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

The drug inhibits H⁺-K⁺-ATP-ase of parietal cells of the stomach, thereby blocking the transfer of hydrogen ions and the final stage of synthesis of hydrochloric acid in the stomach and inhibits the production of hydrochloric acid. Also has a bactericidal action against Helicobacter pylori.

Omeprazole is a prodrug. In the acidic environment of the tubules of parietal cells omeprazole is converted into active metabolites - sulfenamide and sulfenic acid, which inhibit membrane H⁺-TO⁺-ATP phase, connecting with it due to the disulfide bridge. This explains the high selectivity of the action of omeprazole on parietal cells, where there is a medium for the formation of sulfenamide and sulfenic acid. Biotransformation of omeprazole to sulfenamide occurs quickly (in 2-4 minutes). Sulfenamide is a cation and is not absorbed.

Pharmacokinetics:

Quickly and completely absorbed from the gastrointestinal tract. Bioavailability - 30-40% (with liver failure increases almost to 100%),increases in elderly people and in patients with impaired liver function, the failure of renal function has no effect. TC_max - 0,5-3,5 hours. The connection with plasma proteins is 95%, biotransformed in the liver. It is an inhibitor of the isoenzyme CYP2C19. Excreted by the kidneys by 20% and the gastrointestinal tract by 72-80%. Half-life is 30-60 minutes, with chronic liver disease - up to 3 hours.

Indications:

- peptic ulcer of the stomach and duodenum in the phase of exacerbation (including associated with Helicobacter pylori);

- Zollinger-Ellison syndrome;

- reflux esophagitis;

- erosive and ulcerative lesions of the stomach and duodenum, associated with the use of non-steroidal anti-inflammatory drugs.

ICD-10

IV.E15-E16.E16.8 Other specified disorders of internal secretion of the pancreas

XI.K20-K31.K21 Gastroesophageal reflux

XI.K20-K31.K21.0 Gastroesophageal reflux with esophagitis

XI.K20-K31.K25 Stomach ulcer

XI.K20-K31.K26 Duodenal ulcer

XI.K20-K31.K27 Peptic ulcer of unspecified site

XI.K90-K93.K92.9 Disease of digestive organs, unspecified

Contraindications:

- liver disease;

- ghypersensitivity;

- intolerance to fructose;

- deficiency of sugar / isomaltase;

- glucose-galactose malabsorption;

- fromJoint use with clarithromycin in patients with hepatic insufficiency, atazanavir, St. John's wort;

- children's age till 15 years;

- pregnancy and lactation.

Carefully:

Insufficiency of liver function, failure of kidney function, simultaneous use with clarithromycin.

Pregnancy and lactation:

Category FDA - C. There were no adequate and well-controlled studies, not to be used during pregnancy and lactation.

Dosing and Administration:

Dosing regimen is individual. Orally, in the morning before eating or while eating, with a small amount of water; the contents of the capsule can not be chewed, a single dose of 20 to 40 mg. The daily dose is 20-80 mg, the frequency of application is 1-2 times a day. The course of treatment can be from 2 to 8 weeks.

When exacerbation of peptic ulcer, reflux-esophagitis and gastropathy caused by admission non-steroidal anti-inflammatory drugs - 20 mg once a day. For patients with severe reflux esophagitis, the dose is increased to 40 mg once a day. The course of treatment for duodenal ulcer is 2-4 weeks, if necessary - 4-5 weeks; with peptic ulcer of the stomach, with reflux-esophagitis,with erosive-ulcerative lesions of the gastrointestinal tract caused by the admission non-steroidal anti-inflammatory drugs - within 4-8 weeks.

Patients who are resistant to treatment with other antiulcer drugs are prescribed 40 mg per day. The course of treatment for duodenal ulcer is 4 weeks, with peptic ulcer and reflux esophagitis 8 weeks.

When Zollinger-Ellison syndrome - usually 60 mg once a day; if necessary, increase the dose to 80-120 mg per day (the dose is divided into 2 divided doses).

For prevention of recurrences of peptic ulcer - 10 mg once a day.

For eradication of Helicobacter pylori use "triple" therapy (within 1 week: omeprazole 20 mg, amoxicillin 1 g, clarithromycin 500 mg - twice a day; or omeprazole 20 mg, clarithromycin 250 mg, metronidazole 400 mg - twice a day; or omeprazole 40 mg once a day, amoxicillin 500 mg and metronidazole 400 mg - 3 times a day) or "double" therapy (for 2 weeks: omeprazole 20-40 mg and amoxicillin 750 mg - twice a day or omeprazole 40 mg - once a day and clarithromycin 500 mg - 3 times a day or amoxicillin 0,75-1,5 g - 2 times a day).

With hepatic insufficiency appoint 10-20 mg once a day (with severehepatic insufficiency daily dose should not exceed 20 mg); if there is a violation of kidney function and in elderly patients, correction of the dosing regimen is not required.

Side effects:

From the gastrointestinal tract: diarrhea, constipation, nausea, flatulence, abdominal pain, dry mouth, taste disorders, stomatitis, transient increase in the level of hepatic enzymes in plasma; in patients with a previous severe liver disease - hepatitis (including with jaundice), a violation of liver function, a change in the color of the tongue to brownish-black and the appearance of benign salivary gland cysts with concurrent use with clarithromycin, candidiasis, pancreatitis.

From the nervous system: headache, weakness, dizziness, agitation, drowsiness, insomnia, paresthesia, depression, lethargy, anxiety, hallucinations; in patients with severe concomitant somatic diseases, in patients with a previous severe liver disease - encephalopathy.

From the urinary system: proteinuria, hematuria.

From the musculoskeletal system: arthralgia, myalgia, muscle weakness.

From the immune system: rash, urticaria, angioedema, fever, bronchospasm, interstitial nephritis and anaphylactic shock, allergic vasculitis, fever.

From the side of the blood: eosinopenia, hypochromic microcytic anemia in children, neutropenia, thrombocytopenia, leukopenia, pancytopenia, agranulocytosis.

From the side of the organ of vision: visual disturbances, including visual field disturbances, reduced visual acuity and clarity.

From the side of the hearing organ and labyrinthine disorders: disorders of auditory perception, including "ringing in the ears."

Overdose:

Confusion, drowsiness, visual impairment, dry mouth, tachycardia, nausea, headache, flushing to the face, arrhythmia. Treatment is symptomatic.

Interaction:

Clarithromycin - potentiates the effect of each other.

Esters of ampicillin, itraconazole, ketoconazole, iron salts - absorption of these drugs decreasesomeprazole increases the pH of the stomach).

Digoxin - potentiation of the effect due to increased absorption.

Being inhibitors of cytochrome P450, it can increase the concentration and reduce the excretion of diazepam, anticoagulants of indirect action, phenytoin (drugs,are metabolized in the liver by cytochrome CYP2C19), which in some cases may require reducing the dose of these drugs. Can increase the concentration of clarithromycin in the blood plasma.

Increases the inhibitory effect on the hemopoietic system and other medicines.

Special instructions:

Before taking the drug, you must exclude the possibility of a malignant process. The drug may distort the results of laboratory studies of the functional state of the liver.

In the event of difficulties in swallowing the capsule may be swallowed whole of its contents after opening resorption or capsules and can mix the contents of the capsule with slightly acidified liquid (juice, yogurt), and use the resultant suspension within 30 minutes.

In patients with severe hepatic insufficiency, the daily dose should not exceed 20 mg.

Impact on the ability to drive vehicles and manage mechanisms

Not found.

Instructions

Omeprazole (Omeprazolum)