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Product Name
:
PROTOM
Chemical Name
:
Pantoprazole Sodium
Therapeutic Category
:
Gastro-intestinal drugs
Pharmacologic Category
:
Proton Pump Inhibitor - Substituted Benzimidazole
Pharmaceutical Form
:
Tablets
Composition
:
Pantoprazole Sodium 40mg
Dosing
 
Dosing: Adult
Erosive esophagitis associated with GERD:
Oral:
Treatment: 40 mg once daily for up to 8 weeks; an additional 8 weeks may be used in patients who have not healed after an 8-week course
Maintenance of healing: 40 mg once daily
Note: Lower doses (20 mg once daily) have been used successfully in mild GERD treatment and maintenance of healing
Hypersecretory disorders (including Zollinger-Ellison):
Oral: Initial: 40 mg twice daily; adjust dose based on patient needs; doses up to 240 mg/day have been administered
Helicobacter pylori eradication (unlabeled use): Oral: American College of Gastroenterology guidelines (Chey, 2007):
Nonpenicillin allergy: 40 mg twice daily administered with amoxicillin 1000 mg and clarithromycin 500 mg twice daily for 10-14 days
Penicillin allergy: 40 mg twice daily administered with clarithromycin 500 mg and metronidazole 500 mg twice daily for 10-14 days or 40 mg once or twice daily administered with bismuth subsalicylate 525 mg and metronidazole 250 mg plus tetracycline 500 mg 4 times/day for 10-14 days

Dosing: Pediatric

GERD, erosive esophagitis associated with GERD:
Oral:
Children <5 years: Dosage not established.
Children ≥5 years (unlabeled use): 20-40 mg once daily

Dosing: Geriatric

Refer to adult dosing.

Dosing: Renal Impairment

No adjustment is required. Pantoprazole is not removed by hemodialysis.

Dosing: Hepatic Impairment

No adjustment is required.
Use
 
Oral: Treatment and maintenance of healing of erosive esophagitis associated with GERD; reduction in relapse rates of daytime and nighttime heartburn symptoms in GERD; hypersecretory disorders associated with Zollinger-Ellison syndrome or other GI hypersecretory disorders
Adverse Reactions
 
≥1%:
Cardiovascular: Chest pain
Central nervous system: Headache (2% to 9%), insomnia (≤1%), anxiety, dizziness, migraine, pain
Dermatologic: Rash (≤2%)
Endocrine & metabolic: Hyperglycemia (≤1%), hyperlipidemia
Gastrointestinal: Diarrhea (2% to 6%), flatulence (2% to 4%), abdominal pain (1% to 4%), nausea (≤2%), vomiting (≤2%), eructation (≤1%), constipation, dyspepsia, gastroenteritis, rectal disorder
Genitourinary: Urinary frequency, UTI
Hepatic: Liver function tests abnormal (≤2%)
Local: Injection site reaction (includes thrombophlebitis and abscess)
Neuromuscular & skeletal: Arthralgia, back pain, hypertonia, neck pain, weakness
Respiratory: Bronchitis, cough, dyspnea, pharyngitis, rhinitis, sinusitis, upper respiratory tract infection
Miscellaneous: Flu syndrome, infection
Contraindications
 
Hypersensitivity to pantoprazole, substituted benzamidazoles (eg, esomeprazole, lansoprazole, omeprazole, rabeprazole), or any component of the formulation
Canadian labeling: Additional contraindication (not in U.S. labeling): Concomitant use with atazanavir
Warnings / Precautions Drug
 
Concerns related to adverse effects:
• Atrophic gastritis: Long-term pantoprazole therapy (especially in patients who were H. pylori positive) has caused biopsy-proven atrophic gastritis.
• Carcinoma: No occurrences of enterochromaffin-like (ECL) cell carcinoids, dysplasia, or neoplasia, such as those seen in rodent studies, have been reported in humans.
• Fractures: Increased incidence of osteoporosis-related bone fractures of the hip, spine, or wrist may occur with proton pump inhibitor therapy. Patients on high-dose or long-term therapy should be monitored. Use the lowest effective dose for the shortest duration of time, use vitamin D and calcium supplementation, and follow appropriate guidelines to reduce risk of fractures in patients at risk.
• Hypomagnesemia: Reported rarely, usually with prolonged PPI use of >3 months (most cases >1 year of therapy). May be symptomatic or asymptomatic; severe cases may cause tetany, seizures, and cardiac arrhythmias. Consider obtaining serum magnesium concentrations prior to beginning long-term therapy, especially if taking concomitant digoxin, diuretics, or other drugs known to cause hypomagnesemia; and periodically thereafter. Hypomagnesemia may be corrected by magnesium supplementation, although discontinuation of pantoprazole may be necessary; magnesium levels typically return to normal within 1 week of stopping.
• Vitamin B12 malabsorption: Prolonged treatment (typically >3 years) may lead to vitamin B12 malabsorption and subsequent deficiency.
Disease-related concerns:
• Gastric malignancy: Relief of symptoms does not preclude the presence of a gastric malignancy.
• Gastrointestinal infection (eg, Salmonella, Campylobacter): Use of proton pump inhibitors may increase risk of these infections.
Concurrent drug therapy issues:
• Clopidogrel: Proton pump inhibitors may diminish the therapeutic effect of clopidogrel, thought to be due to reduced formation of the active metabolite of clopidogrel; an increase in the risk of cardiovascular events may occur. Of the PPIs, pantoprazole has the lowest degree of CYP2C19 inhibition and is preferred if concomitant use of a PPI is necessary.
Dosage form specific issues:
• Edetate sodium (EDTA): Intravenous preparation contains edetate sodium; use caution in patients who are at risk for zinc deficiency if other EDTA-containing solutions are coadministered.
Other warnings/precautions:
• Appropriate use: Helicobacter pylori eradication: Short-term combination therapy (≤7 days) has been associated with a higher incidence of treatment failure. The American College of Gastroenterology recommends 10-14 days of therapy (triple or quadruple) for eradication of H. pylori (Chey, 2007).
Metabolism/Transport Effects
Substrate of CYP2C9 (minor), 2C19 (major), 2D6 (minor), 3A4 (minor); Inhibits CYP2C9 (weak), 2C19 (moderate), ABCG2; Induces CYP1A2 (weak), 3A4 (weak)
Interactions
 
Amphetamines: Proton Pump Inhibitors may increase the serum concentration of Amphetamines. Specifically, data indicate that Proton Pump Inhibitors may increase the rate at which Amphetamines are absorbed. Total exposure to Amphetamines is not significantly changed. Risk C: Monitor therapy
Atazanavir: Proton Pump Inhibitors may decrease the serum concentration of Atazanavir. Management: Avoid concurrent PPI in HIV treatment-experienced patients. For treatment-naive patients, atazanavir/ritonavir dose should be given approximately 12 hours after the PPI, and the PPI should not exceed the equivalent of 20 mg omeprazole. Risk D: Consider therapy modification
Bisphosphonate Derivatives: Proton Pump Inhibitors may diminish the therapeutic effect of Bisphosphonate Derivatives. Risk C: Monitor therapy
Cefditoren: Proton Pump Inhibitors may decrease the serum concentration of Cefditoren. Management: If possible, avoid use of cefditoren with proton pump inhibitors (PPIs). Consider alternative methods to minimize/control acid reflux (eg, diet modification) or alternative antimicrobial therapy if use of PPIs can not be avoided. Risk D: Consider therapy modification
Clopidogrel: Pantoprazole may decrease serum concentrations of the active metabolite(s) of Clopidogrel. Management: Due to the possible risk for impaired clopidogrel effectiveness, clinicians should carefully consider the need for proton pump inhibitor therapy in patients receiving clopidogrel. Other acid-lowering therapies do not appear to share this interaction. Risk D: Consider therapy modification
Conivaptan: May increase the serum concentration of CYP3A4 Substrates (Low risk). Risk C: Monitor therapy
CYP2C19 Inducers (Strong): May increase the metabolism of CYP2C19 Substrates. Risk C: Monitor therapy
CYP2C19 Substrates: CYP2C19 Inhibitors (Moderate) may decrease the metabolism of CYP2C19 Substrates. Risk C: Monitor therapy
Dabigatran Etexilate: Proton Pump Inhibitors may decrease serum concentrations of the active metabolite(s) of Dabigatran Etexilate. Risk C: Monitor therapy
Dasatinib: Proton Pump Inhibitors may decrease the absorption of Dasatinib. Risk D: Consider therapy modification
Delavirdine: Proton Pump Inhibitors may decrease the serum concentration of Delavirdine. Management: Chronic therapy with proton pump inhibitors (PPIs) should be avoided in patients treated with delavirdine. The clinical significance of short-term PPI therapy with delavirdine is uncertain, but such therapy should be undertaken with caution. Risk X: Avoid combination
Dexmethylphenidate: Proton Pump Inhibitors may increase the absorption of Dexmethylphenidate. Specifically, proton pump inhibitors may interfere with the normal release of drug from the extended-release capsules (Focalin XR brand), which could result in both increased absorption (early) and decreased delayed absorption. Risk C: Monitor therapy
Erlotinib: Proton Pump Inhibitors may decrease the serum concentration of Erlotinib. Risk X: Avoid combination
Fluconazole: May increase the serum concentration of Proton Pump Inhibitors. Risk C: Monitor therapy
Gefitinib: Proton Pump Inhibitors may decrease the serum concentration of Gefitinib. Risk C: Monitor therapy
Indinavir: Proton Pump Inhibitors may decrease the serum concentration of Indinavir. Risk C: Monitor therapy
Iron Salts: Proton Pump Inhibitors may decrease the absorption of Iron Salts. Exceptions: Ferric Gluconate; Ferumoxytol; Iron Dextran Complex; Iron Sucrose. Risk C: Monitor therapy
Itraconazole: Proton Pump Inhibitors may decrease the serum concentration of Itraconazole. Risk D: Consider therapy modification
Ketoconazole: May increase the serum concentration of Proton Pump Inhibitors. Proton Pump Inhibitors may decrease the serum concentration of Ketoconazole. Risk D: Consider therapy modification
Ketoconazole (Systemic): May increase the serum concentration of Proton Pump Inhibitors. Proton Pump Inhibitors may decrease the serum concentration of Ketoconazole (Systemic). Risk D: Consider therapy modification
Mesalamine: Proton Pump Inhibitors may diminish the therapeutic effect of Mesalamine. Proton pump inhibitor-mediated increases in gastrointestinal pH may cause the premature release of mesalamine from specific sustained-release mesalamine products. Management: Consider avoiding concurrent administration of high-dose proton pump inhibitors (PPIs) with sustained-release mesalamine products. Risk D: Consider therapy modification
Methotrexate: Proton Pump Inhibitors may increase the serum concentration of Methotrexate. Risk C: Monitor therapy
Methylphenidate: Proton Pump Inhibitors may increase the absorption of Methylphenidate. Specifically, proton pump inhibitors may interfere with the normal release of drug from the extended-release capsules (Ritalin LA brand), which could result in both increased absorption (early) and decreased delayed absorption. Risk C: Monitor therapy
Mycophenolate: Proton Pump Inhibitors may decrease the serum concentration of Mycophenolate. Specifically, concentrations of the active mycophenolic acid may be reduced. Risk C: Monitor therapy
Nelfinavir: Proton Pump Inhibitors may decrease serum concentrations of the active metabolite(s) of Nelfinavir. Proton Pump Inhibitors may decrease the serum concentration of Nelfinavir. Risk X: Avoid combination
Peginterferon Alfa-2b: May decrease the serum concentration of CYP2D6 Substrates. Risk C: Monitor therapy
Posaconazole: Proton Pump Inhibitors may decrease the serum concentration of Posaconazole. Risk X: Avoid combination
Raltegravir: Proton Pump Inhibitors may increase the serum concentration of Raltegravir. Risk C: Monitor therapy
Rilpivirine: Proton Pump Inhibitors may decrease the serum concentration of Rilpivirine. Risk X: Avoid combination
Saquinavir: Proton Pump Inhibitors may increase the serum concentration of Saquinavir. Risk C: Monitor therapy
Tipranavir: May decrease the serum concentration of Proton Pump Inhibitors. These data are derived from studies with Ritonavir-boosted Tipranavir. Risk C: Monitor therapy
Tocilizumab: May decrease the serum concentration of CYP3A4 Substrates. Risk C: Monitor therapy
Topotecan: BCRP/ABCG2 Inhibitors may increase the serum concentration of Topotecan. Risk D: Consider therapy modification
Voriconazole: Proton Pump Inhibitors may increase the serum concentration of Voriconazole. Risk C: Monitor therapy
Ethanol/Nutrition/Herb Interactions
Ethanol: Avoid ethanol (may cause gastric mucosal irritation).
Herb/Nutraceutical: Prolonged treatment (typically >3 years) may lead to vitamin B12 malabsorption and subsequent deficiency.
Pregnancy
 
B
Pregnancy Implications
Teratogenic effects were not observed in animal studies. There are no adequate and well-controlled studies in pregnant women. Use in pregnancy only if clearly needed.
Lactation
 
Enters breast milk/not recommended
Breast-Feeding Considerations
Not recommended due to carcinogenicity in animal studies.
Monitoring Parameters
 
Hypersecretory disorders: Acid output measurements, target level <10 mEq/hour (<5 mEq/hour if prior gastric acid-reducing surgery)
Mechanism of Action
 
Suppresses gastric acid secretion by inhibiting the parietal cell H+/K+ ATP pump
Pharmacodynamics / Kinetics
 
Absorption: Rapid, well absorbed
Distribution: Vd: 11-24 L
Protein binding: 98%, primarily to albumin
Metabolism: Extensively hepatic; CYP2C19 (demethylation), CYP3A4; no evidence that metabolites have pharmacologic activity
Bioavailability: 77%
Half-life elimination: 1 hour; increased to 3.5-10 hours with CYP2C19 deficiency
Time to peak: Oral: 2.5 hours
Excretion: Urine (71%); feces (18%)
 
   
 
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