Carnozol

Uses

Peptic ulcer disease, dyspepsia .

Short-term treatment in healing and symptomatic relief of duodenal ulcers and erosive or ulcerative Gastroesophageal Reflux Disease (GERD).

Maintaining healing and reducing relapse rates of heartburn symptoms in patients with GERD.

Treatment of daytime and night time heartburn and other symptoms associated with GERD.

Long-term treatment of pathological hypersecretory conditions, including Zollinger Ellison Syndrome.

In combination with Amoxicillin and Clarithromycin to eradicate Helicobacter pylori.

Carnozol is also used to associated treatment for these conditions: Duodenal Ulcer, Gastric Ulcer, Gastro-esophageal Reflux Disease (GERD), Heartburn, Helicobacter Pylori Infection, NSAID Associated Gastric Ulcers, Non-erosive Reflux Esophagitis Disease (NERD), Vomiting, Zollinger-Ellison Syndrome, Erosive reflux esophagitis

How Carnozol works

Polaprezinc increases the expression of various antioxidant enzymes, including superoxide dismutase 1 (SOD-1), SOD-2, heme oxygenase-1 (HO-1), glutathione S-transferase (GST), glutathione peroxidase (GSH-px), peroxidredoxin-1 (PRDX1; PRXI) and PRXD5 (PRXV).

This process occurs in the gastric mucosa, defending mucosal cells against reactive oxygen species. This drug inhibits the activity of the transcription factor nuclear factor-kappaB (NF-kB) and decreases the expression of various inflammatory cytokines, including interleukin (IL) 1beta, IL-6, IL-8, and tumor necrosis factor alpha (TNF-a).

Polaprezinc also promotes the expression of numerous growth factors, including as platelet-derived growth factor-B (PDGF-B), vascular endothelial growth factor (VEGF), and nerve growth factor (NGF), in addition to various heat shock proteins (HSPs), including HSP90, HSP70, HSP60, HSP47, HSP27, and HSP10. This process promotes tissue growth and protects against damage the gastric mucosa .

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 (hydrogen-potassium adenosine triphosphatase) 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 sulfenamide. When studied in vitro, rabeprazole is chemically activated at pH 1.2 with a half-life of 78 seconds.

Dosage

Carnozol dosage

Healing of Erosive or Ulcerative Gastroesophageal Reflux Disease (GERD): 20 mg to be taken once daily for 4 to 8 weeks. For those patients who have not healed after 8 weeks of treatment, an additional 8 week course may be considered.

Maintenance of Healing of Erosive or Ulcerative Gastroesophageal Reflux Disease (GERD Maintenance): The recommended adult oral dose is 20 mg once daily.

Treatment of Symptomatic Gastroesophageal Reflux Disease (GERD):The recommended adult oral dose is 20 mg once daily for 4 weeks. If symptoms do not resolve completely after 4 weeks, an additional course of treatment may be considered.

Healing of Duodenal Ulcers:The recommended adult oral dose is 20 mg once daily after the morning meal for a period up to four weeks. Most patients with duodenal ulcer heal within four weeks. A few patients may require additional therapy to achieve healing.

Helicobacter pylori Eradication:To Reduce the Risk of Duodenal Ulcer Recurrence-

• Rabeprazole Sodium 20 mg Twice Daily for 7 Days
• Amoxicillin 1000 mg Twice Daily for 7 Days
• Clarithromycin 500 mg Twice Daily for 7 Days

All three medications should be taken twice daily with the morning and evening meals. It is important that patients comply with the full 7-day regimen.

Treatment of Pathological Hypersecretory Conditions Including Zollinger-Ellison Syndrome: The dosage of Rabeprazole Sodium 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. Some patients may require divided doses. Doses up to 100 mg QD and 60 mg BID have been administered. Some patients with Zollinger-Ellision syndrome have been treated continuously with Rabeprazole Sodium for up to one year.

Side Effects

Rabeprazole Sodium may sometimes cause headache, diarrhoea, abdominal pain, vomiting, constipation, dry mouth, increased or decreased appetite, muscle pain, drowsiness and dizziness.

Toxicity

Copper deficiency can occur because polaprezinc contains zinc, which inhibits copper absorption. Pancytopenia and anemia, associated with copper deficiency, have been noted in patients with malnutrition . Precautions should be taken to monitor for symptoms of pancytopenia and anemia, especially in patients with poor nutrition. The toxic effects of high polaprezinc dosage were studied in dogs. In the studies, dosages of 50 mg/kg/day and higher resulted in vomiting, diarrhea and hypersalivation, reduced appetite and reduction in body weight gain for females administered high doses. In addition, increased alkaline phosphatase (marker of hepatic damage) and decreased urinary specific gravity (suggestive of renal damage), and pathological tissue changes in the kidney of the high dosed dogs of both genders were noted. These changes resolved upon completing a period of drug withdrawal .

Precaution

Administration of Rabeprazole Sodium to patients with mild to moderate liver impairment resulted in increased exposure and decreased elimination. Caution should be exercised in patients with severe hepatic impairment.

Interaction

Rabeprazole is metabolized by the Cytochrome P-450 (CYP-450) drug metabolizing enzyme system. Rabeprazole does not have clinically significant interactions with other drugs metabolized by the CYP-450 system,such as Warfarin and Theophylline given as single oral dose, Diazepam as a single intravenous dose, and Phenytoin given as a single intravenous dose. In normal subjects, co-administration of Rabeprazole 20 mg QD resulted in an approximately 30% decrease in the bioavailability of Ketoconazole and increase in the AUC and Cmax for digoxin of 90% and 29% respectively.

Elimination Route

Intestinal absorption of L-CAZ was studied in rats by Sano et al. using 14C- and 65Zn-labeled compounds. They suggested that L-CAZ dissociates to its components, L-carnosine and zinc, during intestinal absorption .

Absolute bioavailability is approximately 52%.

Half Life

The half-life of polaprezinc has been studied in rats and found to be approximately 2 hours .

1-2 hours (in plasma)

Elimination Route

Intestinal absorption of the drug was examined using 14C- and 65Zn-labeled compounds. Polaprezinc metabolizes into its components, L-carnosine and zinc, during intestinal absorption. It was found that the excretion rates after one administration using 14C-labeled L-CAZ to rats were 4.1% in urine, 13.3% in feces, and 38.8% in exhalation. The study using 65Zn-labeled Paleprozinc were 0.3% in urine and 85.0% in the feces. The absorption rate of zinc is estimated to be approximately 11% .

Following a single 20 mg oral dose of 14C-labeled rabeprazole, approximately 90% of the drug was eliminated in the urine, primarily as thioether carboxylic acid; its glucuronide, and mercapturic acid metabolites.

Pregnancy & Breastfeeding use

Rabeprazole is FDA Pregnancy Category B. No data is available on administration of Rabeprazole to pregnant women. However this drug should be used during pregnancy, only if clearly needed. There are no data on the excretion of Rabeprazole into the breast milk. A decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the benefit of the drug to the mother.

Contraindication

Rabeprazole Sodium is contraindicated in patient with known hypersensitivity to Rabeprazole or to any component in the product.

Special Warning

Use in pediatric patients: The safety and effectiveness of Rabeprazole in pediatric patients have not been established.

Acute Overdose

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 overdosage, treatment should be symptomatic and supportive.

Storage Condition

Store below 25°C, protected from light and moisture. Keep all medicines out of the reach of the children.

Innovators Monograph

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