Razid-20

Razid-20

rabeprazole

Manufacturer:

Saga Lab

Distributor:

KTZ
Full Prescribing Info
Contents
Rabeprazole sodium.
Description
Each enteric coated tablet contains Rabeprazole Sodium 20 mg.
Excipients/Inactive Ingredients: Q.S.
Colour: Sunset Yellow.
Action
Pharmacology: Pharmacodynamics: Mechanism of Action: Rabeprazole Sodium belongs to the class of antisecretory compounds, the substituted Benzimidazoles, that do not exhibit anticholinergic or H2 histamine antagonist properties, but suppress gastric acid secretion by the specific inhibition of the H+/K+-ATPase enzyme at the secretory surface of the gastric cell. This enzyme system is regarded as the acid (proton) pump, and therefore Rabeprazole Sodium is classified as a gastric proton-pump inhibitor blocking the final step of acid production. This effect is dose-related and leads to inhibition of both basal and stimulated acid secretion irrespective of the stimulus. Animal studies indicate that after administration, Rabeprazole Sodium rapidly disappears from both the plasma and gastric mucosa.
Anti-secretory Activity: After oral administration of a 20 mg dose of Rabeprazole Sodium the onset of the anti-secretory effect occurs within one hour with the maximum effect occurring within two to four hours. Inhibition of basal and food stimulated acid secretion 23 hours after the first dose of Rabeprazole Sodium are 69% and 82% respectively and the duration of inhibition lasts up to 48 hours. This duration of pharmacodynamic action is much longer than the pharmacokinetic half life (approximately one hour) would predict. This effect is probably due to the prolonged binding to the H+/K+-ATPase enzyme. 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 normalises over 2 to 3 days.
Serum Gastrin Effects: In clinical studies patients were treated once daily with 10 or 20 mg Rabeprazole Sodium, for up to 24 months duration. Serum gastrin levels increased during the first 2 to 8 weeks reflecting the inhibitory effects on acid secretion. Gastrin values returned to pre-treatment levels, usually within 1 to 2 weeks after discontinuation of therapy.
Pharmacokinetics: Rabeprazole Sodium is acid-labile, and is therefore administered orally as an enteric-coated (gastro-resistant) tablet formulation. Absorption of Rabeprazole Sodium therefore begins only after the tablet leaves the stomach. Absorption is rapid, with peak plasma levels of Rabeprazole Sodium occurring approximately 3.5 hours after a 20 mg dose. Absolute bioavailability of an oral 20 mg dose (compared to intravenous administration) is about 52% due in large part to pre-systemic metabolism. In patients with chronic hepatic disease, the AUC doubled compared to healthy volunteers, reflecting a decreased first-pass effect, and the plasma half-life increased 2-3 fold.
Rabeprazole Sodium is approximately 97% bound to human plasma proteins. The main plasma metabolites are thioether (M1) and carboxylic acid (M6). Minor metabolites observed at lower levels include sulphone (M2), desmethyl-thioether (M4) and mercapturic acid conjugate (M5). Only the desmethyl metabolite (M3) has a small amount of antisecretory activity, but it is not present in plasma.
Excretion is mainly urinary (90%), with no unchanged drug excreted in the urine. The rest of the metabolites are excreted via the faeces.
Total recovery was 99.8% implying a low biliary excretion of the metabolites of Rabeprazole Sodium.
Indications/Uses
RAZID tablets are indicated for the treatment of: Active duodenal ulcer; Active benign gastric ulcer; Symptomatic erosive or ulcerative gastro-oesophageal reflux disease (GORD); H. pylori-positive duodenal ulcers, as part of the eradication programme with appropriate antibiotics; Maintenance treatment of healed erosive or ulcerative GORD. Efficacy has not been demonstrated for periods exceeding 12 months.
Dosage/Direction for Use
For oral administration.
Adults/elderly: Active Duodenal Ulcer and Active Benign Gastric Ulcer: 20 mg to be taken once daily in the morning.
Erosive or Ulcerative Gastro-Oesophageal Reflux Disease (GORD): 20 mg to be taken once daily for four to eight weeks.
Gastro-Oesophageal Reflux Long-term Management (GORD Maintenance): For longterm management up to 12 months, a maintenance dose of RAZID 10 mg once daily can be used. Some patients may respond to a maintenance dose of 10 mg/day.
Eradication of H. pylori: RAZID 20 is indicated for H. pylori-positive duodenal ulcers, as part of the eradication programme with appropriate antibiotics.
Renal and hepatic impairment: No dosage adjustment is necessary for patients with renal or hepatic impairment.
Caution is however advised when RAZID 20 is first initiated in patients with severe hepatic dysfunction.
Children: RAZID is not recommended for use in children, as there is no experience of its use in this group.
Overdosage
No specific antidote is known. Rabeprazole Sodium is extensively protein bound and is, therefore, not readily dialysable. Treatment should be supportive and symptomatic.
Contraindications
RAZID 20 is contra-indicated in: patients with known hypersensitivity to Rabeprazole sodium, substituted Benzimidazoles or to any excipient used in the formulation; Pregnancy and lactation.
Special Precautions
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 RAZID 20. Although no evidence of significant drug related safety problems was seen in a study of patients with mild to moderate hepatic impairment versus normal age and sex matched controls, the prescriber is advised to exercise caution when treatment with RAZID 20 is first initiated in patients with severe hepatic dysfunction.
Use In Pregnancy & Lactation
Pregnancy: There are no data on the safety of Rabeprazole in human pregnancy. RAZID 20 is contraindicated during pregnancy.
Lactation: It is not known whether Rabeprazole Sodium is excreted in human breast milk. No studies in lactating women have been performed. Rabeprazole Sodium is however excreted in rat mammary secretions. Therefore RAZID 20 should not be used during breast feeding.
Adverse Reactions
The most common adverse events were headache, diarrhoea and nausea. Other adverse events were rhinitis, abdominal pain, asthenia, flatulence, pharyngitis, vomiting, non-specific pain/back pain, dizziness, flu syndrome, infection, cough, constipation and insomnia.
Further less frequent adverse events were rash, myalgia, chest pain, dry mouth, dyspepsia, nervousness, somnolence, bronchitis, sinusitis, chills, eruction, leg cramps, urinary tract infection, arthralgia and fever.
In isolated cases, anorexia, gastritis, weight gain, depression, pruritus, vision or taste disturbances, sweating and leucocytosis have been observed. Increased hepatic enzymes have been observed in 2% of patients. There have been reports of thrombocytopenia, neutropenia and leukopenia.
Drug Interactions
Rabeprazole Sodium, as is the case with other members of the Proton Pump Inhibitor (PPI) class of compounds, is metabolised through the cytochrome P450 (CYP450) hepatic drug metabolising system. Studies in healthy subjects have shown that Rabeprazole Sodium does not have clinically significant interactions with other drugs metabolised by the CYP450 system, such as Warfarin, Phenytoin, Theophylline or Diazepam.
Rabeprazole Sodium produces a profound and long lasting inhibition of gastric acid secretion. An interaction with compounds whose absorption is pH dependent may occur therefore the potential for such interaction was investigated. Co-administration of rabeprazole Sodium results in a 33% decrease in ketoconazole levels and a 22% increase in trough Digoxin levels in normal subjects. Therefore individual patients may need to be monitored to determine if a dosage adjustment is necessary when such drugs are taken concomitantly with RAZID. In clinical trials, antacids were used concomitantly with the administration of RAZID 20 and, in a specific study designed to define this interaction, no interaction with liquid antacids was observed. There was no clinically relevant interaction with food.
In vitro studies with human liver microsomes indicated that Rabeprazole Sodium is metabolised by isoenzymes of CYP450 (CYP2C19 and CYP3A4). The studies suggest a low interaction potential; however the effect on cyclosporin metabolism is similar to that observed for other proton pump inhibitors.
Storage
Store below 25°C.
MIMS Class
Antacids, Antireflux Agents & Antiulcerants
ATC Classification
A02BC04 - rabeprazole ; Belongs to the class of proton pump inhibitors. Used in the treatment of peptic ulcer and gastro-oesophageal reflux disease (GERD).
Presentation/Packing
EC tab 20 mg x 10 x 10's.
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