Omzol

Omzol is used in the treatment of peptic ulcers. Included in the group of drugs IPN.

Indications Omzola

It is used to treat the following disorders:

• gastric ulcer or GERD;
• destruction of H. Pylori microbe (combined with various antibacterial drugs);
• gastrinoma ;
• prolonged prevention of relapses in the treatment of GERD in severe degree;
• prevention and therapy for gastrointestinal ulcers caused by the use of drugs from the NSAID group (antirheumatic drugs or aspirin).

Release form

The drug is produced in capsules with a volume of 0.02 g. Inside the blister pack contains 10 capsules, inside the pack - 2 such packages.

Pharmacodynamics

Omeprazole inhibits the activity of the enzyme H ⁺ / K ⁺ -ATPase, which is responsible for the release of hydrochloric acid through gastric acid cells. Due to this selective intracellular effect, independent of membrane endings, omeprazole is considered to be an independent group of agents that slow the release 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 stimulant does not matter). The drug increases the pH and reduces the excretory volume. Being an easy basis, the active substance promotes the enrichment of the acidic cell medium and acquires an enzyme inhibitory efficiency only after the proton is attached.

At pH <4, the active element undergoes protonation, during which the active part, omeprazole sulfenamide, is formed. It stays within the cell for a longer time than the plasma half-life of the main part of omeprazole. Adequately low pH values can be detected exclusively within the acid cell. This is the high specificity of this drug element. Omeprazole sulfenamide is synthesized with an enzyme, thereby slowing its activity.

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

Pharmacokinetics

Omeprazole, used orally, is absorbed inside the small intestine. The substance reaches Cmax after 1 to 3 hours after the capsule has been consumed. The final term of plasma half-life is about 40 minutes, and the plasma clearance is about 0.3-0.6 l / min. Individual people have a reduced elimination: the half-life is three times higher, and the AUC values are tenfold.

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

As an easy basis, omeprazole cumulates the channels of parietal glandulocytes inside the acid medium. It is here that a proton is attached to it, after which an active ligament is formed - sulfenamide. This element is covalently synthesized with the H ⁺ / K ⁺ -ATPase of the excretory membrane and inhibits its activity. As a result, the blocking effect on the acid is a substantially longer process than the period of the omeprazole base within the plasma.

The activity of acid deceleration is not determined by plasma indices at any of the moments, but has a correlation with the values of AUC.

Almost all omeprazole undergoes hepatic metabolism. Inside the urine, there is no substance in the unmodified state. The presence of sulfide, sulfone, and also hydroxyomeprazole is recorded inside the plasma. All these metabolic products do not have a noticeable effect on the release of acid. About 80% of the portion is excreted in the urine in the form of metabolic products, and another 20% is excreted with feces. The main two metabolic products inside the urine are hydroxyomeprazole with the corresponding carboxylic acid.

Pharmacokinetic characteristics of drugs in people with a deficiency of renal function are similar to the kinetics of healthy patients. But, because elimination through the kidneys is the most important way to remove metabolic products of the drug, their elimination rate decreases in accordance with the degree of expression of renal impairment. Cumulation of the medication with a 1-time dose per day does not occur.

The level of bioavailability of the drug slightly increases in the elderly, while its plasma elimination slows down. But at the same time, their individual indicators can be correlated with the indicators of healthy individuals.

The values of systemic bioavailability increase by approximately 50% with a 5-day intravenous application of 40 mg omeprazole. This effect is explained by a decrease in the level of hepatic clearance.

In people with problems in the liver, the values of Omzol's clearance are reduced, and the plasma half-life can last up to 3 hours. The bioavailability of drugs can exceed 90%. Therapy with 20 mg of medication per day during the first month had good tolerability - no cumulation of either omeprazole or its metabolic products was observed.

The medicine has a moderate ability to pass through the placenta. In sum, its indices inside fetal plasma are approximately 20% of the values of the mother. The substance does not accumulate inside the fetal tissues, because the release of hydrochloric acid begins to function just before birth. The medicine is not able to accumulate, nor is it activated inside the stomach and does not affect the gastrin levels (they are generally slightly elevated in the fetus shortly before birth, moreover, the gastrin does not pass through the placenta). From all this information can be deduced that the drug has no effect on the mucous membranes of the fetus.

When ingesting 40 μmol / kg of the substance in adult rats, the Cmax values reach a level of 0.4-2.4 μmol / l. Half-life is 3 hours. In very young individuals (age within 12-14 days), the plasma Cmax level when using the same dose is 15-26 μmol / l, and its elimination is very slowed down.

Dosing and administration

Capsules are taken orally; it is recommended that you do this in the morning before eating. 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 together with food.

With gastrointestinal ulcers or GERD medication is used in a dosage of 20 mg (corresponds to the 1st capsule), with a 2-fold application per day for 0.5-1 month.

During treatment of gastrinoma, the portion should be selected separately for each patient. First, it is recommended to take 60 mg of the drug 1-fold per day (3 capsules). If necessary, the dosage can be increased to 80-120 mg of the drug (corresponding to 4-6 capsules) per day (in this case, the portion is divided into 2 uses).

When treating or preventing the development of gastrointestinal ulcers, provoked by the action of NSAIDs, take Omzol 1 capsule once a day during the first month. In the absence of the desired effect after a 1-month cycle, a repeated course with the same duration is prescribed.

To destroy the bacterium H.pylori, the drug is used in complex treatment:

• 20 mg of Omzol 2 times a day, 1000 mg of amoxicillin 2 times a day, as well as 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, as well as 120 mg of bismuth subnitrate 4 times a day for 7 days.

[2]

Use Omzola during pregnancy

Pregnant and lactating women can take Omzol only after the doctor has established an accurate diagnosis (before recounting the testimony). There are only limited information on the use of the drug in pregnancy, but during these tests, there were no symptoms of toxic effects of drugs on the fetus.

Contraindications

It is contraindicated to use the medicine if the patient has a hypersensitivity to omeprazole or other medicamentous components.

Side effects Omzola

The use of capsules can trigger the development of certain side-effects:

• disorders of the hemopoiesis: there are separate data on the changes in the blood picture, treatable thrombopenia or leukopenia and pancytopenia, and also about agranulocytosis. But in these cases it was not possible to detect connections using drugs;
• disorders of the gastrointestinal tract: sometimes constipation, nausea, diarrhea, bloating (sometimes with abdominal pain) or vomiting. Often, these manifestations are weakened during the course of therapy. There is a marked dryness or inflammation of the oral mucosa, pancreatitis or candidiasis (in these cases, there was no association with taking the medication). When the drug was combined with clarithromycin, it was sometimes noted that the tongue was colored in a dark brown hue. At the end of the treatment cycle, this effect passes. Single cases were also noted with the emergence of a cyst in the glandular body, which was benign in nature and was held during the suspension of therapy;
• lesions of nails, hair and epidermis: sometimes there is a rash or itching, develops polyiform erythema, alopecia, photosensitivity and hyperhidrosis. In addition, occasionally there was a development of TEN or Stevens-Johnson syndrome;
• problems affecting the work of the liver: sometimes there are transient changes in the values of hepatic activity, disappearing after the completion of therapy. People with already existing hepatic pathology may develop hepatitis, sometimes complicated by jaundice, encephalopathy or liver failure;
• disturbances in the activity of the senses: visual disturbances sometimes occur (such as loss of visual acuity, the appearance of fog in front of the eyes, visual field defects and visual fuzziness), hearing disorders (eg, ear noise) or taste change. Usually all these problems are curable;
• symptoms of intolerance: there may be edema Quincke, urticaria, allergic vasculitis and anaphylaxis, and in addition, an increase in temperature and the constriction of the respiratory ducts;
• lesions affecting the PNS and CNS: sometimes there are sleep disorders, increased fatigue, headaches and dizziness. Usually these signs are weakened during the course of therapy. Perhaps the emergence of hallucinations or clouding of consciousness - mainly in the elderly or seriously ill people. Individual signs of aggression or depression were noted;
• other manifestations: in the course of therapy, peripheral puffiness occurred after it was completed. Occasionally, pain or weakness in the joints or muscles was observed, but in addition numbness. Uniquely reported on the emergence of gynecomastia, hyponatremia or tubulointerstitial nephritis.

[1]

Overdose

Signs of poisoning: a feeling of excitement or drowsiness, eye disorder, headaches, hyperhidrosis, nausea, hot flashes, and also tachycardia and dry mouth mucosa.

Supporting and symptomatic measures are taken to eliminate violations. The medicine does not have an antidote.

Interactions with other drugs

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

We can also expect the development of interaction with other medicines, the metabolic processes of which take place with the help of isozymes of category 2C cytochrome-P450 (for example, hexobarbital).

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

There is an opinion that the medication slows down (for example, ketoconazole) or accelerates (for example, erythromycin) the absorption of drugs whose bioavailability is associated with the pH of the stomach.

[3], [4]

Storage conditions

Omzol should be kept in a dark and dry place, closed from the access of young children. Temperature values are within the limits of 8-15 ° C.

Shelf life

Omzol is allowed to be used within 36 months from the date of manufacture of the therapeutic agent.

Application for children

Experience in the use of medication in pediatrics is lacking, which is why it is not prescribed for children.

Analogues

Analogues of the medication are medicines Pantasan, Omeprez, Omez with Ultop and Omeprazole.