Pantolev

A white or almost white lyophilized powder.
Each vial contains: Pantoprazole Sodium Sesquihydrate BP is eq. to Pantoprazole 40 mg.

Proton Pump Inhibitor.
Pharmacology: Pharmacodynamics: Mechanism of action: Pantoprazole is a substituted benzimidazole which inhibits the secretion of hydrochloric acid in the stomach by specific blockade of the proton pumps of the parietal cells.
Pantoprazole is converted to its active form in the acidic environment in the parietal cells where it inhibits the H+/K+-ATPase enzyme i.e. the final stage in the production of hydrochloric acid in the stomach. The inhibition is dose-dependent and affects both basal and stimulated acid secretion. In most patients, freedom from symptoms is achieved within 2 weeks. As with other proton pump inhibitors and H2 receptor inhibitors, treatment with pantoprazole reduces acidity in the stomach and thereby increases gastrin in proportion to the reduction in acidity. The increase in gastrin is reversible. Since pantoprazole binds to the enzyme distal to the cell receptor level, it can inhibit hydrochloric acid secretion independently of stimulation by other substances (acetylcholine, histamine, gastrin). The effect is the same whether the product is given orally or intravenously.
Pharmacodynamic effects: The fasting gastrin values increase under pantoprazole. On short-term use, in most cases they do not exceed the upper limit of normal. During long-term treatment, gastrin levels double in most cases. An excessive increase, however, occurs only in isolated cases. As a result, a mild to moderate increase in the number of specific endocrine (ECL) cells in the stomach is observed in a minority of cases during long-term treatment (similar to adenomatoid hyperplasia). However, according to the studies conducted so far, the formation of carcinoid precursors (atypical hyperplasia) or gastric carcinoids as were found in animal experiments have not been observed in humans.
An influence of a long term treatment with pantoprazole exceeding one year cannot be completely ruled out on endocrine parameters of the thyroid according to results in animal studies.
During treatment with antisecretory medicinal products, serum gastrin increases in response to the decreased acid secretion. Also CgA increases due to decreased gastric acidity. The increased CgA level may interfere with investigations for neuroendocrine tumours.
Available published evidence suggests that proton pump inhibitors should be discontinued between 5 days and 2 weeks prior to CgA measurements. This is to allow CgA levels that might be spuriously elevated following PPI treatment to return to reference range.
Pharmacokinetics: It is rapidly absorbed after oral administration. The drug is subject to low first-pass hepatic extraction, displaying an estimated absolute oral bioavailability of 77%. Concomitant food intake does not affect bioavailability.
Elimination is predominantly renal, with 80% of an oral or intravenous dose being excreted as urinary metabolites, the remainder is excreted in the faeces and originates primarily from biliary secretion.

Used for the treatment of gastroesophageal reflux disease, peptic ulcer disease and Zollinger-Ellison Syndrome.

Pantoprazole is given intravenously over 2 to 15 minutes, either as a slow injection or a short-term infusion. For peptic ulceration or gastroesophageal reflux disease, the recommended dose is 40 mg daily. A dose of 80 mg once or twice daily may be used for Zollinger-Ellison Syndrome; up to 240 mg daily may be given in divided doses. Patients should be switched to oral therapy as soon as possible.
Or as prescribed by the physician.

There are known symptoms of overdose in man.
Systemic exposure with up to 240 mg administered intravenously over 2 minutes were well tolerated. As pantoprazole is extensively protein bound, it is not readily dialysable.
In case of overdose with clinical signs of intoxication, apart from symptomatic and supportive treatment, no specific therapeutic recommendations can be made.

Contraindicated in patients with known hypersensitivity to any component of the formulation.

In presence of alarm symptoms: In the presence of any alarm symptom (e.g. significant unintentional weight loss, recurrent vomiting, dysphagia, haematemesis, anaemia or melaena) and when gastric ulcer is suspected or present, malignancy should be excluded, as treatment with pantoprazole may alleviate symptoms and delay diagnosis.
Further investigation is to be considered if symptoms persist despite adequate treatment.
Hepatic impairment: In patients with severe liver impairment, the liver enzymes should be discontinued.
Co-administration with atazanavir: Co-administration of atazanavir with proton pump inhibitors is not recommended. If the combination of atazanavir with a proton pump inhibitor is judged unavoidable, close clinical monitoring (e.g. virus load) is recommended in combination with an increase in the dose of atazanavir to 400 mg with 100 mg of ritonavir. A pantoprazole dose of 20 mg per day should not be exceeded.
Gastrointestinal infections caused by bacteria: Pantoprazole, like all proton pump inhibitors (PPIs), might be expected to increase the counts of bacteria normally present in the upper gastrointestinal tract. Treatment with pantoprazole may lead to a slightly increased risk of gastrointestinal infections caused by bacteria (e.g. Salmonella and Campylobacter and C. difficile).
Subacute cutaneous lupus erythematosus (SCLE): Proton pump inhibitors are associated with very infrequent cases of SCLE. If lesions occur, especially in sun-exposed areas of the skin, and if accompanied by arthralgia, the patient should seek medical help promptly and the healthcare professional should consider stopping Pantoprazole. SCLE after previous treatment with a proton pump inhibitor may increase the risk of SCLE with other proton pump inhibitors.
Interference with laboratory tests: Increased Chromogranin A (CgA) level may interfere with investigations for neuroendocrine tumours. To avoid this interference, Pantoprazole 40 mg, powder for solution for injection treatment should be stopped for at least 5 days before CgA measurements. If CgA and gastrin levels have not returned to reference range after initial measurement, measurements should be repeated 14 days after cessation of proton pump inhibitor treatment.
Sodium: This medicinal product contains less than 1 mmol (23 mg) sodium per dose, i.e. essentially "sodium-free".

Pregnancy: There are no adequate data from the use of pantoprazole in pregnant women. Studies in animals have shown reproductive toxicity. The potential risk for humans is unknown.
Pantoprazole should not be used during pregnancy unless clearly necessary.
Lactation: Animal studies have shown excretion of pantoprazole in breast milk. Excretion into human milk has been reported. Therefore, a decision on whether to continue/discontinue breastfeeding or to continue/discontinue therapy with pantoprazole should be made taking into account the benefit of breast-feeding to the child and the benefit of pantoprazole therapy to women.

The most commonly side effects are headache, diarrhoea, dizziness, pruritus, skin rash, flatulence, abdominal pain, rash, eructation, insomnia and hyperglycemia.

Phenazone (antipyrine), diazepam, digoxin, theophylline, carbamazepine, diclofenac, phenprocoumon, phenytoin, warfarin, nifedipine, caffeine, metoprolol or ethanol: No clinically relevant interaction at therapeutic doses.
Oral contraceptives: Does not appear to compromise hormonal contraceptive efficacy as no interaction with low dose combined oral contraceptive has been seen.

Direction for Reconstitution: As sterile freeze-dried powder for reconstitution with 10 mL of Sodium chloride Injection.
Reconstituted injection is to be used within 24 hours if stored at a temperature not exceeding 30°C and within 24 hours if stored in refrigerator. In case of discoloration, do not use and discard the vial.

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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