RABEKIND-20 (Rabeprazole Sodium)
Rabeprazole sodium belongs to the class of anti-secretory compounds, the substituted benzimidazole, that do not exhibit anticholinergic or H2 histamine properties, but suppress gastric secretion by the specific inhibition of the H+/K+-ATPase enzyme (the acid or proton pump). The effect is dose-related and leads to inhibition of both basal and stimulated acid secretion irrespective of the stimulus. As a weak base, rabeprazole is rapidly absorbed following all doses and is concentrated in the acid environment of the parietal cells. Rabeprazole is converted to the active sulphenamide form through protonation and it subsequently reacts with the available cysteines on the proton pump.
After oral administration of a 20mg dose of rabeprazole sodium the onset of the anti-secretory effect occurs within one hour, with the maximum effect occurring with two hours. Inhibition of basal and food stimulated acid secretion 23 hours after the first dose of Rabeprazole sodium are 68% and 82% respectively and the duration of inhibition lasts up to 48 hours. The inhibitory effect of rabeprazole sodium on acid secretion increases slightly with repeated once daily dosing, achieving steady state inhibition after three days. When the drug is discontinued, secretory activity normalizes over 2 to 3 days.
- Active duodenal ulcer
- Active benign gastric ulcer
- Symptomatic erosive or ulcerative gastro-esophageal reflux disease (GORD). Gastro-oesophageal Reflux Disease Long-term management
- Symptomatic treatment of moderate to very severe gastro-oesophageal reflux disease
- Zollinger-Ellison Syndrome
- In combination with appropriate antibacterial therapeutic regimens for the eradication of Helicobacter pylori in patients with peptic ulcer disease
Dosage and administration
Active duodenal ulcer and active benign gastric ulcer: the recommended oral dose for both active duodenal ulcer and active benign gastric ulcer is 20mg to be taken once daily in the morning.
Most patients with active duodenal ulcer heal within four weeks. However a few patients may require an additional four weeks of therapy to achieve healing. Most patients with active benign gastric ulcer heal within six weeks. However again a few patients may require an additional six weeks of therapy to achieve healing
Erosive or ulcerative gastro-oesophageal reflux disease (GORD): The recommended oral dose for this condition is 20mg to be taken once daily for four to eight weeks.
Gastro-oesophageal reflux disease long-term management (GORD Maintenance): For long-term management, a maintenance dose of Rabeprazole tablet 20mg or 10mg once daily can be used depending upon patients’ response.
Symptomatic treatment of moderate to very ssevere gastro-oesophageal reflux disease (symptomatic GORD): 10mg once daily in patients without oesophagitis. If symptoms control has not been achieved during four weeks, the patient should be further investigated. Once symptoms have resolved, subsequent symptom control can be achieved using an on-demand regimen taking 10mg once daily when needed.
Zollinger-Ellison Syndrome: the recommended adult starting dose is 60mg once a day. The dose may be titrated upwards to 120mg/day based on individual patient needs. Single daily doses up to 100mg/day may be given. 120mg dose may require divided doses, 60mg twice daily. Treatment should continue for as long as clinically indicated.
Eradication of H. pylori: patients with H. pylori infection should be treated with eradication therapy. The folloeing combination given for 7 days is recommended.
Rabeprazole 20mg twice daily + clarithromycin 500mg twice daily and amoxicillin 1g twice daily
For indication requiring once daily treatment Rabeprazole sodium tablets should be taken in the morning, before eating.
Mode of administration: For oral use
Rabeprazole sodium tablets should not be chewed or crushed, but should be swallowed whole.
RABEKIND-20 is contraindicated in patients with known hypersensitivity to Rabeprazole sodium, or to any excipient used in the formulation.
RABEKIND-20 is contraindicated in pregnancy and during breast feeding.
Special warnings and precautions for use
Symptomatic response to therapy with Rabeprazole sodium does not preclude the presence of gastric or oesophageal malignancy, therefore the possibility of malignancy should be excluded prior to commencing treatment with Rabeprazole sodium tablets.
Patients on long-term treatment (particularly those treated for more than a year) should be kept under regular surveillance.
A risk of cross-hypersensitivity reactions with other proton pump inhibitor or substituted benzimidazole cannot be excluded.
Rabeprazole is not recommended for use in children, as there is no experience of its use in this group.
No dosage adjustment is necessary for patients with renal and hepatic impairment. In the treatment of patients with severe hepatic dysfunction the prescriber is advised to exercise caution when treatment with Rabeprazole sodium tablet is first initiated in such patients.
Co-administration of atazanavir with rabeprazole is not recommended.
Treatment with proton pump inhibitors, including Rabeprazole may possibly increase the risk of gastrointestinal infections such as Salmonella, Campylobacter and Clostridium difficile.
RABEKIND-20 contains lactose. Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicine.
RABEKIND-20 contains mannitol which may have a mild laxative effect
RABEKIND-20 contains propylene glycol which may cause alcohol-like symptoms
Interactions with other medicinal products and other forms of interactions
Rabeprazole sodium produces a profound and long lasting inhibition of gastric acid secretion. An interaction with compounds whose absorption is pH dependent may occur. Co-administration of rabeprazole with ketoconazole or Itraconazole may result in a significant decrease in antifungal plasma levels. Therefore individual patients may need to be monitored to determine if a dosage adjustment is necessary when ketoconazole or itraconazole are taken concomitantly with rabeprazole.
PPI including Rabeprazole should not be co-administered with atazanavir.
Pregnancy and lactation
Use in pregnancy: there are no adequate and well-controlled studies of Rabeprazole in pregnant women. Rabeprazole should be used during pregnancy only if the potential benefit justifies the potential risk to the foetus.
Use in lactation: there are no adequate and well controlled studies of Rabeprazole in pregnant women and hence should be used only if clearly indicated.
Effect on ability to drive and use machines
Rabeprazole may cause an impairment of driving performance or compromise the ability to use machinery. If however, alertness is impaired due to somnolence, it is recommended that driving and operating complex machinery be avoided.
The most commonly reported adverse drug reactions are headache, diarrhea, abdominal pain, asthenia, flatulence, rash, dry mouth, facial swelling, hypotension, and dyspnea.
Erythema, bullous reactions and hypersensitivity reactions have usually resolved after discontinuation of therapy.
Rare reports of hepatic encephalopathy have been received in patients with underlying cirrhosis.
The maximum established exposure has not exceeded 60mg twice daily, or 160mg once daily. Effects are generally minimal, representative of known adverse event profile and reversible without further medical intervention. No specific antidote is known. Rabeprazole sodium is extensively protein bound and is, therefore, not dialyzable. As in any case of overdose, treatment should be symptomatically and general supportive measures should be utilized.