Barole 20/Barole Injection

Barole 20/Barole Injection

rabeprazole

Manufacturer:

Mega Lifesciences

Distributor:

Metro Drug
Full Prescribing Info
Contents
Rabeprazole sodium.
Description
Barole 20: Each capsule contains: Rabeprazole Sodium 20 mg (As enteric coated pellets).
Inactive Ingredients: Non pareil seeds, Hypromellose, Methacrylic acid copolymer dispersion, Macrogol, Purified Talc, Light Magnesium Carbonate, Sodium Hydroxide, Titanium dioxide, Ferric oxide (Red), Ferric oxide (black).
Barole Injection: Each vial contains: Rabeprazole sodium 20 mg.
Action
Pharmacology: Rabeprazole belongs to a class of antisecretory compounds (substituted benzimidazole proton-pump inhibitors) that do not exhibit anticholinergic or histamine H2-receptor antagonist properties, but suppress gastric acid secretion by inhibiting the gastric H+, K+ ATPase 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.
Pharmacokinetics: Barole 20: After oral administration of 20 mg Rabeprazole, peak plasma concentrations (Cmax) of Rabeprazole occur over a range of 2.0 to 5.0 hours (Tmax). There is no appreciable accumulation when doses of 10 mg to 40 mg are administered every 24 hours; the pharmacokinetics of Rabeprazole is not altered by multiple dosing. The plasma half-life ranges from 1 to 2 hours.
Following oral administration of 20 mg Rabeprazole, it is absorbed and can be detected in plasma by 1 hour. Absolute bioavailability for a 20 mg oral capsule of Rabeprazole is approximately 52%. Rabeprazole is 96.3% bound to human plasma proteins.
Rabeprazole is extensively metabolized. The thioether and sulphone are the primary metabolites measured in human plasma. These metabolites were not observed to have significant antisecretory activity. In vitro studies have demonstrated that Rabeprazole is primarily metabolized in the liver by cytochromes P450 3A (sulphone metabolite) and 2C19 (desmethyl Rabeprazole). 90% of the drug is eliminated in the urine, primarily as thioether carboxylic acid; its glucuronide, and mercapturic acid metabolites.
The anti-secretory effect begins within one hour after oral administration of 20 mg Rabeprazole. The median inhibitory effect of Rabeprazole on 24 hour gastric acidity is 88% of maximal after the first dose. Rabeprazole 20 mg inhibits basal and peptone meal-stimulated acid secretion versus placebo by 86% and 95%, respectively and increases the percent of a 24-hour period that the gastric pH>3 from 10% to 65%. This relatively prolonged pharmacodynamic action compared to the short pharmacokinetic half-life (1-2 hours) reflects the sustained inactivation of the H+, K+ ATPase.
Special Populations: Geriatric: Reported data from clinical studies in healthy elderly subjects indicates that AUC values are approximately doubled and Cmax increased by 60% compared to values in a parallel younger control group. There was no evidence of drug accumulation after once daily dosing.
Pediatric: The pharmacokinetics of Rabeprazole in pediatrics has not been studied.
Gender and race: In analysis of body mass and weight, Rabeprazole pharmacokinetics showed no clinically significant differences between male and female volunteers.
Renal disease: No clinically significant difference was observed in the pharmacokinetics of Rabeprazole between healthy volunteers and patients requiring maintenance haemodialysis.
Hepatic disease: Reported data from single dose clinical study indicates that AUC & elimination half lives are doubled in patients with mild to moderate liver cirrhosis as compared to healthy volunteers. No information exists on Rabeprazole disposition in patients with severe hepatic impairment.
Barole Injection: There is no appreciable accumulation when 10 to 40 mg dose is administered every 24 hours. The pharmacokinetic of Rabeprazole is not altered by multiple dosing. The plasma ½ life ranges from 1 to 2 hours. Absolute bioavailability for a 20 mg oral Rabeprazole compared to intravenous is about 52%. Rabeprazole is 96.3 % bound to plasma proteins. Rabeprazole is extensively metabolized. These metabolites do not have antisecretory activity. Approximately 90% of the drug is eliminated in the urine, primarily as thioether carboxylic acid; its glucuronide, and mercapturic acid metabolites. These metabolites were not observed to have significant anti-secretory activity. No unchanged Rabeprazole is recovered in the urine or feces.
Indications/Uses
Barole 20: Treatment of severe (erosive and ulcerative) gastroesophageal reflux disease, treatment of active peptic ulcer disease and for Zollinger-Ellison syndrome.
Barole Injection: For the treatment of severe gastroesophageal reflux disease, peptic ulcer disease and the Zollinger-Ellison syndrome.
Dosage/Direction for Use
Barole 20: Rabeprazole should be administered before meals.
Healing of Erosive or Ulcerative Gastroesophageal Reflux Disease (GERD): The recommended adult oral dose is 20 mg Rabeprazole to be taken daily for four to eight weeks.
Maintenance of Healing of Erosive or Ulcerative Gastroesophageal Reflux Disease (GERD Maintenance): The recommended adult oral dose is 20 mg Rabeprazole to be taken daily.
Healing of Duodenal Ulcers: The recommended adult oral dose is 20 mg Rabeprazole to be taken daily after the morning meal for a period up to four weeks. Most patients with duodenal ulcer heal within four weeks.
Treatment of Pathological hypersecretory conditions, including Zollinger-Ellison Syndrome: The dosage of Rabeprazole in patients with pathologic hypersecretory conditions varies with the individual patient. The recommended adult oral starting dose is 60 mg once a day. Doses should be adjusted to individual patient needs and should continue for as long as clinically indicated. Doses up to 100 mg QD and 60 mg BID have been administered.
No dosage adjustment is necessary in elderly patients, in patients with renal disease or in patients with mild to moderate hepatic impairment. Administration of Rabeprazole to patients with mild to moderate liver impairment resulted in increased exposure and decreased elimination. Due to the lack of clinical data on Rabeprazole in patients with severe hepatic impairment, caution should be exercised in those patients.
Rabeprazole (Barole) Capsules should be swallowed whole. The capsules should not be chewed, crushed or split.
Barole Injection: The intravenous administration is recommended only in cases where the oral administration is not indicated. As soon as an oral therapy is possible the intravenous therapy should be discontinued.
Recommended dose is intravenous administration of the content of one vial (20 mg Rabeprazole) once daily.
Parenteral routes of administration other than intravenous are not recommended.
Injection: The content of the vial needs to be reconstituted with 5 mL sterile water for injection, which should be given slowly over 5-15 min.
Infusion: For intravenous infusion the reconstituted solution should be further diluted and administered as short term infusion over 15-30 min.
Compatibility with various I.V. fluids: Rabeprazole sodium (Barole) Injection is compatible with Dextrose injection, Dextrose saline injection.
Dosage in Special Populations: No dosage adjustment is necessary in elderly patients, in patients with renal disease or in patients with mild to moderate hepatic impairment. Administration of Rabeprazole to patients with mild to moderate liver impairment results in increased exposure and decreased elimination. Due to the lack of clinical data on Rabeprazole in patients with severe hepatic impairment, caution should be exercised in these patients.
Reconstitution: To reconstitute add 5 mL of sterile water for injection to make a solution.
After preparation, the reconstituted solution must be used within 4 hours if stored at room temperature and within 24 hours if stored in refrigerator and the unused portion should be discarded.
As with all parenteral admixtures, the reconstituted or further diluted solution should be examined for change in colour, precipitation, haziness or leakage. The unused portion should be discarded.
pH of the reconstituted solution: Between 11.2-12.5.
Overdosage
Barole 20: There has been experience with large overdoses with Rabeprazole.
Patients with Zollinger-Ellison syndrome have been treated with up to 120 mg Rabeprazole QD. No specific antidote for Rabeprazole is known. Rabeprazole is extensively protein bound and is not readily dialyzable. In the event of overdosage, treatment should be symptomatic and supportive.
Barole Injection: There has been no experience with large overdoses of Rabeprazole. No specific antidote for Rabeprazole is known. Rabeprazole is extensively protein bound and is not readily dialyzable. In the event of overdosage, treatment should be symptomatic and supportive.
Contraindications
Rabeprazole is contraindicated in patients with known hypersensitivity to Rabeprazole, substituted benzimidazoles or to any component of the formulation.
Special Precautions
Symptomatic response to therapy with Rabeprazole does not preclude the presence of gastric malignancy.
Use in Children: The safety and effectiveness of Rabeprazole in pediatric patients have not been established.
Use in Elderly: No overall differences in safety or effectiveness were observed between geriatric subjects and younger subjects.
Barole Injection: It is an alternative in patients in whom oral administration of Rabeprazole is not indicated.
In case of discoloration of content, please do not use and discard the vial.
Use In Pregnancy & Lactation
Pregnancy: There are 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.
Lactation: Since many drugs are excreted in milk, caution should be exercised when Rabeprazole is administered to a nursing mother.
Adverse Reactions
Adverse effects/events with Rabeprazole are mild to moderate in intensity and included malaise, diarrhea, nausea, skin eruptions, headache and dizziness.
Abnormal laboratory findings (increased hepatic enzymes, LDH, blood urea nitrogen) observed with Rabeprazole were similar in incidence and severity with comparator agents and reversible with cessation of therapy.
Barole 20: Inform the doctor in case of any adverse reactions related to drug use.
Drug Interactions
Barole 20: Rabeprazole is metabolized by the cytochrome P450 (CYP450) drug metabolizing enzyme system. Rabeprazole does not have clinically significant interactions with other drugs metabolized by the CYP450 system, such as warfarin, theophylline, diazepam and phenytoin.
Rabeprazole produces sustained inhibition of gastric acid secretion. An interaction with compounds which are dependent on gastric pH for absorption like ketoconazole may occur due to magnitude of acid suppression observed with Rabeprazole. 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.
Barole Injection: Rabeprazole sodium undergoes an almost complete, mainly non-enzymatic, metabolism with renal elimination of the metabolites, CYP 450 enzymes contributed to the fraction of metabolism, mediated enzymatically. Rabeprazole does not have clinically significant interactions with other drugs metabolized by the CYP 450 system such as warfarin, theophylline, diazepam and phenytoin.
Storage
Barole 20: Store at temperatures not exceeding 30°C, away from direct sunlight.
Barole Injection: Store at temperatures not exceeding 30°C.
Protect from light and moisture.
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
Barole 20: Cap 20 mg (enteric coated pellets) x 30's.
Barole Injection: Powd for inj (vial) 20 mg x 10 mL x 1's.
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