Sufrate Pz Jar

Uses

Pantoprazole is used where suppression of acid secretion is of therapeutic benefit. Pantoprazole Is registered in the foltawing indications:

• Peptic ulcer diseases (PUD)
• Gastro-esophageal reflux diseases
• Treatment of ulcer resistant to M2 blocker
• Treatment of ulcer induced by NSAIDs
• Gl bleeding from stress or acid peptic diseases
• Eradication of Helicobacter pylori
• Zollinger-Ellison syndrome
• Prophylaxis for acid aspiration syndrome during induction of anesthesia

Sucralfate tablet is used for the treatment of acute, nonmalignant gastric and duodenal ulcers. Maintenance therapy to prevent the recurrence of duodenal ulcers.

Sucralfate suspension is used for the short-term (up to 8 weeks) treatment of active duodenal ulcer.

Sufrate Pz Jar is also used to associated treatment for these conditions: Erosive Esophagitis, GERD With Erosive Esophagitis, Gastro-esophageal Reflux Disease (GERD), Healing, Heartburn, Helicobacter Pylori Infection, Stress Ulcers, Zollinger-Ellison Syndrome, Conditions where a reduction of gastric acid secretion is required, Pathological hypersecretory conditionsDyspepsia, Gastric Ulcer, Gastritis, Gastro-esophageal Reflux Disease (GERD), Healing, Mucositis, Peptic Ulcer, Stress Ulcers, Active Duodenal ulcer, Antiplatelet Therapy

How Sufrate Pz Jar works

Hydrochloric acid (HCl) secretion into the gastric lumen is a process regulated mainly by the H(+)/K(+)-ATPase of the proton pump, expressed in high quantities by the parietal cells of the stomach. ATPase is an enzyme on the parietal cell membrane that facilitates hydrogen and potassium exchange through the cell, which normally results in the extrusion of potassium and formation of HCl (gastric acid).

Proton pump inhibitors such as pantoprazole are substituted benzimidazole derivatives, weak bases, which accumulate in the acidic space of the parietal cell before being converted in the canaliculi (small canal) of the gastric parietal cell, an acidic environment, to active sulfenamide derivatives. This active form then makes disulfide bonds with important cysteines on the gastric acid pump, inhibiting its function. Specifically, pantoprazole binds to the sulfhydryl group of H+, K+-ATPase, which is an enzyme implicated in accelerating the final step in the acid secretion pathway. The enzyme is inactivated, inhibiting gastric acid secretion. The inhibition of gastric acid secretion is stronger with proton pump inhibitors such as pantoprazole and lasts longer than with the H(2) antagonists.

The mechanism of action of this drug in the healing duodenal ulcers is not yet completely defined, however, there are several probable mechanisms that adequately describe the healing activity of sucralfate. There is evidence that sucralfate acts locally to aid in tissue healing, and not systemically .

Studies in both humans and animals have indicated that sucralfate forms a complex that binds to protein-rich exudate found on the surface of ulcers. It binds to albumin and fibrinogen preventing blood clot lysis by stomach acid (hydrochloric acid). Sucralfate increases the tissue levels of fibroblast growth factors and epidermal growth factors , leading to an increase in prostaglandins at the gastrointestinal tract lining, which promote the healing of gastrointestinal ulcers .

In the laboratory setting, a sucralfate-albumin film provides a barrier against the entry of hydrogen ions, which are a component of gastric acid. In humans, sucralfate, given at therapeutic doses for ulcers, decreases pepsin activity in gastric fluids by 32% . Pepsin has been shown to be damaging to tissues, further aggravating ulcer lesion inflammation . Bile salts have been implicated in mucosal injury to the gastrointestinal tract . Sucralfate has also been shown to adsorb bile salts in the laboratory, setting, which could further contribute to its beneficial effects in ulcer healing .

Dosage

Sufrate Pz Jar dosage

Tablet:

The usual recommended adult oral dose is 40 mg given once daily, preferably in the morning with or without food. The duration of therapy is ranging from 2-8 weeks.

• Duodenal ulcers: Pantoprazole 40 mg tablet once daily for 2-4 weeks.
• Gastric ulcer: Pantoprazole 40 mg tablet once daily for 4-8 weeks.
• Reflux esophagitis: Pantoprazole 40 mg tabletonce daily for 4-8 weeks.
• Ulcers induced by NSAIDs: Pantoprazole 40 mg tablet once daily.
• Maintenance therapy: Maintenance therapy should involve the lowest effective dose of the drug. Pantoprazole both 20 mg & 40 mg doses are safe and effective in maintaining patients with healed reflux esophagitis and PUD in remission.

IV Injection:

• Duodenal ulcer and gastric ulcer:40 mg once daily for 7-10 days
• Gastroesophageal reflux disease associatedwith a history of erosive esophagitis:40 mg once daily for 7-10 days
• Prevention of rebleeding in peptic ulcer:IV 80 mg, followed by 8 mg/hour infusion for 72 hours
• Prophylaxis of acid aspiration:80 mg IV every 12 h for 24 h, followed by 40mg every 12 h
• Long-term management of Zollinger-Ellison Syndrome and other pathological hypersecretory conditions: 80 mg IV every 12 hours, may increase to 80 mg every 8 hoursif needed, may titrate to higher doses depending on acid output.

Adult: Usual dose 1 gm 4 times daily to be taken 1 hour before meals and at bed time. Maximum daily dose is 8 gm. Four to six weeks treatment is usually needed for ulcer healing but upto twelve weeks may be necessary in resistant cases. Antacids may be used as required for relief of pain, but should not be taken half an hour before or after Gastalfet.

Elderly: There are no special dosage requirements for elderly patients but as with all medicines the lowest effective dose should be used.

children: Safety and efficacy in children have not been established

DIRECTION FOR USE OF IV INJECTION: Pantoprazole lyophilized powder and 0.9% Sodium Chloride Injection is for intravenous administration only and must not be given by any other route. Pantoprazole IV injection should be given as a slow intravenous injection. The solution for IV injection is obtained by adding 10 ml 0.9% Sodium Chloride Injection to the vial containing powder. After reconstitution the injection should be given slowly over a period of at least 2 to 5 minutes. Use only freshly prepared solution. The reconstituted solution may be stored at room temperature (up to 30° C) for a maximum 4 hours.

DIRECTION FOR USE OF IV INFUSION: Pantoprazole IV infusion should be given as an intravenous infusion over a period of approximately 15 minutes. Pantoprazole IV infusion should be reconstituted with 10 ml of 0.9% Sodium Chloride Injection and further diluted (admixed) with 0.9% Sodium Chloride Injection or 5% Dextrose or Lactated Ringer's Injection to a final volume of 100 ml. The reconstituted solution may be stored at room temperature (up to 30° C) for a maximum 4 hours prior to further dilution. The admixed solution may be stored at room temperature (up to 30° C) and must be used within 24 hours from the time of initial reconstitution.

Side Effects

No potentially life-threatening effects have been reported with Pantoprazole. Symptomatic adverse effects include headache and diarrhoea are two common reported adverse effects. Peripheral edema has been occasionally reported in female patients. Other side effects may include abdominal pain, dizziness, nausea, epigastric discomfort, flatulence, skin rash, pruritus etc.

The incidence and severity of side effects from sucralfate are very low. Mild side effect like constipation has been reported in some patients.

Toxicity

Rat Oral LD 50 747 mg/kg

Tumorigenicity

Because of the chronic nature of GERD, there may be a potential for long-term administration of pantoprazole. In long-term rodent studies, pantoprazole was carcinogenic and its administration lead to rare types of gastrointestinal tumors. The relevance of these findings to tumor development in humans is unknown at this time.

Teratogenic Effects

This drug falls under pregnancy category B category. Reproduction studies have been performed in rats at oral doses up to 88 times the recommended human dose (RHD), as well as in rabbits at oral doses up to 16 times the RHD, and have shown no evidence of impaired fertility or harm to the fetus caused by pantoprazole. No adequate and well-controlled studies in pregnant women have been completed. Because animal reproduction studies are not always predictive of human response, this drug should only be used during pregnancy if clearly required.

Nursing Mothers

Pantoprazole and its metabolites have been found to be excreted in the milk of rats. Pantoprazole excretion in human milk has been found in a study performed with a single nursing mother after one 40 mg oral dose. The clinical relevance of this finding is not known, however, it is advisable to take note of this finding when considering pantoprazole use during nursing. Many drugs excreted in human breastmilk have a risk for serious adverse effects in nursing infants.

Overdose

Overdosage has never been observed with sucralfate . It is unlikely, as administering a maximum dose of up to 12 g/kg/body weight in several animal species did not result in death. The lethal dose could not be determined in these studies . It is likely that overdose of sucralfate in humans would result in constipation, and supportive treatment would be advised .

Use in pregnancy

This drug is considered a pregnancy Category B drug. Studies have been performed in rodents and rabbits at doses up to 50 times the recommended human dose. No harm to the fetus has been observed in the abovementioned studies. Sufficient and well-controlled clinical trials have not been performed in pregnant women. Due to the fact that the results of animal studies are not always relevant to human response, sucralfate should be used during pregnancy only if it is deemed essential for the mother's health .

Use in nursing

Whether this drug is excreted in human milk is currently unknown. Many drugs are excreted in breast milk, therefore, if sucralfate is administered to a lactating and nursing woman, caution should be observed .

Carcinogenesis

24 month toxicity studies were performed in rodents, and the dose of sucralfate reached up to 1 g/kg (equivalent to 12 times the recommended human dose). No signs of sucralfate-related tumors were noted.

Precaution

Patients should be cautioned that Pantoprazole tablet should not be split, crushed or chewed. The tablet should be swallowed whole, with or without food in the stomach. Concomitant administration of antacid does not affect the absorption of Pantoprazole.

The product should only be used with caution in patients with renal dysfunction

Interaction

There is no interaction with concomitantly administered antacids. No dosage adjustment is needed with combination use of the following drugs: Theophylline, Caffeine, Diazepam, Digoxin, Ethanol, Metoprolol, Nifedipine or Warfarin.

Concomitant use of sucralfate may reduce the bioavailability of certain drugs as has been observed in animal studies with tetracycline, phenytoin and cimetidine and in human studies with digoxin. Administration of sucralfate with any of these drugs should be separated by two hours. Since sucralfate may hinder warfarin absorption, caution should be exercised when these two drugs are used together.

Volume of Distribution

The apparent volume of distribution of pantoprazole is approximately 11.0-23.6 L, distributing mainly in the extracellular fluid.

This drug is absorbed in a very small quantity, and normally localizes to inflamed gastrointestinal lesions .

Elimination Route

Pantoprazole is absorbed after oral administration as an enteric-coated tablet with maximum plasma concentrations attained within 2 – 3 hours and a bioavailability of 77% that does not change with multiple dosing . Following an oral dose of 40mg, the Cmax is approximately 2.5 μg/mL with a tmax of 2 to 3 hours. The AUC is approximately 5 μg.h/mL. There is no food effect on AUC (bioavailability) and Cmax.

Delayed-release tablets are prepared as enteric-coated tablets so that absorption of pantoprazole begins only after the tablet leaves the stomach.

This drug is absorbed from the gastrointestinal tract in very minimal quantities . The adsorbed sulfated disaccharide is excreted in the urine . This drug contains aluminum and after the administration of 1 g of sucralfate 4 times per day, about 0.001% to 0.017% of this aluminum content is absorbed in patients with normal renal function . This number is expected to increase in those with impaired renal function .

Half Life

About 1 hour

The half-life is not known. In animals, the elimination half-life of the sucrose component of this drug is from 6-20 h .

Clearance

Adults: With intravenous administration of pantoprazole to extensive metabolizers, total clearance is 7.6-14.0 L/h. In a population pharmacokinetic analysis, the total clearance increased with increasing body weight in a non-linear fashion.

Children: clearance values in the children 1 to 5 years old with endoscopically proven GERD had a median value of 2.4 L/h.

Sucralfate contains aluminum. The administration of sucralfate in non-dialyzed chronic renal failure patients warrants careful consideration from the treating physician as the excretion of absorbed aluminum may be decreased, causing possible aluminum toxicity .

In dialyzed patients diagnosed with chronic renal failure, aluminum toxicity related to sucralfate has been observed and reported. The daily amount of aluminum ingestion (including sucralfate) should be carefully examined before administering sucralfate in combination with other drugs also containing aluminum, including various antacids .

Elimination Route

After a single oral or intravenous (IV) dose of 14C-labeled pantoprazole to healthy, normal metabolizing subjects, about 71% of the dose was excreted in the urine, with 18% excreted in the feces by biliary excretion. There was no kidney excretion of unchanged pantoprazole.

The negligible amount of this drug that is absorbed is excreted mainly in the urine within 48 hours .

Pregnancy & Breastfeeding use

There are no adequate or well-controlled studies in pregnant women. Pantoprazole should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

It is not known whether Pantoprazole is excreted in human breast milk. Pantoprazole should be used during lactation only if the potential benefit justifies the potential risk.

Although animal studies show no evidence of foetal malformation, safety in pregnant women has not been established and Sucralfate should be used in pregnancy only if clearly needed.

It is not known whether this drug is excreted in human milk. Caution should be exercised when sucralfate is administered to nursing mothers.

Contraindication

It is contraindicated in patients with known hypersensitivity to Pantoprazole.

There are no known contraindications

Acute Overdose

There are no known symptoms of overdosage in humans. Since Pantoprazole is highly protein bound, it is not readily dialyzable. Apart from symptomatic and supportive management, no specific therapy is recommended.

There is no experience in human with overdosage

Storage Condition

Store in a cool, dry place and away from light. Keep out of the reach of children.

Store at 20-25° C.

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