Barole

Barole

rabeprazole

Manufacturer:

Mega Lifesciences

Distributor:

Maxxcare
Full Prescribing Info
Contents
Rabeprazole sodium.
Description
Barole also contains the following inactive ingredients: Hypromellose, methacrylic acid copolymer, macrogol, povidone, purified talc, light magnesium carbonate and sodium hydroxide.
Rabeprazole is a substituted benzimidazole that inhibits gastric acid secretion. It is 2-[[4-(3-methoxypropoxy)-3-methyl-2-pyridinyl]sulfinyl]-1H-benzimidazole sodium salt. It has an empirical formula of C18H20N3Na03S and a molecular weight of 381.43.
Action
Pharmacology: Pharmacodynamics: 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 if 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: After oral administration of rabeprazole 20 mg, peak plasma concentrations (Cmax) of rabeprazole occur over a range of 2-5 hrs (Tmax). There is no appreciable accumulation when doses of 10-40 mg are administered every 24 hrs; the pharmacokinetics of rabeprazole is not altered by multiple-dosing. The plasma half-life (t½) ranges from 1-2 hrs.
Following oral administration of rabeprazole 20 mg, it is absorbed and can be detected in plasma by 1 hr. Absolute bioavailability for a rabeprazole 20-mg oral compared to IV is about 52%. Rabeprazole is 96.3% bound to human plasma proteins.
Rabeprazole is extensively metabolized. The thioether and sulfone 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 (CYP450) 3A (sulfone metabolite) and 2C19 (desmethyl rabeprazole). Approximately, 90% of the drug is eliminated in the urine, primarily as thioether carboxylic acid; its glucuronide and mercapturic acid metabolites.
The antisecretory effect begins within 1 hr after administration of rabeprazole 20 mg. The median inhibitory effect of rabeprazole on 24-hr 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-hr period that the gastric pH >3 from 10-65%. This relatively prolonged pharmacodynamic action compared to the short pharmacokinetic half-life (1-2 hrs) reflects the sustained inactivation of the H+/K+-ATPase.
Injection: These metabolites were not observed to have significant anti-secretory activity. No unchanged rabeprazole is recovered in the urine or faeces.
Capsule: Special Populations: Geriatric: Reported data from clinical studies in healthy elderly subjects indicates that area under the time-concentration (AUC) values are approximately doubled and peak plasma concentration (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 pediatric patients 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 and 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.
Indications/Uses
Capsule: Short-term (4-8 weeks) treatment in the healing and symptomatic relief of erosive or ulcerative gastroesophageal reflux disease (GERD).
Maintenance for healing and reduction in relapse rates of heartburn symptoms in patients with erosive or ulcerative GERD.
Short-term (up to 4 weeks) treatment in the healing and symptomatic relief of duodenal ulcers. Most patients heal within 4 weeks.
Long-term treatment of pathological hypersecretory conditions including Zollinger-Ellison syndrome.
Injection: It is an alternative in patients for whom oral administration of rabeprazole is not indicated. Treatment of active duodenal ulcer with bleeding or severe erosions; active gastric ulcer with bleeding or severe erosions; short-term treatment of erosive or ulcerative gastroesophageal reflux disease (GERD); prevention of acid-aspiration during surgery; prevention of stress-induced mucosal injury in critical care; pathological hypersecretory conditions, including Zollinger-Ellison syndrome. 
Dosage/Direction for Use
Capsule: Barole should be administered before meals.
Adults: Healing of Erosive or Ulcerative GERD: Recommended Dose: One 20-mg cap once daily for 4-8 weeks.
Maintenance for Healing of Erosive or Ulcerative GERD (GERD Maintenance): Recommended Dose: One 20-mg cap once daily.
Healing of Duodenal Ulcers: Recommended Dose: One 20-mg cap once daily after the morning meal for a period up to 4 weeks. Most patients with duodenal ulcer heal within 4 weeks.
Treatment of Pathological Hypersecretory Conditions Including Zollinger-Ellison Syndrome: The dosage varies with the individual patient. Recommended Starting Dose: 60 mg once a day. Doses should be adjusted to individual patient's needs and should be continued as long as clinically indicated. Doses up to 100 mg four times daily and 60 mg twice daily 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.
Barole capsules should be swallowed whole. The capsules should not be chewed, crushed or split.
Injection: Recommended Dose: 1 vial (rabeprazole 20 mg) once daily.
The content of the vial needs to reconstituted with sterile water for injection 5 mL which should be given slowly over 5-15 min. 
Infusion: For IV infusion the reconstituted solution should be further diluted and administered as short-term infusion over 15-30 min.
Compatibility with Various IV Fluids: Barole injection is compatible with dextrose injection, dextrose saline injection. 
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.
Administration: The IV administration is recommended only in cases where the oral administration is not indicated. As soon as an oral therapy is possible the IV therapy should be discontinued. 
Parenteral routes of administration other than IV are not recommended.
Overdosage
There has been no experience with large overdoses with rabeprazole.
Patients with Zollinger-Ellison syndrome have been treated with up to rabeprazole 120 mg 4 times daily. 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
Hypersensitivity to rabeprazole, substituted benzimidazoles or to any component of Barole.
Special Precautions
General: It is an alternative in patients whom oral administration of rabeprazole is not indicated. Symptomatic response to therapy with rabeprazole does not preclude the presence of gastric malignancy.
In case of discoloration of content, please do not use and discard the vial.
Use in pregnancy & lactation: There are no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, rabeprazole should be used during pregnancy only if clearly needed.
Since many drugs are excreted in milk, caution should be exercised when rabeprazole is administered to a nursing mother.
Use in children: The safety and effectiveness of rabeprazole in pediatric patients have not been established.
Use in the elderly: No overall differences in safety or effectiveness were observed between geriatric and younger subjects.
Use In Pregnancy & Lactation
There are no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, rabeprazole should be used during pregnancy only if clearly needed.
Since many drugs are excreted in milk, caution should be exercised when rabeprazole is administered to a nursing mother.
Side Effects
Adverse effects with rabeprazole are mild to moderate in intensity and included malaise, diarrhea, nausea, skin eruptions, headache and dizziness. Abnormal laboratory findings [increased hepatic enzymes, lactate dehydrogenase (LDH), blood urea nitrogen] observed with rabeprazole were similar in incidence and severity with comparator agents and reversible with cessation of therapy. Inform the physician in case of any adverse reactions related to rabeprazole use.
Drug Interactions
Rabeprazole is metabolized by the CYP450 drug metabolizing enzyme system. Rabeprazole sodium undergoes an almost complete, mainly non-enzymatic, metabolism with renal elimination of the metabolites, CYP450 enzymes contributed to the fraction of metabolism, mediated enzymatically (injection only). Rabeprazole does not have clinically significant interactions with other drugs metabolized by the CYP450 system eg, warfarin, theophylline, diazepam and phenytoin.
Rabeprazole producers sustained inhibition of gastric acid secretion. An interaction with compounds which are dependent on gastric pH for absorption eg, ketoconazole may occur due to the 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.
Caution For Usage
Read instructions thoroughly before use. Use upon physician's prescription only. Do not use if there are any significant changes in appearance of the capsules.
Injection: Instructions for Use, Handling and Disposal: Reconstitution: To reconstitute add water for injection 5 mL to make a solution. 
After the preparation, the reconstituted solution must be used within 4 hours if stored at room temperature and within 24 hrs 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 color, precipitation, haziness or leakage. The unused portion should be discarded.
pH of the Reconstituted Solution: Between 11.2-12.5.
Storage
Store at temperatures below 25°C. Protect from light and moisture.
Shelf-Life: 24 months.
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 cap 20 mg x 30's. Inj (lyophilized in vial) 20 mg x 10 mL x 1's.
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