Durazol

Each EC tablet contains: Pantoprazole (as Sodium Sesquihydrate), USP 40 mg.
Pantoprazole (Durazol) is a cream to creamy yellow enteric-coated tablet, oval shaped, biconvex and plain on both sides.
The active ingredient in Pantoprazole for delayed-release tablet is a substituted benzimidazole, sodium 5-(difluoromethoxy)-2[[3,5- dimethoxy-2- pyridinyl)methyl]methyl )sulfinyl] 1H-benzimidazole sesquihydrate, a compound that inhibits gastric acid secretion. Its empirical formula is C₁₆H₁₄F₂N₃NaO₄S x 1.5 H₂O, with a molecular weight of 432.4. Pantoprazole sodium sesquihydrate is a white to off-while crystalline powder and is racemic. Pantoprazole has weakly basic and acidic properties. Pantoprazole sodium sesquihydrate is freely soluble in water, very slightly soluble in phosphate buffer at pH 7.4, and practically insoluble in n-hexane.
Pantoprazole is a proton pump inhibitor. It inhibits secretion of gastric acid by irreversibly blocking the enzyme system of hydrogen/potassium adenosine triphosphatase (H+/K+ ATPase), the "proton pump" of the gastric parietal cell. It is used in conditions where inhibition of the gastric acid secretion may be beneficial, including aspiration syndromes, dyspepsia, gastro-esophageal reflux disease, peptic ulcer disease and the Zollinger-Ellison syndrome.

Pharmacology: Pharmacokinetics: Pantoprazole is rapidly variably absorbed following oral administration. Absorption is not affected by food. Pantoprazole is acid-labile and pharmacokinetics may vary between the various formulations developed to improve oral bioavailability. The absorption of pantoprazole also appears to be dose-dependent, increasing the dosage above 40 mg has been reported to increase the plasma concentrations in a non-linear fashion because of saturable first-pass hepatic metabolism. In addition, absorption is higher after long-term administration. Bioavailability of pantoprazole may be increased in elderly patients, in some ethnic groups, such as Chinese, and in patients with impaired hepatic function, but is not markedly affected in patients with renal impairment.
Following absorption pantoprazole is almost completely metabolized in the liver, primarily by the cytochrome P450 isoenzyme CYP2C19, to des-methylpantoprazole; small amounts are also metabolized by CYP3A4, CYP2D6, and CYP2C9. Metabolites are excreted mainly (about 80%) in the urine, with the remainder being excreted in the bile. The terminal elimination half-life is about 1 hour and is prolonged in hepatic impairment, the half-life in patients with cirrhosis was 3 to 6 hours.

Pantoprazole is used for the treatment and relief of acid-related dyspepsia: gastroesophageal reflux disease, NSAID-associated ulceration, Zollinger-Ellison syndrome and in the management of peptic ulcer disease. It is also used for the prophylaxis of acid aspiration during general anesthesia.

Gastro-esophageal reflux disease: 20 mg to 40 mg once daily for 4 weeks or as prescribed by the physician.
Dyspepsia: 10 to 20 mg daily for 2 to 4 weeks or as prescribed by the physician.
Peptic ulcer disease: 20 mg daily as single dose, or 40 mg in severe cases or as prescribed by the physician.
NSAID-associated ulceration: 20 mg daily or as prescribed by the physician.
Zollinger-Ellison syndrome: 40 mg once daily or as prescribed by the physician.
Acid aspiration prophylaxis during general anesthesia: 40 mg in the evening before surgery and a further 40 mg two to six hours before the procedure or as prescribed by the physician.

There are no known symptoms of overdosage in man.

Patients known to be hypersensitive to pantoprazole.

Before giving pantoprazole to patients with gastric ulcers the possibility of malignancy should be considered since these drugs may mask symptoms and delay diagnosis. It should be used with caution in hepatic impairment.

Clinical experience in pregnant women is limited. In animal reproduction studies, signs of slight fetotoxicity were observed at doses above 5 mg/kg. There is no information on the excretion of pantoprazole into human breast milk. Pantoprazole tablets should only be used when the benefit to the mother is considered greater than the potential risk to the fetus/baby.

Adverse effects reported most frequently with pantoprazole have been headache, diarrhea and skin rashes: they have sometimes been severe enough to require discontinuation of treatment. Other effects include pruritus: fatigue, constipation, nausea and vomiting, flatulence, abdominal pain, arthralgia and myalgia, urticaria and dry mouth.
Pantoprazole may also increase the risk of gastrointestinal infections because of their acid suppressive effects.

Pantoprazole may increase gastrointestinal pH, concurrent use with ampicillin esters, iron salts or ketoconazole may result in a reduction in absorption of these medications.
Inhibition of the cytochrome P-450 enzyme system by pantoprazole, especially in high doses, may cause a decrease in the hepatic metabolism of anticoagulants (coumarin or indadione-derivative), diazepam or phenytoin, which may result in delayed elimination and increased blood concentrations, when these medications are used concurrently with pantoprazole.
Concurrent use of pantoprazole with bone marrow depressants may increase the leukopenic and/or thrombocytopenic effects of both medications. If concurrent use is required, dose observation for toxic effects should be considered.

Store at temperatures not exceeding 30°C.

Antacids, Antireflux Agents & Antiulcerants

A02BC02 - pantoprazole ; Belongs to the class of proton pump inhibitors. Used in the treatment of peptic ulcer and gastro-oesophageal reflux disease (GERD).

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