Products
Rabeprazole is commercially available in the form of film-coated tablets (Pariet, generic). It has been approved in many countries since 1999. Generic versions have been available since 2012.
Structure and properties
Rabeprazole (C18H21N3O3S, Mr = 359.4 g/mol) is a benzimidazole and pyridine derivative and a racemate. It is present in drugs as rabeprazole sodium, a white to yellowish-white powder that is highly soluble in water.
Effects
Rabeprazole (ATC A02BC04) reduces gastric acid secretion 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. Rabeprazole is acid labile and must be administered in enteric-coated dosage forms. It has a short half-life of approximately one hour but has a long duration of action.
Indications
- Gastroesophageal reflux, reflux esophagitis.
- Stomach burning, acid regurgitation
- Stomach and intestinal ulcers
- Helicobacter pylori eradication in combination with antibiotics.
Dosage
According to the professional information. The tablets are usually taken once a day before breakfast.
Contraindications
- Hypersensitivity
For complete precautions, see the drug label.
Interactions
Rabeprazole is metabolized by CYP3A and CYP2C19. Corresponding interactions are possible. Interactions may occur with warfarin, ciclosporin, and clarithromycin. Increasing gastric pH may affect the absorption of other drugs.
Adverse effects
The most common possible adverse effects include indigestion, cough, sore throat, rhinitis, infections, fatigue, headache, dizziness, insomnia, and pain.
