Each vial contains: Pantoprazole Sodium equivalent to Pantoprazole 40 mg (Suitably buffered), Diluent (10ml glass ampoule).
Each ml contains: Sodium chloride injection BP 9 mg, Sterilized Water for injection BP q.s.
FOR I.V USE ONLY.
Pharmacology: Pantoprazole is a proton pump inhibitor. It inhibits specifically and dose-proportionately H+/K+ ATPase, the enzyme which is responsible for gastric acid secretion in the parietal cells of the stomach. The substance is a substituted benzimidazole which accumulates in the acidic environment of the parietal cells after absorption. There, it is converted into the active form, a cyclic sulphenamide which binds to the H+/K+ ATPase, thus inhibiting the proton pump and causing potent and long-lasting suppression of basal and stimulated gastric acid secretion.
Pharmacokinetics: A considerably higher Cmax occurs after intravenous administration compared with oral administration. In a study in healthy volunteers given 40 mg/day for 5 days, the steady state Cmax was 5.9 mg/L after intravenous administration and 1.7 mg/L after oral administration. Terminal half life is approximately 1 h. Volume of distribution is approximately 0.15 L/kg and clearance is approximately 0.1 L/h/kg. Pharmacokinetics do not vary after single or repeated administration. The plasma kinetics of pantoprazole are linear (in the dose range of 10 to 80 mg) after both oral and intravenous administration.
The serum protein binding of pantoprazole is approximately 98%. Pantoprazole is rapidly eliminated from serum and is almost exclusively metabolised in the liver. Renal elimination represents the most important route of excretion (approximately 80%) for the metabolites of pantoprazole, the rest are excreted with the faeces.
The main metabolite in both the serum and urine is desmethyl-pantoprazole which is conjugated with the sulphate. The half-life of the main metabolites (approximately 1.5 h) is not much longer than that of pantoprazole.
In studies in healthy volunteers, 2% of subjects showed a slower elimination of pantoprazole from serum/plasma, with an increase in terminal elimination half-life of up to 10 h. Patients with half-life of greater than 3.5 h and with an apparent clearance of less than 2 L/h/kg are considered to be slow metabolisers of pantoprazole.
Duodenal ulcer; Gastric ulcer; Moderate and severe reflux oesophagitis; Zollinger-Ellison Syndrome and other pathological hypersecretory conditions.
Duodenal ulcer, Gastric ulcer, moderate and severe reflux esophagitis: The recommended intravenous dosage is one vial (40mg pantoprazole) per day.
Long-term management of Zollinger-Ellison Syndrome and other pathological hypersecretory conditions. Patients should start their treatment with a daily dose of 80mg. Thereafter, the dosage can be titrated up or down as needed using measurements of gastric acid secretion to guide. With dose above 80mg daily, the dose should be divided and given twice daily. A temporary increase of the dosage above 160mg pantoprazole is possible but should not be applied longer than required for adequate acid control. In case of rapid acid control is required a starting dose of 2x80mg pantoprazole is sufficient to manage a decrease of acid output into the target range (<10mEq/h) within one hour in the majority of patients. Transition from intravenous to oral formulations of pantoprazole should be performed as soon as it is clinically justified.
Reconstitution: A ready-to-use solution is prepared by injecting 10ml of physiological sodium chloride solution into the vial containing the dry powder. Reconstituted solution may be given intravenously (over 2 minutes) or may be added to 100ml of 0.9% sodium chloride injection or 5% glucose injection (for 15-minute infusion at a rate of approximately 7ml/min).
The admixed solution is stable up to 24 hours at 30°C.
Stripole should not be prepared or mixed with solvents other than those stated.
As soon as oral therapy is possible, treatment with pantoprazole I.V should be discontinued and 40mg oral pantoprazole should be administered instead.
The drug should be administered intravenously over 2-15 minutes.
Use in children: There are no data currently available on the use of pantoprazole in children.
Use in Elderly: Dosage adjustment not required.
Renal impairment: Dosage adjustment not required.
Hepatic impairment: Dosage adjustment not required. In patients with severe hepatic impairment the dose should be reduced to 20mg per day.
There are no known symptoms of overdosage in human. Dose up to 240mg i.v were administered without adverse effects. Symptomatic and supportive treatment are required in the case of overdosage.
Hypersensitivity to Pantoprazole, substituted benzimidazoles or any component of the formulation.
Check the following before use: The intravenous administration of Pantoprazole for injection is recommended only if oral application is not appropriate.
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.
Clinical experiment in pregnant women is limited. In animal reproduction studies, signs of slight fetotoxicity were observed at dosed above 5mg/kg. There is no information on the excretion of pantoprazole into human breast milk. Pantoprazole should not be used when the benefit to the mother is considered greater than potential risk to the foetus/baby.
Body as a whole: Fatigue, asthenia, increased sweating. Rare reports of fever, anaphylactic reactions including anaphylactic shock and peripheral oedema. Very rare reports of substernal chest pain and hot flushes.
Central and peripheral nervous system disorders: Headache. Uncommon reports of dizziness. Very rare reports of reduced movement and speech disorder.
Gastrointestinal system disorders: Diarrhoea, severe eructation, constipation or flatulence, dry mouth, upper abdominal pain. Uncommon reports of nausea and vomiting. Very rare reports of faecal discolouration and increased saliva.
Skin and appendages: Uncommon reports of allergic reactions such as pruritus and skin rash. Rare reports of angioedema, urticaria. Very rare reports of severe skin reactions such as Stevens Johnson Syndrome, toxic epidermal necrolysis, erythema multiforme, Lyell syndrome and photosensitivity.
Pantoprazole is metabolised in the liver via the cytochrome P450 enzyme system. An interaction of pantoprazole with other drugs or compounds which are metabolised using the same enzyme system cannot be excluded. However, no clinically significant interactions were observed in specific tests with a number of such drugs or compounds, namely carbamazepine, caffeine, diazepam, diclofenac, digoxin, ethanol, glibenclamide, metoprolol, nifedipine, phenytoin, theophylline, and oral contraceptive. There was also no interaction with a concomitantly administered antacid (aluminium hydroxide and magnesium hydroxide).
Store at a temperature below 30°C, protect from light.
A02BC02 - pantoprazole ; Belongs to the class of proton pump inhibitors. Used in the treatment of peptic ulcer and gastro-oesophageal reflux disease (GERD).
Sign Out
