Trade Names:Aciphex- Tablets, delayed-release 20 mgPariet (Canada)
Suppresses gastric acid secretion by blocking acid (proton) pump within gastric parietal cells.
T max is 2 to 5 h. Oral bioavailability is about 52%.
Protein binding is 96.3%.
Extensively metabolized in liver by CYP3A to sulfone metabolite and CYP2C19 to desmethyl rabeprazole. Thioether metabolite is formed by reduction of rabeprazole. These metabolites do not have significant antisecretory activity. CYP2C19 exhibits genetic polymorphism caused by deficiency in some subpopulations (white patients, 3% to 5%; Asian patients, 17% to 20%).
Plasma t ½ is 1 to 2 h. Eliminated in urine (90% as thioether carboxylic acid, glucuronide, and mercapturic acid); remainder recovered in feces. No unchanged drug recovered.
No pharmacokinetic differences were observed in 10 patients with end-stage renal disease compared with 10 healthy volunteers.Hepatic Function Impairment
For chronic mild to moderate hepatic function impairment, AUC approximately doubled and elimination t ½ was 2 to 3 fold higher, total Cl decreased to less than half. For mild to moderate hepatic function impairment, C max increased about 20% (not significant).Elderly
AUC values doubled, C max increased 60%.Children
Pharmacokinetics in patients 12 to 16 yr of age with GERD were within range observed in healthy adults.Gender
Pharmacokinetics did not differ between men and women.Race
Values for AUC for healthy Japanese men were approximately 50% to 60% higher than values for healthy men in the United States.
Short-term treatment in healing and symptomatic relief of duodenal ulcers and erosive or ulcerative gastroesophageal reflux disease (GERD); maintaining healing and reducing relapse rates of heartburn symptoms in adults and children 12 yr of age and older with GERD; treatment of daytime and nighttime heartburn and other symptoms associated with GERD; long-term treatment of pathological hypersecretory conditions, including Zollinger-Ellison syndrome; in combination with amoxicillin and clarithromycin to eradicate Helicobacter pylori .
Known hypersensitivity to rabeprazole or substituted benzimidazoles.
PO 20 mg/day after the morning meal for 4 wk; additional therapy may be required for some patients.Short-Term Treatment of GERDAdults and Children 12 yr of age and older
PO 20 mg once daily for up to 8 wk.Treatment of Erosive or Ulcerative GERDAdults
PO 20 mg/day for 4 to 8 wk; an additional 8 wk may be considered for patients who do not heal.Maintenance of Erosive or Ulcerative GERDAdults
PO 20 mg/day.Treatment of Pathological Hypersecretory ConditionsAdults
PO 60 mg/day. Doses up to 100 mg daily or 60 mg twice daily have been administered.H. Pylori Eradication to Reduce Risk of Duodenal Ulcer RecurrenceAdults
PO rabeprazole 20 mg plus amoxicillin 1,000 mg plus clarithromycin 500 mg twice daily for 7 days with morning and evening meals.
Store tablets at controlled room temperature (59° to 86°F). Protect from moisture.
Atazanavir plasma concentrations may be reduced, decreasing the efficacy. Coadministration is not recommended.Drugs dependent on gastric pH for absorption (eg, digoxin, ketoconazole)
Plasma levels of digoxin may be increased, while ketoconazole concentrations may be decreased.Warfarin
Increased INR and PT have been reported with concurrent rabeprazole.
None well documented.
Headache (10%); dizziness; disorientation/delirium (postmarketing).
Bullous eruptions, severe dermatologic eruptions including erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis (postmarketing).
Diarrhea, nausea (5%); abdominal pain, vomiting (4%); flatulence (3%); constipation (2%); abdominal pain; dry mouth.
Interstitial nephritis (postmarketing).
Hepatic encephalopathy; hepatitis; increased hepatic enzymes; jaundice (postmarketing).
Agranulocytosis, hemolytic anemia, leukopenia, pancytopenia, thrombocytopenia (postmarketing).
Hyperammonemia, TSH elevations (postmarketing).
Arthralgia; myalgia; rhabdomyolysis (postmarketing).
Interstitial pneumonia (postmarketing).
Pain (3%); infection (2%); peripheral edema; anaphylaxis, angioedema, coma, sudden death (postmarketing).
Category B .
Safety and efficacy not established in the short-term treatment of GERD in children younger than 12 yr of age. For other indications, safety and efficacy not established.
Use with caution in patients with severe hepatic function impairment.
Symptomatic response to rabeprazole does not preclude gastric malignancy.
No experience with large doses.
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