Rabeprazole

Pronunciation

(ra BE pray zole)

U.S. Brand Names

Aciphex®

Synonyms

Pariprazole

Generic Available

Canadian Brand Names

Aciphex®; Pariet®

Use

Short-term (4-8 weeks) treatment and maintenance of erosive or ulcerative gastroesophageal reflux disease (GERD); symptomatic GERD; short-term (up to 4 weeks) treatment of duodenal ulcers; long-term treatment of pathological hypersecretory conditions, including Zollinger-Ellison syndrome; H. pylori eradication (in combination with amoxicillin and clarithromycin)

Use - Unlabeled/Investigational

Maintenance of duodenal ulcer

Pregnancy Risk Factor

Pregnancy Implications

Not shown to be teratogenic in animal studies, however, adequate and well-controlled studies have not been done in humans; use during pregnancy only if clearly needed

Lactation

Excretion in breast milk unknown/not recommended

Contraindications

Hypersensitivity to rabeprazole, substituted benzimidazoles (ie, esomeprazole, lansoprazole, omeprazole, pantoprazole), or any component of the formulation

Warnings/Precautions

Use caution in severe hepatic impairment; relief of symptoms with rabeprazole does not preclude the presence of a gastric malignancy

Adverse Reactions

1% to 10%: Central nervous system: Headache

<1%: Abdomen enlarged (rare), abdominal pain, abnormal dreams, abnormal stools, abnormal vision, agitation (rare), allergic reaction, alopecia, amblyopia, amnesia (rare), anemia, angina pectoris, anorexia, anxiety, apnea (rare), appetite increased, arthritis, arthrosis, asthma, bloody diarrhea (rare), blurred vision (rare), bone pain, bradycardia (rare), breast enlargement, bundle branch block, bursitis, cataract, chest pain substernal, chills, cholangitis (rare), cholecystitis, cholelithiasis, colitis, confusion (rare), constipation, convulsions, corneal opacity (rare), cystitis, deafness, deafness (rare), dehydration, depression, diaphoresis, diarrhea, diplopia (rare), dizziness, dry eyes, dry mouth, dry skin (rare), duodenitis (rare), dysmenorrhea, dyspepsia, dysphagia, dyspnea, dysuria, ecchymosis, edema, electrocardiogram abnormal, epistaxis, eructation, esophagitis, extrapyramidal syndrome (rare), eye pain (rare), facial edema (rare), fever, flatulence, gastroenteritis, gastrointestinal hemorrhage (rare), gingivitis, glaucoma, glossitis, gout, hangover effect (rare), hematuria (rare), hepatic encephalopathy (rare), hepatitis (rare), hepatoma (rare), herpes zoster (rare), hiccups, hyperkinesia (rare), hypertension, hyperthyroidism, hypertonia, hyperventilation, hypochromic anemia, hypothyroidism, hypoventilation (rare), impotence (rare), insomnia, kidney calculus, laryngitis, leg cramps, leukorrhea (rare), libido decreased, liver fatty deposit (rare), lymphadenopathy, malaise, melena, menorrhagia (rare), metrorrhagia, MI, migraine, mouth ulceration, myalgia, nausea, neck rigidity, nervousness, neuralgia, neuropathy, orchitis (rare), otitis media, palpitation, pancreatitis, paresthesia, peripheral edema, photosensitivity reaction, polyuria, proctitis, pruritus, psoriasis (rare), pulmonary embolus (rare), rash, rectal hemorrhage, retinal degeneration (rare), salivary gland enlargement (rare), sinus bradycardia, skin discoloration (rare), somnolence, stomatitis, strabismus (rare), supraventricular tachycardia (rare), syncope, tachycardia, thirst (rare), tinnitus, tremor, twitching (rare), urinary frequency, urinary incontinence (rare), urticaria, vertigo, vomiting, weakness, weight gain/loss

Postmarketing and/or case reports: Sudden death, coma, hyperammonemia, jaundice, rhabdomyolysis, disorientation, delirium, anaphylaxis, angioedema, bullous and other drug eruptions of the skin, interstitial pneumonia, TSH elevations; in most instances, the relationship to rabeprazole sodium was unclear. In addition, agranulocytosis, erythema multiforme, hemolytic anemia, leukopenia, pancytopenia, Stevens-Johnson syndrome, thrombocytopenia, and toxic epidermal necrolysis have been reported.

Overdosage/Toxicology

No experience with large overdose; rabeprazole is not dialyzable. Treatment of overdosage should be symptomatic and supportive.

Drug Interactions

Substrate (major) of CYP2C19, 3A4; Inhibits CYP2C19 (moderate), 2DC (weak), 3A4 (weak)

CYP2C19 inducers: May decrease the levels/effects of rabeprazole. Example inducers include aminoglutethimide, carbamazepine, phenytoin, and rifampin.

CYP2C19 substrates: Rabeprazole may increase the levels/effects of CYP2C19 substrates. Example substrates include citalopram, diazepam, methsuximide, phenytoin, propranolol, and sertraline.

CYP3A4 inducers: CYP3A4 inducers may decrease the levels/effects of rabeprazole. Example inducers include aminoglutethimide, carbamazepine, nafcillin, nevirapine, phenobarbital, phenytoin, and rifamycins.

Itraconazole and ketoconazole: Proton pump inhibitors may decrease the absorption of itraconazole and ketoconazole; concurrent use is contraindicated.

Protease inhibitors: Proton pump inhibitors may decrease absorption of some protease inhibitors (atazanavir and indinavir).

Ethanol/Nutrition/Herb Interactions

Ethanol: Avoid ethanol (may cause gastric mucosal irritation).

Food: High-fat meals may delay absorption, but Cmax and AUC are not altered.

Stability

Rapidly degraded in acid conditions.

Mechanism of Action

Potent proton pump inhibitor; suppresses gastric acid secretion by inhibiting the parietal cell H+/K+ ATP pump

Pharmacodynamics/Kinetics

Onset of action: 1 hour

Duration: 24 hours

Absorption: Oral: Well absorbed within 1 hour

Distribution: 96.3%

Protein binding, serum: 94.8% to 97.5%

Metabolism: Hepatic via CYP3A and 2C19 to inactive metabolites

Bioavailability: Oral: 52%

Half-life elimination (dose dependent): 0.85-2 hours

Time to peak, plasma: 2-5 hours

Excretion: Urine (90% primarily as thioether carboxylic acid); remainder in feces

Dosage

Oral: Adults >18 years and Elderly:

GERD: 20 mg once daily for 4-8 weeks; maintenance: 20 mg once daily

Duodenal ulcer: 20 mg/day before breakfast for 4 weeks

H. pylori eradication: 20 mg twice daily for 7 days; to be administered with amoxicillin 1000 mg and clarithromycin 500 mg, also given twice daily for 7 days.

Hypersecretory conditions: 60 mg once daily; dose may need to be adjusted as necessary. Doses as high as 100 mg once daily and 60 mg twice daily have been used.

Dosage adjustment in renal impairment: No dosage adjustment required

Dosage adjustment in hepatic impairment:

Mild to moderate: Elimination decreased; no dosage adjustment required

Severe: Use caution

Administration

May be administered with or without food; best if taken before breakfast. Do not crush, split, or chew tablet. May be administered with an antacid.

Dietary Considerations

May be taken with or without food; best if taken before breakfast.

Patient Education

Take as directed. Swallow whole, do not crush, split, or chew. Follow recommended diet and activity instructions. Avoid alcohol. You may experience headache (use of mild analgesic may help) or other side effects. Report these to prescriber if they persist. Breast-feeding precaution: Breast-feeding is not recommended.

Dental Health: Effects on Dental Treatment

No significant effects or complications reported

Dental Health: Vasoconstrictor/Local Anesthetic Precautions

No information available to require special precautions

Mental Health: Effects on Mental Status

May cause insomnia, anxiety, dizziness, depression, nervousness, somnolence, vertigo, convulsions, abnormal dreams; may rarely cause agitation, amnesia, confusion, extrapyramidal syndrome

Mental Health: Effects on Psychiatric Treatment

None reported

Dosage Forms

Tablet, delayed release, enteric coated, as sodium: 20 mg

References

Cockayne SE, Glet RJ, Gawkrodger DJ, et al, "Severe Erythrodermic Reactions to the Proton Pump Inhibitors Omeprazole and Lansoprazole," Br J Dermatol ,1999, 141(1):173-5.

Natsch S, Vinks MH, Voogt AK, et al, "Anaphylactic Reactions to Proton-Pump Inhibitors," Ann Pharmacother , 2000, 34(4):474-6.

Wolfe MM and Sachs G, "Acid Suppression: Optimizing Therapy for Gastroduodenal Ulcer Healing, Gastroesophageal Reflux Disease, and Stress-Related Erosive Syndrome," Gastroenterology , 2000,118(2 Suppl 1):9-31.

International Brand Names

Aciphex® (CA); Pariet® (AR, AT, BE, BG, BR, CA, CH, CO, CR, DE, DK, DO, ES, FI, FR, GB, GT, HN, HU, ID, IE, IT, JP, MX, NL, PA, PL, PT, RO, SE, SG, SV, TH, ZA); Rabec® (AR); Rabeloc® (IN)

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