ACIPHEX SPRINKLE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ACIPHEX SPRINKLE (ACIPHEX SPRINKLE).
Rabeprazole is a proton pump inhibitor (PPI) that suppresses gastric acid secretion by specific inhibition of the H+/K+-ATPase enzyme system at the secretory surface of gastric parietal cells.
| Metabolism | Hepatic metabolism via CYP2C19 and CYP3A4 isoenzymes. |
| Excretion | Primarily hepatic metabolism (CYP2C19 and CYP3A4); <1% excreted unchanged in urine; approximately 90% of the dose excreted as metabolites in urine and feces via biliary elimination. |
| Half-life | Terminal elimination half-life is approximately 1-2 hours in healthy subjects; prolonged in CYP2C19 poor metabolizers (up to 3-4 hours). Clinically, the short half-life results in rapid clearance but sustained acid suppression due to irreversible binding to the proton pump. |
| Protein binding | Approximately 96-97% bound to plasma proteins, primarily albumin and alpha1-acid glycoprotein. |
| Volume of Distribution | Mean volume of distribution is approximately 0.15-0.3 L/kg (about 11-22 L in a 70 kg adult), indicating limited extravascular distribution. |
| Bioavailability | Oral: Absolute bioavailability is approximately 52% (range 30-80%) after a single 20 mg dose; food may delay absorption but does not significantly affect extent of absorption. |
| Onset of Action | Oral: Onset of acid suppression occurs within 1-2 hours after administration, with maximal effect after 3-4 days of once-daily dosing. |
| Duration of Action | Duration of acid suppression persists for up to 24 hours after a single dose, allowing once-daily dosing. However, maximal effect requires 3-4 days of continuous administration. |
| Molecular Weight | 381.43 |
20 mg orally once daily as delayed-release capsules; maximum dose 40 mg per day.
| Dosage form | CAPSULE, DELAYED RELEASE |
| Renal impairment | No dose adjustment required for mild to moderate renal impairment. Severe impairment (CrCl <30 mL/min): maximum dose 20 mg per day. |
| Liver impairment | Child-Pugh Class A: no adjustment; Class B or C: maximum dose 20 mg per day. |
| Pediatric use | Children 1 year and older: weight-based dosing is not established; use 10 mg once daily for up to 12 weeks for GERD. For adolescents: 20 mg once daily. |
| Geriatric use | No specific dose adjustment; consider lower starting doses due to potential for decreased hepatic and renal function but no evidence of significant differences in safety or efficacy. |
| 1st trimester | Studies in animals have shown risk to fetus; no adequate human studies. Use only if clearly needed. |
| 2nd trimester | PPIs may be associated with possible risk of fetal harm; avoid prolonged use. |
| 3rd trimester | PPIs may be associated with possible risk of fetal harm; avoid prolonged use. |
Clinical note
Comprehensive clinical and safety monograph for ACIPHEX SPRINKLE (ACIPHEX SPRINKLE).
| Placental transfer | Rabeprazole crosses the placenta in animal studies; human data limited. |
| Breastfeeding | Rabeprazole is excreted in breast milk in low amounts; not expected to cause adverse effects in infants. Use caution, especially with high doses or prolonged therapy. |
| Lactation Rating |
■ FDA Black Box Warning
No FDA black box warning.
| Serious Effects |
Hypersensitivity to rabeprazole or any component of the formulationConcomitant use with rilpivirine
| Precautions | Gastric malignancy: Symptomatic response does not preclude gastric malignancy., Acute interstitial nephritis has been observed., Cyanocobalamin (Vitamin B12) deficiency: Long-term use may lead to malabsorption., Clostridium difficile-associated diarrhea: Increased risk with prolonged therapy., Bone fracture: Long-term use may increase risk of osteoporosis-related fractures., Hypomagnesemia: Prolonged use can cause symptomatic hypomagnesemia. |
| Food/Dietary | AcipHex Sprinkle should be taken at least 30 minutes before a meal. Food delays and reduces absorption; however, when sprinkled on soft food like applesauce, the effect is minimal. Avoid high-fat meals which may decrease efficacy. No specific food restrictions, but acidic foods (e.g., citrus, tomatoes) may exacerbate symptoms and should be limited. |
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| Teratogenic Risk | FDA Pregnancy Category B. Animal studies (rats, rabbits) at doses up to 390 mg/kg/day (rat) and 50 mg/kg/day (rabbit) showed no evidence of fetal harm. No adequate controlled studies in pregnant women. First trimester: limited human data; theoretical risk based on increased gastric pH affecting absorption of folate and other nutrients. Second/third trimester: no known specific risks; use only if clearly needed. Postnatal: animal studies showed no adverse effects on offspring. |
| Fetal Monitoring | Monitor maternal gastric acidity symptoms and signs of gastrointestinal bleeding if used for erosive esophagitis. Fetal monitoring: standard obstetric surveillance; no specific fetal monitoring required. Assess maternal vitamin B12 and iron levels if prolonged therapy due to possible malabsorption from reduced gastric acid. |
| Fertility Effects | Animal studies: no impairment of fertility in rats at oral doses up to 150 mg/kg/day (about 60 times human dose). Human data: no reported effects on fertility. Theoretical: changes in gastric pH may affect absorption of minerals (zinc, calcium) possibly influencing reproductive function, but not clinically documented. |
| Clinical Pearls | AcipHex Sprinkle (rabeprazole delayed-release capsules) can be opened and sprinkled on soft food or liquid for patients with difficulty swallowing. Administer 30 minutes before a meal for maximal acid suppression. Monitor for Clostridium difficile infection and magnesium depletion with prolonged use. Not effective for immediate symptom relief; use with antacids if needed. Avoid concurrent use with atazanavir, rilpivirine, and certain antifungal/anticancer drugs due to altered absorption. |
| Patient Advice | Sprinkle capsule contents on a spoonful of applesauce, yogurt, or juice; swallow immediately without chewing. · Take exactly as prescribed, usually once daily before a meal. · Do not crush or chew the pellets. · Contact your doctor if you experience severe diarrhea, muscle cramps, or irregular heartbeat. · Long-term use may increase risk of bone fractures or vitamin B12 deficiency. · Avoid alcohol and smoking as they can worsen acid reflux symptoms. · Store at room temperature away from moisture and heat. |