Adult: 20 mg once daily for 4-8 weeks. Maintenance: 10 or 20 mg once daily depending on patient response.
Oral Gastro-oesophageal reflux disease
Adult: Usual dose: 20 mg once daily for 4-8 weeks. Maintenance: 10 or 20 mg daily depending on the response. In patients with symptomatic disease without oesophagitis: 10 or 20 mg once daily for 4 weeks. Once symptoms have resolved, 10 mg once daily as needed. Child: 1-11 years <15 kg: 5 mg once daily, may increase up to 10 mg once daily if necessary, for up to 12 weeks. ≥15 kg: 10 mg once daily for up to 12 weeks. ≥12 years 20 mg once daily for up to 8 weeks.
Oral Peptic ulcer
Adult: 20 mg once daily for 4-8 weeks (duodenal ulcer) or for 6-12 weeks (gastric ulcer).
Oral Eradication of H. pylori associated with peptic ulcer disease
Adult: In combination with clarithromycin 500 mg bid and amoxicillin 1 g bid: 20 mg bid for 7 days.
Oral Zollinger-Ellison syndrome
Adult: 60 mg once daily, may titrate up to 100 mg daily as single dose or up to 120 mg daily in 2 divided doses if necessary.
Special Patient Group
Pharmacogenomics:
CYP2C19 is one of the major enzymes in the metabolism of rabeprazole. CYP2C19 exhibits a known genetic polymorphism due to its deficiency in certain populations (3-5% of Caucasians, 17-20% of Asians) which may result in slower metabolism. These sub-populations are referred as poor metabolisers.
In a clinical study evaluating rabeprazole sodium delayed-release tablets in Japanese adult patients that was categorised by CYP2C19 genotype (n=6 per genotype category) showed that gastric acid suppression was higher in poor metabolisers as compared to extensive metabolisers. This could be due to higher rabeprazole plasma levels in poor metabolisers.
Administration
delayed-release: May be taken with or without food.
Contraindications
Concomitant use with rilpivirine.
Special Precautions
Patients at risk of osteoporosis, reduced body stores or with risk factors for vitamin B12 malabsorption, PPI-induced autoimmune disease. Severe hepatic impairment. Children and elderly. Pregnancy and lactation.
Adverse Reactions
Significant: New-onset or exacerbation of subacute cutaneous and systemic lupus erythematosus, osteoporosis-related bone fractures, fundic gland polyps, acute interstitial nephritis, Clostridium difficile-associated diarrhoea (hospitalised patients). Rarely, hypomagnesaemia, vitamin B12 deficiency. Gastrointestinal disorders: Diarrhoea, vomiting, nausea, abdominal pain, constipation, flatulence. General disorders and admin site conditions: Back pain, asthenia, influenza-like illness. Hepatobiliary disorders: Hepatic encephalopathy, hepatitis. Infections and infestations: Infection (e.g. Salmonella, Campylobacter). Investigations: Increased liver enzymes. Nervous system disorders: Headache, dizziness. Psychiatric disorders: Insomnia. Respiratory, thoracic and mediastinal disorders: Cough, pharyngitis, rhinitis.
This drug may cause somnolence, if affected, do not drive or operate machinery.
Monitoring Parameters
Monitor magnesium levels prior to initiation of therapy and periodically thereafter on long-term treatments or in patients taking digoxin, diuretics or other drugs that cause hypomagnesaemia.
Drug Interactions
May decrease serum concentration of ketoconazole, itraconazole, atazanavir, nelfinavir. Increased INR and prothrombin time with concomitant use of warfarin. Increased serum concentrations of methotrexate, tacrolimus, saquinavir. Potentially Fatal: Decreased serum concentrations and reduced antiviral effect of rilpivirine.
Lab Interference
May lead to false-positive results in the diagnosis of neuroendocrine tumour and urine screening tests for tetrahydrocannabinol. May suggest false result of gastrinoma in secretin stimulation test.
Action
Description: Rabeprazole is a proton pump inhibitor that suppresses the gastric acid secretion by inhibiting H+/K+ ATPase at the secretory surface of the gastric parietal cell. Onset: Within 1 hour. Duration: 24 hours. Pharmacokinetics: Absorption: Well absorbed from the gastrointestinal tract. Food delays absorption. Bioavailability: Approx 52% (tablet). Time to peak plasma concentration: 2-5 hours; range: 1-6.5 hours (capsule). Distribution: Plasma protein binding: 96.3%. Metabolism: Mainly metabolised via non-enzymatic reduction and to a lesser extent via CYP3A and CYP2C19 isoenzymes. Excretion: Mainly via urine (90% as thioether carboxylic acid metabolites); faeces. Elimination half-life: 1-2 hours; increased by 1.6 times in CYP2C19 slow metabolisers.
Chemical Structure
Rabeprazole Source: National Center for Biotechnology Information. PubChem Database. Rabeprazole, CID=5029, https://pubchem.ncbi.nlm.nih.gov/compound/Rabeprazole (accessed on Jan. 22, 2020)
A02BC04 - rabeprazole ; Belongs to the class of proton pump inhibitors. Used in the treatment of peptic ulcer and gastro-oesophageal reflux disease (GERD).
References
Horai, Y, Kimura, M, Furuie, H et al. Pharmacodynamic Effects and Kinetic Disposition of Rabeprazole in Relation to CYP2C19 Genotypes. Alimentary Pharmacology & Therapeutics. 15(6):793–803. doi: 10.1046/j.1365-2036.2001.00980.x. Accessed 06/11/2019. PMID: 11380317Yang J, Yang, Y, Uang Y et al. Pharmacokinetic-Pharmacodynamic Analysis of the Role of CYP2C19 Genotypes in Short-term Rabeprazole-based Triple Therapy Against Helicobacter pylori. British Journal of Clinical Pharmacology. 2009 May;67(5):503-510. doi: 10.1111/j.1365-2125.2009.03393.x. Accessed 06/11/2019. PMID: 19552744Anon. CYP2C19 - Rabeprazole (Pharmacogenomics). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 06/11/2019.Anon. Rabeprazole. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 06/11/2019.Buckingham R (ed). Rabeprazole Sodium. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 06/11/2019.Clinical Annotation for CYP2C19*1, CYP2C19*2, CYP2C19*3; Rabeprazole; Gastroesophageal Reflux and Helicobacter Infections (level 2A Metabolism/PK). Pharmacogenomics Knowledgebase (PharmGKB). https://www.pharmgkb.org/. Accessed 06/11/2019.Rabeprazole Capsule (Sarras Health, LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 06/11/2019.Rabeprazole Tablet (Aurobindo Pharma Limited). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 06/11/2019.
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