More info
Active ingredients
Omeprazole
Release form
Capsules
Composition
Omeprazol 40 mg; Excipients: mannitol - 236 mg, crospovidone - 18 mg, poloxamer (407) - 5 mg, hypromellose (1828) - 8 mg, meglumine - 3 mg. Coating composition: povidone K30 - 26.8 mg.; Composition enteric coating: copolymer of methacrylic acid and ethyl acrylate [1: 1] (methacrylic acid copolymer [type C]) - 72 mg, triethyl acetate - 7.2 mg, magnesium stearate - 4 mg; Capsule body composition: brilliant blue dye (E133), dye sunny sunset yellow (E110), charming red dye (E129), phloxin B dye (red D & C red # 28 dye), titanium dioxide (E 171), sodium lauryl sulfate, water, gelatin; Capsule lid composition: iron dye yellow oxide (E172), titanium dioxide (E171), sodium lauryl sulfate, water, gelatin; Black inscription on the capsules: ink S-1-8114 : shellac (20% esterified) in ethanol, iron dye black oxide (E172), n-butanol, propylene glycol (E1520), indigo carmine dye (E132), charming red dye (E129), quinoline yellow dye (E104), brilliant blue dye (E133); S-1-8115 ink: shellac (20% esterified) in ethanol, iron dye black oxide (E172), ethanol, methanol, indigo carmine dye (E132), charming red dye (E129), quinoline yellow dye (E104), diamond dye blue (E133).
Pharmacological effect
Specific proton pump inhibitor: inhibits the activity of H + -K + -ATP-ase in the parietal cells of the stomach, blocking the final stage of secretion of hydrochloric acid, thereby reducing the production of hydrochloric acid; The effect is dose-dependent and provides effective inhibition of both basal and stimulated acid secretion, regardless of the nature of the stimulating factor.; Antisecretory effect after administration of 20 m occurs within the first hour, maximum - in 2 hours. Inhibition of 50% of the maximum secretion lasts 24 hours; A single dose per day provides rapid and effective inhibition of day and night gastric secretion, reaching its maximum after 4 days of treatment and disappearing by the end of 3- 4 days after the end of the reception. In patients with duodenal ulcer, taking 20 mg of omeprazole maintains intragastric pH above 3 for 17 hours.
Pharmacokinetics
Absorption; Absorption - high, time to reach Cmax - 0.5-3.5 h.Bioavailability is 30-40%; Distribution; Possessing high lipophilicity, it easily penetrates into the parietal cells of the stomach. Plasma protein binding (albumin and acid alpha1-glycoprotein) - 90-95%; Metabolism; Almost completely metabolized in the liver with the participation of cytochrome P450 (CYP) enzyme system, with the formation of 6 pharmacologically inactive metabolites (hydroxyomeprazole, sulfide and sulfone derivatives etc.) It is an inhibitor of the isoenzyme CYP2C19.; Elimination; T1 / 2 is 0.5-1 h; total plasma clearance is from 0.3 to 0.6 l / min. There is no change in T1 / 2 during the course of treatment. Excreted in the urine (70-80%) and bile (20-30%) .; Pharmacokinetics in special clinical cases; In liver failure, bioavailability increases to almost 100%; T1 / 2 is 3 hours. In chronic renal failure, excretion decreases in proportion to the decrease in CC.; In elderly patients, excretion decreases, bioavailability increases.
Indications
- peptic ulcer of the stomach and duodenum (including prevention of relapse); - reflux esophagitis; - hypersecretory conditions (Zollinger-Ellison syndrome, stressful ulcers of the gastrointestinal tract, polyendocrine adenomatosis, systemic mastocytosis); - NSAID-gastropathy; - eradication of Helicobacter pylori in infected patients with gastric ulcer and duodenal ulcer (as part of combination therapy); - prevention of aspiration of the acidic contents of the stomach into the respiratory tract during general anesthesia (Mendelssohn's syndrome).
Contraindications
- childhood; - pregnancy; - lactation period; - Hypersensitivity to the drug. With caution should be prescribed the drug in renal and / or liver failure.
Use during pregnancy and lactation
The drug is contraindicated for use during pregnancy and lactation.
Dosage and administration
It is taken orally with a small amount of water (the contents of the capsule cannot be chewed), 30 minutes before a meal or just before a meal. With an exacerbation of gastric ulcer and duodenal ulcer, reflux esophagitis and NSAID gastropathy - 20 mg 2 times / day. The course of treatment for duodenal ulcer - 2-3 weeks, if necessary - 4-5 weeks; with gastric ulcer and reflux esophagitis - 4-8 weeks; In Zollinger-Ellison syndrome, the dose is adjusted individually depending on the initial level of gastric secretion,usually starting at 60 mg / day; if necessary, increase the dose to 80-120 mg / day (in this case, it is prescribed in 2–3 doses); For the prevention of Mendelssohn’s syndrome — 40 mg 1 hour before surgery; To prevent a recurrence of gastric ulcer and duodenal ulcer — 10 -20 mg 1 time / day; Anti-relapse treatment of reflux esophagitis - 20 mg / day for a long period.; For Helicobacter pylori eradication - 20 mg 2 times / day for 7-14 days (depending on the treatment regimen used) in combination with antibacterial agents.; Elderly patients do not need to adjust the dose.
Side effects
The frequency of side effects is classified depending on the frequency of occurrence of the case: often (1-10%), sometimes (0.1-1%), rarely (0.01-0.1%), very rarely (less than 0.01%, including individual messages) .; hematopoietic system: very rarely - leukopenia, thrombocytopenia, agranulocytosis, pancytopenia. From the alimentary system: sometimes - diarrhea or constipation, abdominal pain, nausea, vomiting, flatulence; rarely - increased liver enzymes, taste disorders; very rarely - dry mouth, stomatitis, in patients with previous severe liver disease - hepatitis (including jaundice), abnormal liver function. From the nervous system: in patients with severe concomitant somatic diseases - dizziness, headache pain, agitation, depression, in patients with previous severe liver disease - encephalopathy. From the musculoskeletal system: very rarely - arthralgia, myasthenia, myalgia. From the skin: rarely - skin rash and / or itching; in some cases - photosensitization, erythema multiforme exudative, alopecia.; Allergic reactions: often - urticaria; very rarely - angioedema, fever, bronchospasm, interstitial nephritis and anaphylactic shock; Other: rarely - gynecomastia, malaise, visual impairment, peripheral edema, increased sweating, the formation of gastric glandular cysts during long-term treatment (resulting from inhibition of salt secretion, prolonged salt therapy benign, reversible character).
Overdose
Symptoms: confusion, blurred vision, drowsiness, dry mouth, headache, nausea, tachycardia, arrhythmia.; Treatment: conducting symptomatic therapy, hemodialysis is not effective enough.
Interaction with other drugs
May reduce the absorption of ampicillin esters of iron salts, itraconazole and ketoconazole (omeprazole increases the pH of the stomach); As an inhibitor of cytochrome P450, it can increase the concentration and reduce the excretion of diazepam, indirect-acting anticoagulants (warfarin), phenytoin (drugs, we are already in circulation). CYP 2C19), which in some cases may require a reduction in doses of these medicines.; At the same time, long-term use of omeprazole in a dose of 20 mg 1 time / day in combination with caffeine, theoph illino, piroxicam, diclofenac, naproxen, metoprolol, propranolol, ethanol, cyclosporine, lidocaine, quinidine and estradiol did not change their concentration in plasma. Plasma concentrations of omeprazole and clarithromycin increased in the oral administration of these drugs, including in people who received oralprazole and clarithromycin, clarinromine, quinidine and estradiol. as evidence of the interaction of omeprazole with metronidazole and amoxicillin was not detected.; No interaction with simultaneously taken antacids was observed.
special instructions
Before starting therapy, it is necessary to exclude the presence of a malignant process (especially in case of gastric ulcer), since treatment, masking the symptoms, may delay the correct diagnosis.; Taking the drug along with food does not affect its effectiveness.; Impact on the ability to drive motor vehicles and control mechanisms; The impact of omeprazole on driving and the use of other equipment is unlikely.