Peptazol (Tablets) 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

Proton pump inhibitor

Pharmacological Action

Pantoprazole is an H⁺-K⁺-ATPase inhibitor. It blocks the final stage of hydrochloric acid secretion, reducing the level of both basal and stimulated (regardless of the type of stimulus) hydrochloric acid secretion in the stomach.

In duodenal ulcer disease associated with Helicobacter pylori, this reduction in gastric secretion increases the microorganism’s sensitivity to antibiotics. Pantoprazole has its own antimicrobial activity against Helicobacter pylori.

Pharmacokinetics

Pantoprazole is rapidly absorbed after oral administration. The C_max after the first 20 mg dose is approximately 1.0-1.5 µg/ml.

The pharmacokinetics of pantoprazole after single and multiple administration are identical. In the dose range of 10-80 mg, the pharmacokinetics of pantoprazole in plasma remain linear for both oral and intravenous administration.

The absolute bioavailability of pantoprazole after oral administration is about 77%. Plasma protein binding is 98%. The V_d is 0.15 l/kg.

It is metabolized primarily in the liver. The main metabolic pathway is demethylation by CYP2C19 followed by sulfate conjugation. Other metabolic pathways include oxidation by CYP3A4.

The terminal T_1/2 is approximately 1 hour, and clearance is about 0.1 l/h/kg.

The main route of excretion is via the kidneys (about 80%) as pantoprazole metabolites, with the remainder excreted in feces.

Indications

Gastric and duodenal ulcer in the acute phase, erosive gastritis (including that associated with NSAID use), stress ulcers and their complications (bleeding, perforation, penetration); Zollinger-Ellison syndrome; eradication of Helicobacter pylori (in combination with antibacterial therapy); gastroesophageal reflux disease; erosive reflux esophagitis.

ICD codes

Dosage Regimen

Take tablets orally, swallowed whole with water before a meal. Do not crush or chew.

For erosive reflux esophagitis, use 40 mg once daily for 4-8 weeks. For maintenance therapy, use 20 mg once daily.

For gastric and duodenal ulcers in the acute phase, use 40 mg once daily for 2-4 weeks.

For Helicobacter pylori eradication, use 40 mg twice daily in combination with two antibiotics for 7-14 days.

For Zollinger-Ellison syndrome, use an initial dose of 80 mg twice daily. Adjust the dose individually; daily doses above 160 mg divide into three administrations.

For NSAID-associated gastric erosions and ulcers, use 20 mg once daily.

In patients with severe hepatic impairment, do not exceed a maximum daily dose of 20 mg.

In patients with renal impairment or the elderly, do not exceed a maximum daily dose of 40 mg.

The duration of treatment is determined by the indication and clinical response. Do not use for longer than prescribed.

Adverse Reactions

Hematopoietic system: rarely – agranulocytosis; very rarely – thrombocytopenia, leukopenia, pancytopenia.

Nervous system: infrequently – headache, dizziness; rarely – taste disturbances; frequency unknown – paresthesia.

Psychiatric disorders: infrequently – sleep disorders; rarely – depression (including exacerbation of existing disorders); very rarely – disorientation (including exacerbation of existing disorders); frequency unknown – hallucinations, confusion (especially in predisposed patients), as well as possible exacerbation of symptoms if they existed prior to the start of therapy.

Organ of vision: rarely – blurred vision.

Digestive system: frequently – gastric fundic gland polyps (benign); infrequently – diarrhea, nausea, vomiting, abdominal distension, flatulence, constipation, dry mouth, abdominal discomfort and pain.

Liver and biliary tract: infrequently – increased activity of liver enzymes (transaminases, γ-glutamyltransferase); rarely – increased bilirubin levels; frequency unknown – hepatocellular damage, jaundice, hepatocellular failure.

Urinary system: frequency unknown – interstitial nephritis.

Musculoskeletal system: infrequently – fractures of the wrist, hip, spine; rarely – arthralgia, myalgia.

Metabolism: rarely – hyperlipidemia, changes in body weight; frequency unknown – hyponatremia, hypomagnesemia.

Immune system: rarely – hypersensitivity reactions (including anaphylactic reactions and anaphylactic shock), angioedema.

Reproductive system: rarely – gynecomastia.

Skin and subcutaneous tissues: infrequently – exanthema/rash, itching, dermatitis; rarely – urticaria; frequency unknown – malignant exudative erythema (Stevens-Johnson syndrome), exudative erythema multiforme, toxic epidermal necrolysis, photosensitivity, subacute cutaneous lupus erythematosus.

General reactions: infrequently – weakness, fatigue, general malaise; rarely – increased body temperature, peripheral edema.

Contraindications

Hypersensitivity to pantoprazole; neurogenic dyspepsia, malignant diseases of the gastrointestinal tract, severe hepatic insufficiency; pregnancy, lactation (breastfeeding); childhood; use of HIV protease inhibitors such as atazanavir and nelfinavir, whose absorption depends on gastric juice pH (for oral administration).

Use with caution in hepatic insufficiency.

Use in Pregnancy and Lactation

Contraindicated for use during pregnancy and lactation (breastfeeding).

If use during lactation is necessary, the issue of discontinuing breastfeeding should be considered.

Use in Hepatic Impairment

Contraindicated for use in severe hepatic insufficiency. When used in patients with impaired liver function, plasma liver enzyme activity should be regularly monitored and Pantoprazole should be discontinued if it increases.

Use in Renal Impairment

In case of impaired renal function, it is not recommended to exceed the dose of 40 mg/day.

Pediatric Use

Use in children and adolescents under 18 years of age is contraindicated.

Geriatric Use

Proton pump inhibitors, especially when used in high doses and for long periods (more than 1 year), may moderately increase the risk of fractures of the hip, wrist, and spine, predominantly in the elderly. In elderly patients, it is not recommended to exceed the dose of 40 mg/day.

Special Precautions

Intravenous use of pantoprazole is recommended only if oral administration is not possible.

Before starting therapy, the possibility of a malignant neoplasm in the stomach and esophagus should be excluded, because the use of pantoprazole reduces the severity of symptoms and may delay the establishment of a correct diagnosis. The diagnosis of reflux esophagitis requires mandatory endoscopic confirmation.

In elderly patients and in patients with impaired renal function, it is not recommended to exceed the dose of 40 mg/day.

When used in patients with impaired liver function, plasma liver enzyme activity should be regularly monitored and Pantoprazole should be discontinued if it increases.

Proton pump inhibitors, especially when used in high doses and for long periods (more than 1 year), may moderately increase the risk of fractures of the hip, wrist, and spine, predominantly in the elderly or in the presence of other risk factors.

Effect on ability to drive vehicles and operate machinery

During the use of pantoprazole, patients should exercise caution when driving vehicles and operating machinery, as well as when engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Drug Interactions

With simultaneous use, Pantoprazole may alter the absorption of drugs whose absorption depends on the pH of the gastric contents (e.g., ketoconazole, itraconazole, posaconazole and other drugs such as erlotinib).

Concomitant use of pantoprazole and HIV protease inhibitors, whose absorption depends on the acidity (pH) of gastric juice, such as atazanavir, nelfinavir, significantly reduces their bioavailability.

Since Pantoprazole is metabolized in the liver by the cytochrome P450 enzyme system, the possibility of drug interaction with drugs metabolized by the same enzyme system cannot be excluded.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

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.