ACIPHEX
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ACIPHEX (ACIPHEX).
Rabeprazole is a proton pump inhibitor that suppresses gastric acid secretion by specific inhibition of the H+/K+ ATPase enzyme system at the secretory surface of gastric parietal cells.
| Metabolism | Primarily hepatic via CYP2C19 and CYP3A4; metabolites include thioether and sulfone; renal excretion of metabolites. |
| Excretion | Hepatic metabolism, primarily via CYP2C19 and CYP3A4; ~90% eliminated as metabolites in urine, <1% unchanged; remainder in feces. |
| Half-life | Plasma half-life 1-2 hours, but pharmacodynamic half-life (acid suppression) >24 hours due to accumulation in parietal cell canaliculi. |
| Protein binding | 96-98% bound to plasma proteins, primarily albumin and alpha1-acid glycoprotein. |
| Volume of Distribution | Vd ~0.5 L/kg, indicating distribution primarily into extracellular fluid; small distribution into total body water. |
| Bioavailability | Oral bioavailability ~52%, increases with multiple dosing (no clinically relevant accumulation); food delays absorption but does not reduce extent. |
| Onset of Action | Oral: Maximal acid suppression effect within 2-4 hours after first dose; some effect within 1 hour. |
| Duration of Action | Duration of acid suppression >24 hours after a single dose; inhibition of gastric acid secretion persists for up to 72 hours. |
20 mg orally once daily; duration: 4-8 weeks for erosive esophagitis, 4 weeks for GERD, 24 weeks for H. pylori eradication (triple therapy: AcipHex 20 mg + amoxicillin 1000 mg + clarithromycin 500 mg twice daily for 7 days), 4 weeks for duodenal ulcer, up to 12 months for pathological hypersecretory conditions.
| Dosage form | TABLET, DELAYED RELEASE |
| Renal impairment | No dose adjustment required for mild to moderate renal impairment. Severe renal impairment (CrCl <30 mL/min): maximum dose 20 mg once daily. |
| Liver impairment | Child-Pugh Class A or B: no adjustment. Child-Pugh Class C: maximum dose 20 mg once daily. |
| Pediatric use | GERD: 12 years and older: 20 mg once daily for 4-8 weeks. Erosive esophagitis: 12 years and older: 20 mg once daily for 4-8 weeks. Safety and efficacy not established in children under 12 years. |
| Geriatric use | No dose adjustment needed based on age alone. However, monitor for increased risk of hip fracture, Clostridium difficile infection, and vitamin B12 deficiency with long-term use. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for ACIPHEX (ACIPHEX).
| Breastfeeding | Rabeprazole is excreted in human milk; the M/P ratio is unknown. Because of the potential for adverse reactions in nursing infants, caution should be exercised; consider alternative agents or discontinue nursing if no suitable alternative. |
| Teratogenic Risk | FDA Pregnancy Category B. No evidence of teratogenicity in animal studies at doses up to 13 times the human dose. Limited human data; however, studies have not shown an increased risk of major birth defects. Use only if clearly needed. |
| Fetal Monitoring |
■ FDA Black Box Warning
No FDA black box warning.
| Serious Effects |
["Hypersensitivity to rabeprazole, substituted benzimidazoles, or any component of the formulation","Concomitant use with rilpivirine-containing products"]
| Precautions | ["Gastric malignancy: symptomatic response does not preclude presence of gastric malignancy","Acute interstitial nephritis observed","Clostridium difficile-associated diarrhea: increased risk with PPI use","Bone fracture: long-term use may increase risk of osteoporosis-related fractures","Cutaneous lupus erythematosus and systemic lupus erythematosus: reported","Cyanocobalamin (Vitamin B12) deficiency: long-term use may impair absorption","Hypomagnesemia: reported with prolonged use, especially with concomitant diuretics","Increased risk of fundic gland polyps with long-term use","Interference with secretin stimulation test and chromogranin A levels"] |
| Food/Dietary | ACIPHEX can be taken with or without food, but for best results, take it before a meal (food slightly increases absorption). Avoid excessive alcohol and spicy or acidic foods that may exacerbate symptoms. No specific food-drug interactions; however, PPIs may reduce absorption of certain nutrients like vitamin B12, calcium, and magnesium with long-term use. |
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| Monitor maternal symptoms of GERD; no specific fetal monitoring required. Assess maternal thyroid function if used long-term due to potential B12 deficiency. |
| Fertility Effects | Animal studies showed no impairment of fertility. No human data available; unlikely to significantly affect fertility. |
| Clinical Pearls | ACIPHEX (rabeprazole) is a proton pump inhibitor (PPI) with rapid onset of action; it can be taken without regard to meals but for optimal acid suppression, take before breakfast. Avoid concurrent use with clopidogrel due to possible reduced antiplatelet effect; consider alternative PPI if needed. Monitor for hypomagnesemia, vitamin B12 deficiency, and increased risk of Clostridioides difficile infection with long-term use. Short-term use (≤8 weeks) is recommended for initial therapy of GERD; reassess need for continued therapy. |
| Patient Advice | Take ACIPHEX exactly as prescribed, usually once daily before a meal (preferably breakfast). · Do not crush, chew, or split the delayed-release tablets; swallow them whole with a glass of water. · Inform your doctor if you have liver disease, osteoporosis, or low magnesium levels. · Common side effects include headache, diarrhea, and nausea; contact your doctor if you experience severe diarrhea, rash, or signs of low magnesium (muscle cramps, irregular heartbeat). · Long-term use may increase risk of bone fractures, vitamin B12 deficiency, and kidney problems; discuss with your doctor if you need treatment beyond 8 weeks. · Do not take other acid reducers (e.g., antacids, H2 blockers) without consulting your doctor. |