Dosing and uses of AcipHex (rabeprazole)
Adult dosage forms and strengths
tablet, delayed-release
- 20mg
Duodenal Ulcer
Indicated for short-term (up to 4 weeks) treatment in healing and symptomatic relief of duodenal ulcers
20 mg PO qDay after morning meal for up to 4 weeks; to achieve healing, some patients may require additional therapy
Helicobacter Pylori Eradication
In combination with amoxicillin and clarithromycin for treatment of H pylori infection and duodenal ulcer disease (active or history within past 5 yr)
20 mg PO BID for 7 days with morning and evening meals; take with amoxicillin 1000 mg PO BID and clarithromycin 500 mg BId
Gastroesophageal Reflux Disease
Healing or erosive or ulcerative GERd
- 20 mg PO qDay for 4-8 weeks; if not healed after 8 weeks, an additional 8-week course may be considered
- Maintenance dosing (20 mg/day for up to 12 months) shown to reduce relapse rates
Symptomatic GERd
- Treatment of daytime and nighttime heartburn and other symptoms associated with GERD
- 20 mg PO qDay for 4 weeks; if symptoms not completely resolved after 4 weeks, an additional course may be considered
Hypersecretory Conditions
Long-term treatment of pathologic hypersecretory conditions, including Zollinger-Ellison syndrome
60 mg PO qDay initially; may increase to 100 mg PO qDay or 60 mg PO q12hr
Dosing considerations
- Continue use as long as clinically needed; some patients with SE have been treated continuously for up to 1 yr
Administration
Administer with or without meals
Swallow tablet whole; do not chew or crush
Dosing Modifications
Renal impairment: Dose adjustment not necessary
Hepatic impairment
- Mild to moderate: Dose adjustment not necessary
- Severe: Not studied
Pediatric dosage forms and strengths
tablet, delayed-release
- 20mg
capsule, sprinkle
- 5mg
- 10mg
Gastroesophageal Reflux Disease
Delayed-release tablet
- Indicated for short-term treatment of symptomatic GERD in adolescents
- <12 years: Safety and efficacy not established
- ≥12 years: 20 mg PO qDay for up to 8 weeks
Delayed-release capsule (sprinkles)
- <1 year: Safety and efficacy not established
- 1-12 years (<15 kg): 5 mg PO qDay 30 minutes before a meal, for up to 12 weeks; may increase to 10 mg/day if inadequate response
- 1-12 years (≥15 kg): 10 mg PO qDay 30 minutes before a meal, for up to 12 weeks
Administration
Delayed-release tablet
- Administer with or without meals
- Swallow tablet whole; do not chew or crush
Delayed-release capsule
- Take 30 minutes before a meal
- Granules should not be chewed or crushed; open capsule and sprinkle entire contents on small amount of soft food (eg, applesauce, fruit- or vegetable-based baby food, or yogurt) or empty contents into a small amount of liquid (eg, infant formula, apple juice, or pediatric electrolyte solution)
- The whole dose should be taken within 15 minutes of preparation
- Food or liquid should be at or below room temperature; do not store mixture for future use
AcipHex (rabeprazole) adverse (side) effects
1-10%
Headache (2-10%)
Constipation (2%)
Diarrhea (2-5%)
Flatulence (3%)
Pain (3%)
Pharyngitis (3%)
Abdominal pain (4%)
<1%
Agitation
Agranulocytosis
Alopecia
Anemia
Angioedema
Chest pain
Delirium
Erythema
Hypokalemia
Hypomagnesemia
Hyponatremia
Jaundice
Leukocytosis
Leukopenia
Migraine
Osteoporosis related fracture
Rhabdomyolysis
Stevens-Johnson syndrome
Sudden death
Toxic epidermal necrolysis
Abnormal taste
Warnings
Contraindications
Hypersensitivity to rabeprazole or other proton pump inhibitors (PPIs)
Rilpivirine-containing products
Cautions
PPIs are possibly associated with increased incidence of Clostridium difficile-associated diarrhea (CDAD); consider diagnosis of CDAD for patients taking PPIs with diarrhea that does not improve
Liver disease: May require dosage reduction
Atrophic gastritis may occur as has occurred with omeprazole
Contains enteric coated granules (acid labile); do not chew or crush
Use of proton pump inhibitors may increase risk of salmonella and campylobacter infection
Reduce of symptoms does not eliminate presence of gastric malignancy
Published observational studies suggest that PPI therapy may be associated with an increased risk of osteoporosis-related fractures of the hip, wrist, or spine; particularly with prolonged (>1 yr), high-dose therapy
Decreased gastric acidity increases serum chromogranin A (CgA) levels and may cause false positive diagnostic results for neuroendocrine tumors; temporarily discontinue PPIs before assessing CgA levels
Hypomagnesemia may occur with prolonged use (ie, >1 yr); adverse effects, such as tetany, arrhythmias, or seizures, may result; in 25% of cases reviewed, magnesium supplementation alone did not improve low serum magnesium levels, and the PPI had to be discontinued
Monitor for increases in INR and prothombin time when coadministered with warfarin
Daily long-term use (e.g., longer than 3 years) may lead to malabsorption or a deficiency of cyanocobalamin
Acute interstitial nephritis reported in patients taking proton pump inhibitors
Concomitant use of proton pump inhibitors with methotrexate, primarily at high dose, may elevate and prolong serum concentrations of methotrexate and/or its metabolite, possibly leading to methotrexate toxicities; in high-dose methotrexate administration, a temporary withdrawal of the PPI may be considered in some patients
Pregnancy and lactation
Pregnancy category: C
Lactation: Unknown whether rabeprazole is distributed into breast milk; use caution
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of AcipHex (rabeprazole)
Mechanism of action
Proton pump inhibitor (PPI); binds to H+/K+-exchanging ATPase (proton pump) in gastric parietal cells, blocking acid secretion
Absorption
Bioavailability: 52%
Onset: Within 1 hr
Duration: 24 hr
Peak plasma time: 2-5 hr (tablet); 1-6.5 hr (capsule)
Distribution
Protein bound: 95-98%
Metabolism
Metabolism: Liver; extensively by hepatic P450 enzyme CYP2C19; second pathway through CYP3A4; also by non-enzymatic reduction
Metabolites (presumed inactive): Rabeprazole thioether, sulfone metabolite, desmethyl metabolite, desmethyl thioether, thioether carboxylic acid
CYP2C19 substrate (minor)
Elimination
Half-life elimination: 1-2 hr, depending on dose
Dialyzable: No
Total body clearance: 4-8 mL/min/kg
Excretion: Urine (90%); feces (10%)
