Elsevier

Clinical Therapeutics

Volume 22, Issue 11, November 2000, Pages 1268-1293
Clinical Therapeutics

New drugs
Pantoprazole: A new proton pump inhibitor

https://doi.org/10.1016/S0149-2918(00)83025-8Get rights and content

Abstract

Objective: This paper reviews the pharmacology, clinical efficacy, and tolerability of pantoprazole in comparison with those of other available proton pump inhibitors (PPIs).

Methods: Relevant English-language research and review articles were identified by database searches of MEDLINE®, International Pharmaceutical Abstracts®, and UnCover, and by examining the reference lists of the articles so identified. In selecting data for inclusion, the author gave preference to full-length articles published in peer-reviewed journals.

Results: Like other PPIs, pantoprazole exerts its pharmacodynamic actions by binding to the proton pump (H+,K+-adenosine triphosphatase) in the parietal cells, but, compared with other PPIs, its binding may be more specific for the proton pump. Pantoprazole is well absorbed when administered as an enteric-coated, delayed-release tablet, with an oral bioavailability of ∼77%. It is hepatically metabolized via cytochrome P2C19 to hydroxy-pantoprazole, an inactive metabolite that subsequently undergoes sulfate conjugation. The elimination half-life ranges from 0.9 to 1.9 hours and is independent of dose. Pantoprazole has similar efficacy to other PPIs in the healing of gastric and duodenal ulcers, as well as erosive esophagitis, and as part of triple-drug regimens for the eradication of Helicobacter pylori from the gastric mucosa. It is well tolerated, with the most common adverse effects being headache, diarrhea, flatulence, and abdominal pain. In clinical studies, it has been shown to have no interactions with various other agents, including carbamazepine, cisapride, cyclosporine, digoxin, phenytoin, theophylline, and warfarin.

Conclusions: Pantoprazole appears to be as effective as other PPIs. Its low potential for drug interactions may give it an advantage in patients taking other drugs.

References (104)

  • G Sachs

    Proton pump inhibitors and acid-related diseases

    Pharmacotherapy

    (1997)
  • G Sachs et al.

    Gastric acid secretion: Activation and inhibition

    Yale J Biol Med

    (1994)
  • R Huber et al.

    Review article: The continuing development of proton pump inhibitors with particular reference to pantoprazole

    Aliment Pharmacol Ther

    (1995)
  • W Kromer

    Similarities and differences in the properties of substituted benzimidazoles: A comparison between pantoprazole and related compounds

    Digestion

    (1995)
  • A Fitton et al.

    Pantoprazole. A review of its pharmacological properties and therapeutic use in acid-related disorders

    Drugs

    (1996)
  • B Simon et al.

    Effect of repeated oral administration of BY 1023/SK&F 96022—a new substituted benzimidazole derivative—on pentagastrin-stimulated gastric acid secretion and pharmacokinetics in man

    Aliment Pharmacol Ther

    (1990)
  • B Simon et al.

    Single intravenous administration of the H+,K+-ATPase inhibitor BY 1023/SK&F 96022—inhibition of pentagastrin-stimulated gastric acid secretion and pharmacokinetics in man

    Aliment Pharmacol Ther

    (1990)
  • B Simon et al.

    Pentagastrin-stimulated gastric acid secretion and pharmacokinetics following single and repeated intravenous administration of the gastric H+,K+-ATPase-inhibitor pantoprazole (BY 1023/SK&F96022) in healthy volunteers

    Z Gastroenterol

    (1990)
  • V Savarino et al.

    Comparison of 24-h control of gastric acidity by three different dosages of pantoprazole in patients with duodenal ulcer

    Aliment Pharmacol Ther

    (1998)
  • A Hannan et al.

    Effects of oral pantoprazole on 24-hour intragastric acidity and plasma gastrin profiles

    Aliment Pharmacol Ther

    (1992)
  • H Koop et al.

    Intragastric pH and serum gastrin during administration of different doses of pantoprazole in healthy subjects

    Eur J Gastroenterol Hepatol

    (1996)
  • S Mussig et al.

    Morning and evening administration of pantoprazole: A study to compare the effect on 24-hour intragastric pH

    Eur J Gastroenterol Hepatol

    (1997)
  • M Hartmann et al.

    Equipotent inhibition of gastric acid secretion by equal doses of oral or intravenous pantoprazole

    Aliment Pharmacol Ther

    (1998)
  • M Hartmann et al.

    Twenty-four-hour intragastric pH profiles and pharmacokinetics following single and repeated oral administration of the proton pump inhibitor pantoprazole in comparison to omeprazole

    Aliment Pharmacol Ther

    (1996)
  • HG Dammann et al.

    Pantoprazole versus omeprazole: Influence on meal-stimulated gastric acid secretion

    Eur J Gastroenterol Hepatol

    (1999)
  • C Florent et al.

    Twenty-four-hour monitoring of intragastric acidity: Comparison between lansoprazole 30mg and pantoprazole 40mg

    Eur J Gastroenterol Hepatol

    (1997)
  • U Armbrecht et al.

    Treatment of reflux oesophagitis of moderate and severe grade with ranitidine or pantoprazole—comparison of 24-hour intragastric and oesophageal pH

    Aliment Pharmacol Ther

    (1997)
  • J Mossner et al.

    A double-blind study of pantoprazole and omeprazole in the treatment of reflux oesophagitis: A multicentre trial

    Aliment Pharmacol Ther

    (1995)
  • J Escourrou et al.

    Maintenance therapy with pantoprazole 20 mg prevents relapse of reflux oesophagitis

    Aliment Pharmacol Ther

    (1999)
  • (2000)
  • M Dattilo et al.

    Helicobacter pylori infection, chronic gastritis, and proton pump inhibitors

    J Clin Gastroenterol

    (1998)
  • S Suerbaum et al.

    Antibacterial activity of pantoprazole and omeprazole against Helicobacter pylori

    Eur J Clin Microbiol Infect Dis

    (1991)
  • T Andersson

    Pharmacokinetics, metabolism and interactions of acid pump inhibitors. Focus on omeprazole, lansoprazole and pantoprazole

    Clin Pharmacokinet

    (1996)
  • R Huber et al.

    Pharmacokinetics of pantoprazole in man

    Int J Clin Pharmacol Ther

    (1996)
  • M Tanaka et al.

    Pharmacokinetics and tolerance of pantoprazole, a proton pump inhibitor, after single and multiple oral doses in healthy Japanese volunteers

    Int J Clin Pharmacol Ther

    (1996)
  • H Bliesath et al.

    Dose linearity of the pharmacokinetics of the new H+/K+-ATPase inhibitor pantoprazole after single intravenous administration

    Int J Clin Pharmacol Ther

    (1994)
  • MA Pue et al.

    Pharmacokinetics of pantoprazole following single intravenous and oral administration to healthy male subjects

    Eur J Clin Pharmacol

    (1993)
  • UA Meyer

    Interaction of proton pump inhibitors with cytochromes P450: Consequences for drug interactions

    Yale J Biol Med

    (1996)
  • M Tanaka et al.

    Metabolic disposition of pantoprazole, a proton pump inhibitor, in relation to S-mephenytoin 4′-hydroxylation phenotype and genotype

    Clin Pharmacol Ther

    (1997)
  • T Andersson et al.

    Pharmacokinetics and effect on caffeine metabolism of the proton pump inhibitors, omeprazole, lansoprazole, and pantoprazole

    Br J Clin Pharmacol

    (1998)
  • P Unge et al.

    Drug interactions with proton pump inhibitors

    Drug Saf

    (1997)
  • V Kliem et al.

    Pharmacokinetics of pantoprazole in patients with end-stage renal failure

    Nephrol Dial Transplant

    (1998)
  • M Rehner et al.

    Comparison of pantoprazole versus omeprazole in the treatment of acute duodenal ulceration—a multicentre study

    Aliment Pharmacol Ther

    (1995)
  • JA Beker et al.

    Double-blind comparison of pantoprazole and omeprazole for the treatment of acute duodenal ulcer

    Eur J Gastroenterol Hepatol

    (1995)
  • TS Chen et al.

    The efficacy of the third proton pump inhibitor—pantoprazole—in the short-term treatment of Chinese patients with duodenal ulcer

    Hepato-Gastroenterology

    (1999)
  • W Schepp et al.

    Pantoprazole and ranitidine in the treatment of acute duodenal ulcer. A multicentre study

    Scand J Gastroenterol

    (1995)
  • M Cremer et al.

    A double-blind study of pantoprazole and ranitidine in the treatment of acute duodenal ulcer. A multicenter trial

    Dig Dis Sci

    (1995)
  • G Judmaier et al.

    Comparison of pantoprazole and ranitidine in the treatment of acute duodenal ulcer

    Aliment Pharmacol Ther

    (1994)
  • L Witzel et al.

    Pantoprazole versus omeprazole in the treatment of acute gastric ulcers

    Aliment Pharmacol Ther

    (1995)
  • J Hotz et al.

    Pantoprazole is superior to ranitidine in the treatment of acute gastric ulcer

    Scand J Gastroenterol

    (1995)
  • Cited by (76)

    • Peroxidation and photo-peroxidation of pantoprazole in aqueous solution using silver molybdate as catalyst

      2021, Chemosphere
      Citation Excerpt :

      Pantoprazole (PAN) (Fig. S1A) is one of the most commonly consumed drugs worldwide (Ortiz de García et al., 2013), and approximately 70–95% of the consumed PAN is excreted as inactive or pharmaceutically active metabolites in urine and feces (Kosma et al., 2016). PAN residues are present in domestic wastewaters, in concentrations of up to 0.18 μg L−1 (Barreiro et al., 2011; Gracia-Lor et al., 2012), and although PAN species (Fig. S1B) are unstable at acidic pH (Jungnickel, 2000), its removal and/or mineralization by wastewaters treatment plant has not been completely studied. PAN is well removed by adsorption onto iron-based nanoparticles (89% removal in 30 min) (Ali et al., 2016), but the mineralization efficiency through AOPs (e.g. heterogeneous Fenton-like processes using Fe3O4/CeO2) is rather low (Gan et al., 2017).

    • A new strategy for extraction and depuration of pantoprazole in rat plasma: Vortex assisted dispersive micro-solid-phase extraction employing metal organic framework MIL-101(Cr) as sorbent followed by dispersive liquid–liquid microextraction based on solidification of a floating organic droplet

      2019, Journal of Pharmaceutical and Biomedical Analysis
      Citation Excerpt :

      The method is especially suited to extract organic compounds with relative lower polarity [17]. Pantoprazole is a selective and irreversible proton pump inhibitor for the treatment of acid-related hypersecretory gastrointestinal disorders [18–20]. Up to now, multiple quantitative methods have been established for monitoring the concentration of pantoprazole in plasma.

    • A new pollen-derived microcarrier for pantoprazole delivery

      2017, Materials Science and Engineering C
      Citation Excerpt :

      Pantoprazole (PaNa) is a proton pump inhibitor and widely used for healing of duodenal ulcer, gastric ulcers and gastroesophageal reflux disease. It is effective in reducing acid secretion and elevates pH levels of gastric juice [1,2]. It selectively binds to cysteine residues of H+/K+–adenosine triphosphatase in the apical membrane of the gastric parietal cells, thereby inhibiting acid secretion [3].

    View all citing articles on Scopus
    View full text