 
COMPOSITION
ProtolocTM20 : Each enteric coated tablet contains Pantoprazole Sodium Sesquihydrate INN equivalent to Pantoprazole 20 mg.
ProtolocTM40 : Each enteric coated tablet contains Pantoprazole Sodium Sesquihydrate INN equivalent to Pantoprazole 40 mg.
PHARMACOLOGICAL INFORMATION
Mechanism of Action
Pantoprazole is chemically a novel substituted benzimidazole derivative, which suppresses the final step in gastric acid production by forming a covalent bond to two sites of the H+K+ATPase enzyme system at the secretory surface of the gastric parietal cell. This leads to inhibition of both basal and stimulated gastric acid secretion irrespective of the stimulus. The binding to the H+K+ATPase results in duration of antisecretory effect that persists longer than 24 hours.
PHARMACOKINETICS
Absorption
The absorption of pantoprazole is rapid, with a Cmax of 2.5 µg/mL that occurs approximately 2.5 hours after single or multiple oral 40 mg doses. Pantoprazole is well absorbed; it undergoes little first-pass metabolism resulting in an absolute bioavailability of approximately 77%. Pantoprazole absorption is not affected by concomitant administration of antacids. Administration of pantoprazole with food may delay its absorption up to 2 hours or longer; however, the Cmax and the extent of pantoprazole absorption (AUC) are not altered. Thus, pantoprazole may be taken without regard to timing of meals.
Distribution
The apparent volume of distribution of pantoprazole is approximately 11.0-23.6L, distributing mainly in extracellular fluid. The serum protein binding of pantoprazole is about 98%, primarily to albumin.
Metabolism
Pantoprazole is extensively metabolized in the liver through the cytochrome P450 (CYP) system. Pantoprazole metabolism is independent of the route of administration (intravenous or oral). The main metabolic pathway is demethylation, by CYP2C19, with subsequent sulfation; other metabolic pathways include oxidation by CYP3A4. There is no evidence that any of the pantoprazole metabolites have significant pharmacologic activity.
Elimination
After a single oral or intravenous dose of pantoprazole to healthy, normal metabolizer volunteers, approximately 71% of the dose was excreted in the urine with 18% excreted in the feces through biliary excretion. There was no renal excretion of unchanged pantoprazole.
CLINICAL INFORMATION Therapeutic Indications
Pantoprazole is indicated where suppression of acid secretion is of therapeutic benefit. Pantoprazole is registered for the following indications: -
Peptic ulcer disease (PUD)
Gastro esophageal reflux disease (GERD)
Treatment of ulcer resistant to H2 receptor antagonist (H2RAs)
Treatment of ulcers induced by NSAIDs
Gastrointestinal (GI) bleeding from stress or acid peptic disease
Eradication of Helicobacter pylori (in combination with antibiotics)
Zollinger-Ellison syndrome
Prophylaxis for acid aspiration syndrome during induction of anesthesia
Dosage And Administration
Pantoprazole enteric coated tablets are available for oral administration only. 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 to 4 weeks. Duodenal ulcer generally heals within 2 weeks.
Gastric ulcers: Pantoprazole 40 mg tablet, once daily for 4 to 8 weeks. Gastric ulcer generally heals within 4 weeks.
Reflux esophagitis: Pantoprazole 40 mg tablet, once daily for 4 to 8 weeks. Reflux esophagitis generally heals within 4 weeks of treatment.
In resistant ulcers: Pantoprazole 40 mg tablet, once daily for 8 weeks.
Ulcers induced by NSAIDs: Pantoprazole 40 mg tablet once daily, in patients receiving continuous treatment with NSAIDs. Eradication of Helicobacter pylori: Triple therapy of Pantoprazole 40 mg twice daily in combination with appropriate antibiotic for one week achieved eradication rates of 90 to100%.
Zollinger-Ellison syndrome: Pantoprazole 40 mg 4 tablets per day. Once control of acid secretion has been achieved, the dose should be gradually reduced to the lowest effective dose that maintains acid control.
Prophylaxis for acid aspiration syndrome during induction of anaesthesia: 1 or 2 Pantoprazole 40 mg tablet should be given the evening before surgery and repeated again the morning of surgery.
Maintenance therapy: Maintenance treatment should involve the lowest dose of the drug. Both 20 and 40 mg doses of Pantoprazole are safe and effective in maintaining patients with healed reflux esophagitis and PUD in remission.
Use In Pregnancy & Lactation
Pregnancy category B. There are no adequate and well-controlled studies in pregnant women. But animal reproduction studies have failed to demonstrate a risk to the fetus. Therefore, pantoprazole can be used during pregnancy 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 riskUse In Children Safety and effectiveness in pediatric patients have not been established. Use In Patient with Renal Impairment No dosage adjustment is necessary in patients with renal impairment or in patients undergoing hemodialysis.
Side Effects
Headache (1.3%) and diarrhoea (1.5%) are the two commonest reported adverse events. It doesn't influence renal, cardiovascular, respiratory, endocrine, cognitive or motor functions and no consistent change have been found in any biochemical or haematological parameters. Peripheral edema has occasionally been reported in female patients. Other side effects may include abdominal pain, dizziness, nausea, epigastric discomfort, flatulence, skin rash, pruritus etc.
Contraindications
Pantoprazole enteric coated tablets are contraindicated in patients with known hypersensitivity to any of the formulation.
Precautions
Patients should be cautioned that Pantoprazole enteric coated tablets should not be split, chewed or crushed.
Drug Interaction
Pantoprazole is metabolized through the cytochrome P-450 system, and subsequently undergoes Phase II conjugation. Based on studies evaluating possible interactions of Pantoprazole with other drugs metabolized by the cytochoreme P-450 system, no interaction has been observed and no dosage adjustment is needed with concomitant use of the following drugs; theophylline, antipyrine, caffeine, carbamazepine, diazepam, diclofenac, digoxin, ethanol, glyburide, an oral contraceptive (Levonorgestrel/ethinyl estradiol), metoprolol, nifedipine, phenytion, or warfarin. There was also no interaction with concomitantly administered antacids and food.
Over Dosage
There are no known symptoms of over dosage in humans. Since Pantoprazole is highly protein bound, it is not readily dialyzable. Apart from symptomatic and supportive management, no specific therapy is recommended.
PHARMACEUTICAL INFORMATION
Storage Conditions
Store in a cool and dry place, away from light. Keep out of reach of children.
Presentation & Packaging
ProtolocTM20 : Each commercial box contains 50 tablets in Alu-Alu blister pack.
ProtolocTM40 : Each commercial box contains 50 tablets in Alu-Alu blister pack. |