Description

Simple

A medication used to treat and heal conditions caused by exposure to stomach acid or higher than normal levels of gastric acid.

Clinical

A proton pump inhibitor used to treat erosive esophagitis, gastric acid hypersecretion, and to promote healing of tissue damage caused by gastric acid.

Overview

Pantoprazole is a first-generation proton pump inhibitor (PPI) used for the management of gastroesophageal reflux disease (GERD), for gastric protection to prevent recurrence of stomach ulcers or gastric damage from chronic use of NSAIDs, and for the treatment of pathological hypersecretory conditions including Zollinger-Ellison (ZE) Syndrome. It can also be found in quadruple regimens for the treatment of _H. pylori_ infections along with other antibiotics including [amoxicillin], [clarithromycin], and [metronidazole], for example.[10][23] Its efficacy is considered similar to other medications within the PPI class including [omeprazole], [esomeprazole], [lansoprazole], [dexlansoprazole], and [rabeprazole].

Pantoprazole exerts its stomach acid-suppressing effects by preventing the final step in gastric acid production by covalently binding to sulfhydryl groups of cysteines found on the (H+, K+)-ATPase enzyme at the secretory surface of gastric parietal cell. This effect leads to inhibition of both basal and stimulated... Read more

Pharmacology

Indication


**Pantoprazole Injection**:

**Treatment of gastroesophageal reflux disease associated with a history of erosive esophagitis**

Pantoprazole for injection is indicated for short-term treatment (7-10 days) of patients having gastroesophageal reflux disease (GERD) with a history of erosive esoph... Read more

Pharmacodynamic

This drug acts to decrease gastric acid secretion, which reduces stomach acidity. Pantoprazole administration leads to long-lasting inhibition of gastric acid secretion.[16]

**General Effects**

Pantopr... Read more

Mechanism of action

Hydrochloric acid (HCl) secretion into the gastric lumen is a process regulated mainly by the H(+)/K(+)-ATPase of the proton pump, expressed in high quantities by the parietal cells of the stomach.[ Read more

Absorption

Pantoprazole is absorbed after oral administration as an enteric-coated tablet with maximum plasma concentrations attained within 2 – 3 hours and a bioavailability of 77% that does not change with multiple dosing [ Read more

Protein binding

Approximately 98%[FDA label]

Volume of distribution

The apparent volume of distribution of pantoprazole is approximately 11.0-23.6 L, distributing mainly in the extracellular fluid.[FDA label]

Clearance

*Adults**: With intravenous administration of pantoprazole to extensive metabolizers, total clearance is 7.6-14.0 L/h.[16]In a population pharmacokinetic analysis, the total clearance increased with increasi... Read more

Half life

About 1 hour[19]

Route of elimination

After a single oral or intravenous (IV) dose of 14C-labeled pantoprazole to healthy, normal metabolizing subjects, about 71% of the dose was excreted in the urine, with 18% excreted in the feces by biliary excretion. There was no kidney excretion of unchanged pantoprazole.[ Read more

Toxicity

**Rat Oral LD 50** 747 mg/kg[17]

**Tumorigenicity**

Because of the chronic nature of GERD, there may be a potential for long-term administration of pantoprazole. In long-term rodent studies, pantoprazole was... Read more

Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Headache US
  • adult
  • Kind: experimental
    • Percent: 12%
  • Kind: placebo
    • Percent: 9%
  • Clinical Trial
    Nausea US
    • adult
  • Kind: experimental
    • Percent: 7%
  • Kind: placebo
    • Percent: 10%
  • Clinical Trial
    Diarrhea US
    • adult
  • Kind: experimental
    • Percent: 9%
  • Kind: placebo
    • Percent: 5%
  • Clinical Trial
    Abdominal Pain US
    • adult
  • Kind: experimental
    • Percent: 6%
  • Kind: placebo
    • Percent: 6%
  • Clinical Trial
    Vomiting US
    • adult
  • Kind: experimental
    • Percent: 4%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Constipation US
  • Kind: experimental
    • Percent: ≤4%
  • Clinical Trial
    Flatulence US
  • Kind: experimental
    • Percent: ≤4%
  • Clinical Trial
    Nausea US
  • Kind: experimental
    • Percent: ≤4%
  • Clinical Trial
    Elevated Triglycerides US
  • Kind: experimental
    • Percent: ≤4%
  • Clinical Trial
    Elevated Liver Enzymes US
  • Kind: experimental
    • Percent: ≤4%
  • Clinical Trial
    Elevated creatine kinase US
  • Kind: experimental
    • Percent: ≤4%
  • Clinical Trial
    Arthralgia US
  • Kind: experimental
    • Percent: ≤4%
  • Clinical Trial
    Myalgia US
  • Kind: experimental
    • Percent: ≤4%
  • Clinical Trial
    Dizziness US
  • Kind: experimental
    • Percent: ≤4%
  • Clinical Trial
    Vertigo US
  • Kind: experimental
    • Percent: ≤4%
  • Clinical Trial
    Urticaria US
  • Kind: experimental
    • Percent: ≤4%
  • Clinical Trial
    Flatulence US
    • adult
  • Kind: experimental
    • Percent: 4%
  • Kind: placebo
    • Percent: 4%
  • Clinical Trial
    Upper Respiratory Infection US
    • pediatric
  • Kind: experimental
    • Percent: >4%
  • Clinical Trial
    Vomiting US
    • pediatric
  • Kind: experimental
    • Percent: >4%
  • Clinical Trial
    Diarrhea US
    • pediatric
  • Kind: experimental
    • Percent: >4%
  • Clinical Trial
    Fever US
    • pediatric
  • Kind: experimental
    • Percent: >4%
  • Clinical Trial
    Headache US
    • pediatric
  • Kind: experimental
    • Percent: >4%
  • Clinical Trial
    Facial edema US
  • Kind: experimental
    • Percent: ≤4%
  • Clinical Trial
    Allergic Reaction US
  • Kind: experimental
    • Percent: ≤4%
  • Clinical Trial
    Abdominal Pain US
    • pediatric
  • Kind: experimental
    • Percent: >4%
  • Clinical Trial
    Rash US
    • pediatric
  • Kind: experimental
    • Percent: >4%
  • Clinical Trial
    Arthralgia US
    • adult
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Dizziness US
    • adult
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Allergic Reaction US
    • adult
  • Kind: experimental
    • Percent: ≤2%
  • Clinical Trial
    Facial edema US
    • adult
  • Kind: experimental
    • Percent: ≤2%
  • Clinical Trial
    Constipation US
    • adult
  • Kind: experimental
    • Percent: ≤2%
  • Clinical Trial
    Pyrexia US
    • adult
  • Kind: experimental
    • Percent: ≤2%
  • Clinical Trial
    Photosensitivity reaction US
    • adult
  • Kind: experimental
    • Percent: ≤2%
  • Clinical Trial
    Leukopenia US
    • adult
  • Kind: experimental
    • Percent: ≤2%
  • Clinical Trial
    Thrombocytopenia US
    • adult
  • Kind: experimental
    • Percent: ≤2%
  • Clinical Trial
    Dry Mouth US
    • adult
  • Kind: experimental
    • Percent: ≤2%
  • Clinical Trial
    Hepatitis US
    • adult
  • Kind: experimental
    • Percent: ≤2%
  • Clinical Trial
    Elevated Triglycerides US
    • adult
  • Kind: experimental
    • Percent: ≤2%
  • Clinical Trial
    Liver enzymes elevated US
    • adult
  • Kind: experimental
    • Percent: ≤2%
  • Clinical Trial
    Elevated creatine kinase US
    • adult
  • Kind: experimental
    • Percent: ≤2%
  • Clinical Trial
    Generalized edema US
    • adult
  • Kind: experimental
    • Percent: ≤2%
  • Clinical Trial
    Urticaria US
    • adult
  • Kind: experimental
    • Percent: ≤2%
  • Clinical Trial
    Vertigo US
    • adult
  • Kind: experimental
    • Percent: ≤2%
  • Clinical Trial
    Depression US
    • adult
  • Kind: experimental
    • Percent: ≤2%
  • Clinical Trial
    Myalgia US
    • adult
  • Kind: experimental
    • Percent: ≤2%
  • Clinical Trial
    Blurred vision US
    • adult
  • Kind: experimental
    • Percent: ≤2%
  • Clinical Trial
    Pruritus US
    • adult
  • Kind: experimental
    • Percent: ≤2%
  • Clinical Trial
    Rash US
    • adult
  • Kind: experimental
    • Percent: ≤2%
  • Clinical Trial
    Contusion Canada
  • Kind: experimental
    • Percent: 0.1-1
  • Clinical Trial
    Cystitis Canada
  • Kind: experimental
    • Percent: 0.1-1
  • Clinical Trial

    Contraindications

    • Route:
      • Oral
    • Hypersensitivity:
      • true
      • Substituted benzimidazoles
    • Regions: US
    • Route:
      • Oral
    • Hypersensitivity:
      • true
    • Regions: US
    • Regions: Canada
    • With Drugs:
        • Name: Saquinavir
        • Drugbank Id: DB01232
    • Regions: Canada
    • With Drugs:
        • Name: Nelfinavir
        • Drugbank Id: DB00220
    • Regions: Canada
    • With Drugs:
        • Name: Atazanavir
        • Drugbank Id: DB01072
    • Regions: Canada
    • With Drugs:
        • Name: Rilpivirine
        • Drugbank Id: DB08864
    • Regions: EU
    • Patient Conditions:
        • Name: Patients on an HIV protease inhibitors for which absorption is dependent on acidic intragastric pH such as atazanavir, nelfinavir
        • Drugbank Id: DBCOND0117231
    • Patient Conditions Associated With:
        • Name: HIV+
        • Drugbank Id: DBCOND0048079

    Food Interactions

    Take with or without food. The absorption is unaffected by food.