Sunpraz^® (Tablets, Lyophilisate) Instructions for Use

ATC Code

A02BC02 (Pantoprazole)

Active Substance

Pantoprazole (Rec.INN registered by WHO)

Clinical-Pharmacological Group

H⁺-K⁺-ATPase inhibitor. Antiulcer drug

Pharmacotherapeutic Group

Acid-related disorder treatment agents; antiulcer agents for the treatment of gastroesophageal reflux disease (GERD); proton pump inhibitors

Pharmacological Action

H⁺-K⁺-ATPase inhibitor. It blocks the final stage of hydrochloric acid secretion, reducing both basal and stimulated (regardless of the nature of the stimulus) secretion. In Helicobacter pylori-associated duodenal ulcer disease, the reduction in gastric secretion increases the microorganism’s sensitivity to antibiotics.

It does not affect gastrointestinal motility.

With intravenous administration of 80 mg, the antisecretory effect reaches its maximum within 1 hour and lasts for 24 hours. Secretory activity normalizes 3-4 days after discontinuation of the drug.

Pharmacokinetics

In the dose range from 10 to 80 mg, the pharmacokinetic parameters of pantoprazole show linear dependence after intravenous administration. The drug does not accumulate. The values of pantoprazole pharmacokinetic parameters after multiple and single administrations are comparable.

Distribution

V_d is 0.15 L/kg. The drug is mainly distributed in the extracellular fluid. Plasma protein binding is 98%.

Metabolism

It is extensively metabolized in the liver, primarily by the CYP2C19 enzyme system. The main metabolite in plasma and urine is desmethylpantoprazole, conjugated with sulfate.

Excretion

T_1/2 after intravenous administration averages 1 hour. Most of the drug is excreted by the kidneys as inactive metabolites. Small amounts are excreted via the intestines.

Pharmacokinetics in special clinical situations

In patients with renal impairment, pharmacokinetics do not change significantly.

In hepatic impairment, the duration of T_1/2 increases to 7-9 hours. AUC values are 5-7 times higher and C_max is 1.5 times higher in patients with hepatic impairment compared to healthy volunteers.

Indications

• Gastric and duodenal ulcer (in the acute phase), erosive gastritis (including that associated with NSAID use);
• Gastroesophageal reflux disease (GERD): erosive reflux esophagitis (treatment), symptomatic treatment of GERD (i.e., NERD – non-erosive reflux disease);
• Zollinger-Ellison syndrome;
• Eradication of Helicobacter pylori in combination with antibacterial agents;
• Treatment and prevention of stress ulcers, as well as their complications (bleeding, perforation, penetration).

ICD codes

Dosage Regimen

Tablets

For gastric and duodenal ulcers, erosive gastritis, the drug is prescribed at 40-80 mg/day. The course of treatment for exacerbation of duodenal ulcer is 2 weeks, and for gastric ulcer – 4-8 weeks.

For prevention of exacerbations of gastric and duodenal ulcers, 20 mg/day is prescribed.

For eradication of Helicobacter pylori, take 40 mg twice daily in combination with antimicrobial agents. The course of therapy is 7-14 days.

For erosive-ulcerative lesions of the stomach and duodenum associated with NSAID use, 40-80 mg/day is prescribed. The course of treatment is 4-8 weeks. For prevention of erosive lesions during long-term NSAID use – 20 mg/day.

For reflux esophagitis, 20-40 mg/day is prescribed. The course of therapy is 4-8 weeks. For prevention of exacerbations, take 20 mg/day.

In patients with severe hepatic impairment, the dose should be reduced to 40 mg once every 2 days, and blood biochemical parameters should be monitored. If liver enzyme activity increases, the drug should be discontinued.

The tablets should be taken orally whole (without chewing or dissolving), with a sufficient amount of fluid. The drug is recommended to be taken 1 hour before breakfast; if taken twice daily, the second dose should be taken 1 hour before dinner.

Lyophilisate

This dosage form of Sunpraz^® is indicated only for intravenous administration. The drug is recommended only in cases where oral administration of pantoprazole is not indicated. As soon as oral therapy becomes possible, intravenous administration should be discontinued.

The recommended dose for intravenous administration is the contents of one vial (40 mg pantoprazole) once daily. Data on intravenous administration allow for use for 7-10 days; extension of the treatment course depends on clinical necessity.

For long-term treatment of Zollinger-Ellison syndrome and other pathological hypersecretory conditions, the recommended initial daily dose is 80 mg of Sunpraz^®. After that, the dose may be increased or decreased. If the drug is used at a daily dose exceeding 80 mg, the dose should be divided and administered twice daily. A temporary increase in the daily dose to 160 mg of Sunpraz^® is possible.

For eradication of Helicobacter pylori in combination with antibacterial agents, the recommended daily dose is 80 mg of Sunpraz^® for 7-10 days; the dose should be divided and administered twice daily.

In severe hepatic impairment, the daily dose must be reduced to 20 mg of pantoprazole. Furthermore, such patients require regular monitoring of liver enzyme activity during treatment with the drug. If liver enzyme activity increases, treatment must be discontinued.

For elderly patients, as well as patients with impaired renal function (including those on hemodialysis), there is no need to increase the daily dose of pantoprazole 40 mg.

Rules for preparation and administration of the drug

The contents of the vial must be reconstituted before injection using 10 ml of 0.9% sodium chloride solution.

This solution is administered as a bolus injection or as an infusion after mixing with 100 ml of 0.9% sodium chloride solution, 5% glucose solution, or 10% glucose solution. The pH value of the ready-to-use solution should be in the range of 9-10.

The duration of administration should be 2-15 minutes. The prepared solution should be used within 3 hours after preparation.

Adverse Reactions

When taking Sunpraz^® according to the indications and in recommended doses, adverse reactions occur extremely rarely.

From the central nervous system sometimes – headache; rarely – depression, hallucinations (especially in predisposed patients), disorientation and confusion; in isolated cases – dizziness or visual disturbance.

From the digestive system sometimes – pain in the upper abdomen, diarrhea, constipation, flatulence; rarely – nausea, vomiting, dry mouth; very rarely – hepatocellular failure leading to jaundice with or without hepatic failure, increased activity of liver enzymes (transaminases, glutamyltranspeptidase).

From the musculoskeletal system rarely – arthralgia; in isolated cases – myalgia.

From the hematopoietic system very rarely – leukopenia, thrombocytopenia.

Allergic reactions very rarely – anaphylactic reactions, including anaphylactic shock, urticaria, angioedema.

Dermatological reactions very rarely – itching, skin rash, severe skin reactions (Stevens-Johnson syndrome, erythema multiforme, photosensitivity, Lyell’s syndrome);

Local reactions very rarely – phlebitis, thrombophlebitis.

Other very rarely – peripheral edema, increased triglycerides, interstitial nephritis; in isolated cases – increased body temperature.

Contraindications

• Dyspepsia of neurotic origin,
• Lactation period;
• Children under 18 years of age;
• Hypersensitivity to the drug.

With caution, the drug should be used during pregnancy and in hepatic insufficiency.

Use in Pregnancy and Lactation

Experience with the drug during pregnancy and lactation is limited. The drug can be used during pregnancy only if the benefit to the mother outweighs the potential risk to the fetus.

There are no data on the excretion of pantoprazole into breast milk. Breastfeeding should be discontinued during drug administration.

In experimental studies of reproductive function, slight embryotoxicity was noted at doses exceeding 5 mg/kg.

Use in Hepatic Impairment

In severe hepatic impairment, the daily dose must be reduced to 20 mg of pantoprazole. Furthermore, such patients require regular monitoring of liver enzyme activity during treatment with the drug. If liver enzyme activity increases, treatment must be discontinued.

Use in Renal Impairment

Patients with impaired renal function (including those on hemodialysis) do not require an increase in the daily dose of pantoprazole 40 mg.

Pediatric Use

Contraindication: children under 18 years of age.

Geriatric Use

Elderly patients do not require an increase in the daily dose of pantoprazole 40 mg.

Special Precautions

The use of pantoprazole for dyspepsia of neurogenic origin is not effective.

In the presence of any alarm symptoms (e.g., significant unintentional weight loss, recurrent vomiting, dysphagia, anemia, or melena) and in case of suspected or confirmed gastric ulcer, the possibility of a malignant neoplasm should be excluded, because treatment with pantoprazole may alleviate symptoms and delay the correct diagnosis. If symptoms persist despite adequate treatment, further investigation should be performed.

Endoscopic control before and after treatment is mandatory to exclude the possibility of malignant diseases of the stomach or esophagus, as treatment may mask symptoms and delay correct diagnosis.

Use in pediatrics

There is insufficient data on the use of the drug in children under 18 years of age.

Effect on ability to drive vehicles and operate machinery

The use of the drug does not affect the patient’s ability to perform work requiring increased attention and speed of psychomotor reactions.

Overdose

Symptoms of overdose in humans are unknown. Doses up to 240 mg with intravenous administration were well tolerated.

Treatment in case of overdose with signs of intoxication includes general detoxification measures, symptomatic therapy, hemodialysis.

Drug Interactions

Concomitant use of Sunpraz^® may reduce the absorption of drugs whose bioavailability depends on gastric pH (including ketoconazole, iron salts, ritonavir).

When Sunpraz^® is used concomitantly with atazanavir, plasma concentrations of atazanavir decrease and its therapeutic effect is reduced.

In specific tests of Sunpraz^® with drugs such as digoxin, nifedipine, metoprolol, amoxicillin, clarithromycin, oral contraceptives (levonorgestrel/ethinyl estradiol), diclofenac, phenazone, naproxen, piroxicam, glibenclamide, levothyroxine sodium, diazepam, carbamazepine, phenytoin, cyclosporine, tacrolimus, cisapride, midazolam, metronidazole, theophylline, caffeine, ethanol, no clinically significant interaction was found.

According to post-marketing data, concomitant use of the drug with warfarin increases prothrombin time, which can lead to bleeding, including fatal outcomes. It is recommended to determine prothrombin time.

Storage Conditions

The drug should be stored in a dry, light-protected place, out of the reach of children, at a temperature not exceeding 25°C (77°F).

Shelf Life

Shelf life of the lyophilisate is 2 years, of the solvent – 3 years.

Dispensing Status

The drug is dispensed by prescription.

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.