Omeprazole 40 mg N1 lyophilisate for solution preparation

Omeprazole is an antisecretory drug used in the treatment of peptic ulcers and erosive-inflammatory diseases of the upper gastrointestinal tract. Acting at the molecular level, Omeprazole suppresses the production and reduces the damaging effect of hydrochloric acid on the gastric mucosa, restores the pH of gastric juice and reduces its activity after meals.

The drug is used for stomach ulcers

By provoking a persistent decrease in acidity, the drug creates optimal conditions for the destruction of H. pylory, which is often the cause of gastritis and peptic ulcers. It is worth noting that Omeprazole becomes active only when it enters the acidic environment of the stomach.

Omeprazole not only significantly improves the well-being of patients, causes a rapid regression of diseases of the stomach and/or duodenum caused by acid disorders, and reduces the likelihood of relapse and the development of complications. Its action begins within 1 hour after ingestion and continues throughout the day.

Indications

Omeprazole has wide indications for diseases of the upper gastrointestinal tract. The drug is usually prescribed to adults and children over 5 years of age in the following cases:

• stomach and duodenal ulcers;
• erosive and ulcerative esophagitis;
• NSAID gastropathy (ulcerative process resulting from potentiated use of non-steroidal anti-inflammatory drugs);
• Zollinger-Ellinson syndrome;
• systemic mastocytosis;
• polyendocrine adenomatosis;
• stress, aspirin and chronic duodenal ulcers of the digestive tract;
• therapy for reflux esophagitis (including long-term treatment of patients with an inactive form of the disease);
• treatment of symptomatic GERD;
• treatment of ulcerogenic adenoma of the pancreas;
• eradication of H. pylori in peptic ulcer disease (in combination with appropriate antibacterial agents);
• to eliminate uncomplicated heartburn that lasts more than 2 days during the week.

Overdose

Symptoms of overdose are blurred vision, drowsiness, agitation, confusion, headache, increased sweating, dry mouth, nausea, arrhythmia.

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

Interaction with other drugs

Long-term use of omeprazole at a dose of 20 mg 1 time per day in combination with caffeine, theophylline, piroxicam, diclofenac, naproxen, metoprolol, propranolol, ethanol, cyclosporine, lidocaine, quinidine and estradiol did not lead to changes in their plasma concentrations.

When used simultaneously with omeprazole, an increase or decrease in absorption of drugs whose bioavailability is largely determined by the acidity of gastric juice (including erlotinib, ketoconazole, itraconazole, posaconazole, iron supplements and cyanocobalamin) may be observed.

When used concomitantly with omeprazole, a significant decrease in plasma concentrations of atazanavir and nelfinavir may be observed.

When used concomitantly with omeprazole, an increase in plasma concentrations of saquinavir/ritonavir is observed by up to 70%, while the tolerability of treatment in patients with HIV infection does not deteriorate.

The bioavailability of digoxin when used simultaneously with 20 mg of omeprazole increases by 10%. Caution should be exercised when these drugs are used concomitantly in elderly patients.

When used simultaneously with omeprazole, it is possible to increase the plasma concentration and increase the half-life of warfarin (R-warfarin) or other vitamin K antagonists, cilostazol, diazepam, phenytoin, as well as other drugs metabolized in the liver via the CYP2C19 isoenzyme (a dose reduction of these drugs may be required) . Concomitant treatment with omeprazole at a daily dose of 20 mg leads to a change in coagulation time in patients taking warfarin for a long time, therefore, when using omeprazole in patients receiving warfarin or other vitamin K antagonists, it is necessary to monitor the International Normalized Ratio (INR); In some cases, it may be necessary to reduce the dose of warfarin or another vitamin K antagonist.

The use of omeprazole at a dose of 40 mg once daily resulted in an increase in the maximum plasma concentration and AUC of cilostazol by 18% and 26%, respectively; for one of the active metabolites of cilostazol, the increase was 29% and 69%, respectively.

Omeprazole, when used simultaneously, increases the plasma concentration of tacrolimus, which may require dose adjustment. During combination treatment, tacrolimus plasma concentrations and renal function (creatinine clearance) should be carefully monitored.

Inducers of the isoenzymes CYP2C19 and CYP3A4 (for example, rifampicin, preparations of St. John's wort (Hypericum perforatum), when used simultaneously with omeprazole, can increase its metabolism, thereby reducing its concentration in plasma.

There was no interaction with concomitantly taken antacids. May reduce the absorption of ampicillin esters, iron salts, itraconazole and ketoconazole (omeprazole increases gastric pH). Being an inhibitor of cytochrome P450, it can increase the concentration and reduce the excretion of diazepam, indirect anticoagulants, phenytoin (drugs that are metabolized in the liver via cytochrome CYP2C19), which in some cases may require a reduction in the doses of these drugs. Strengthens the inhibitory effect on the hematopoietic system of other drugs.

When methotrexate was co-administered with proton pump inhibitors, a slight increase in the concentration of methotrexate in the blood was observed in some patients. When treated with high doses of methotrexate, omeprazole should be temporarily discontinued.

When omeprazole is taken together with clarithromycin or erythromycin, the concentration of omeprazole in the blood plasma increases.

Co-administration of omeprazole with amoxicillin or metronidazole does not affect the concentration of omeprazole in the blood plasma.

Contraindications

Omeprazole should not be taken in the following cases:

• individual intolerance to the components of the drug;
• pregnancy and lactation;
• age up to 5 years;
• severe forms of liver and kidney failure (with caution);
• malignant tumors of the digestive tract;
• gastrointestinal infections (Omeprazole may increase their reproduction);
• osteoporosis (Omeprazole leaches calcium from bones).

As for osteoporosis, in extreme cases, the attending physician may prescribe complex therapy, including calcium supplements and vitamin D.

The drug should not be taken during pregnancy

Omeprazole also helps reduce the acidity of gastric juice. In this regard, it is not prescribed for gastritis with low acidity and atrophic gastritis.

Carefully

• renal and/or liver failure;
• patients with osteoporosis;
• pregnancy;
• simultaneous use with atazanavir (the dose of omeprazole should not exceed 20 mg per day), clopidogrel, itraconazole, warfarin, cilostazol, diazepam, phenytoin, saquinavir, tacrolimus, clarithromycin, voriconazole, rifampicin;
• the presence of “alarming” symptoms: significant weight loss, repeated vomiting, vomiting with blood, difficulty swallowing, change in the color of stool (tarry stools);
• deficiency of vitamin B12 (cyanocobalamin).

Side effects

Omeprazole is well tolerated and therefore side effects are quite rare. As a rule, they occur with improper or prolonged use of the drug (more than 2-3 months in a row).

Side effect of Omeprazole: abdominal pain

Side effects of the drug appear as:

• dysfunction of the digestive system (abdominal pain, stool disorders, nausea, vomiting, increased activity of liver enzymes, flatulence, taste disturbances, stomatitis, dry mouth, liver dysfunction, hepatitis may develop in patients with previous severe liver pathology);
• dysfunction of the hematopoietic organs, the symptoms of which are leuko-, pancyto-, thrombocytopenia, agranulocytosis;
• dysfunction of the musculoskeletal system (myalgia, arthralgia, myasthenia gravis);
• skin disorders (photosensitivity, skin rashes, itching, alopecia, exudative erythema multiforme);
• dysfunction of the NS: in patients with concomitant severe somatic pathologies, dizziness, headaches, depression or agitation are possible; in patients with previous severe liver disease - encephalopathy;
• hypersensitivity reactions: bronchospasm, fever, angioedema, urticaria, anaphylactic shock, interstitial nephritis;
• other disorders: gynecomastia, general malaise, peripheral edema, visual impairment, hyperhidrosis, formation of benign glandular (glandular) cysts in the stomach (pathology develops with long-term use of the drug as a result of suppression of HCl secretion and is reversible). With long-term use and/or high doses of Omeprazole capsules, there may be an increased risk of fractures of the hip, wrist, and spine.

Pharmacokinetics

Omeprazole is rapidly absorbed from the gastrointestinal tract, Cmax in plasma is achieved in 0.5–1 hour. Bioavailability is 30–40%. Plasma protein binding is about 90%. Omeprazole is almost completely metabolized in the liver. T1/2 - 0.5–1 hour. Excreted mainly by the kidneys in the form of metabolites. In chronic renal failure, excretion decreases in proportion to the decrease in creatinine clearance. In elderly patients, excretion decreases and bioavailability increases. In case of liver failure, bioavailability is 100%, T1/2 is 3 hours.

How to take Omeprazole

Omeprazole is recommended to be taken in the morning, immediately before meals. Capsules are taken orally with a small amount of liquid (can be with food), without crushing, chewing, or damaging the integrity of the shell. If it is necessary to take the drug again during the day, it is usually prescribed in the evening.

Omeprazole can be dissolved in yogurt or juice

For patients with swallowing disorders or children, Omeprazole can be dissolved in acidified water, yogurt or juice (15-20 ml). The diluted drug is prepared immediately before use or no more than 30 minutes before use. In severe cases, especially if the patient is in the intensive care unit, Omeprazole can be administered through a catheter directly into the stomach, or sterile solutions can be used for intravenous infusion. The standard dose for intravenous administration is 40 mg 1 time/day as an infusion lasting 20-30 minutes.

Before administration, the contents of the bottle are dissolved in a volume of 5 ml, and then the volume is immediately adjusted to 100 ml. A 5% glucose solution or a 0.9% NaCl solution is used as a solvent.

A single dose of Omeprazole (tablets/capsules) is 20 mg, but it can be adjusted by the doctor depending on the severity of the disease and the general condition of the patient.

Omeprazole is prescribed in courses of no more than 2 months, after which a break is necessary.

For ulcerogenic adenoma of the pancreas, the course of treatment can last up to 5 years.

Omeprazole during pregnancy and lactation

It has been clinically proven that taking Omeprazole in the first trimester of pregnancy provokes the risk of developing pathology of the cardiovascular system in the fetus. In the second and third trimester, Omeprazole is prescribed with great caution and only when the benefits of the drug outweigh the possible risks. The drug penetrates into the bloodstream and breast milk, so it is not prescribed during lactation.

The therapeutic course of Omeprazole is not intended for children under 5 years of age. However, for Zollinger-Ellison syndrome and some other acute diseases of the upper digestive tract, the doctor may prescribe treatment with the drug. In this case, the dose of the drug is calculated based on the child’s body weight:

• with body weight up to 10 kg: 5 mg/day;
• with body weight from 10 to 20 kg: 10 mg/day;
• with a body weight of 20 kg or more: 20 mg/day.

Omeprazole for gastritis

Omeprazole is prescribed only in cases where gastritis with high acidity is diagnosed. For normo- and hypoacid gastritis, Omeprazole is contraindicated and can provoke thinning of the mucous membrane, a decrease in the number of glands and secretory insufficiency of the stomach and the development of atrophic gastritis with zero acidity of gastric juice.

Omeprazole is prescribed for gastritis with high acidity

The maximum effect from a single dose of Omeprazole at an average therapeutic dose of 20 mg (1 capsule) occurs after 1.5-2 hours. The therapeutic effect of the drug lasts from 18 to 24 hours. The duration of the course is usually 2–3 weeks. During this time, the acidity of the stomach is normalized and the main symptoms of gastritis are eliminated. If the disease is associated with H. pylori infection, then complex therapy is used, supplemented with antibacterial drugs according to one of the generally accepted regimens.

Description:

hard gelatin capsules No. 2 with a transparent body and a brown cap, containing white or almost white spherical pellets (granules).

Pharmacotherapeutic group:

a drug that reduces the secretion of gastric glands - a proton pump inhibitor.

ATX code:

A02BC01.

Pharmacological properties

Pharmacodynamics

Inhibits the enzyme H+K+ATPase (“proton pump”) in the parietal cells of the stomach and thereby blocks the final stage of hydrochloric acid synthesis. This leads to a decrease in the level of basal and stimulated secretion, regardless of the nature of the stimulus. After a single dose of the drug orally, the effect of omeprazole occurs within the first hour and continues for 24 hours, the maximum effect is achieved after 2 hours. After stopping the drug, secretory activity is completely restored after 3–5 days. Due to a decrease in the secretion of hydrochloric acid, the concentration of chromogranin A (CgA) increases. Increased concentrations of CgA in blood plasma may affect the results of examinations to detect neuroendocrine tumors.

Pharmacokinetics

Distribution

Omeprazole is absorbed in the small intestine, usually within 3-6 hours. Bioavailability after oral administration is approximately 60%. Food intake does not affect the bioavailability of omeprazole.

The binding rate of omeprazole to plasma proteins is about 95%, the volume of distribution is 0.3 l/kg.

Metabolism

Omeprazole is completely metabolized in the liver. The main enzymes involved in the metabolic process are CYP2C19 and CYP3A4. The resulting metabolites - sulfone-, sulfide- and hydroxy-omeprazole do not have a significant effect on the secretion of hydrochloric acid.

The total plasma clearance is 0.3-0.6 l/min. The bioavailability of omeprazole increases by approximately 50% with repeated doses compared to a single dose.

Removal

The half-life is approximately 40 minutes (30-90 minutes). About 80% is excreted as metabolites by the kidneys, and the rest by the intestines.

Special patient groups

There were no significant changes in the bioavailability of omeprazole in elderly patients or patients with impaired renal function. In patients with impaired liver function, there is an increase in the bioavailability of omeprazole and a significant decrease in plasma clearance.

Omeprazole analogues

The high effectiveness and positive recommendations of Omeprazole naturally pushed the pharmaceutical market to offer analogues and generic drugs that contain the same main active ingredient, but differ in price, contraindications and side effects. So, in the pharmacy you can find:

Synonyms (based on the same active ingredient as Omeprazole): Omeprazole-Acri, Omeprazole-Teva, Gastrozole, Omeprazole-STADA, Zerocid, Omez, Omipix, Omitox, Omizak, Omeprazole-Richter, Promez, Ultop, Helitsid.

Omeprazole analogues

Analogs (drugs with a similar therapeutic effect): Helicol, Crosacid, Lansofed, Lancid, Pariet, Parkour, Ontime, Nolpaza, Nexium, Ulthera, Epicurus, Neo-Zext, Razo, Peptazol, Pantoprazole, Rabeprazole, De-Nol, Esomeprazole.

Omez or Omeprazole?

Often, to treat certain problems with the gastrointestinal tract, the attending physician can prescribe medications or replace drugs that seem to be similar in composition and therapeutic effect with one another. A reasonable question arises: which is better - Omez or Omeprazole? Both drugs are based on the same active ingredient - omeprazole - which enters the acidic environment of the stomach and affects its mucous membranes. This determines the similarity of the therapeutic effect.

Therefore, the treatment regimen according to which Omez or Omeprazole should be taken for gastritis or ulcers is identical.

The difference between the drugs is the presence of auxiliary components. This should not be underestimated, because the patient may be allergic to some of them, or this will provoke an adverse reaction.

Also, Omeprazole represents the active substance in the maximum volume, and Omez is a drug that contains omeprazole and excipients that mitigate side effects and help the perception of the medicine.

As a result, the choice between these two drugs must be made by the doctor, based on the course of the disease, the severity of its symptoms and the individual indications of the patient.

Composition per capsule:

Active substance:

omeprazole pellets – 235 mg, containing omeprazole – 20 mg.

Auxiliary substances included in the pellets:

methacrylic acid and ethyl acrylate copolymer [1:1] (acrylic coating L30D) – 18.90%, calcium carbonate – 2.975%, potassium hydrogen phosphate (dipotassium phosphate) – 1.275%, hydroxypropyl methylcellulose (hypromellose) –

6.25%, mannitol – 17.0%, sugar pellets (sucrose) – 8.0%, sugar syrup (sucrose) – 30.25%, polyethylene glycol 6000 – 2.45%, povidone-K30 (polyvinylpyrrolidone K 30) – 0.075%, sodium hydroxide – 0.125%, sodium lauryl sulfate – 0.45%, talc – 2.45%, titanium dioxide – 0.80%, polysorbate-80 (Tween 80) – 0.50%.

Capsule shell (body):

gelatin up to 100%, water 14-15%;
(lid):
gelatin up to 100%, water – 14-15%, crimson dye (Ponceau 4R) – 0.6666%, quinoline yellow dye – 0.1000%, patent blue dye – 0.0200%, titanium dioxide – 1 .2999%.

special instructions

Before starting therapy, it is necessary to exclude the presence of a malignant process (especially with a stomach ulcer), because Treatment, masking symptoms, can delay the correct diagnosis.

Taking with food does not affect effectiveness.

If you have difficulty swallowing a whole capsule, you can swallow its contents after opening or dissolving the capsule, or you can mix the contents of the capsule with a slightly acidified liquid (juice, yogurt) and use the resulting suspension for 30 minutes.

In patients with severe liver failure, the daily dose should not exceed 20 mg.

general information

Omeprazole is the first PPI, synthesized back in 1978 and entering clinical practice 10 years later. 40 years later, it became one of the best-selling drugs in the world: in the United States alone, 58 million prescriptions for this drug were issued in 2021. The actual sales volumes of the drug are much higher, since one of its forms belongs to the OTC group, both in the Russian Federation and in many other countries of the world [1].

Pantoprazole appeared a little later than its predecessor: its research began in 1985, and in 1994 the drug was already registered in Germany. In 2021, there were approximately 29 million prescriptions written for pantoprazole in the United States [1].