Pantoprazole Sodium (pantoprazole sodium)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Pantoprazole sodium, commonly referred to as an acid- or proton-pump inhibitor (PPI), is a gastric antisecretory agent
Pantoprazole sodium, a proton-pump inhibitor (PPI), is a gastric antisecretory agent that is a substituted benzimidazole. The activated form covalently binds to 2 sites of the hydrogen/potassium ATPase in the gastric parietal cells; inactivation of this enzyme system (also known as the proton, hydrogen, or acid pump) blocks the final step in the secretion of hydrochloric acid by these cells, resulting in potent, long-lasting inhibition of gastric acid secretion.
Pantoprazole is well absorbed from the GI tract with an absolute oral bioavailability of 77%. Following single or multiple oral doses pantoprazole 40 mg delayed-release tablets, peak plasma concentrations are attained in approximately 2.5 hours. The time to peak plasma concentration is similar (2-2.5 hours) when the delayed-release suspension is administered orally or via nasogastric (NG) tube.
Administration of the delayed-release oral suspension in apple juice via NG tube is bioequivalent to oral administration of the delayed-release oral suspension in applesauce or apple juice. Following administration of a single oral 40 mg delayed-release tablet, AUC is increased by approximately 39% in pediatric patients 6 to 11 years of age and approximately 10% in adolescents 12 to 16 years of age compared to adults. Peak plasma concentrations and AUC increase in a dose proportional manner for oral and IV doses of pantoprazole ranging from 10-80 mg.
Following multiple daily doses, there is no accumulation and the pharmacokinetics of pantoprazole remain unaltered. The duration of antisecretory effect for all routes of pantoprazole administration continues for more than 24 hours. Within 2.5 hours of administration of a 40-mg oral dose to healthy individuals, gastric acid secretion was inhibited by a mean of 51%, which increased to a mean of 85% following administration of 40 mg orally once daily for 7 days.
Gastric acid secretion returned to normal within a week after pantoprazole discontinuance, and there was no evidence of rebound hypersecretion. Because the pantoprazole molecule is acid labile, the drug is commercially available for oral administration as delayed-release, enteric-coated formulations (tablets, granules for oral suspension) that increase oral bioavailability by delaying absorption until after the preparation leaves the stomach. The duration of antisecretory effect of IV pantoprazole was 24 hours.
Following IV administration of a single 20- to 120-mg dose of pantoprazole to healthy individuals, onset of gastric acid suppression occurred within 15-30 minutes, and suppression of cumulative 24-hour acid output was dose dependent for doses of 20-80 mg. Within 2 hours of IV administration of pantoprazole 80 mg, complete suppression of acid output was achieved; no substantial additional suppression was observed following a 120-mg dose of the drug.
Pantoprazole is extensively metabolized, mainly via hepatic cytochrome P-450 (CYP) 2C19 isoenzyme; CYP3A4, CYP2D6, and CYP2C9 isoenzymes metabolize the drug to a much lesser extent. Pantoprazole is approximately 98% protein bound, principally to albumin. Following a single radiolabeled dose of pantoprazole, approximately 71% of the dose was excreted in the urine and 18% excreted in the feces through biliary excretion.
No unchanged pantoprazole was excreted renally. Following oral or IV administration, plasma concentrations of pantoprazole decrease biexponentially, with an elimination half-life of approximately 1 hour. Pharmacokinetic analyses in pediatric patients indicate the following dosage regimens will achieve comparable steady state plasma concentrations to that observed in adults administered 40 mg of IV pantoprazole daily: 0.8 mg/kg once daily (patients 3 months to <1 year of age), 10 mg once daily (patients 1 to 17 years of age with body weight <15kg), 20 mg once daily (patients 1 to 17 years of age with body weight >=15 kg but <40 kg), and 40 mg once daily (patients 1 to 17 years of age with body weight >=40 kg).
Pharmacokinetics of IV pantoprazole in pediatric patients <3 months of age have not been characterized. Repeated administration of IV pantoprazole in geriatric patients 65 to 76 years of age results in a similar half-life to that observed in younger adults. In adults with poor CYP2C19 metabolizer phenotype, metabolism is slower than in those with extensive (or rapid) metabolizer phenotype; the elimination half-life in such patients is 3.5-10 hours, but minimal accumulation occurs with once-daily dosing.
In pediatric patients, oral clearance in poor metabolizers (CYP2C19 *2/*2 genotype) is about 10-fold lower than in extensive metabolizers (CYP2C19 *1/*1) and AUC is more than 6-fold higher than in extensive or intermediate (CYP2C19*1/*x) metabolizers.
A moderate increase in enterochromaffin-like cell (ECL) density, which began after the first year of therapy and appeared to plateau after 4 years, occurred in patients receiving pantoprazole dosages of 40-240 mg daily for up to 5 years. Dose-related increases in ECL-cell proliferation and gastric neuroendocrine-cell tumors were observed in animal studies.
USES: Pantoprazole is used to treat certain stomach and esophagus problems (such as acid reflux). It works by decreasing the amount of acid your stomach makes. This medication relieves symptoms such as heartburn, difficulty swallowing, and cough.
It helps heal acid damage to the stomach and esophagus, helps prevent ulcers, and may help prevent cancer of the esophagus. Pantoprazole belongs to a class of drugs known as proton pump inhibitors (PPIs). The injection form of this drug is used for a short time when you cannot take the medication by mouth.
When possible, your doctor should switch you to the form that is taken by mouth.
Generic name: pantoprazole sodium
Pronunciation: (pan-TOE-pra-zole)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Pantoprazole Sodium
Indications
The following indications are listed for Pantoprazole Sodium:
- Erosive Esophagitis
- Gastric Hypersecretion With Systemic Mastocytosis
- Gastroesophageal Reflux Disease
- Pathological Gastric Acid Hypersecretory Condition
- Zollinger-Ellison Syndrome
Also known as: Adenomatosis Partial Multiple Endocrine, Gastric Acid Hypersecretory Conditions Due To Disease, Gastro-Esophageal Reflux, Ge Reflux Disease, Pancreatic Ulcerogenic Tumor Syndrome, Pathological Gastric Acid Hypersecretory States, Pathological Hypersecretion State, Pathological Hypersecretory Condition, Systemic Mast Cell Disease With Gastric Hypersecretion, Z-E Syndrome.
Dosing
Dosage of pantoprazole sodium is expressed in terms of pantoprazole.
Safety and efficacy of IV pantoprazole for the treatment of upper GI bleeding has not been established in adult or pediatric patients.
Pantoprazole sodium is administered orally or IV; it is not intended for other parenteral routes of administration. Pantoprazole is administered once daily in the management of gastroesophageal reflux disease (GERD) and erosive esophagitis; in the management of pathologic GI hypersecretory conditions, pantoprazole generally is given twice daily, although it may be given IV every 8 hours if necessary.
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.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
Pantoprazole is extensively metabolized, mainly via hepatic cytochrome P-450 (CYP) 2C19 isoenzyme; CYP3A4, CYP2D6, and CYP2C9 isoenzymes metabolize the drug to a much lesser extent. There is no evidence that metabolites of pantoprazole have significant pharmacologic activity.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
*Known hypersensitivity to pantoprazole, any other ingredient in the formulation, or other substituted benzimidazoles (e.g., esomeprazole, lansoprazole, omeprazole, rabeprazole).
*Concomitant use of rilpivirine-containing products.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
Adverse effects occurring in >2% of adult patients receiving oral pantoprazole and reported more frequently with pantoprazole than with placebo include headache, diarrhea, nausea, abdominal pain, vomiting, flatulence, dizziness, and arthralgia.
Adverse effects occurring in >4% of pediatric patients receiving oral pantoprazole and reported more frequently with pantoprazole than with placebo include upper respiratory tract infection, headache, diarrhea, abdominal pain, vomiting, fever, and rash.
The most common adverse effects occurring in >2% of patients receiving IV pantoprazole include headache, diarrhea, nausea, abdominal pain, vomiting, flatulence, dizziness, and arthralgia.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
No enhanced messaging available.
Efficacy and safety of oral pantoprazole for short-term treatment of erosive esophagitis associated with GERD in pediatric patients 1 to 16 years of age are supported by controlled clinical trials in adults and additional safety, efficacy, and pharmacokinetic studies in pediatric patients. However, because an appropriate dosage formulation is not available for children <5 years of age, oral pantoprazole is labeled for use only in children >=5 years of age. Safety and efficacy of oral pantoprazole for uses other than treatment of erosive esophagitis have not been established in pediatric patients.
Oral pantoprazole was evaluated in several clinical trials in pediatric patients 1 to 16 years of age with endoscopically diagnosed or symptomatic GERD, including a limited number of patients with endoscopically diagnosed erosive esophagitis. Because these clinical trials had no placebo or active comparator group and provided no evidence of a dose-related response to the pantoprazole dosages studied, the results were inconclusive regarding efficacy of pantoprazole for the treatment of symptomatic GERD in pediatric patients. Adverse effects reported in more than 4% of patients included upper respiratory tract infection, headache, fever, diarrhea, vomiting, rash, and abdominal pain. Following oral administration of a single 40-mg dose of pantoprazole, exposure to the drug was about 39% higher in children 6 to 11 years of age and about 10% higher in adolescents 12-16 years of age compared with adults.
Efficacy of oral pantoprazole in infants <1 year of age has not been established. In a treatment-withdrawal study in infants 1 to 11 months of age with symptomatic GERD, pantoprazole was not more effective than placebo.
Safety and efficacy of short-term (up to 7 days) treatment with IV pantoprazole sodium for GERD associated with a history of erosive esophagitis have been established in patients >=3 months of age. Use of IV pantoprazole for this indication is supported by evidence from adequate, well-controlled studies of IV and oral pantoprazole in adults and oral pantoprazole in pediatric patients, with additional pharmacokinetic and safety data with IV pantoprazole in pediatric patients >=1 year of age and oral pantoprazole in pediatric patients >=3 months of age. Adverse reactions were generally similar to those reported in adults receiving IV or oral pantoprazole.
Safety and efficacy of IV pantoprazole sodium for the treatment of GERD associated with a history of erosive esophagitis have not been established in pediatric patients <3 months of age.
Safety and efficacy of IV pantoprazole sodium have not been established for the treatment of pathological hypersecretory conditions (including Zollinger-Ellison syndrome) in pediatric patients.
Available observational data have not demonstrated an association between pantoprazole and major fetal malformations or other adverse pregnancy outcomes.
Animal reproductive studies of IV pantoprazole sodium administered at dosages up to 20 mg/kg daily (4 times the recommended human dose) in rats and up to 15 mg/kg daily (6 times the recommended human dose) in rabbits during organogenesis did not reveal evidence of fetal harm.
Available human data from observational studies have not demonstrated an association between pantoprazole and adverse pregnancy-related outcomes. Methodological limitations of this observational data cannot definitively establish or rule out any drug-associated risk during pregnancy. A prospective study by the European Network of Teratology Information Services found no difference in the rate of major malformations between 53 females receiving a median dose of 40 mg of pantoprazole daily compared to a control group of 868 females. A population-based retrospective cohort study of 549 live births in Denmark from 1996 to 2008 also found no substantial increase in major birth defects with first trimester exposure to pantoprazole. A meta-analysis of 1,530 pregnant females exposed to PPIs during the first trimester compared to 133,410 unexposed pregnant females also found no significant increase in the risk of congenital malformations or spontaneous abortion with PPI exposure.
Limited data from a case report indicate that pantoprazole passes into breast milk. Following a 40 mg dose of oral pantoprazole, the drug was detectable in the milk only 2 and 4 hours after the dose and was not detectable (<10 mcg/mL) in milk at 6, 8, and 24 hours. The relative dose to the infant was estimated to be 7.3 mcg, which is 0.14% of the weight-adjusted maternal dose. There were no effects on the breast-fed infant from pantoprazole exposure. It is not known if pantoprazole affects milk production.
The manufacturer makes no specific dosage recommendations for geriatric patients.
No clinically meaningful differences in pharmacokinetics were observed in geriatric patients compared to younger adults. No overall differences in safety or efficacy were observed between geriatric patients and younger adults. Other reported clinical experience has not identified differences in response between geriatric patients and younger adults, although a greater sensitivity of some geriatric patients cannot be ruled out.
ICD codes
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Last reviewed · Source: First Databank (FDB) drug data
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