PANTALIX-40

(PANTOPRAZOLE 40mg TABLETS)

DESCRIPTION

PANTALIX-40 is Pantoprazole Delayed-Release Tablets. Pantoprazole is a white to off-white crystalline powder which melts with decomposition at about 155°C. It is a weak base, freely soluble in ethanol and methanol, and slightly soluble in acetone and isopropanol and very slightly soluble in water.

CLINICAL PHARMACOLOGY

Pharmacokinetics and Metabolism: Pantoprazole

PANTALIX-40 Tablets contain an enteric-coated Pantoprazole. Absorption of Pantoprazole begins only after the it leave the stomach. Absorption is rapid, with peak plasma levels of Pantoprazole occurring within 0.5 to 3.5 hours. Peak plasma concentrations of Pantoprazole and AUC are approximately proportional to doses up to 40 mg, but because of a saturable first pass effect, a greater than linear response in peak plasma concentration and AUC occurs with doses greater than 40 mg. The bioavailability of Pantoprazole increases slightly upon repeated administration of PANTALIX-40 Tablets.

Pharmacodynamics

Mechanism of Action

Pantoprazole belongs to the class of anti-secretory compounds, the substituted benzimidazoles, that do not exhibit anti cholinergic or H2 histamine antagonistic properties, but that suppress gastric acid secretion by specific inhibition of the H+/K+ ATPase enzyme system at the secretory surface of the gastric parietal cell.

Because this enzyme system is regarded as the acid (proton) pump within the gastric mucosa, Pantoprazole has been characterized as a gastric acid-pump inhibitor, in that it blocks 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 rapid disappearance from plasma, Pantoprazole can be found within the gastric mucosa for a day or more.

Antisecretory Activity

After oral administration, the onset of the anti-secretory effect of Pantoprazole occurs within one hour, with the maximum effect occurring within two hours. Inhibition of secretion is about 50% of maximum at 24 hours and the duration of inhibition lasts up to 72 hours. The anti-secretory effect thus lasts far longer than would be expected from the very short (less than one hour) plasma half-life, apparently due to prolonged binding to the parietal H+/K+ ATPase enzyme. When the drug is discontinued, secretory activity returns gradually, over 3 to 5 days. The inhibitory effect of Pantoprazole on acid secretion increases with repeated once-daily dosing, reaching a plateau after four days.

INDICATIONS AND USAGE

Duodenal Ulcer

PANTALIX-40 Delayed-Release Tablets are indicated for short-term treatment of active duodenal ulcer. Most patients heal within four weeks. Some patients may require an additional four weeks of therapy.

PANTALIX-40 Delayed-Release Tablets, in combination with clarithromycin and amoxicillin, are indicated for treatment of patients with H. pylori infection and duodenal ulcer disease (active or up to 1-year history) to eradicate H. pylori. Eradication of H. pylori has been shown to reduce the risk of duodenal ulcer recurrence.

Gastric Ulcer

PANTALIX-40 Delayed-Release Tablets are indicated for short-term treatment (4-8 weeks) of active benign gastric ulcer.

Treatment of Gastroesophageal Reflux Disease (GERD)

Symptomatic GERD

PANTALIX-40 Delayed-Release Tablets are indicated for the treatment of heartburn and other symptoms associated with GERD.

Erosive Esophagitis

PANTALIX-40 Delayed-Release Tablets are indicated for the short term treatment (4-8 weeks) of erosive esophagitis which has been diagnosed by endoscopy.

Maintenance of Healing of Erosive Esophagitis

PANTALIX-40 Delayed-Release Tablets are indicated to maintain healing of erosive esophagitis.

Pathological Hypersecretory Conditions

PANTALIX-40 Delayed-Release Tablets are indicated for the long-term treatment of pathological hypersecretory conditions (eg,Zollinger-Ellison syndrome, multiple endocrine adenomas and systemic mastocytosis).

CONTRAINDICATIONS

Pantoprazole

PANTALIX-40 Delayed-Release Tablets are contraindicated in patients with known hypersensitivity to any component of the formulation.

Dosage 40-160mg/twice a day