Pronunciation: Online audio
proton pump inhibitors
- Gastroesophageal reflux disease (GERD).
- Duodenal ulcers (including combination therapy with clarithromycin and amoxicillin to erradicate H. pylori and prevent recurrence).
- Pathological hypersecretory conditions, including Zollinger-Ellison syndrome.
Binds to an enzyme in the presence of acidic gastric pH, preventing the final transport of hydrogen ions into the gastric lumen.
- Diminished accumulation of acid in the gastric lumen, with lessened acid reflux.
- Healing of duodenal ulcers and esophagitis.
- Decreased acid secretion in hypersecretory conditions.
Absorption: Delayed-release tablet is designed to allow rabeprazole, which is not stable in gastric acid, to pass through the stomach intact. Subsequently 52% is absorbed after oral administration.
Protein Binding: 96.3%.
Metabolism and Excretion: Mostly metabolized by the liver (hepatic cytochrome P450 3A and 2C19 enzyme systems) (the CYP2C19 enzyme system exhibits genetic polymorphism; 15–20% of Asian patients and 3–5% of Caucasian and Black patients may be poor metabolizers and may have significantly ↑ rabeprazole concentrations and an ↑ risk of adverse effects); 10% excreted in feces; remainder excreted in urine as inactive metabolites.
Half-life: 1–2 hr.
TIME/ACTION PROFILE (acid suppression)
|PO||within 1 hr||unknown||24 hr|
Suppression continues to increase over the first week of therapy
Hypersensitivity to rabeprazole or related drugs (benzimidazoles).
Use Cautiously in:
- Severe hepatic impairment (dose reduction may be necessary)
- Patients using high-doses for >1 year (↑ risk of hip, wrist, or spine fractures)
- OB: Lactation: Pedi: Pregnancy, lactation, or children <12 yr (breastfeeding not recommended; use in pregnancy only if needed; safety not established).
Adverse Reactions/Side Effects
CNS: dizziness, headache, malaise
GI: abdominal pain, constipation, diarrhea, nausea
Derm: photosensitivity, rash
F and E: hypomagnesemia (especially if treatment duration ≥3 mo)
MS: bone fracture, neck pain
Misc: allergic reactions, chills, fever
* CAPITALS indicate life-threatening.
Italics indicate most frequent.
- Rabeprazole is metabolized by the CYP450 enzyme system and may interact with other drugs metabolized by this sytem.
- Hypomagnesemia ↑ risk of digoxin toxicity.
- May ↑ the risk of bleeding with warfarin (monitor INR/PT).
PO: (Adults) GERD, duodenal ulcers–20 mg once daily; prevention of duodenal ulcer recurrence–20 mg twice daily for 7 days with amoxicillin 1000 mg twice daily for 7 days and clarithromycin 500 mg twice daily for 7 days; hypersecretory conditions–60 mg once daily initially, may be adjusted as needed and continued as necessary; doses up to 100 mg daily or 60 mg twice daily have been used.
PO: (Children ≥12 yr): GERD–20 mg once daily.
Delayed-release tablets: 10 mg, 20 mg
Assess routinely for epigastric or abdominal pain and frank or occult blood in the stool, emesis, or gastric aspirate.
Lab Test Considerations:
Monitor CBC with differential periodically during therapy.
- May cause hypomagnesemia. Monitor serum magnesium prior to and periodically during therapy.
- Do not confuse rabeprazole with aripiprazole. Do not confuse Aciphex with Accupril or Aricept.
- PO: Administer doses before meals, preferably in the morning. Tablets should be swallowed whole; do not break, crush, or chew.
- Instruct patient to take medication as directed for the full course of therapy, even if feeling better. Take missed doses as soon as remembered but not if almost time for next dose. Do not double doses.
- May cause occasional drowsiness or dizziness. Caution patient to avoid driving or other activities requiring alertness until response to medication is known.
- Advise patient to avoid alcohol, products containing aspirin or NSAIDs, and foods that may cause an increase in GI irritation.
- Caution patients to wear sunscreen and protective clothing to prevent photosensitivity reactions.
- Advise patient to report onset of black, tarry stools; diarrhea; abdominal pain; or persistent headache to health care professional promptly.
- Advise female patients to notify health care professional if pregnancy is planned or suspected or if breastfeeding.
- Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications.
- Decrease in abdominal pain or prevention of gastric irritation and bleeding. Healing of duodenal ulcers can be seen on x-ray examination or endoscopy.
- Decrease in symptoms of GERD. Therapy is continued for 4–8 wk after initial episode.