Pantasan

Pantasan is a drug used to treat GERD and ulcers. It is a proton pump inhibitor.

Indications Pantasana

It is used for the following pathologies: peptic ulcer in the duodenum, as well as gastric ulcer, gastroesophageal reflux, and in addition gastrinoma and other diseases that develop against the background of hypersecretion.

Release form

It is released in powder form (a sublimated substance used in the manufacture of injection solutions). It is contained in a glass bottle with a volume of 40 mg. Inside a separate package there is 1 bottle.

Pharmacodynamics

The active component of the drug is pantoprazole. This substance inhibits the secretion of hydrochloric gastric acid (specifically affects the proton pump of parietal cells).

In an acidic environment (in the gastric parietal cells), pantoprazole is converted into its own active form, inhibiting H ⁺ /K ⁺ -ATPase (the final stage of hydrogen chloride formation). This process occurs regardless of the origin of the irritant that stimulates its formation.

The strength of suppression depends on the dose of the drug and affects stimulated and unstimulated secretion of gastric juice. The use of pantoprazole reduces the gastric acidity index, accordingly increasing the secretion of gastrin (this process can be reversed).

Because the active substance is synthesized with enzymes that are distant from the cell receptors, it stimulates the release of hydrogen chloride regardless of the action of other elements (such as histamine and acetylcholine, as well as gastrin).

Pharmacokinetics

The distribution volume is 0.15 l/kg, and its clearance rate is approximately 0.1 l/h/kg. The half-life is approximately 1 hour. Since pantoprazole acts specifically inside the parietal cells, its half-life does not correlate with the duration of action (suppression of the acid secretion process).

Pharmacokinetic properties are unchanged in both single and multiple doses of the drug. Within the dosage range of 10-80 mg, the substance has linear pharmacokinetics both when taken orally and when administered intravenously.

The drug is 98% synthesized with plasma protein.

The substance is metabolized in the liver. The main route of excretion of decay products is the kidneys (about 80%), and 20% is excreted with feces. The main decay product (in both urine and serum) is the component dismethylpantoprazole, which is associated with sulfate. The half-life of the main decay product (1.5 hours) is only slightly longer than that of pantoprazole.

Dosing and administration

The medicine may be used only under the supervision of a physician.

The intravenous administration of the solution should be performed only when oral administration is impossible. There is information that the duration of the course of treatment with intravenous administration of the drug may not exceed 7 days. As a result, if there is a therapeutic opportunity, a transition from intravenous administration of the drug to its oral use occurs.

Gastroesophageal reflux, as well as gastric ulcers and ulcerative diseases in the duodenum.

The recommended daily dosage is 40 mg of the drug (1 bottle).

Elimination of gastrinoma and other diseases associated with the development of hypersecretion.

In long-term treatment of the above-mentioned diseases, it is necessary to administer the drug in a dose of 80 mg per day. If there is such a need, it is allowed to titrate the dosage, decreasing or increasing it taking into account the amount of secreted gastric acid. Daily dosages that exceed the limit of 80 mg must be divided into 2 applications. For a while, the dose can be increased to 160 mg, but the duration of use should be limited exclusively to the period needed for adequate monitoring of acid secretion.

If a rapid reduction in acidity is required, most patients will benefit from an initial dose of 2×80 mg to achieve the desired level (<10 mEq/hour) within 1 hour.

Sodium chloride solution (0.9%; take 10 ml of solution) must be added to the vial with the powder. Then it is immediately administered to the patient, or pre-mixed with 100 ml of glucose solution (5%) or sodium chloride (0.9%), using glass/plastic vials for this purpose.

The diluted medicine retains the stability of its physical and chemical properties for 12 hours after production (temperature 25°C). Microbiology suggests that the solution should be used immediately after dilution.

It is prohibited to mix the medicine with solvents other than those listed above.

The medicine is administered intravenously for about 2-15 minutes.

The bottle is intended for single use only. Before starting the procedure, it is necessary to inspect it, checking the color of the medicine, as well as the presence of sediment. The diluted solution should be transparent, with a yellowish tint.

People suffering from liver dysfunction (severe) should not exceed the daily dose, which is half of the standard bottle – 20 mg.

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Use Pantasana during pregnancy

There are limited data on the use of the drug in pregnant women. Embryotoxic properties were detected at doses greater than 5 mg/kg. It is unknown whether there is a risk to humans. The drug is only approved for use in pregnant women when the potential benefit to the woman outweighs the risk of complications to the fetus.

There is information about the active ingredient getting into breast milk, therefore, before deciding on prescribing the drug, it is necessary to assess the benefit-risk ratio of its use.

Contraindications

Contraindications of the drug include: intolerance to the active ingredient of the drug and its auxiliary elements, as well as benzimidazole derivatives. In addition, it cannot be prescribed to children, because information about the effectiveness of the drug and the safety of its use in this group of patients is limited.

Side effects Pantasana

Using the medicine may cause the following side effects:

• hematopoietic system: thrombocyto-, leukopenia-, as well as pancytopenia and agranulocytosis;
• immune system organs: manifestations of hypersensitivity, including anaphylaxis and anaphylactic symptoms;
• metabolic disorders: development of hyperlipidemia with an increase in lipid indices (cholesterol with triglycerides), and in addition hypomagnesemia with hyponatremia and changes in weight;
• mental disorders: hallucinations, sleep problems and the development of confusion (often occurs in people who are prone to such disorders; if they are present, the pathology worsens), as well as a feeling of disorientation and depression (accompanied by complications);
• nervous system organs: occurrence of dizziness or headaches, as well as disturbance of taste perception;
• visual organs: blurred vision or its impairment;
• digestive tract organs: the appearance of constipation or diarrhea, vomiting, flatulence, nausea, abdominal pain or discomfort in this area, as well as dryness of the oral mucosa;
• organs of the hepatobiliary system: an increase in bilirubin and liver enzymes (such as GGT and transaminases), as well as the development of hepatocellular insufficiency or jaundice and damage to hepatocytes;
• skin disorders: rashes, urticaria with itching, development of Lyell's or Stevens-Johnson syndromes, Quincke's edema, erythema multiforme and photosensitivity;
• organs of muscular and skeletal structures: development of myalgia or arthralgia, as well as fractures in the area of the wrists, hips and spine;
• urinary system organs: development of tubulointerstitial nephritis (may later develop into renal failure);
• reproductive organs: occurrence of gynecomastia;
• systemic disorders: the appearance of peripheral edema, the development of malaise, severe fatigue or asthenia, as well as an increase in temperature and thrombophlebitis at the injection site;
• unknown adverse effects (available information does not allow us to determine them): the appearance of paresthesia, the development of hypokalemia or hypocalcemia (in this case, it can develop together with hypomagnesemia) and muscle spasms (due to electrolyte imbalance).

Interactions with other drugs

The effect of pantoprazole on the absorption of other drugs.

The substance may reduce the absorption of drugs whose bioavailability level depends on the pH of the stomach (for example, this includes certain antifungal drugs, including posaconazole with ketoconazole and itraconazole, or other drugs, such as erlotinib).

Medicines used to treat HIV (eg, atazanavir).

Combination of the drug with atazanavir and other anti-HIV drugs whose absorption rate changes in accordance with pH level may cause a significant decrease in the bioavailability of these drugs, and also affect their effectiveness. For this reason, such a drug combination is considered undesirable.

Indirect anticoagulants (such as phenprocoumon with warfarin).

Although no interactions have been observed when Pantasan is combined with warfarin or phenprocoumon, there have been isolated reports of changes in INR values. Therefore, regular monitoring of INR/PT values is required in individuals taking indirect anticoagulants together with pantoprazole, as well as after its withdrawal or in case of irregular use of this substance.

Methotrexate.

Combination of the drug with methotrexate (often in high doses) may cause an increase in serum levels of methotrexate or its breakdown product hydromethotrexate. As a result of such a change in values, toxicity of the substance may develop. Therefore, people who use methotrexate in high doses, as well as those who have psoriasis or cancer, are advised to stop using pantoprazole for the duration of treatment.

Other interactions.

A significant portion of pantoprazole undergoes intrahepatic metabolism (using the enzyme system of hemoprotein P450). The main route of this process is demethylation, in which the element 2C19 is involved. The effect is also carried out using other metabolic pathways (including oxidation using the enzyme CYP3A4). Tests of drugs that are metabolized in the same way (diazepam with phenprocoumon, carbamazepine with glibenclamide and nifedipine, as well as oral contraception containing the substances ethinyl estradiol with levonorgestrel) did not reveal interactions that are significant for treatment.

Studies on the possible development of interactions have shown that the active substance of Pantasan does not affect the process of metabolism of components that are modified by the following elements:

• CYP1A2 (this is theophylline with caffeine);
• CYP2C9 (this includes naproxen and piroxicam with diclofenac);
• CYP2D6 (for example, the substance metoprolol);
• CYP2E1 (including ethanol).

The drug does not affect the activity of p-glycoprotein, which ensures the absorption of the substance digoxin.

Combination with antacid drugs does not cause the development of significant interactions.

Studies of the interaction between pantoprazole and individual antibiotics (eg, amoxicillin, as well as clarithromycin and metronidazole) failed to identify significant interactions.

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Storage conditions

The medicine should be stored in places inaccessible to small children. The temperature limit is no more than 25°C.

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Shelf life

Pantasan is suitable for use for a period of 2 years from the date of release of the medicinal powder.