Rabeprazole
Mechanism :
Suppress gastric acid secretion by inhibiting the gastric H+/K+ ATPase (hydrogen-potassium adenosine triphosphatase) at the secretory surface of the gastric parietal cell. Because this enzyme is regarded as the acid (proton) pump within the parietal cell, rabeprazole has been characterized as a gastric proton-pump inhibitor. Rabeprazole blocks the final step of gastric acid secretion. In gastric parietal cells, rabeprazole is protonated, accumulates, and is transformed to an active sulfonamide.
Indication :
Contraindications :
Hypersensitivity, Caution in severe hepatic failure, hypomagnesemia, long term use.
Dosing :
GERD:
<12 year:
Safety and efficacy not established.
12 years or above:
20 mg orally once a day for 8 weeks.
H. Pylori infection:
1.5 to 2.5 mg/kg/day PO divided twice daily (Max: 20 mg/dose) in combination with
amoxicillin and metronidazole/clindamycin for 14 days.
Adverse Effect :
Blood dyscrasias, hepatic impairment, hypersensitivity reaction, anaphylaxis, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis, pancreatitis, interstitial nephritis, rhabdomyolysis, fractures, hyponatremia, hypomagnesemia (long-term use), atrophic gastritis (long-term use), clostridium difficile associated diarrhea, headache, nausea/vomiting, diarrhea, abdominal pain, fever, rash, dizziness, flatulence, arthralgia.
Interaction :
Atazanavir: Rabeprazole may decrease the serum levels and therapeutic effects of atazanavir.
Cefditoren: Proton pump inhibitors such as rabeprazole may decrease the serum concentration of cefditoren. If possible, avoid use of cefditoren with proton pump inhibitors (PPIs). Consider alternative methods to minimize/control acid reflux (e.g., diet modification) or alternative antimicrobial therapy if use of PPIs cannot be avoided.
Clopidogrel: Rabeprazole may decrease serum concentrations of the active metabolite(s) of clopidogrel. Due to the possible risk for impaired clopidogrel effectiveness with this combination, clinicians should carefully consider the need for concurrent rabeprazole therapy in patients receiving clopidogrel. Monitor response to clopidogrel closely when using clopidogrel with rabeprazole. Whether there are differences among individual proton pump inhibitors is unclear. Other acid-lowering therapies (e.g., H2-receptor antagonists, antacids, etc.) do not appear to share this interaction with clopidogrel.
Dasatinib: Rabeprazole may decrease the serum level of dasatinib.
Digoxin: Rabeprazole increases the effect of digoxin.
Enoxacin: Rabeprazole may decrease the absorption of enoxacin.
Indinavir: Omeprazole decreases the absorption of indinavir.
Itraconazole: The proton pump inhibitor, rabeprazole, may decrease the absorption of itraconazole.
Ketoconazole: The proton pump inhibitor, rabeprazole, may decrease the absorption of ketoconazole.
Rilpivirine: Proton-pump inhibitors increase gastric pH which causes a decrease in the exposure of rilpivirine thus reducing efficacy.
Tretinoin: The moderate CYP2C8 inhibitor, Rabeprazole, may decrease the metabolism and clearance of oral Tretinoin. Monitor for changes in Tretinoin effectiveness and adverse/toxic effects if Rabeprazole is initiated, discontinued to dose changed.
Renal Dose :
Dose in Renal Impairment GFR (mL/min)
| 20-50 | Dose as in normal renal function |
| 10-20 | Dose as in normal renal function |
| <10 | Dose as in normal renal function |
Dose in Patients undergoing Renal Replacement Therapies
| CAPD | Unlikely to be dialysed. Dose as in normal renal function |
| HD | Not dialysed. Dose as in normal renal function |
| HDF/High flux | Unlikely to be dialysed. Dose as in normal renal function |
| CAV/VVHD | Unlikely to be dialysed. Dose as in normal renal function |
Hepatic Dose :
Mild to moderate hepatic impairment: dose adjustment is not be required but starting therapy with lower dose is reasonable.
Severe hepatic impairment: Use is contraindicated, however if administered, start with low dose and monitor closely.