INDICATIONS     CONTRA-INDICATIONS     DOSAGE     SIDE-EFFECTS     PREGNANCY     OVERDOSE     IDENTIFICATION     PATIENT INFORMATION

Logo PANTOCID 20 enteric-coated tablets
PANTOCID 40 enteric-coated tablets

SCHEDULING STATUS:
S4

PROPRIETARY NAME
(and dosage form):

PANTOCID 20 enteric-coated tablets
PANTOCID 40 enteric-coated tablets

COMPOSITION:
PANTOCID 20:
Active ingredient:
Each tablet contains pantoprazole sodium sesquihydrate equivalent to 20 mg
pantoprazole.
PANTOCID 40:
Active ingredient:
Each tablet contains pantoprazole sodium sesquihydrate equivalent to 40 mg pantoprazole.

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

PHARMACOLOGICAL ACTION:
Pharmacodynamics
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 sulphonamide, 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
Following oral administration, pantoprazole inhibits the pentagastrin-stimulated gastric acid secretion. The mean acid inhibition was 85%, 2½ to 3½ hours after dosing with 40 mg/day for 7 days. Pantoprazole maintains the physiological pH-rhythm. The values, however, are shifted to higher levels. During the night, periods of pH values approximating placebo have been found to occur.
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
Pantoprazole is unstable in acid and is administered orally in the form of an enteric-coated tablet. Absorption takes place in the small intestine. On average, the maximum serum/plasma concentrations are approximately 2 to 3 µg/mL about 2½ hours after administration of 40 mg pantoprazole daily, as a single or multiple dose in healthy volunteers. The absolute systemic bioavailability of pantoprazole from single and multiple oral doses of pantoprazole is approximately 77%.
The plasma kinetics for pantoprazole after oral administration are linear over the dose range 10 –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 mild to moderately severe hepatic cirrhosis the elimination half-life values increase between 7 to 9 hours. The AUC values increase by a factor of 5 to 8, while the maximum serum concentration only increases by a factor of 1,5 in comparison with healthy subjects.
In patients with renal impairment the half-life of the main metabolite is moderately increased, but there is no accumulation at therapeutic doses. The half-life of pantoprazole in patients with renal impairment is comparable to the half-life of pantoprazole in healthy subjects. Pantoprazole is poorly dialysed.
A slight increase in AUC and C
max occurs in elderly volunteers compared with younger people.

INDICATIONS:
PANTOCID 40
is indicated for the short-term treatment of duodenal ulcer, gastric ulcer and reflux oesophagitis. If the duodenal ulcer has been demonstrated to be associated with Helicobacter pylori infection, PANTOCID 40 used in combination with appropriate antibiotics may be useful.
PANTOCID 40 is indicated for the treatment of Zollinger-Ellison Syndrome.
PANTOCID 20 is indicated for the symptomatic improvement (e.g. heartburn, acid regurgitation, pain on swallowing) and healing of mild gastro-esophageal reflux disease (GERD).
PANTOCID 20 is indicated for long-term management and prevention of relapse in gastro-esophageal reflux disease (GERD).

CONTRA-INDICATIONS:
Hypersensitivity to pantoprazole, or to any of the ingredients of PANTOCID.
Safety and efficacy in children has not been established.
Severely impaired liver function (see SPECIAL PRECAUTIONS).

WARNINGS:
See SPECIAL PRECAUTIONS

INTERACTIONS:
Concomitant intake of food has no influence on the bioavailability.
PANTOCID may reduce or increase the absorption of medicines whose absorption is pH-dependent, e.g. ketoconazole.
Atazanavir: It has been shown that co-administration of atazanavir/ritonavir with omeprazole or atazanavir with lansoprazole resulted in a substantial reduction in the bioavailability of atazanavir. The absorption of atazanavir is pH-dependent. Therefore, pantoprazole must not be co-administered with atazanavir (see CONTRA-INDICATIONS).
The active ingredient of PANTOCID is metabolised in the liver via the cytochrome P450 enzyme system. An interaction of PANTOCID with other medicines 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 medicines or compounds, namely antipyrine, caffeine, carbamazepine, diazepam, diclofenac, digoxin, ethanol, glibenclamide, metoprolol, naproxen, nifedipine, phenytoin, piroxicam, theophylline, warfarin and oral contraceptives. However, the response to anti-coagulants, such as warfarin, may be affected by any concomitant medication. Therefore, monitoring the patient with additional PT (prothrombin time) / INR (International normalised ratio) determinations when PANTOCID is initiated, discontinued or taken irregularly would be a good practice.

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

DOSAGE AND DIRECTIONS FOR USE:
The recommended once daily dose of PANTOCID should be taken in the morning. PANTOCID should be swallowed whole with a little water either before or during breakfast.
Duodenal ulcer
The recommended oral dose is 40 mg of PANTOCID once daily. The total treatment with pantoprazole should be 2 to 4 weeks. If the duodenal ulcer has been demonstrated to be associated with Helicobacter pylori infection, 40 mg of PANTOCID used in combination with appropriate antibiotics may be useful.
Gastric ulcer
The recommended oral dose is 40 mg of PANTOCID 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 oral dose is 40 mg of PANTOCID once daily in the morning for 4 to 8 weeks.
Zollinger-Ellison Syndrome
For the management of Zollinger-Ellison Syndrome patients should start their treatment with a daily dose of 80 mg of PANTOCID (two PANTOCID 40 tablets). Thereafter, the dosage can be titrated up or down, as needed using measurements of gastric acid secretion as a guide. With doses above 80 mg daily, the dose should be divided and given twice daily.
Mild gastro-oesophageal reflux disease (GERD)
The recommended oral dose is 20 mg of PANTOCID per day. A 4-week period is usually required for healing of mild GERD. If this is not sufficient, healing will usually be achieved within a further 4 weeks.
Long-term management and prevention of relapse in GERD
For long-term management a maintenance dose of one 20 mg PANTOCID tablet per day is recommended, increasing to 40 mg PANTOCID per day if a relapse occurs. After healing of the relapse, the dose can be reduced to 20 mg of PANTOCID. Experience with long-term administration is limited.
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:
Blood and lymphatic system
Less frequent: Leukopenia, thrombocytopenia.
Gastro-intestinal disorders
Frequent: Gastro-intestinal complaints such as upper abdominal pain, diarrhoea, constipation or flatulence.
Less frequent: Nausea, vomiting.
Rare: Dry mouth
Hepatobiliary disorders
Less frequent: Severe hepatocellular damage leading to jaundice with or without hepatic failure.
Immune system disorders
Less frequent: Anaphylactic reactions including anaphylactic shock.
Metabolic disorders
Less frequent: Increased liver enzymes (transaminases, gamma-GT), elevated triglycerides and increased body temperature.
Musculoskeletal, connective tissue and bone disorders
Less frequent: Arthralgia, myalgia.
Nervous system disorders
Frequent: Headache.
Less frequent: Dizziness or disturbances in vision (blurred vision).
Psychiatric disorders
Less frequent: Mental depression.
Renal and urinary system disorders
Less frequent: Interstitial nephritis.
Skin and subcutaneous tissue disorders
Less frequent: Allergic reactions such as pruritus, and skin rash, 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, particularly on long-term use. In the case of a rise of the liver enzymes PANTOCID should be discontinued.
PANTOCID 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 may alleviate the symptoms of malignant ulcers and can thus delay diagnosis.
Diagnosis of reflux oesophagitis should be confirmed by endoscopy.
Daily treatment with any acid-blocking medicines over a long period of time (e.g. longer than 3 years) may lead to malabsorption of cyanocobalamin caused by hypo- or achlorhydria. Rare cases of cyanocobalamin deficiency under acid-blocking therapy have been reported in the literature. This should be considered when respective clinical symptoms are observed.

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.
Treatment is symptomatic and supportive.

IDENTIFICATION:
PANTOCID 20:
Yellow, circular, biconvex, coated tablet imprinted “144” on one side and plain on the other side.
PANTOCID 40: Yellow, circular, biconvex, coated tablet imprinted “124” on one side and plain on other side.

PRESENTATION:
PANTOCID 20
is available in pack sizes of 7’s and 30 are packed in white smooth round HDPE containers.
PANTOCID 40 is available in pack sizes of 30 are packed in white smooth round HDPE containers.

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

REGISTRATION NUMBERS:
PANTOCID 20:
41/11.4.3/0787
PANTOCID 40: A40/11.4.3/0482

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

DATE OF PUBLICATION OF THIS INSERT:
1 October 2010

New addition to this site: May 2014
Source: Pharmaceutical Industry

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