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 [DB01060], [DB01211], and [DB00916], for example.[10][23] Its efficacy is considered similar to other medications within the PPI class including [DB00338], [DB00736], [DB00448], [DB05351], and [DB01129].

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 gastric acid secretion, irrespective of th... 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

Contraindications

  • 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
  • Regions: US
  • Patient Conditions:
      • Name: Patients with known hypersensitivity to any component of the formulation or any substituted benzimidazole
      • Drugbank Id: DBCOND0117161

Food Interactions

  • Take without regard to meals.

Interactions

Type in a drug name to check for interaction with Pantoprazole
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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
(R)-warfarin
The metabolism of (R)-warfarin can be decreased when combined with Pantoprazole.
(S)-Warfarin
The metabolism of (S)-Warfarin can be decreased when combined with Pantoprazole.
Abacavir
Pantoprazole may decrease the excretion rate of Abacavir which could result in a higher serum level.
Abatacept
The metabolism of Pantoprazole can be increased when combined with Abatacept.
Abemaciclib
The serum concentration of Abemaciclib can be increased when it is combined with Pantoprazole.
Abiraterone
The metabolism of Pantoprazole can be decreased when combined with Abiraterone.
Acarbose
Pantoprazole may decrease the excretion rate of Acarbose which could result in a higher serum level.
Acebutolol
The serum concentration of Acebutolol can be increased when it is combined with Pantoprazole.
Aceclofenac
Aceclofenac may decrease the excretion rate of Pantoprazole which could result in a higher serum level.
Acemetacin
Acemetacin may decrease the excretion rate of Pantoprazole which could result in a higher serum level.
Acenocoumarol
The metabolism of Acenocoumarol can be decreased when combined with Pantoprazole.
Acetaminophen
The serum concentration of Acetaminophen can be increased when it is combined with Pantoprazole.
Acetyldigoxin
Pantoprazole may decrease the excretion rate of Acetyldigoxin which could result in a higher serum level.
Acetylsalicylic acid
The serum concentration of Acetylsalicylic acid can be increased when it is combined with Pantoprazole.
Aclidinium
Pantoprazole may decrease the excretion rate of Aclidinium which could result in a higher serum level.
Acrivastine
Pantoprazole may decrease the excretion rate of Acrivastine which could result in a higher serum level.
Acyclovir
Acyclovir may decrease the excretion rate of Pantoprazole which could result in a higher serum level.
Adalimumab
The metabolism of Pantoprazole can be increased when combined with Adalimumab.
Adefovir
Adefovir may decrease the excretion rate of Pantoprazole which could result in a higher serum level.
Adefovir dipivoxil
Adefovir dipivoxil may decrease the excretion rate of Pantoprazole which could result in a higher serum level.
23 References
  1. 1 . Mathews S, Reid A, Tian C, Cai Q: An update on the use of pantoprazole as a treatment for gastroesophageal reflux disease. Clin Exp Gastroenterol. 2010;3:11-6. Epub 2010 Jan 20.PubMed: 21694841
  2. 2 . Dabrowski A, Stabuc B, Lazebnik L: Meta-analysis of the efficacy and safety of pantoprazole in the treatment and symptom relief of patients with gastroesophageal reflux disease - PAN-STAR. Prz Gastroenterol. 2018;13(1):6-15. doi: 10.5114/pg.2018.74556. Epub 2018 Mar 26.PubMed: 29657605
  3. 3 . Strand DS, Kim D, Peura DA: 25 Years of Proton Pump Inhibitors: A Comprehensive Review. Gut Liver. 2017 Jan 15;11(1):27-37. doi: 10.5009/gnl15502.PubMed: 27840364
  4. 4 . Jungnickel PW: Pantoprazole: a new proton pump inhibitor. Clin Ther. 2000 Nov;22(11):1268-93.PubMed: 11117653
  5. 5 . Shin JM, Kim N: Pharmacokinetics and pharmacodynamics of the proton pump inhibitors. J Neurogastroenterol Motil. 2013 Jan;19(1):25-35. doi: 10.5056/jnm.2013.19.1.25. Epub 2013 Jan 8.PubMed: 23350044
  6. 6 . Bardou M, Martin J: Pantoprazole: from drug metabolism to clinical relevance. Expert Opin Drug Metab Toxicol. 2008 Apr;4(4):471-83. doi: 10.1517/17425255.4.4.471 .PubMed: 18433349
  7. 7 . Shin JM, Sachs G: Differences in binding properties of two proton pump inhibitors on the gastric H+,K+-ATPase in vivo. Biochem Pharmacol. 2004 Dec 1;68(11):2117-27. doi: 10.1016/j.bcp.2004.07.035.PubMed: 15498502
  8. 8 . Huber R, Hartmann M, Bliesath H, Luhmann R, Steinijans VW, Zech K: Pharmacokinetics of pantoprazole in man. Int J Clin Pharmacol Ther. 1996 May;34(1 Suppl):S7-16.PubMed: 8793599
  9. 9 . Lewin MJ: Cellular mechanisms and inhibitors of gastric acid secretion. Drugs Today (Barc). 1999 Oct;35(10):743-52.PubMed: 12973369
  10. 10 . Fallone CA, Chiba N, van Zanten SV, Fischbach L, Gisbert JP, Hunt RH, Jones NL, Render C, Leontiadis GI, Moayyedi P, Marshall JK: The Toronto Consensus for the Treatment of Helicobacter pylori Infection in Adults. Gastroenterology. 2016 Jul;151(1):51-69.e14. doi: 10.1053/j.gastro.2016.04.006. Epub 2016 Apr 19.PubMed: 27102658
  11. 11 . Tanus-Santos JE, Pinheiro LC: Proton pump inhibitors: new mechanisms of action. Basic Clin Pharmacol Toxicol. 2019 Apr 13. doi: 10.1111/bcpt.13237.PubMed: 30980783
  12. 12 . Haastrup PF, Thompson W, Sondergaard J, Jarbol DE: Side Effects of Long-Term Proton Pump Inhibitor Use: A Review. Basic Clin Pharmacol Toxicol. 2018 Aug;123(2):114-121. doi: 10.1111/bcpt.13023. Epub 2018 May 24.PubMed: 29658189
  13. 13 . Reimer C, Sondergaard B, Hilsted L, Bytzer P: Proton-pump inhibitor therapy induces acid-related symptoms in healthy volunteers after withdrawal of therapy. Gastroenterology. 2009 Jul;137(1):80-7, 87.e1. doi: 10.1053/j.gastro.2009.03.058. Epub 2009 Apr 10.PubMed: 19362552
  14. 14 . Ghebremariam YT, LePendu P, Lee JC, Erlanson DA, Slaviero A, Shah NH, Leiper J, Cooke JP: Unexpected effect of proton pump inhibitors: elevation of the cardiovascular risk factor asymmetric dimethylarginine. Circulation. 2013 Aug 20;128(8):845-53. doi: 10.1161/CIRCULATIONAHA.113.003602. Epub 2013 Jul 3.PubMed: 23825361
  15. 15 . Tommasi S, Elliot DJ, Hulin JA, Lewis BC, McEvoy M, Mangoni AA: Human dimethylarginine dimethylaminohydrolase 1 inhibition by proton pump inhibitors and the cardiovascular risk marker asymmetric dimethylarginine: in vitro and in vivo significance. Sci Rep. 2017 Jun 6;7(1):2871. doi: 10.1038/s41598-017-03069-1.PubMed: 28588208
  16. 16 . Pantoprazole Tablets, Monograph File
  17. 17 . Pfizer Safety Data Sheet File
  18. 18 . Assessment Report, Pantozol File
  19. 19 . Protonix delayed release and oral suspension FDA label File
  20. 20 . Pantoloc EMA label File
  21. 21 . Sandoz Pantoprazole DRT Monograph File
  22. 22 . Health Canada Label - Pantoprazole File
  23. 23 . TOP Guidelines - H pylori File