PANORAM [Pantoprazole] 40 mg Powder for intravenous solution

PANORAM

instructions for medical use of the medicinal product

Tradename

Panoram, Панорам

International non-proprietary name

Pantoprazole, Пантопразол

Composition

Each vial contains:

active ingredient: pantoprazole (as sodium salt) C P 40 mg

excipients: mannitol.

Dosage form

Lyophilized powder for solution for injection.

Pharmacotherapeutic group

proton pump inhibitors.

Pharmacological properties

Pharmacodynamics

Pantoprazole is a substituted benzimidazole that inhibits gastric acid secretion by specific blockade of the parietal cell proton pump. Pantoprazole is converted to its active form, cyclic sulfenamide, in an acidic environment in parietal cells, where it inhibits the enzyme H ⁺ , K ⁺ -ATPase, i.e. the final stage in the formation of hydrochloric acid in the stomach.

The inhibition is dose dependent and affects both basal and stimulated acid secretion. Relief of symptoms of heartburn and acid reflux is achieved within two weeks. As with other proton pump inhibitors and H2 receptor inhibitors, treatment with pantoprazole reduces acidity in the stomach and thereby increases gastrin levels in proportion to the decrease in acidity. The increase in gastrin content is reversible . Because the drug binds to an enzyme distal to the receptor, it can inhibit the secretion of hydrochloric acid, regardless of stimulation by other substances (acetylcholine, histamine, gastrin). The effect is the same regardless of whether the active substance is taken orally or intravenously.

Pharmacokinetics

Pantoprazole is rapidly absorbed, and the maximum plasma concentration (C max) is reached after a single dose of 40 mg. On average, 2.5 hours after administration, the maximum serum concentration is reached at a level of about 2-3 μg / ml, the concentration remains stable after repeated administration. Pharmacokinetic properties do not change after a single or repeated administration. In the dose range from 10 to 80 mg, the pharmacokinetics of pantoprazole in blood plasma remains linear, both when administered orally and intravenously. It is established that the bioavailability of tablets is about 77%. Simultaneous ingestion of food does not affect the area under the concentration-time curve (AUC) or maximum concentration, and, accordingly, bioavailability. With the simultaneous intake of food, only the variability of the latent period increases.

Plasma protein binding is 98%. The volume of distribution is 0.15 l/kg, the clearance is 0.1 l/h/kg.

Metabolized in the liver. The main metabolite in plasma and urine is desmethylpantoprazole, conjugated with sulfate.

The half-life (T1 / 2) of pantoprazole is 1 hour, the metabolite is 1.5 hours. The main route of elimination is through the kidneys (about 80%) in the form of metabolites of pantoprazole, a small amount is excreted through the intestines.

Indications for use

Reflux esophagitis.

Duodenal ulcer.

Gastric ulcer.

Zollinger-Ellison syndrome and other hypersecretory pathological conditions.

Contraindications

Dyspepsia of neurotic origin.

Malignant diseases of the gastrointestinal tract.

Hypersensitivity to pantoprazole.

Children's age up to 18 years.

Dosage and administration

Intravenously. Intravenous use of the drug is recommended only if it is impossible to use the oral form of the drug. When clinically possible, the transition from intravenous administration of Panoram to oral is carried out.

The drug should be used by adults as directed and under the direct supervision of a physician.

Reflux esophagitis, duodenal ulcer, gastric ulcer

The recommended dose is 40 mg pantoprazole (1 vial) per day.

Treatment of Zollinger-Ellison syndrome and other hypersecretory pathological conditions

For long-term treatment of Zollinger-Ellison syndrome and other hypersecretory pathological conditions, the recommended dose of pantoprazole is 80 mg per day. If necessary, the dose can be titrated, increasing or decreasing, depending on the indicators of acid secretion in the stomach. Doses exceeding 80 mg per day should be divided into two doses. It is possible to temporarily increase the dose of pantoprazole to more than 160 mg, but the duration of use should be limited only to the period necessary to adequately control acid secretion.

In the event that a rapid reduction in acidity is required, for most patients an initial dose of 2×80 mg is sufficient to achieve the desired level (<10 meq/h) within 1 hour.

Preparation for use

Dissolve the powder in 10 ml of 0.9% sodium chloride solution, which is added to the vial. The solution can be administered directly or after mixing with 100 ml of 0.9% sodium chloride solution or 5% glucose solution in plastic or glass vials.

After dilution, the chemical and physical stability of the drug is maintained for 12 hours at a temperature of 25 ° C. The diluted drug must be used immediately.

Pantoprazole must not be prepared or mixed with other solvents than those mentioned above.

The introduction of the drug should be carried out within 2-15 minutes.

Patients with severely impaired liver function should not exceed a daily dose of 20 mg (½ bottle of pantoprazole, 40 mg powder).

Special instructions and precautions

Before starting treatment with the drug, the possibility of a malignant neoplasm should be excluded, since the drug may mask the symptoms and delay the correct diagnosis.

The diagnosis of reflux esophagitis requires mandatory endoscopic confirmation.

Pantoprazole is not recommended for use together with HIV protease inhibitors, the absorption of which depends on the pH of the stomach (for example, atazanovir), due to a significant decrease in their bioavailability.

Long-term therapy, especially for more than 1 year, requires regular monitoring of patients.

In patients with severe hepatic impairment, liver enzymes should be regularly monitored during treatment with pantoprazole, especially with long-term use. In case of increased activity of liver enzymes, treatment should be discontinued.

In patients with Zollinger-Ellison syndrome and other pathological hypersecretory conditions requiring long-term therapy, pantoprazole, like all antisecretory agents, may reduce the absorption of vitamin B ₁₂ (cyanocobalamin) due to hypo- or achlorhydria. This should be considered in patients with reduced stores of this vitamin or in the presence of risk factors for reducing its absorption during long-term therapy or in the presence of relevant clinical symptoms.

Treatment with pantoprazole may lead to a slightly increased risk of gastrointestinal infections caused by bacteria such as Salmonella and Campylobacter or   C. difficile .

Patients over the age of 55 with new or recently changed symptoms should consult a physician.

Influence on the ability to drive vehicles and mechanisms

You should refrain from driving vehicles and other mechanisms that require increased attention, due to the likelihood of dizziness.

Use during pregnancy and during breastfeeding

During pregnancy, it is possible only under strict indications, when the benefit to the mother outweighs the potential risk to the fetus. At the time of treatment should stop breastfeeding.

Interaction with other drugs

If you are taking any other medicines, be sure to inform your doctor, and if you are self-treating, consult your doctor about the possibility of using the drug.

Attention should be paid to concomitant use with drugs whose absorption is pH-dependent (ketoconazole, itraconazole, posaconazole, erlotinib), due to changes in the absorption of these drugs.
When used together, it significantly reduces the effectiveness of atazanavir.

In the setting of high-dose methotrexate for cancer and psoriasis, temporary withdrawal of pantoprazole may be considered.
Side effect

On the part of the digestive system: polyps from the fundic glands (benign), diarrhea, nausea, vomiting, bloating, constipation, dry mouth, abdominal pain and discomfort, microscopic colitis, increased levels of liver enzymes (transaminases, g-HT), increased bilirubin level.

From the nervous system: headache, dizziness, taste disturbances, sleep disorders, depression, confusion.

On the part of the organs of vision: blurred vision, blurred vision.

From the skin and subcutaneous tissues: skin rash, rash, itching, urticaria, angioedema, Stevens-Johnson syndrome, Lyell's syndrome, erythema multiforme.

From the blood and lymphatic system: agranulocytosis, leukopenia, thrombocytopenia.

Metabolism and metabolic disorders: hyperlipidemia and increased lipid levels (triglycerides, cholesterol), changes in body weight.

General disorders: thrombophlebitis at the injection site, asthenia, fatigue, malaise, fever, peripheral edema.

Overdose

In case of overdose with clinical signs of intoxication, apart from symptomatic and supportive treatment, there are no separate therapeutic recommendations.

Storage conditions

Store in a place protected from light, at a temperature not exceeding 30 ⁰ С.

Keep out of the reach of children!

Best before date

3 years. Do not use after the expiry date stated on the packaging.

Holiday conditions

Released by prescription.

Release form

1 bottle with instructions for use in a cardboard box.