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Logo PANTOCID 40 MG INJECTION

SCHEDULING STATUS:
S4

PROPRIETARY NAME
(and dosage form):

PANTOCID 40 MG INJECTION
Lyophilised Powder for Injection.

COMPOSITION
Each vial contains pantoprazole sodium equivalent to 40 mg
pantoprazole.

PHARMACOLOGICAL CLASSIFICATION
A. 11.4.3 Medicines acting on the gastro-intestinal tract.

PHARMACOLOGICAL ACTION
Site and mechanism of action
Pantoprazole is a proton pump inhibitor, i.e. it inhibits specifically and dose-proportionally H+ , K+ ,-ATPase, the enzyme which is responsible for gastric acid secretion in the parietal cells of the stomach.
Pantoprazole is a substituted benzimidazole which accumulates in the acidic compartment of the parietal cells after absorption. In the parietal cell it is protonated and chemically re-arranged to the active inhibitor, a cyclic sulphenamide, which binds to the H+, K+ ,-ATPase, thus inhibiting the proton pump and causing suppression of stimulated and basal gastric acid secretion after single and multiple intravenous and oral pantoprazole dosing. Because pantoprazole acts distal to the receptor level, it can influence gastric acid secretion irrespective of the nature of the stimulus.
Pantoprazole exerts its full effect in a strongly acidic environment (pH<3) and remains mostly inactive at higher pH values, which explains its selectivity for the acid secreting parietal cells of the stomach. Therefore, the complete pharmacological and therapeutic effect for pantoprazole can only be achieved in the acid-secreting parietal cells. By means of a feedback mechanism this effect is diminished at the same rate as acid secretion is inhibited.
Effect on gastric acid secretion
Although pantoprazole has a half-life of approximately 1 hour, the antisecretory effect increases during repeated once daily administration, demonstrating that the duration of action markedly exceeds the serum elimination half-life.

Pharmacokinetics
Absorption and distribution
Following intravenous administration of pantoprazole, serum/plasma concentrations decline biexponentially. The terminal half-life (t½) is about 1 hour. The total serum clearance is approximately 0,1 l/h/kg and the volume of distribution is about 0,15 l/kg.
The plasma kinetics for pantoprazole after both oral and intravenous administration is linear over the dose range 10 to 80 mg.
Metabolism
Pantoprazole is almost exclusively metabolised in the liver. The main metabolite is desmethylpantoprazole, which is conjugated with sulphate.
Elimination
Renal elimination represents the most important route of excretion (approximately 80%) for the metabolites of pantoprazole. The balance is excreted with the faeces. The half-life of the main metabolite is approximately 1½ hours which is slightly longer than that of pantoprazole.
Pharmacokinetic profile in patients with impaired liver or renal function
For patients with hepatic cirrhosis the elimination half-life values increased to between 7 to 9 hours. The AUC values increase by a factor of 5 to 7, while the maximum serum concentration only increases by a factor of 1,5 in comparison with healthy subjects.
A slight increase in AUC and Cmaxoccurs in elderly volunteers compared with younger patients.

INDICATIONS
PANTOCID 40 MG INJECTION is indicated for:
Short-term treatment of duodenal ulcer, gastric ulcer and reflux oesophagitis for intravenous administration to patients who cannot be treated orally.
If the duodenal ulcer has been demonstrated to be associated with Helicobacter pylori infection, pantoprazole used in combination with appropriate antibiotics may be useful.

CONTRA-INDICATIONS
Hypersensitivity to pantoprazole.
Safety and efficacy in children has not been established.
Severely impaired liver function (See SPECIAL PRECAUTIONS).

WARNINGS
PANTOCID 40MG INJECTION should only be administered intravenously,
and must not be given by any other route.

INTERACTIONS
Concomitant intake of food has no influence on the bioavailability.
PANTOCID 40 MG INJECTION may reduce or increase the absorption of medicines whose bioavailability is pH-dependent, e.g. ketoconazole.
The active ingredient of PANTOCID 40 MG INJECTION is metabolised in the liver via the cytochrome P450 enzyme system. An interaction of PANTOCID 40 MG INJECTION with other drugs or compounds which are metabolised using the same enzyme system cannot be excluded.
No clinically significant interactions were, however, observed in specific tests with a number of such drugs or compounds, namely antipyrine, caffeine, carbamazepine, diazepam, diclofenac, digoxin, ethanol, glibenclamide, metoprolol, naproxen, nifedipine, phenytoin, piroxicam, theophylline, warfarin and oral contraceptives.
There were also no interactions with concomitantly administered antacids.

PREGNANCY AND LACTATION
Safety in pregnancy and during lactation has not been established.

DOSAGE AND DIRECTIONS FOR USE
The recommended dosage is one vial PANTOCID 40 MG INJECTION per day administered intravenously over 2 to15 minutes.
PANTOCID 40 MG INJECTION should be reconstituted with 10 mL of physiological sodium chloride solution into the vial containing the dry substance. The solution may be administered directly or it may be further diluted by mixing with 100 mL physiological sodium chloride solution or 5% glucose ONLY.
After preparation the solution must be used within 12 hours and any unused portion discarded after the 12 hours.
Duodenal ulcer
The recommended dosage is one vial PANTOCID 40 MG INJECTION once daily. The total treatment with intravenous and oral pantoprazole should be 2 to 4 weeks. If the duodenal ulcer has been demonstrated to be associated with Helicobacter pylori infection, PANTOCID 40 MG INJECTION used in combination with appropriate antibiotics may be useful.
Gastric ulcer
The recommended dose is PANTOCID 40 MG INJECTION once daily for 4 to 8 weeks.
In the case of a suspected gastric ulcer, malignancy of the gastric ulcer should be excluded, as treatment could conceal the symptoms and may delay diagnosis.
Reflux oesophagitis
The recommended intravenous dose is one vial PANTOCID 40 MG INJECTION once daily for 4 to 8 weeks.
Long-term management
Long-term treatment with PANTOCID 40 MG INJECTION is currently not indicated as there is insufficient clinical data.
Elderly patients
No dosage adjustment is necessary in the elderly.
Impaired renal and liver function
No dosage adjustment is required in the presence of impaired renal function. A daily dose of 20 mg of PANTOCID should not be exceeded in patients with mild to moderately severe liver impairment (see Pharmacokinetics and SPECIAL PRECAUTIONS).

SIDE EFFECTS AND SPECIAL PRECAUTIONS
Side Effects
Very common (10%); common (1% - <10%); uncommon (0,1% - <1%); rare (0,01% - <0,1%); very rare (<0,01%) including isolated cases.
Blood and lymphatic system
Very rare: Leukopenia, thrombocytopenia.
Gastro-intestinal disorders
Common: Gastro-intestinal complaints such as upper abdominal pain, diarrhoea, constipation or flatulence.
Uncommon: Nausea, vomiting.
Rare: Dry mouth.
General disorders and administration site conditions
Very rare: Injection site thrombophlebitis and peripheral oedema.
Hepatobiliary disorders
Very rare: Severe hepatocellular damage leading to jaundice with or without hepatic failure.
Immune system disorder
Very rare: Anaphylactic reactions including anaphylactic shock.
Metabolic disorders
Very rare: Increased liver enzymes (transaminases, gamma-GT), elevated triglycerides and increased body temperature.
Musculoskeletal, connective tissue and bone disorders
Rare: Arthralgia.
Very rare: Myalgia.
Nervous system disorders
Common: Headache.
Uncommon: Dizziness or disturbances in vision (blurred vision).
Psychiatric disorders
Very rare: Mental depression.
Renal and urinary system disorders
Very rare: Interstitial nephritis.
Skin and subcutaneous tissue disorders
Uncommon: Allergic reactions such as pruritus, and skin rash.
Very rare: Urticaria, angioedema and severe skin reactions such as Stevens-Johnson Syndrome, erythema multiforme, Lyell Syndrome and photosensitivity.

Special Precautions
In patients with severe liver impairment the liver enzymes should be monitored regularly during treatment with PANTOCID 40 MG INJECTION, particularly on long-term use. In the case of a rise of the liver enzymes PANTOCID 40 MG INJECTION should be discontinued. PANTOCID 40 MG INJECTION is not indicated for mild gastro-intestinal complaints such as nervous dyspepsia.
Prior to treatment the possibility of malignancy of gastric ulcer or a malignant disease of the oesophagus should be excluded, as the treatment with PANTOCID 40 MG INJECTION may alleviate the symptoms of malignant ulcers and can thus delay diagnosis.
Diagnosis of reflux oesophagitis should be confirmed by endoscopy.

KNOWN SYMPTOMS OF OVERDOSAGE AND PARTICULARS OF ITS TREATMENT
There are no known symptoms of overdosage in man. No specific therapeutic recommendation can be made in cases of overdosage.

IDENTIFICATION
A white to off-white lyophilised cake in a 10 mL colourless glass vial for intravenous injection.
The reconstituted solution is a clear yellowish solution.

PRESENTATION
PANTOCID 40 MG INJECTION is packed into 10 mL colourless USP type I tubular glass vial with 20 mm grey bromobutyl rubber stopper and 20 mm flip off aluminium seals with red colour.

STORAGE INSTRUCTIONS
Store below 25 ºC. Protect from light.
KEEP OUT OF REACH OF CHILDREN.

REGISTRATION NUMBER
A40/11.4.3/0072

NAME AND BUSINESS ADDRESS OF THE HOLDER OF REGISTRATION CERTIFICATE
Pharmaplan (Pty) Ltd.
106 16th Road
Midrand

DATE OF PUBLICATION OF THIS INSERT
7 April 2006

New addition to this site: April 2010
Source: Pharmaceutical Industry

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