Pantokar

Pantokar is a medicine used for therapy of acid-dependent pathologies. It is included in the group of drugs that slow down the activity of the proton pump.

Indications Pantocara

It is used to eliminate the following violations:

• moderate and severe stages of reflux esophagitis;
• destruction of the H.pylori bacteria in individuals with peptic ulcer disease caused by this bacteria (in combination with a certain type of antibiotic);
• peptic ulcer disease in the gastrointestinal tract;
• gastrinoma and other pathological conditions that result in hypersecretion.

Release form

The release occurs in enteric-coated tablets of 40 mg, 10 pieces per blister. There are 3 blisters in a pack.

Pharmacodynamics

The component pantoprazole is the main active medicinal element of Pantokar. It inhibits the process of secretion of hydrochloric acid. This occurs by implementing a specific effect on parietal glandulocytes (more specifically, on the proton pump).

Pantoprazole is converted into the active component in an acidic environment. In the gastric parietal glandulocytes, it inhibits the final stage of hydrochloric acid formation (H ⁺ /K ⁺ -ATPase), regardless of the origin of the stimulating substance that stimulates its formation. The degree of inhibition is determined by the dosage. The drug also inhibits stimulated and basal secretion of gastric juice.

Therapy using Pantokar reduces gastric pH, proportionally causing increased secretion of gastrin. The drug has an antibacterial effect on Helicobacter pylori and supports the manifestations of anti-Helicobacter properties of other drugs.

The pharmacological effect after a single use of the drug begins quickly and lasts for 24 hours. The drug promotes rapid weakening of pathological symptoms and healing of intestinal ulcers.

Pharmacokinetics

Absorption.

Pantoprazole is rapidly absorbed. Peak plasma levels are observed after a single dose of 40 mg. After 2.5 hours of use, on average, peak serum levels of approximately 2-3 mcg/ml are observed, and this value remains the same after repeated use. The medicinal properties of single and multiple tablets remain the same.

At doses within 10-80 mg, the pharmacokinetic properties of the drug in plasma remain linear both in the case of oral administration and intravenous injection. It was found that the bioavailability index of tablets is approximately 77%.

When combined with food, no change in AUC or peak serum values is observed, therefore, the bioavailability index is not changed. When taken with food, only the variability of the latent phase increases.

Distribution.

Protein synthesis of pantoprazole in plasma is approximately 98%. The distribution volume is approximately 0.15 l/kg.

Metabolism.

The active component undergoes almost complete hepatic metabolism. Its main route is the demethylation process involving the CYP2C19 element. Then sulfur conjugation occurs. Another route is the oxidation process involving the CYP3A4 component.

Excretion.

The terminal half-life is approximately 1 hour, with a clearance rate of 0.1 L/h/kg. Several cases of delayed excretion have been reported. Due to the specific synthesis process of pantoprazole with the proton pump located within the parietal glandulocytes, the half-life does not correlate with a longer duration of action (slowing of acid secretion).

Most of the breakdown products of the active substance are excreted in the urine (approximately 80%), and the remainder in the faeces. The main metabolite in both serum and urine is the component dismethylpantoprazole, which has undergone conjugation with sulfate.

The half-life of desmethylpantoprazole (approximately 1.5 hours) is only slightly longer than the half-life of pantoprazole.

Dosing and administration

The medicine is intended for oral use - the tablet should not be chewed, it should be swallowed whole with water.

To treat intestinal or stomach ulcers and GERD, adults should take 40 mg of the drug twice a day.

The course of therapy for a peptic ulcer of the stomach is 0.5-1.5 months; for a similar intestinal ulcer - 0.5-1 month; for GERD - 1-2 months.

When conducting maintenance treatment for GERD, it is necessary to take 40 mg of the drug once a day for 1 year.

During the treatment of exacerbated chronic hyperacid gastritis or non-ulcer dyspepsia, 40-80 mg of the drug should be taken per day for 2-3 weeks.

When treating gastrinoma, the initial dose of the drug is 3 tablets per day. If necessary, this dose can be increased. In general, dosages are selected for each person individually.

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Use Pantocara during pregnancy

Pantokar can be prescribed to nursing and pregnant women only in cases where the likelihood of benefit to the woman is higher than the risk of complications in the fetus/child.

Contraindications

Main contraindications:

• hypersensitivity to pantoprazole or other components of the drug;
• complex treatment to destroy the H.pylori bacteria in individuals with moderate or severe renal failure;
• use in combination with atazanavir,
• children under 12 years of age.

Side effects Pantocara

The use of the drug may lead to the appearance of some side effects:

• development of leukopenia or thrombocytopenia;
• epigastric pain, constipation, diarrhea or bloating;
• nausea or vomiting;
• dryness of the oral mucosa;
• edema of a peripheral nature;
• increased liver enzyme levels, increased temperature, severe hepatocellular pathology, which subsequently develops into jaundice;
• anaphylactic manifestations, including anaphylaxis;
• signs of allergy (skin rashes and itching);
• myalgia or arthralgia, erythema multiforme, TEN, urticaria, Quincke's edema and photosensitivity;
• visual disturbances, dizziness or headaches;
• tubulointerstitial nephritis;
• the appearance of hallucinations, a feeling of anxiety or disorientation, the development of depression.

Overdose

During intoxication, the patient develops a feeling of weakness or drowsiness, vomiting, dizziness, and diarrhea.

To eliminate the disorders, it is necessary to perform gastric lavage, as well as give the patient plenty of fluids and maintain the balance of water and electrolytes in the body.

Interactions with other drugs

The effect of the drug on the degree of absorption of other drugs.

Pantoprazole can reduce the absorption of medications whose bioavailability is determined by gastric pH (this list includes certain antifungal drugs - itraconazole with ketoconazole, as well as posaconazole, or other drugs such as erlotinib).

Medicines used to treat HIV (such as atazanavir).

The combination of Pantocar with atazanavir and other HIV medications, the degree of absorption of which is determined by the level of gastric pH, can cause a significant decrease in their bioavailability, and in addition affect the expression of their properties. For this reason, it is prohibited to combine these drugs in treatment.

Combination with indirect anticoagulants (such as warfarin with phenprocoumon).

Despite the absence of drug interactions when combining the drug with warfarin or phenprocoumon during clinical trials, changes in INR values were noted in post-marketing studies. Therefore, individuals using drugs from the above category need to monitor the INR/PV level from the start of therapy, after its completion, or with intermittent use of pantoprazole.

Methotrexate.

There is information about the combined use of methotrexate in large doses (for example, 0.3 g) with Pantokar. In this case, some patients experienced an increase in methotrexate levels in the blood. People using methotrexate in large doses (for example, when treating psoriasis or cancer) should temporarily stop using pantoprazole.

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Storage conditions

Pantokar should be kept in a place where moisture does not penetrate. The temperature level should not exceed 25°C.

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Shelf life

Pantokar can be used for 2 years from the date of manufacture of the drug.