Pantasan

Pantasan is a medicine used to eliminate GERD and ulcer diseases. Proton pump inhibitor.

Indications of the pantasana

It is used in the following pathologies: peptic ulcer in the area of the 12-colon, as well as gastric ulcer, gastroesophageal reflux, and in addition gastrinoma and other diseases that develop against a background of hypersecretion.

Release form

The release is carried out in a powder form (a sublimated substance used in the manufacture of injection solutions). Contained in a glass vial with a volume of 40 mg. Inside a separate package - 1 bottle.

Pharmacodynamics

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

In acid medium (in gastric lining cells) pantoprazole is converted into its own active form, suppressing H ⁺ / K ⁺ -ATPase (the final stage of hydrogen chloride formation). This process occurs regardless of the origin of the stimulus, which stimulates its formation.

The suppression force depends on the dose of the drug and affects the stimulated and unstimulated release of gastric juice. The use of pantoprazole reduces the index of gastric acidity, according to which the secretion of gastrin increases (this process can be reversed).

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

Pharmacokinetics

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

Pharmacokinetic properties are unchanged both in the case of single-use and repeated use of the drug. Within the limits of 10-80 mg, the substance has linear pharmacokinetics both for oral use and for administration of the IV solution.

The medicine is 98% synthesized with plasma protein.

The metabolism of the substance is carried out inside the liver. The main way of excretion of decay products is the kidneys (about 80%), and with feces 20% are excreted. The main product of disintegration (both in urine and in serum) is the component of dimethylpentoprazole, which is bound to sulfate. The half-life of the main decay product (1.5 hours) is only slightly longer than the analogous period for pantoprazole.

Dosing and administration

The medicine is allowed to be used exclusively under the supervision of the attending physician.

Administration of the solution in / in the method should be performed only when oral administration is not possible. There is information that the duration of the course of treatment with intravenous administration of the drug can be no more than 7 days. Consequently, in the case of a therapeutic option, there is a transition from intravenous administration of drugs to its oral use.

Gastroesophageal reflux, as well as gastric ulcers and ulcerative diseases in the area of the 12-colon.

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

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

With prolonged treatment of the above diseases, it is required to administer a drug in a dose of 80 mg per day. If there is such a need, it is allowed to titrate the dosage, reducing or increasing it taking into account the amount of secreted stomach acid. Daily dosages, which exceed the limit of 80 mg, are required to be divided into 2 applications. For a while, you can increase the dose to 160 mg, but the duration of use should be limited solely to the period that is needed to adequately monitor the release of acid.

If it is necessary to rapidly reduce acidity, most patients will have enough initial dosage of 2 × 80 mg to get the required value (<10 meq / h) during the first hour.

In a vial of powder, add a solution of sodium chloride (0.9%, take 10 ml of solution). Then it is immediately injected to the patient, or premixed with 100 ml of a solution of glucose (5%) or sodium chloride (0.9%), using a glass / plastic vial.

Diluted medicine retains the stability of its physical and chemical properties during the 12 hours after manufacture (temperature 25 ° C). Microbiology also suggests that the use of the solution should occur immediately after its dilution.

Do not mix the drug with other solvents, other than the above.

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

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

Persons suffering from disorders in the work of the liver (severe) should not exceed the daily dose, which is half of the standard 20 mg bottle.

[1]

Use of the pantasana during pregnancy

There are only limited data on the use of the drug in pregnant women. When appointing dosages more than 5 mg / kg, embryotoxic properties were revealed. It is not known whether there is a risk for a person. The medication is allowed to be prescribed to pregnant women only in cases when the probable benefit for a woman exceeds the possibility of the appearance of complications in the fetus.

There is information about the ingestion of the active ingredient in breast milk, so before deciding on the prescription of a medicine, it is required to evaluate the ratio of the benefit and the risk of its use.

Contraindications

Among the contraindications of drugs: intolerance of the active component of the drug and its auxiliary elements, as well as benzimidazole derivatives. In addition, one should not prescribe it 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 of the pantasana

Use of the medicine may cause the following side effects:

• hemopoietic system: thrombocyto-, leuko-, as well as pancytopenia and agranulocytosis;
• organs of the immune system: manifestations of hypersensitivity, including anaphylaxis and anaphylactic symptoms;
• metabolic disorders: the development of hyperlipidemia with an increase in lipid values (cholesterol with triglycerides), and in addition hypomagnesemia with hyponatraemia and changes in weight;
• mental disorders: hallucinations, sleep problems, and the development of confusion (often occurs in people with a tendency to such disorders, if there is an exacerbation of pathology), as well as a sense of disorientation and the state of depression (accompanied by complications);
• organs of the National Assembly: the occurrence of dizziness or headaches, as well as a violation of taste perception;
• visual organs: blurred vision or its violation;
• organs of the digestive tract: 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 hepatic-cell insufficiency or jaundice and hepatocyte damage;
• disorders of the skin: rashes, urticaria with pruritus, the development of Lyell's syndromes or Stevens-Johnson, edema Quinck, polyiform erythema and photosensitivity;
• organs of the muscular and bone structures: the development of myalgia or arthralgia, as well as fractures in the wrists, thighs and spine;
• organs of the urination system: the development of tubulointerstitial nephritis (in the future can develop into kidney failure);
• Reproductive organs: occurrence of gynecomastia;
• systemic disorders: the appearance of peripheral edemas, the development of malaise, severe fatigue or asthenia, as well as an increase in temperature and thrombophlebitis at the site of administration;
• unknown negative manifestations (the available information does not allow to determine them): the appearance of paresthesias, the development of hypokalemia or hypocalcemia (in this case can develop together with hypomagnesemia) and muscle spasms (due to an electrolyte balance disorder).

Interactions with other drugs

Influence of pantoprazole on the absorption of other drugs.

The substance can weaken the absorption of drugs, the level of bioavailability of which depends on the pH of the stomach (for example, this includes individual antimycotics, among which posaconazole with ketoconazole and itraconazole or other drugs, eg erlotinib).

Drugs used to treat HIV (eg, atazanavir).

The combination of the drug with the substance atazanavir and other drugs against HIV, the absorption index of which varies in accordance with the pH level, can cause a significant decrease in the bioavailability of these drugs, and in addition, affect their effectiveness. Because of this, such a drug combination is considered undesirable.

Anticoagulants of indirect action (such as fenprokumone with warfarin).

Although interactions in the case of a combination of Pantasana with warfarin or fenprocumone are not observed, information about changes in the values of PSI was isolated. Therefore, it is required to perform regular monitoring of the PIF / PI indicators in persons taking indirect anticoagulants together with pantoprazole, and also after its cancellation or in the case of an occasional use of this substance.

Methotrexate.

The combination of a drug with methotrexate (often in high doses) can cause an increase in the serum levels of methotrexate or its degradation product of hydrometotrexate. As a result of such a change in the values, the development of toxicity of the substance is possible. Therefore, people who use methotrexate in large doses, as well as those who suffer from psoriasis or cancer, are advised to cancel the use of pantoprazole for the duration of treatment.

Other interactions.

A significant part of pantoprazole undergo intrahepatic metabolism (with the help of the enzyme system of hemoprotein P450). The main way of this process is demethylation, in which the element 2C19 participates. The effect is carried out and with the use of other metabolic pathways (among them, oxidation with the help of the enzyme CYRZA4). Tests of drugs, the metabolism of which occurs in the same way (it is diazepam with fenprokumone, carbamazepine with glibenclamide and nifedipine, and oral contraception containing substances ethinyl estradiol with levonogestrel), did not reveal significant treatment interactions.

Studies on the possible development of interactions have shown that the active substance Pantasana does not affect the metabolism of components that change with the help of the following elements:

• CYP1A2 (this theophylline with caffeine);
• CYP2S9 (here include naproxen and piroxicam with diclofenac);
• CYP2D6 (for example, metoprolol substance);
• CYP2E1 (among these are ethanol).

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

Combination with antacid medicines does not cause significant interactions.

When studying the relationship between pantoprazole and individual antibiotics (for example, amoxicillin, as well as clarithromycin and metronidazole), it was not possible to identify important interactions.

[2], [3]

Storage conditions

The medicine should be stored in places inaccessible to young children. The temperature limit is not more than 25 ° C.

[4]

Shelf life

Pantasan is suitable for use in the period of 2 years since the release of the medicinal powder.