Pantoprol

Pantoprazole.

1 vial contains 40 mg of pantoprazole correspond to 46 mg of pantoprazole sodium sesquihydrate.

Pharmacology: Pantoprazole is a proton pump inhibitor. It accumulates in the acidic compartment of parietal cells and is converted to the active form, a sulfanilamide, which binds to hydrogen-potassium-ATP-ase at the secretory surface of gastric acid production, leading to inhibition of both basal and stimulated acid secretion. The duration of inhibition of acid secretion does not correlate with the much shorter elimination half-life of pantoprazole.
Pharmacokinetics: Absorption: Rapidly absorbed. However, absorption may be delayed up to 2 hours or more if pantoprazole is taken with food. Bioavailability (oral) 77%.
Distribution: Vd: Following intravenous administration to extensive metabolizers: 0.17 L per kg (11 to 23.6 L).
Protein binding: Very high (98%), primarily to albumin.
Biotransformation: Hepatic, extensive. The major enzyme involved in the metabolism of pantoprazole is the polymorphically expressed cytochrome P450 isoform S-mephenytoin hydroxylase, also known as CYP2C19. The primary metabolite is the conjugate desmethvlpantoprazole. Some patients who are deficient in this enzyme system will be slow metabolizers of pantoprazole. Patient who are slow metabolizers (3% of Caucasians of African-Americans; 17% to 23% of Asians) can produce plasma concentrations 5 times or more higher than patients with the enzyme present.
Half-life: Elimination-following oral or intravenous administration; 1 hour.
The half-life of pantoprazole is prolonged (7 to 9 hours) in patients with cirrhosis of the liver and in genetically determined slow metabolizers (3.5 to 10 hours).
Elimination: Renal 71%, fecal 18% (biliary excretion). Dialysis removes insignificant amounts of pantoprazole.

Treatment and symptomatic relief of erosive esophagitis In patients with gastroesophageal reflux disease (GERD).
Pathologic GI hypersecretory conditions associated with Zollinger-Ellison syndrome or other neoplastic conditions.

Gastroesophageal reflux disease: Intravenous infusion 40 mg at a rate of 3 mg (7 mL) per minute over approximately fifteen minutes each day for seven to ten days.
Pathologic GI hypersecretory conditions: Intravenous infusion 80 mg at a rate of 3 mg (7 mL) per minute over approximately fifteen minutes every 12 hours. Dosing frequency can be adjusted to individual patient needs base on acid output, measurements. In those patients needing a higher dose, 80 mg every 8 hours is expected to maintain acid output below 10 mEq per hour.
Note: Dosage adjustments are not necessary in patients with renal or hepatic impairment or in patients undergoing hemodialysis.
Treatment with Pantoprol should be discontinued as soon as the patient is able to resume taking pantoprazole delayed-release.

Limited experience. No adverse reactions were reported with pantoprazole 400 to 600 mg.
Treatment of overdose: Decontamination-activated charcoal, gastric lavage. Symptomatic and supportive-therapy as indicated.

Known hypersensitivity to Pantoprol, any other ingredient in the formulation, or other substituted benzimidazoles (e.g., esomeprazole, lansoprazole, omeprazole, rabeprazole).

Sensitivity Reactions: Anaphylaxis has been reported with the use of IV pantoprazole sodium. Immediate medical intervention and drug discontinuance are required if anaphylaxis or other severe hypersensitivity reactions occurs.
GI Effects: In long term animal studies, pantoprazole caused rare types of GI tumors, although the relevance of these finding to humans is unknown.
Respiratory Effects: Administration of proton-pump inhibitors has been associated with an increased risk for developing certain infections (e.g. community-acquired pneumonia).
Hepatic Effects: Mild, transient elevation of serum ALT (SGPT) have been reported with oral pantoprazole therapy. Serum ALT increase exceeding 3 times the upper limit of normal occurred in 0.4% of patients receiving pantoprazole 40 mg daily in short-term studies.
Use in Children: Safety and efficacy in children younger than 18 years of age have not been established.
Use in the Elderly: No dosage adjustment is necessary in geriatric patients.

Pregnancy: Category B. Animal reproduction studies have failed to demonstrate a risk to the fetus and there are no adequate and well-controlled studies in pregnant women or animal studies have shown an adverse effect, but adequate and well-controlled studies in pregnant women have failed to demonstrate a risk to the fetus in any trimester.
Lactation: Pantoprazole is distributed into milk: discontinue nursing or the drug because of potential risk in nursing infants.

Incidence less frequent or rare: Anaphylaxis: change in facial skin color, fast or irregular breathing, puffiness or swelling of the eyelids or around the eyes, shortness of breath, troubled breathing, tightness in chest, and/or wheezing, skin rash, hives, and itching.
Angioedema: large, hive-like swellings on eyelids, face, lips, mouth, and/or tongue.
Chest pain.
Dyspnea: shortness of breath.
Erythema multiforme: pain in joints or muscles, itching of redness of skin, bull's eye-like lesion on skin.
Gastroenteritis: abdominal pain, anorexia, diarrhea, nausea, weakness.
Hyperglycemia: increased frequency and volume of urination, unusual thirst.
Infection.
Injection site reaction: bleeding, blistering, burning, coldness, discoloration of skin, feeling of pressure, hives, infection, inflammation, itching, lumps, numbness, pain, rash, redness, scarring, soreness, stinging, swelling, tenderness, tingling, ulceration, warmth.
Jaundice: yellow eyes or skin.
Optic neuropathy, anterior ischemic: loss of vision sudden.
Pancreatitis: abdominal pain, nausea, vomiting.
Speech disorder.
Stevens-Johnson syndrome: aching joints and muscles, blistering, loosening, peeling, or redness of skin, unusual tiredness or weakness.
Toxic epidermal necrolysis: itching or redness skin, loosening and/or stripping off of top layer of skin, skin tenderness with burning.
Urinary tract infection: difficulty urinating, frequent urge to urinate, painful urination.
Incidence not determined-Observed during clinical practice with pantoprazole IV; estimates of frequency can not be determined.
Anterior ischemic optic neuropathy: blindness, blurred vision, decreased vision.
Hepatic failure: headache, stomach pain, continuing vomiting, dark-colored urine, general feeling of tiredness or weakness, light-colored stools, yellow eyes or skin.
Interstitial nephritis: bloody or cloudy urine, fever, skin rash, swelling of feet or lower legs, greatly decreased frequency of urination or amount of urine.
Pancytopenia: high fever, chills, unexplained bleeding or bruising, bloody, black, or tarry stools, pale skin, unusual tiredness or weakness, cough, shortness of breath, sores ulcers, or white spots on lips or in mouth, swollen glands.
Rhabdomyolysis: dark-colored urine, fever, muscle cramps or spasms, muscle pain or stiffness, unusual tiredness or weakness.

Gastric pH-Dependent Drugs: Pharmacokinetic interaction theoretically possible when pantoprazole is used concomitantly with gastric pH-dependent drugs (e.g., ampicillin esters, iron salts, ketoconazole); increased or decreased drug absorption at increased gastric pH values.
Drugs Affecting Hepatic Microsomal Isoenzymes: Pharmacokinetic interaction unlikely.
Warfarin: Potential increased international normalized ratio (INR) and prothrombin time when warfarin is used concomitantly with proton-pump inhibitors, including pantoprazole. Potential for abnormal bleeding and death; monitor for INR and prothrombin time increase when Pantoprol is used concomitantly with warfarin.
Sucralfate: Potential delayed absorption and decreased bioavailability of proton-pump inhibitor (e.g., lansoprazole, omeprazole); administer proton-pump inhibitor at least 30 minutes before sucralfate.
General Advice: For the treatment of gastroesophageal reflux disease (GERD), one vial of Pantoprol injection should be reconstituted with 10 mL of 0.9% sodium chloride injection to provide a solution containing about 4 mg/mL of Pantoprol; the reconstituted solution may be injected IV over not less than 2 minutes. Alternatively, the reconstituted solution may be diluted with 100 mL of 0.9% sodium chloride injection or 5% dextrose injection, to provide a final concentration of about 0.4 mg/mL. The diluted solution may be infused IV over a period of about 15 minutes (about 2.7 mg of the drug or 7 mL of solution per minute).
For the treatment of hypersecretory conditions, each of two 40-mg (of pantoprazole) vials of Pantoprol injection should be reconstituted with 10 mL of 0.9% sodium chloride injection: the total volume (approximately 20 mL) of reconstituted solution may be injected IV over not less than 2 minutes. Alternatively, the contents of both vials may be combined and diluted with 80 mL of 0.9% sodium chloride injection or 5% dextrose injection to a final volume of about 100 mL, providing a final concentration of about 0.8 mg/mL. The diluted solution may be infused IV over a period of about 15 minutes (about 5.3 mg of the drug or 7 mL of solution per minute ).
Reconstituted solutions may be stored for up to 2 hours at room temperature before further dilution, and diluted solutions may be stored for up to 12 hours at room temperature. Neither reconstituted nor diluted solutions need to be protected from light.
Health-care personnel (e.g., pharmacists, nurses) preparing reconstituted solutions using spiked IV system adapters should use caution because of the potential for breakage of the glass vial.
Pantoprol should be administered IV through a dedicated IV line or via a Y-site. Parenteral pantoprazole sodium solutions should be inspected visually for particulate matter and discoloration prior to administration whenever solution and container permit. Pantoprol for injection is incompatible by Y-site administration with midazolam hydrochloride injection and may be incompatible with solutions containing zinc. Y-site administration of Pantoprol IV should be discontinued immediately if precipitation or discoloration occurs.
For the treatment of pathologic hypersecretory conditions associated with Zollinger-Ellison syndrome or other neoplastic conditions, pantoprazole sodium for injection is administered IV every 8 or 12 hours. The frequency of administration may be individualized based on acid output measurements. Patients with Zollinger-Ellison syndrome may be vulnerable to serious complications of increased gastric acid secretion, even after a brief loss of gastric acid suppression.Therefore, transition from oral to IV and IV to oral formulations of gastric acid inhibitors should be performed in such a manner to ensure continuity of gastric acid suppression effects.

Store below 30°C. Protect powder for injection from light. Do not freeze reconstituted.

Antacids, Antireflux Agents & Antiulcerants

A02BC02 - pantoprazole ; Belongs to the class of proton pump inhibitors. Used in the treatment of peptic ulcer and gastro-oesophageal reflux disease (GERD).

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