Description
Pharmacological action
Omeprazole has a highly selective mechanism of action, as a result of which the secretion of gastric juice is reduced. It is a specific inhibitor of the proton pump of the parietal cells of the stomach. The action of the drug occurs quickly and is mediated by a reversible inhibition of gastric acid secretion. Omeprazole is a weak base. It is concentrated in the acidic environment of the secretory tubules of the parietal cells of the gastric mucosa, is activated and inhibits the proton pump, the enzyme H + -K + -ATPase. The effect of omeprazole on the last stage of the formation of hydrochloric acid in the stomach is dose-dependent and provides highly effective inhibition of basal and stimulated secretion of hydrochloric acid, regardless of the stimulating factor.
Omeprazole with daily oral administration provides fast and effective inhibition of day and night secretion of hydrochloric acid. The maximum effect is achieved within 4 days of treatment. In patients with a duodenal ulcer, omeprazole at a dose of 20 mg causes a steady decrease in 24-hour gastric acidity by at least 80%. In this case, a decrease in the average Cmax of hydrochloric acid after stimulation with pentagastrin by 70% for 24 hours is achieved.
In patients with a duodenal ulcer, omeprazole maintains an acid value in the intragastric medium at a pH of> 3 for an average of 17 for daily use in a dose of 20 mg including
Inhibition of hydrochloric acid secretion depends on the AUC of omeprazole, and not on the concentration of the drug in blood plasma at a given time.
Omeprazole has a bactericidal effect against Helicobacter pylori in vitro. Helicobacter pylori eradication with omeprazole in combination with antibacterial agents is accompanied by a rapid elimination of symptoms, a high degree of healing of gastrointestinal mucosa defects and a long-term remission of peptic ulcer, which reduces the likelihood of complications such as bleeding, as well as constant maintenance therapy.
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 ulcerous ulcer disease associated with Helicobacter pylori (as part of complex therapy)
– Zollinger-Ellison syndrome.
Contraindications
Hypersensitivity to the drug, children, pregnancy, lactation.
Special instructions
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. If after the start of the use of the drug Omeprazole Zentiva for 5 days there is no improvement or heartburn worsens, it is necessary to interrupt treatment and consult a doctor.
Patients older than 45 years with symptoms of first-time heartburn can take Omeprazole Zentiva only after consulting a doctor. Omeprazole Zentiva should not be taken without medical supervision if one of the following symptoms or one of the conditions is present:
weight loss without an obvious cause and / or lack of appetite,
fatigue prolonged abdominal pain
gastric and / or duodenal ulcer history of
frequent vomiting
swallowing disorder / pain when swallowing
bloody vomiting / melena / rectal bleeding more severe mild jaundice
chest pain (especially compression in the chest or pain radiating to the neck or upper limbs) in combination with sweating, shortness of breath or dizziness
history of stomach or esophagus cancer relatives of
liver failure
rare inherited disorders, such as galactose intolerance, lapp lactase deficiency, fructose deficiency, impaired glucose-galactose absorption, or sucrose-isomaltase deficiency.
If any of these symptoms / conditions occurs, treatment should be done under medical supervision.
Risk of fractures of the hip, wrist, and vertebrae
Proton pump inhibitors, especially when using the drug in high doses and with prolonged use (> 1 year), can moderately increase the risk of fractures of the hip, bones of the wrist and vertebrae, especially in elderly patients or the presence of other risk factors. Observational studies suggest that proton pump inhibitors may increase the overall risk of fractures by 10 40%. Patients at risk of developing osteoporosis should receive treatment in accordance with the latest clinical recommendations.
Hypomagnesemia
Severe hypomagnesemia has been reported in patients receiving omeprazole for at least 3 months. Fatigue, light-headedness, convulsions, dizziness, and ventricular arrhythmia may occur. In most patients, hypomagnesemia was stopped after discontinuation of proton pump inhibitors and administration of magnesium preparations. In patients who are planning long-term therapy or are prescribed omeprazole with digoxin or other drugs that can cause hypomagnesemia (for example, diuretics), the magnesium content should be evaluated before starting therapy and periodically monitored during treatment.
Effect on the absorption of vitamin B12 (cyanocobalamin)
Omeprazole, like all drugs that reduce acidity, can lead to a decrease in the absorption of vitamin B12 (cyanocobalamin), because it causes hypo- or achlorhydria. This should be remembered in relation to patients with a reduced supply of vitamin B12 in the body or with risk factors for vitamin B12 malabsorption during prolonged therapy.
Other effects associated with the inhibition of secretion of hydrochloric acid
In patients taking drugs that lower the secretion of the glands of the stomach for a long period of time, the formation of glandular cysts in the stomach, which pass on their own against the background of continued therapy, is more often noted. These phenomena are due to physiological changes as a result of inhibition of hydrochloric acid secretion.
Decreased secretion of hydrochloric acid in the stomach by proton pump inhibitors or other acid-inhibiting agents leads to increased growth of normal intestinal microflora, which in turn can lead to a slight increase in the risk of developing intestinal infections caused by bacteria of the genus Salmonella spp. and Campylobacter spp. and probably also the bacterium Clostridium difficile in hospitalized patients.
Due to a decrease in the secretion of hydrochloric acid, the concentration of chromogranin A (CgA) increases. An increase in the concentration of CgA may affect the results of examinations to detect neuroendocrine tumors. To prevent this effect, it is necessary to temporarily stop the use of omeprazole 5 days before the study of the concentration of CgA.
Taking the drug at the same time as food does not affect its effectiveness.
Influence on the ability to drive vehicles and control mechanisms
There is no data on the effect of the drug on the ability to drive a car or other mechanisms. However, due to the fact that during therapy dizziness, blurred vision and drowsiness may be observed, caution should be exercised when driving vehicles or while working with mechanisms that require an increased concentration of attention and speed of psychomotor reactions.
Composition
1 capsule contains the active substance: omeprazole pellet – 235 mg in terms of 20 mg of omeprazole.
Dosage and administration
Inside with a small amount of water (do not chew the contents of the capsule). 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.
Side effects of
Side effects of omeprazole are usually mild and reversible. The following side effects may occur, which are divided into organ-system classes according to the classification of the Medical Dictionary of Regulatory Activities (MedDRA). The WHO classification was used to indicate the incidence of side effects: very often ( 10%), often ( 1% and <10%), infrequently ( 0.1% and <1%), rarely ( 0.01% and <0.1% ), very rarely (<0.01%), unknown frequency (according to available data, it is not possible to determine the incidence of side effects). From the hemopoietic system: rarely – leukopenia, thrombocytopenia very rarely – agranulocytosis, pancytopenia. On the part of the immune system: rarely, hypersensitivity reactions (eg, fever, angioedema, anaphylactic reaction / anaphylactic shock). From the side of metabolism: rarely – hyponatremia unknown frequency – hypomagnesemia. Mental disorders: infrequently – insomnia rarely – agitation, confusion, depression very rarely – aggression, hallucinations. From the nervous system: often – headache infrequently – dizziness, paresthesia, drowsiness rarely – taste disturbance. From the side of the organ of vision: rarely – blurred vision. On the part of the organ of hearing and labyrinth disorders: infrequently – dizziness. From the respiratory system: rarely – bronchospasm. From the digestive system: often – diarrhea, constipation, nausea, vomiting, flatulence, abdominal pain infrequently – increased activity of liver enzymes rarely – dry mouth, stomatitis, gastrointestinal candidiasis, hepatitis (with or without jaundice) very rarely – liver failure , encephalopathy in patients with liver disease. From the skin and subcutaneous tissues: infrequently – dermatitis, itching, rash, urticaria, rarely – alopecia, photosensitivity very rarely – erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis. From the musculoskeletal system: infrequently – fractures of the thigh, bones of the wrist and vertebrae rarely – arthralgia, myalgia very rarely – muscle weakness. From the urinary system: rarely – interstitial nephritis. From the genitals and mammary gland: very rarely – gynecomastia. General disorders and disorders at the injection site: infrequently – malaise, peripheral edema rarely – excessive sweating. Cases of the formation of gastric glandular cysts during prolonged treatment with proton pump inhibitors have been reported (due to inhibition of hydrochloric acid secretion, it is benign and reversible). Overdose of With the use of omeprazole in adults in a single dose of 560 mg, symptoms of moderate intoxication were noted. A case of the use of omeprazole in a single dose of 2400 mg is described, which did not cause any severe toxic symptoms. With increasing dose, the elimination rate of the drug did not change (first-order kinetics), and specific treatment was not required. Symptoms: dizziness, confusion, apathy, depression, headache, tachycardia, nausea, vomiting, flatulence, diarrhea, Treatment: symptomatic treatment if necessary – gastric lavage, purpose of activated carbon. Storage conditions The drug should be stored out of the reach of children at a temperature not exceeding 25 ° C. Expiration 2 years Dosage form capsules
