Products
Pantoprazole is commercially available in the form of enteric-coated tablets and has been approved in many countries since 1997 (Pantozol, generic). Less commonly used are the granules and the injectable.
Structure and properties
Pantoprazole (C16H15F2N3O4S, Mr = 383.37 g/mol) is a benzimidazole derivative and a racemate. In tablets, it is present as sodium salt and sesquihydrate (1.5 H2O), a white powder that is soluble in water.
Effects
Pantoprazole (ATC A02BC02) reduces secretion of gastric acid by inhibiting the proton pump (H+/K+-ATPase) in the gastric vestibular cells irreversibly. It does not act locally in the lumen of the stomach but is absorbed in the intestine and travels to the vestibular cells via the systemic circulation. It is a prodrug and is converted from acid to its active form only in the canaliculi of the vestibular cells, where it binds covalently to the proton pump, inhibiting it. Pantoprazole is acid labile and must be administered in enteric-coated dosage forms. Inhibition of gastric acid secretion is dose-dependent and the full effect is delayed within 3 to 5 (max. 7) days. Because of covalent binding, pantoprazole is effective for much longer than its short half-life of 1.5 h would suggest, and once-daily dosing is sufficient in most patients.
Indications
- Self-medication: short-term treatment of reflux symptoms (e.g., burning stomach, acid regurgitation) in adults 18 years of age and older.
- Reflux disease, reflux esophagitis.
- Infection with Helicobacter pylori in combination with two antibiotics for gastric or intestinal ulcer.
- Prevention of gastric and intestinal ulcers caused by treatment with NSAIDs (gastroprotection).
- Zollinger-Ellison syndrome and other diseases with increased formation of gastric acid.
Dosage
According to the professional information. The tablets are taken once or twice a day, depending on the indication, and before meals.
Contraindications
- Hypersensitivity
- Children, pregnancy and lactation: see SmPC.
For full precautions, see the drug label.
Interactions
Because pantoprazole inhibits gastric acid secretion, it may affect the absorption of drugs if this is pH-dependent. This is true, for example, of the antimyotic ketoconazole, which dissolves more poorly in the basic range because it is deprotonated and thus becomes more lipophilic. It is recommended that ketoconazole be taken with an acidic beverage (e.g., Coca-Cola). The absorption of the HIV protease inhibitor atazanavir is pH-dependent and its bioavailability is significantly impaired by pantoprazole. Therefore, concomitant use is not recommended. Pantoprazole is biotransformed to inactive metabolites by CYP2C19 and CYP3A. According to the SmPC, no clinically relevant interactions have been demonstrated to date. The interaction potential is considered to be lower compared with omeprazole. Prothrombin time/INR should be monitored in patients treated with vitamin K antagonists.
Adverse effects
The most common adverse effects include:
- Headache, dizziness
- Visual disturbances (blurred vision)
- Nausea, vomiting, diarrhea, constipation, abdominal pain, upper abdominal discomfort, flatulence.
- Allergy and itching
Magnesium deficiency may occur under PPI, especially during long therapy. In long-term therapy, magnesium levels should be monitored regularly. The intake of vitamin B12 may also be reduced.