Omzol

Omzol is used in the treatment of peptic ulcers. It is included in the group of PPI drugs.

Indications Omzola

It is used to treat the following disorders:

• stomach ulcer or GERD;
• destruction of the H.pylori microbe (in combination with various antibacterial drugs);
• gastrinoma;
• long-term prevention of relapses in the treatment of severe GERD;
• prevention and treatment of ulcers in the gastrointestinal tract caused by the use of drugs from the NSAID group (antirheumatic drugs or aspirin).

Release form

The drug is released in capsules with a volume of 0.02 g. There are 10 capsules inside a blister pack, and 2 such packs inside a pack.

Pharmacodynamics

Omeprazole inhibits the activity of the enzyme H ⁺ /K ⁺ -ATPase, which is responsible for the secretion of hydrochloric acid through gastric acid cells. Due to such a selective intracellular effect, independent of membrane endings, omeprazole is classified as an independent group of agents that slow down the secretion of hydrochloric acid and block the final stage of the excretory process.

The therapeutic effect of Omzol allows to reduce not only basal acid secretion, but also stimulated secretion (the type of stimulator does not matter). The drug increases pH values and reduces the excretory volume. Being a light base, the active substance contributes to the enrichment of the acidic cellular environment and acquires enzyme inhibitory efficiency only after the attachment of a proton.

At pH <4, the active element undergoes protonation, during which the active part is formed - omeprazole sulfenamide. It remains inside the cell for a longer time than the plasma half-life of the main part of omeprazole. Adequately low pH values can be found only inside the acidic cell. This is the high specificity of this medicinal element. Omeprazole sulfenamide is synthesized with an enzyme, thereby slowing down its activity.

After the enzyme system is blocked and the pH level increases, the drug accumulates or is transformed into an active metabolic product in smaller quantities. This is due to the fact that the accumulation of omeprazole is regulated by a feedback mechanism.

Pharmacokinetics

Omeprazole taken orally is absorbed in the small intestine. The substance reaches Cmax values 1-3 hours after taking the capsule. The terminal plasma half-life is about 40 minutes, and plasma clearance is approximately 0.3-0.6 l/minute. In some people, decreased elimination is observed: the half-life is three times higher, and the AUC values are ten times higher.

Omeprazole has a relatively small distribution volume (only 0.3 l/kg body weight), which corresponds to the volume of extracellular fluid. Protein synthesis is approximately 90%.

Being a light base, omeprazole accumulates inside the acidic environment of the parietal glandulocyte channels. It is here that a proton is attached to it, after which an active link is formed - sulfenamide. This element is covalently synthesized with H ⁺ /K ⁺ -ATPase of the excretory membrane and inhibits its activity. As a result, the blocking effect on the acid is a significantly longer process than the period of presence of the omeprazole base in the plasma.

Acid inhibition activity is not determined by plasma parameters at any time point, but is correlated with AUC values.

Almost all omeprazole undergoes hepatic metabolism. No unchanged substance is found in the urine. In the plasma, the presence of sulfide, sulfone, and hydroxyomeprazole is recorded. All these metabolic products do not have a noticeable effect on acid excretion. About 80% of the portion is excreted in the urine as metabolic products, and another 20% is excreted in the feces. The two main metabolic products in the urine are hydroxyomeprazole with the corresponding carboxylic acid.

Pharmacokinetic characteristics of the drug in people with renal insufficiency are similar to the kinetics of healthy patients. However, since elimination through the kidneys is the most important way of removing the drug's metabolic products, their elimination rate decreases in accordance with the severity of the renal disorder. There is no accumulation of the drug with a single dose per day.

The bioavailability of the drug is slightly increased in elderly people, while its plasma elimination is slower. However, their individual indicators can be compared with those of healthy individuals.

Systemic bioavailability values are increased by approximately 50% following 5-day intravenous administration of 40 mg omeprazole. This effect is explained by a decrease in hepatic clearance.

In people with liver problems, the clearance values of Omzol are reduced, and the plasma half-life can reach 3 hours. At the same time, the bioavailability of the drug can exceed 90%. Therapy using 20 mg of the drug per day for 1 month was well tolerated - no accumulation of either omeprazole or its metabolic products was observed.

The drug has a moderate ability to pass through the placenta. In total, its indicators in fetal plasma are approximately 20% of the values in the mother. The substance does not accumulate in fetal tissues, because the secretion of hydrochloric acid begins to function immediately before birth. The drug is not able to accumulate, and is not activated in the stomach and does not affect gastrin indicators (they are generally slightly elevated in the fetus shortly before birth; in addition, gastrin does not pass through the placenta). From all this information, it can be concluded that the drug does not affect the mucous membranes of the fetus in the womb.

When 40 μmol/kg of the substance is ingested, the Cmax values in adult rats reach 0.4-2.4 μmol/l. The half-life is 3 hours. In very young rats (aged 12-14 days), the plasma Cmax level when using the same portion is 15-26 μmol/l, and its elimination is very slow.

Dosing and administration

The capsules are taken orally; it is recommended to do this in the morning before meals. The capsule does not need to be chewed or crushed - it should be swallowed and washed down with plain water. It is also acceptable to use it with food.

For gastrointestinal ulcers or GERD, the medication is used in a dosage of 20 mg (equivalent to 1 capsule), 2 times a day for 0.5-1 month.

During treatment of gastrinoma, the dose should be selected individually for each patient. At first, it is recommended to take 60 mg of the drug once a day (3 capsules). If necessary, the dosage can be increased to 80-120 mg of the drug (corresponds to 4-6 capsules) per day (in this case, the dose is divided into 2 uses).

When treating or preventing the development of gastrointestinal ulcers caused by NSAIDs, take 1 capsule of Omzol once a day for 1 month. If there is no desired effect after a 1-month cycle, a repeat course of the same duration is prescribed.

To destroy the H.pylori bacteria, the drug is used in combination treatment:

• 20 mg of Omzol 2 times a day, 1000 mg of amoxicillin 2 times a day, and 500 mg of clarithromycin 2 times a day for 7 days;
• 20 mg of the drug 2 times a day, 500 mg of tetracycline 4 times a day, 500 mg of metronidazole 3 times a day, and 120 mg of bismuth subnitrate 4 times a day for 7 days.

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Use Omzola during pregnancy

Pregnant and lactating women can take Omzol only after the doctor has established an accurate diagnosis (before recalculating the indications). There is only limited information regarding the use of the drug during pregnancy, but during these tests no symptoms of toxic effects of the drug on the fetus were found.

Contraindications

It is contraindicated to use the drug if the patient has hypersensitivity to omeprazole or other medicinal components.

Side effects Omzola

The use of capsules may provoke the development of certain side effects:

• disorders of hematopoiesis: there are isolated data on changes in the blood picture, treatable thrombopenia or leukopenia and pancytopenia, and also on agranulocytosis. But in these cases, it was not possible to find a connection with the use of drugs;
• Gastrointestinal dysfunction: sometimes constipation, nausea, diarrhea, bloating (sometimes with abdominal pain) or vomiting develop. Often, these symptoms subside during therapy. Dryness or inflammation of the oral mucosa, pancreatitis or candidiasis are noted isolatedly (in these cases, no connection with taking the drug was found). When combining the drug with clarithromycin, dark brown coloring of the tongue was sometimes noted. At the end of the treatment cycle, this effect passes. There were also isolated cases of the development of a cyst in the glandular body, which was benign and passed when therapy was stopped;
• nail, hair and epidermal lesions: sometimes a rash or itching appears, erythema multiforme, alopecia, photosensitivity and hyperhidrosis develop. In addition, the development of TEN or Stevens-Johnson syndrome has been occasionally noted;
• problems affecting liver function: sometimes transient changes in liver function values are observed, which disappear after completion of therapy. In people with existing liver pathology, hepatitis may develop, sometimes complicated by jaundice, encephalopathy or liver failure;
• sensory disorders: sometimes visual disturbances (such as loss of visual acuity, foggy vision, visual field defects, and blurred vision), hearing disturbances (such as tinnitus), or taste changes occur. These problems are usually treatable;
• symptoms of intolerance: possible occurrence of Quincke's edema, urticaria, allergic vasculitis and anaphylaxis, as well as an increase in temperature and constriction of the respiratory tract;
• lesions affecting the PNS and CNS: sleep disorders, increased fatigue, headaches and dizziness are sometimes observed. Usually these symptoms weaken during the course of therapy. Hallucinations or clouding of consciousness may occur - mainly in elderly or seriously ill people. Symptoms of aggression or depression have been noted sporadically;
• Other manifestations: during the course of therapy, edema of a peripheral nature occurred, which passed after its completion. Occasionally, pain or weakness in the area of joints or muscles, as well as numbness, were observed. The occurrence of gynecomastia, hyponatremia, or tubulointerstitial nephritis was reported in isolated cases.

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Overdose

Signs of poisoning: a feeling of excitement or drowsiness, visual disturbances, headaches, hyperhidrosis, nausea, hot flashes, as well as tachycardia and dry mouth.

Supportive and symptomatic measures are taken to eliminate the disorders. The drug has no antidote.

Interactions with other drugs

Omzol is metabolized mainly by cytochrome P450 category 2C isoenzymes (element S-mephenytoin hydroxylase). The excretion of phenytoin and diazepam with R-warfarin (active components, the metabolism of which also occurs with the participation of category 2C isoenzymes) is slowed down in case of combination with the drug. Therefore, it is necessary to conduct constant monitoring of patients using anticoagulants such as phenytoin or warfarin. Sometimes it may be necessary to reduce the dose of these drugs.

It is also possible to expect the development of interactions with other medications whose metabolic processes occur with the help of isoenzymes of category 2C cytochrome P450 (for example, hexobarbital).

The combined use of omeprazole with clarithromycin causes an increase in plasma levels of both drugs. A similar effect is observed when combining drugs with other macrolides. When combining Omzol and clarithromycin, other medications should be administered very carefully, especially in people with severe kidney or liver problems.

It is believed that the drug slows down (for example, ketoconazole) or accelerates (for example, erythromycin) the absorption of drugs whose bioavailability is associated with gastric pH.

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Storage conditions

Omzol should be stored in a dark and dry place, out of the reach of small children. Temperature values are within the range of 8-15°C.

Shelf life

Omzol can be used within 36 months from the date of manufacture of the therapeutic agent.

Application for children

There is no experience of using the drug in pediatrics, which is why it is not prescribed to children.

Analogues

Analogues of the drug are Pantasan, Omeprazole, Omez with Ultop and Omeprazole.