S (-) Pantoprazole Sodium Tablets
Nexpan®-10/20 Tablets
Therapeutic category: Antiulcerative.
Composition:
Nexpan®-10 Tablets
Each enteric coated tablet contains:
S (-) Pantoprazole Sodium equivalent to
S (-) Pantoprazole ...... ............10 mg
Colours:Red Oxide of Iron,Yellow Oxide of Iron &
Titanium Dioxide IP
Nexpan®- 20 Tablets
Each enteric coated tablet contains:
S (-) Pantoprazole Sodium equivalent to
S (-) Pantoprazole ...... ............20 mg
Colours:Red Oxide of Iron,Yellow Oxide of Iron &
Titanium Dioxide IP
Description:
S (-) Pantoprazole sodium, the chirally pure
S-enantiomer of racemic pantoprazole, is a substituted
benzimidazole, sodium-5-(difluoromethoxy)-2-[[(3,4-
dimethoxy-2-pyridinyl) methyl] sulfinyl]-1H-
benzimidazole sesquihydrate, a compound that inRiBits
gastric acid secretion. Its empirical formula is
C,,H,,F,N,NaO,S x 1.5 Hg0, with a molecular weight
of 432.4.
Mechanism of Action:
S (-) Pantoprazole is a proton pump inhibitor (PPI)
that 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 effect is dose-
related and leads to inhibition of both basal and
stimulated gastric acid secretion irrespective of the
stimulus. The binding to the (H+, K+)-ATPase results
in a duration of antisecretory effect that persists longer
than 24 hours.
Pharmacokinetics:
S (-) Pantoprazole is prepared as an enteric coated
tablet so that absorption of Pantoprazole begins only
after the tablet leaves the stomach. S (-) Pantoprazole
absorption is not affected by concomitant administration
of antacids. Administration of S (-) PantoprazoJe with
food may delay its absorption; however, the Cmax and
the extent of Pantoprazole absorption (AUC) are not
altered. Thus, S (-) Pantoprazole may be taken without
regard to timing of meals. Pantoprazole is metabolized
in the liver.
Indications: For the treatment of:
• Duodenal ulcer and gastric ulcer
• Gastroesophageal Reflux Disease (GERD).
Dosage and Administration:
The usual recommended adult oral dose is 20 mg given
once daily for up to 8 weeks. Higher or lower doses
may be used at the discretion of the physician.
S (-) Pantoprazole enteric coated tablet should be
swallowed completely without chewing or crushing the
tablet, with or without food.
Contraindications:
Patients with known hypersensitivity to any component
of the formulation.
Precautions:
Should be used with caution in severe hepatic
impairment; pregnant and lactating women. Safety and
effectiveness in pediatric patients have not been
established.
Tablet to be swallowed whole.
It should not to be chewed.
Drug Interactions:
No clinically significant drug interactions.
Adverse effects:
Although clinical trials with S (-) Pantoprazole have
not shown any adverse event, the most common side
effects reported with pantoprazole are abdominal pain,
asthenia, chest pain, diarrhea, dizziness, headache,
pruritus, and rash.
Overdosage:
Reports of overdosage with S (-) Pantoprazole have
not been received.
Storage:
Store in a cool, dry and dark place.
Proton pump inhibitors are the most effective drugs used in antiulcer therapy
and have found worldwide popularity over the past decade.
These agents potently inhibit all phases of acid secretion. They have become the
mainstay of treatment of acid-related gastrointestinal diseases, including peptic ulcer disease and gastroesophagea! reflux disease. Proton pump inhibitors are considered to be drugs of choice in treating patients with duodenal ulcer, gastric ulcer, gastroesophageal reflux disease, erosive esophagitis and Zollinger-Ellison syndrome. They are also used in combination with antibiotics to eradicate Helicobacter pylori and thereby reduce the risk of peptic ulcer recurrence.
These are the most potent acid inhibitory agents available. The onset of
action is rapid, with a maximum acid inhibitory effect between 2 and 6 hours after administration and duration of inhibition lasting up to 72 to 96 hours.
The proton pump inhibitors are racemic mixtures containing equal amounts
of R- and S- enantiomers of the product. The S-enantiomer is thought to be more
potent than the R- enantiomer and a single enantiomeric product, the S-enantiomer of omeprazole has been approved by the US - FDA. Use of the single S-enantiomer decreases the interpatient variability in the pharmacokinetics of proton pump inhibitors.
Pantoprazole is an irreversible proton pump inhibitor (PPI) that reduces
gastric acid secretion and is an effective agent in the management of acid-related disorders. The currently used pantoprazole is a racemic mixture of equal amounts of R-and S-enantiomers.
The pure S-enantiomer of pantoprazole has recently been introduced.
Experimental studies as well as clinical data have demonstrated that S-pantoprazole confers varied advantages of pharmacokinetic consistency, safety and lower interaction potential over the racemate. This is in addition to the advantages of racemic pantoprazole including higher specificity in proton pump inhibition and higher bioavailability being retained in the single enantiomer.