cavity, taste disturbances, stomatitis, transient increase in the activity of “liver” enzymes in plasma; in patients with a previous severe liver disease - hepatitis (including jaundice), impaired liver function.
From the nervous system: in patients with severe concomitant somatic diseases - dizziness, headache, agitation, depression, in patients with previous severe liver disease - encephalopathy.
From the musculoskeletal system: muscle weakness, myapgia, arthrapgy. From the hemopoietic system: leukopenia, thrombocytopenia, agranulocytosis, pancytopenia. From the skin: skin rash and / or itching, photosensitivity, erythema multiforme, alopecia. Allergic reactions: urticaria, angioedema, bronchospasm, interstitial nephritis and anaphylactic shock.
Other: visual impairment, peripheral edema, increased sweating, fever, gynecomastia; the formation of gastric glandular cysts during prolonged treatment (a consequence of the inhibition of the secretion of hydrochloric acid, is benign, reversible).
Special conditions:
Before starting therapy, it is necessary to exclude the presence of a malignant process (especially with gastric ulcer), because treatment, masking symptoms, may delay the correct diagnosis. Reception at the same time with food does not affect its effectiveness. If you have difficulty swallowing an entire capsule, you can swallow its contents after opening or absorbing the capsule, you can also mix the contents of the capsule with a slightly acidified liquid (juice, yogurt) and use the resulting suspension for 30 minutes. In patients with severe hepatic insufficiency, the daily dose should not exceed 20 mg.
INFLUENCE ON THE ABILITY TO DRIVE A VEHICLE AND WORK WITH MECHANISMS
In case of adverse reactions from the nervous system, patients are advised to refrain from driving and other mechanisms, as well as to exercise caution when engaging in activities that require an increased concentration of attention and speed of psychomotor reactions.
Contraindications:
Hypersensitivity to the drug, childhood, pregnancy, lactation.
Drug Interactions:
Long-term use of omeprazole at a dose of 20 mg once a day in combination with caffeine, theophylline, piroxicam, diclofenac, naproxen, metoprolol, propranolol, ethanol, cyclosporine, lidocaine, quinidine and estradiol did not lead to a change in their plasma concentration. No interaction with concomitantly taken antacids was noted. Changes the bioavailability of any drug whose absorption depends on pH (e.g. iron salts)
Dosage:
Inside, washed down with a small amount of water (the contents of the capsule should not be chewed). Peptic ulcer in the exacerbation phase - 1 capsule (20 mg) per day for 2-4 weeks (in resistant cases, up to 2 capsules per day). Peptic ulcer in the exacerbation phase and erosive-ulcerative esophagitis - 1-2 capsules per day for 4-8 weeks. Erosive and ulcerative lesions of the gastrointestinal tract caused by NSAIDs - 1 capsule per day for 4-8 weeks. Helicobacter pylori eradication - 1 capsule 2 times a day for 7 days in combination with antibacterial agents. Anti-relapse treatment of gastric ulcer and duodenal ulcer - 1 capsule per day. Anti-relapse treatment of reflux esophagitis - 1 capsule per day for a long time (up to 6 months). Zola Inger-El L Ison Syndrome - the dose is selected individually depending on the initial level of gastric secretion, usually starting with 60 mg per day. If necessary, the dose is increased to 80-120 mg per day, in this case it is divided into 2 doses.
Overdose:
Symptoms of an overdose are blurred vision, drowsiness, agitation, confusion, headache, increased sweating, dry mouth, nausea, arrhythmia. There is no specific antidote. The treatment is symptomatic. Hemodialysis is not effective enough.
