Omeprazole

When ATH:
A02BC01

Characteristic.

White or off-white crystalline powder, soluble in methanol and ethanol, weak-in acetone and isopropanol, very little is in the water. It is weak ground, pH dependent stability: It undergoes rapid degradation in acidic medium, relatively stable in the alkaline.

Pharmacological action.
Antiulcer.

Application.

Gastric ulcer and duodenal ulcer in the acute phase, gastroesophageal reflux disease, incl. refractory to therapy H2-antihistaminics, reflux esophagitis, incl. erosive and ulcerative, pathological hypersecretory conditions (Zollinger - Ellison, multiple endocrine adenomatosis, systemic mastocytosis, stressovaya ulcer, incl. prevention), peptic ulcer gastrointestinal tract, caused Helicobacter pylori, NSAID-gastroenteropathy, erosive and ulcerative lesions of the stomach and duodenum in HIV-infected patients, neyazvennaya dyspepsia.

Contraindications.

Hypersensitivity, pregnancy, lactation.

Restrictions apply.

Chronic liver disease, childhood (the exception is Zollinger-Ellison Syndrome).

Pregnancy and breast-feeding.

Category actions result in FDA - C. (The study of reproduction in animals has revealed adverse effects on the fetus, and adequate and well-controlled studies in pregnant women have not held, However, the potential benefits, associated with drugs in pregnant, may justify its use, in spite of the possible risk.)

During pregnancy is possible only for health reasons.

At the time of treatment should stop breastfeeding.

Side effects.

From the digestive tract: dry mouth, anorexia, nausea, vomiting, flatulence, abdominal pain, diarrhea, constipation, in some cases — to change the gustatory sensitivity, stomatitis and gastrointestinal candidiasis, polyposis fundus, gastratrophia, increase in liver enzymes.

From the nervous system and sensory organs: headache, rarely is a malaise, asthenia, dizziness, sleep disturbance, drowsiness, paresthesia, in some cases, anxiety, excitation, alarm, depression, reversible mental impairment, hallucinations, visual impairment, incl. Irreversible.

On the part of the musculoskeletal system: in some cases, artralgia, muscular weakness.

Cardio-vascular system and blood: in some cases, thrombocytopenia, leukopenia, neutropenia, eosinopenia, pancytopenia, leukocytosis, anemia.

With the genitourinary system: rarely hematuria, proteinuria, peripheral edema, urinary infection.

For the skin: in some cases, photosensitization, erythema multiforme, alopecia.

Allergic reactions: seldom - skin rash, hives, itch, in some cases, bronchospasm, angioedema, interstitial nephritis, anaphylactic shock.

Other: in some cases, chest pain, gynecomastia.

Cooperation.

Changes the bioavailability of any drug, absorption is pH dependent (ketoconazole, salts of iron and other.). Slows elimination of drugs, metabolized in the liver by microsomal oxidation (warfarin, diazepam, phenytoin and the like.).

It enhances the effect of coumarin and difenina, does not alter-NPVS. Increases (mutually) the blood concentration of clarithromycin. May increase leykopenicheskoe and thrombocytopenic effects of drugs, oppressive blood. Substance for in / infusion is only compatible with the physiological solution and dextrose solution (the use of other solvents may decrease the stability of omeprazole for pH changes of the infusion medium).

Overdose.

Symptoms: dry mouth, nausea, blurred vision, headache, increased sweating, flushing, tachycardia, drowsiness, confusion.

Treatment: symptomatic; dialysis maloeffyektivyen.

Dosing and Administration.

Inside, preferably in the morning before a meal, without chewing, no crushing or damaging capsule, drinking a small amount of liquid (can receive food). In gastric ulcer, duodenal, ezofagealnom reflux is 20 mg 1 once a day, When reflux-ezofagite-20-40 mg 1 once a day. Course Length: ulcer duodenal ulcer is 2-4 weeks, reflux-ezofagite- 4 Sun, stomach ulcer and reflux ezofagealnom-4-8 weeks. To prevent the recurrence of duodenal ulcer and reflux-esophagitis possible long-term prescription dose 10 mg.

In heavy over ulcers and/or inability destination inside — I / dose 40 mg for 20-30 minutes 1 once a day. Rr infusion is prepared time by dissolving 40 mg substance/in infusions 100 ml of physiological solution, or 5% dextrose. Patients in critical condition possible intragastric gavage encapsulated. In the syndrome Zollinger-Ellison dose adjusted individually, as measured by the level of gastric secretion (should not exceed 10 mmol HCl / h or 5 mmol HCl / h after resection), initial dose is 20-60 mg/day, optionally up 120 mg / day 3 admission (daily dose above 80 mg should be appointed in divided doses) for 2-8 weeks (the long reception is possible — to 5 years). Peptic ulcer, caused Helicobacter pylori, in combination: omeprazole 20 mg, amoksiцillin 1 g, klaritromicin 250-500 mg or omeprazol 20 mg, metronidazol 400 mg, klaritromicin 250-500 mg 2 twice a day for 7 days. When gastroenteropathy, associated with the admission npvs- 20 mg 1 once a day for 4-8 weeks. When eroziveh and began losing stomach and duodenal ulcers in HIV-infected patients is on 20 mg daily for 4 Sun.

Precautions.

Before treatment, exclude malignancy in the gastrointestinal tract, especially gastric ulcer (because of the potential smoothing symptoms and to increase the time of diagnosis). Against the backdrop of severe hepatic insufficiency treatment is possible only under close medical supervision (dose should not exceed 20 mg / day). For patients from Asia likely need to adjust the dose, especially in long-term anti-treatment. When concomitant administration of warfarin is recommended that monitoring of anticoagulant concentration in serum or regular determination of the prothrombin time, followed by a dose adjustment. It is necessary to take into account, that continuous preventive treatment with omeprazole need the following groups of patients: with severe and frequent symptoms and / or endoscopically proven stage III-IV gastroesophageal reflux disease (GERD) on Savary-Miller, in the presence of complications (Barrett's esophagus, stricture or ulcer), chronic administration of drugs, contributing to the emergence of GERD, symptoms persist after healing, long duration of symptoms prior to initiating therapy, very low basal pressure in the lower esophageal sphincter. At stage II esophagitis (on Savary-Miller) maintenance therapy is recommended after two relapses. Efficacy permanent therapy with the combination treatment of GERD increases prokinetic agents. In the case of maintenance treatment in patients with GERD, associated with N. pylori, for the prevention of mucosal atrophy suitable bacterial eradication.

Cautions.

Cooked recovery solution can be used no later than 12 no (when dissolved at physiological saline) or 6 no (solvent-dekstroza).


Cooperation

Active substanceDescription of interaction
AlprazolamFKV. Against the background of omeprazole (an inhibitor of microsomal oxidation) slowing biotransformation and prolonged effect.
AmoksiцillinFKV. FMR: synergism. Against the backdrop of slowing biotransformation of omeprazole and amplifies the effect of H. pylori.
WarfarinFKV. FMR. Against the background of omeprazole (blocks microsomal oxidation), slows and amplifies the effect of biotransformation.
DiazepamFKV. FMR. Against the background of omeprazole (an inhibitor of microsomal oxidation) slowing biotransformation and prolonged effect.
DisulьfiramFKV. Against the background of omeprazole (an inhibitor of CYP450) zamedlyaetsya biotransformation.
Ferrous gluconateFKV. Against the background of omeprazole (blocks the secretion of hydrochloric acid) snizhaetsya absorption.
Iron sulfateFKV. Against the background of omeprazole (reduces the acidity of gastric contents), reduces the absorption of.
Iron fumarateFKV. Against the background of omeprazole (blocks the secretion of hydrochloric acid) snizhaetsya absorption.
KetoconazoleFKV. Against the background of omeprazole (blocks the secretion of hydrochloric acid) reduced absorption and bioavailability.
ClarithromycinFKV. Slows (mutually) biotransformation, increases the equilibrium concentration in plasma, FROMmax, AUC0–24 and T1/2.
ClonazepamFKV. Against the background of omeprazole (inhibits CYP450 system) slowing biotransformation and prolonged effect.
LorazepamFKV. Against the background of omeprazole (inhibits CYP450 system) slowing biotransformation and prolonged effect.
MidazolamFKV. Against the background of omeprazole (reduces the activity of CYP450) biotransformation and slows down the effect can be enhanced.
OxazepamFKV. Against the background of omeprazole (inhibits CYP450 system) slowing biotransformation and prolonged effect.
PhenytoinFKV. Against the background of omeprazole (an inhibitor of microsomal oxidation) slows and amplifies the effect of biotransformation.
XlordiazepoksidFKV. Against the background of omeprazole (inhibits CYP450 system) slowing biotransformation and prolonged effect.
CyclosporineFKV. Slows (mutually) biotransformation (It competes for CYP450) and increases the concentration in the blood.

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