Trade Names:Protonix- Tablets, delayed-release 20 mg- Tablets, delayed-release 40 mg- Granules for oral suspension, delayed-release 40 mg
Trade Names:Protonix IV- Injection, lyophilized powder for solution 40 mgPanto IV (Canada)Pantoloc (Canada)PMS-Pantoprazole IV (Canada)
Suppresses gastric acid secretion by blocking acid (proton) pump within gastric parietal cells.
C max is 2.5 mcg/mL (oral) and 5.52 mcg/mL (IV); bioavailability is approximately 77% (oral). T max is 2.5 h (oral). Oral administration with food may delay absorption up to 2 h or longer.
Pantoprazole distributes mainly in extracellular fluid. Vd is 11 to 23.6 L. Protein binding is approximately 98%, mainly to albumin.
Extensively metabolized in the liver through CYP-450. The main metabolic pathway is demethylation by CYP2C19 and oxidation by CYP3A4. No evidence of metabolites with pharmacologic activity. CYP2C19 displays genetic polymorphism because of deficiency in some populations (3% of white and black patients and 17% to 23% of Asian patients); these patients are known to be slow metabolizers of pantoprazole.
Urine (71%), feces (18%); no renal excretion of unchanged drug. The t ½ is 1 h, and 3.5 to 10 h in slow metabolizers. Total Cl is 7.6 to 14 L/h.
More than 24 h.
No adjustment in dosage is needed.Hepatic Function Impairment
Increase in serum elimination half-life to 7 to 9 h; AUC increases by 5- to 7-fold. No dosage adjustment is necessary.Elderly
Moderate increase in AUC (43%) and C max (26%) after oral administration. No dosage adjustment is recommended.Gender
A modest increase in AUC and C max in women. No dosage adjustment is recommended.
Short-term (up to 8 wk) treatment in the healing and symptomatic relief of erosive esophagitis associated with gastroesophageal reflux disease (GERD); long-term treatment of pathological hypersecretory conditions, including Zollinger-Ellison syndrome; maintenance of healing of erosive esophagitis associated with GERD.IV
Short-term (7- to 10-day) treatment of GERD associated with a history of erosive esophagitis, as an alternative to oral therapy in patients unable to continue oral pantoprazole; hypersecretory conditions associated with Zollinger-Ellison syndrome or other neoplastic conditions.
Laryngitis (oral only).
PO 40 mg/day.Pathological Hypersecretion Conditions Including Zollinger-Ellison SyndromeAdults
PO Recommended starting dosage is 40 mg twice daily, adjusting the dose to the patient's needs and continuing therapy as long as clinically indicated. Dosages up to 240 mg/day have been used. IV 80 mg every 12 h; based upon individual patient needs, the dosage may be increased to 80 mg every 8 h. Daily dosages of more than 240 mg or administered for more than 6 days have not been studied.Treatment of Erosive Esophagitis Associated With GERDAdults
PO 40 mg/day for up to 8 wk; an additional 8-wk course of treatment may be considered in patients who have not healed after 8 wk. IV 40 mg/day for 7 to 10 days.
Store tablets and granules for oral suspension at 68° to 77°F. Store injection at 59° to 86°F. Protect powder for injection from light. Reconstituted solution may be stored for up to 6 h at room temperature prior to further dilution. Admixed solution may be stored for up to 24 h at room temperature prior to IV infusion.
Plasma concentrations may be reduced by pantoprazole. Coadministration with atazanavir is not recommended.Azole antifungals (eg, itraconazole, ketoconazole)
Plasma levels of certain azole antifungals may be reduced. Avoid this combination if possible.Digoxin
Proton pump inhibitors may increase serum digoxin levels.Drugs depending on gastric pH for bioavailability (eg, ampicillin, iron salts, itraconazole, ketoconazole)
Absorption of these drugs may be affected.Gingko biloba
May reduce pantoprazole plasma concentrations. Avoid combination if possible.Midazolam, zinc
Incompatible with IV pantoprazole.Salicylates
Enteric-coated salicylates may dissolve more rapidly, increasing gastric adverse reactions.Warfarin
Increased INR and PT have been reported. Monitor INR and PT.
False-positive urine screening for tetrahydrocannabinol (THC).
Headache (9%); anxiety, asthenia, dizziness, hypertonia, migraine (1% or more); insomnia (1%); anterior ischemic optic neuropathy, confusion, hypokinesia, speech disorder, tinnitus, vertigo (postmarketing).
Rash (2%); severe dermatologic reactions (eg, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis) (postmarketing).
Pharyngitis, rhinitis (more than 1%); blurred vision (postmarketing).
Diarrhea (6%); abdominal pain, flatulence (4%); nausea, vomiting (2%); constipation, dyspepsia, gastroenteritis, GI disorder, rectal disorder (1% or more); eructation (1%); increased salivation, pancreatitis (postmarketing).
Urinary frequency, UTI (at least 1%); creatinine increased; interstitial nephritis (postmarketing).
Abnormal LFTs (2%); increased ALT (1% or more); hepatocellular damage leading to jaundice and hepatic failure (postmarketing).
Elevated CPK (postmarketing).
Injection-site reactions (including abscess, thrombophlebitis) (more than 1%).
Hyperlipidemia (at least 1%); hyperglycemia (1%); hypercholesterolemia, hyperuricemia.
Arthralgia, back pain, neck pain (at least 1%); rhabdomyolysis (postmarketing).
Bronchitis, cough increased, dyspnea, sinusitis, upper respiratory tract infection (at least 1%).
Chest pain, flu syndrome, infection, pain (1% or more); anaphylaxis, angioedema (postmarketing).
Category B .
Safety and efficacy not established.
Anaphylaxis has been reported with the use of IV pantoprazole.
May occur, particularly in patients who were once Helicobacter pylori positive.
Symptomatic response to therapy does not preclude the presence of gastric malignancy.
In long-term rodent studies, pantoprazole was carcinogenic and caused rare types of GI tumors. The relevance of these findings to tumor development in humans is unknown.
IV product contains edetate disodium. Consider zinc supplements in patients who are prone to zinc deficiency.
No adverse reactions were reported with pantoprazole 400 to 600 mg.
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