Omal - instructions for use, dose, side effects, contraindications

Omeprazole reduces the secretion of hydrochloric acid in the stomach due to specific inhibition of the proton pump in parietal cells. With a single dosing per day, the drug acts quickly and causes acid blockage in the stomach.

Omeprazole is a weak base, concentrated and converted into an active form in the acidic environment of the secretory tubules of parietal cells of the gastric mucosa, where it inhibits the enzyme H⁺-TO⁺-ATPase (proton pump).

The drug has a dose-dependent effect on the final stage of acid synthesis and inhibits both basal and stimulated acid secretion in the stomach, regardless of the nature of the stimulus.The antisecretory effect is maintained for 24 hours. The degree of oppression of hydrochloric acid secretion is proportional to the area under the concentration-time curve (AUC), but does not depend on the immediate concentration of omeprazole in the blood plasma.

Pharmacokinetics:

The distribution volume is approximately 0.3 l / kg. The connection with plasma proteins is 97%. It is subject to complete metabolism involving the cytochrome P450 system (CYP). The main part is metabolized with the participation of polymorphic isoenzyme CYP 2C19, which is responsible for the formation of the main metabolite of hydroxyomeprazole. The metabolism of the remainder is carried out by isoenzyme CYP 3A4 with the formation of omeprazole sulfone. Metabolites have no significant effect on the secretion of acid in the stomach. The half-life after intravenous administration is 40 minutes and does not change with prolonged treatment. About 80% of the dose of omeprazole is excreted by the kidneys, the remainder is excreted through the intestine, mainly with bile. Metabolism of omeprazole in patients with impaired liver function is slowed, which leads to an increase AUC. In patients with reduced renal function, pharmacokinetics, including systemic bioavailability and rate of excretion, remain unchanged.The rate of metabolism of omeprazole in elderly patients is somewhat reduced.

Indications:

- Stomach ulcer and duodenal ulcer (including prevention of relapses);

- erosive and ulcerative lesions of the stomach and duodenum, associated with Helicobacter pylori (as part of complex therapy);

- erosive and ulcerative lesions of the stomach and duodenum associated with the use of non-steroidal anti-inflammatory drugs (NSAIDs);

- prevention of stress ulcers;

- reflux esophagitis;

- symptomatic gastroesophageal reflux disease (GERD);

- Zollinger-Ellison syndrome.

Contraindications:

- Hypersensitivity to omeprazole or other components of the drug;

- simultaneous use with erlotinib, posaconazole, nelfinavir and atazanavir;

- the period of breastfeeding;

- Children under 18 years of age (efficacy and safety not established for this dosage form).

Carefully:

- Renal failure;

- liver failure;

- osteoporosis;

- pregnancy;

- simultaneous use with clopidogrel, itraconazole, warfarin, cilostazol, diazepam, phenytoin, saquinavir, tacrolimus,clarithromycin, vorikanazole, rifampicin, preparations of St. John's wort perfumed.

Pregnancy and lactation:

The use of the drug during pregnancy is possible only in cases where the intended use for the mother is a potential risk to the fetus.

Omeprazole is excreted in breast milk. If you need to use the drug during lactation, you need to decide whether to stop breastfeeding or stop taking the drug.

Dosing and Administration:

The drug is administered intravenously at a dose of 40 mg once a day in those cases when oral administration of the drug is not possible.

Zollinger-Ellison Syndrome

The dose is selected individually depending on the initial level of gastric secretion, usually starting at 60 mg per day. If necessary, increase the dose to 80-120 mg per day, dividing it into two injections.

The duration of treatment in each case is determined by the doctor depending on the patient's condition.

To prepare a solution for intravenous administration a vial containing a single dose of 40 mg of lyophilized omeprazole is diluted with 10 ml of sterile water for injection.The resulting solution at a concentration of 4 mg / ml slowly (more than 5 minutes) is administered intravenously.

For the preparation of infusion solution a vial containing a single dose of 40 mg is dissolved in 100 ml of 0.9% solution of sodium chloride or 100 ml of a 5% solution of glucose. Use of other solutions is not allowed. Infusion should be performed within 20-30 minutes.

The reconstituted solution is used for 3 hours from the time of preparation, the unused solution is destroyed.

Freezing of reconstituted solution is not allowed.

Side effects:

From the digestive system: abdominal pain, constipation, diarrhea, flatulence, nausea, vomiting, dry mouth, stomatitis, gastrointestinal candidiasis, microscopic colitis, transient increase in the activity of "liver enzymes," a violation of liver function, hepatitis, hepatic insufficiency.

From the nervous system: encephalopathy in patients with previous severe impairment of liver function, headache, dizziness, paresthesia, insomnia, drowsiness, impaired taste, confusion, state of arousal, depression, aggression, hallucinations.

From the organs of hearing: vertigo.

From the side of the musculoskeletal system: myalgia, arthralgia, muscle weakness, hip fractures, wrist bones, vertebrae.

On the part of the organs of hematopoiesis: leukopenia, thrombocytopenia, agranulocytosis, pancytopenia.

From the skin: pruritus, peripheral edema, skin rash, dermatitis, urticaria, alopecia, photosensitivity, erythema multiforme exudative, Stevens-Johnson syndrome, toxic epidermal necrolysis.

Allergic reactions: interstitial nephritis, angioedema, anaphylactic reactions, anaphylactic shock, bronchospasm.

Other: visual impairment, gynecomastia, general weakness, increased sweating, hyponatremia, hypomagnesemia.

Overdose:

Symptoms: confusion, blurred vision, drowsiness, dry mouth, headache, nausea, tachycardia, arrhythmia.

Treatment: symptomatic. Hemodialysis is not effective enough. There is no specific antidote.

Interaction:

Can reduce the absorption of esters of ampicillin, iron salts, itraconazole, posaconazole and ketoconazole (omeprazole increases the pH of the stomach).

It can increase the concentration and reduce the excretion of diazepam, anticoagulants of indirect action, phenytoin, which in some cases may require a reduction in the doses of these drugs.

With the combined use of omeprazole with nelfinavir and atazanavir, there is a decrease in their concentration in the blood plasma.

The use of omeprazole in combination with saquinovir / ritoninavir resulted in an increased concentration of saquinovir in the blood plasma, which was accompanied by good tolerability in HIV-infected patients.

Omeprazole can increase the bioavailability of digoxin and the effectiveness of clopidogrel.

The use of tacrolimus in combination with omeprazole may cause an increase in its concentration in the blood plasma.

Clarithromycin and voriconazole can cause an increase in the level of omeprazole in blood plasma as a result of a decrease in metabolic rate.

Rifampicin and preparations of St. John's wort can lead to a decrease in the concentration of omeprazole in the blood plasma due to the acceleration of the metabolism of omeprazole.

Omeprazole inhibits isoenzyme CYP2C19 - the main isoenzyme involved in its metabolism.Simultaneous use of omeprazole with other drugs, in the metabolism of which takes part isoenzyme CYP2C19, such as diazepam, warfarin or other antagonists of vitamin K, phenytoin and cilostazol, can lead to a slowdown in the metabolism of these drugs.

Special instructions:

Before the start of therapy, it is necessary to exclude the presence of a malignant process (especially with gastric ulcer), since treatment, masking the symptoms, can delay the setting of the correct diagnosis.

Five days before the measurement CgA treatment with omeprazole should be discontinued.

Treatment with proton pump inhibitors can lead to a slight increase in the risk of infectious diseases of the gastrointestinal tract.

Effect on the ability to drive transp. cf. and fur:

Care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased attention and speed of psychomotor reactions.

Form release / dosage:

Lyophilizate for the preparation of a solution for intravenous administration, 40 mg.

Packaging:

40.0 mg omeprazole per vial of light-protective glass USP (type 1), sealed with a rubber stopper of gray color and an aluminum lid (under running) with a plastic lid.

1 bottle per cardboard pack together with instructions for use.

Storage conditions:

In a dry, the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use after the expiration date stated on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-003416

Date of registration:18.01.2016

Expiration Date:18.01.2021

The owner of the registration certificate:FARMGID CJSCFARMGID CJSC Russia

Manufacturer: & nbsp

LYKA LABS, Ltd. India

Representation: & nbspPharmgid, OOOPharmgid, OOO

Information update date: & nbsp06.06.2017

Illustrated instructions

Instructions

Omal (Omal)