RAPIDYX Rabeprazole Sodium Tablets 20 mg.
For the use only of a Registered Medical Practitioner or a Hospital or A Laboratory.
Composition :
Each Enteric Coated Tablets Contains :
Rabeprazole sodium BP…20mg.
Excipients:……………………Q.S.
Colour:………..Sunset yellow
Description
Rabeprazole sodium is a substituted benzimidazole that inhibits gastric acid secretion. It is a proton pump inhibitor.
Pharmacology
Mechanism of Action
Rabeprazole sodium belongs to a class of antisecretory compounds (substituted benzimidazole proton-pump inhibitors) that do not exhibit anticholinergic or histamine HZ receptor antagonist properties, but suppress gastric acid secretory by inhibiting the gastirc ATPase at the secretory surface of the gastric parietal cell. Rabeprazole blocks the final step of gastric acid secretion. In gastric parietal cells, rabeprazole is protonated, accumulates, and is transformed to an active sulfonamide.
Pharmacokinetics
After oral administration of 20mg, Cr.„ of rabeprazole occurred over a range of 2.0 to 5.0 hours (Tn. The rabeprazole and C„ AUC are linear over and oral dose range of
10 mg. to 40 mg. There is no appreciable accumulation when doses of 10 mg. to 40 mg. are administered every 24 hours; multiple dosing dose not alter the pharmacokinetics of Rabeprazole. The plasma half-life ranges from 1 to 2 hours. Absolute bioavailability for a 20mg oral tablet of rabeprazole (compared to intravenous administration) is approximately 52%. The effects of food on the absorption of rabeprazole have not been evaluated. Rabeprazole is extensively metabolized. The thioether and sulphone are the primary metabolites measure in human plasma. Rabeprazole is primary metabolized in the liver by cytochromes P450 3A (sulphone metabolite) and P450 2C19 (desmethyl rabeprazole). The thioether metabolite is formed by reduction of rabeprazole.
Following a single 20mg oral dose of 14C-labeled rabeprazole, approximately 90% of the drug was eliminated in the urine, primary as thioether carboxylic acid; Its glucuronide, and mercapturic acid metabolites. The remainder of the dose was recovered in the feces. Total recovery of radioactivity was 99.85%. No unchanged rabeprazole was recovered in the urine of feces.
In patients with stable, end-stages, renal faliure requiring maintenance haemodialysis (creatinine clearance < 5mUmin1.73 m2), the disposition of rabeprazole sodium was very similar to that in health volunteers. Elimination of rabeprazole sodium was some what decreased in the elderly Following 7 days of daily dosing with 20mg of rabeprazole sodium, the AUC approximately doubled, the C. increased by 60% as compared to young healthy volunteers. However there was no evidence of rabeprazole sodium accumulation.
Indications
Rabeprazole sodium is indicated in the treatment of
- Gastroesophageal Reflux Disease (GERD)
- Duodenal Ulcers
- Zollinger Ellison Syndrome
Contraindications
Rabeprazole is contraindicated in patients with known hypersensitivity to rabeprazole, substituted benzimidazoles or to any component of the formulation.
Precautions
Symptomatic response to therapy with rabeprazole sodium dose not precludes the presence of gastric or esophageal mailgnancy, therefore the possibilty of malignancy should be excluded prior to commencing treatment with Rabeprazole.
Caution should be exercised when treatment with rabeprazole is first initiated in patients with severe hepatic dysfunction.
Pregnancy (Pregnancy Category B)
Animal studies reveled no evidence of impaired fertility or harm to the fetus due to rabeprazole. There are, however no adequate and well controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed.
Nursing Mothers
It is not known if unmetabolized rabeprazole is excreted in human breast milk and hence should be used with caution in nursing mother.
Pediatric Use
The safely and effectiveness of rebeprazole in pediatric patients have not been established.
Drug Interactions
The cytochrome P4S0 (CYP4S0) drug metabolizing enzyme system metabolizes Rabeprazole. Studies in healthy subjects have shown that rabeprazole does not have clinically significant interactions with other drugs metabolized by the CYP450 system, such as warfarin and theophylline given as single oral doses, diazepam as a single intravenous dose. In vitro incubations employing human liver microsomes indicated that rabeprazole inhibited cyclosporine metabolism with an IC50 of 62 micromolar, a concentration that is over 50 time higher than Cmax In healthy volunteers following 14 days of dosing with 20mg of rebeprazole.
In normal subjects, co-administretion of rabeprazole 20mg QD resulted in an approximately 30% decreases in the bioavailibility of ketoconazole and increases the AUC and C,n,®, of digoxin by 19% and 29%, respectively. Therefore, patients may need to be monitored when such drugs are taken concomitantly with rabeprazole. Co-administration of rabeprazole and antacids produced no clinically relevant changes in plasma rabeprazole concentrations.
Adverse Reactions
The most common adverse event was headache, diarrhoea and nausea. Other adverse events were rhinitis, abdominal pain, asthenia, flatulence, pharyngitis, vomiting, nonspecific back pain, dizziness, flu syndrome, infections, cough, constipation and insomnia. Further less frequent adverse events were rash, myalgia, chest pain, dry; mouth, dyspepsia, nervousness, somnolence, bronchitis, sinusitis, chills, leg cramps, urinary tract infections, arthralgia and fever.
Increased hepatic enzymes have been observed in 2% of patients.
Treatment should be stopped immediately at the recurrence of skin lesions.
Overdosage
There has been no experience with large overdoses with rabeprazole. No specific antidote for rabeprazole is known. Rabeprazole is extensively protein bound and is not readily dialyzable. In the event of over dosages, treatment should be symptomatic and supportive. Gastric lavage is recommended.
Dosage and Administration
Usually given as Single dose in the morning.
Swallow Whole tablet. Do not crush or chew.
Indication | Dosage |
| Gastroesophageal Reflux Disease (DERD) | 20 mg once daily for 4-8 weeks |
| Duodenal Ulcers (DU) | 20 mg once daily for 4 weeks |
| Zollinger Ellison Syndrome | 60 mg once daily |
No dosage adjustment is necessary in elderly patients, in with renal disease or in patients with mild to moderate hepatic impairment.
Storage: Store in a cool & dry place Protect from light & moisture.
Keep medicines out of reach of Children.
Presentation 28 Tablets
Marketed by:
PYXUS PHARMACEUTICALS PVT. LTD.
