Pantoprazole

Pantoprazole
Clinical data
Trade names Protonix
AHFS/Drugs.com Monograph
MedlinePlus a601246
License data
Pregnancy
category
  • AU: B3
  • US: B (No risk in non-human studies)
Routes of
administration
By mouth and intravenous
ATC code A02BC02 (WHO)
Legal status
Legal status
  • ℞ (Prescription only)
Pharmacokinetic data
Bioavailability 77%
Metabolism Liver (CYP2C19)
Biological half-life 1-2 hours
Excretion Urine, Feces
Identifiers
CAS Number 102625-70-7 YesY
PubChem (CID) 4679
IUPHAR/BPS 7260
DrugBank DB00213 YesY
ChemSpider 4517 YesY
UNII D8TST4O562 YesY
KEGG D05353 YesY
ChEBI CHEBI:7915 YesY
ChEMBL CHEMBL1502 YesY
ECHA InfoCard 100.111.005
Chemical and physical data
Formula C16H15F2N3O4S
Molar mass 383.371 g/mol
3D model (Jmol) Interactive image
Chirality Racemic
  (verify)

Pantoprazole, sold under the brand name Protonix among others, is used for short-term treatment of erosive esophagitis associated with gastroesophageal reflux disease (GERD), maintenance of healing of erosive esophagitis, and pathological hypersecretory conditions including Zollinger–Ellison syndrome.[1]

Some common side effects of pantoprazole use in adults include: headache, diarrhea, nausea, abdominal pain, vomiting, flatulence, dizziness, and joint pain (>2%).[1] Use of pantoprazole for a long period of time may lead to chronic inflammation of stomach lining or atrophic gastritis, vitamin B-12 deficiency, and low magnesium.[1][2]

Pantoprazole is a proton pump inhibitor drug that inhibits gastric acid secretion. It works on gastric parietal cells to irreversibly inhibit (H+/K+)-ATPase function and suppress the production of gastric acid.[1][3]

Medical uses

Pantoprazole is used for short-term treatment of erosion and ulceration of the esophagus for adults and pediatric patients 5 years of age and older caused by gastroesophageal reflux disease.[1] It can be used as a maintenance therapy for long-term use after initial response is obtained, but there have not been any controlled studies about the use of pantoprazole past a duration of 12 months.[1] Pantoprazole may also be used in combination with antibiotics to treat ulcers caused by Helicobacter pylori.[4] It can also be used for long-term treatment of Zollinger-Ellison syndrome.[1]

Pregnancy

U.S.A Pregnancy Category B: In reproductive studies using doses largely greater than the recommended doses performed on rats and rabbits, there was no evident harm on the development of the baby.[1]

Breast feeding

Pantoprazole has been found to pass through the breast milk. However, in rodent cancer studies, pantoprazole has been shown to potentially cause tumor growth. The clinical relevance of the finding is unknown, but risks and benefits are recommended for consideration in determining the use of therapy for the mother and child.[1]

Children

Pantoprazole is only indicated for the short-term treatment of erosive esophagitis in children ages 5 and older; and the safety and effectiveness of pantoprazole have only been established in the treatment of erosive esophagitis in children.[1]

Elderly

The incidence of adverse effects occurring in patients aged 65 years and older were similar to those in patients aged 65 years and less.[1]

Adverse effects

Common

Rare

Long-term Use

Interactions

Pharmacology

Wyeth pantoprazole 20-mg

The mechanism of action of pantoprazole is to inhibit the final step in gastric acid production.[1] In the gastric parietal cell of the stomach, pantoprazole covalently binds to the H+/K+ ATP pump to inhibit gastric acid and basal acid secretion.[1] The covalent binding prevents acid secretion of up to 24 hours and longer.[1]

Pantoprazole is metabolized in the liver by the cytochrome P450 system.[9] Metabolism mainly consists of demethylation by CYP2C19 followed by sulfation. Another metabolic pathway is oxidation by CYP3A4. Pantoprazole metabolites are not thought to have any pharmacological significance. It is usually given with a prokinetic drug because of inactivity in the acidic environment of the stomach. Pantoprazole binds irreversibly to H+K+ATPase (proton pumps) to suppress the secretion of acid. Due to irreversible binding of the pumps, new pumps have to be made before acid production can be resumed.[3] The drug's plasma half-life is about 2 hours.[10]

See also

References

  1. 1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16 17 18 19 20 21 22 23 "Prescribing Info". Protonix package insert. Retrieved November 3, 2015.
  2. 1 2 Research, Center for Drug Evaluation and. "Drug Safety and Availability - FDA Drug Safety Communication: Low magnesium levels can be associated with long-term use of Proton Pump Inhibitor drugs (PPIs)". www.fda.gov. Retrieved 2015-11-03.
  3. 1 2 Richardson, Paul; Hawkey, Christopher J.; Stack, Dr William A. (2012-11-29). "Proton Pump Inhibitors". Drugs. 56 (3): 307–335. doi:10.2165/00003495-199856030-00002. ISSN 0012-6667. PMID 9777309.
  4. Dammann, Hans-Gerd; Fölsch, Ulrich R.; Hahn, Eckhart G.; Von Kleist, Detlef-Hasso; Klör, Hans-Ulrich; Kirchner, Thomas; Strobel, Sonja; Kist, Manfred (2000-03-01). "Eradication of H. pylori with Pantoprazole, Clarithromycin, and Metronidazole in Duodenal Ulcer Patients: A Head-to-Head Comparison Between Two Regimens of Different Duration". Helicobacter. 5 (1): 41–51. doi:10.1046/j.1523-5378.2000.00006.x. ISSN 1523-5378. PMID 10672051.
  5. Herzig, SJ; Doughty, C; Lahoti, S; Marchina, S; Sanan, N; Feng, W; Kumar, S (November 2014). "Acid-suppressive medication use in acute stroke and hospital-acquired pneumonia.". Annals of Neurology. 76 (5): 712–8. doi:10.1002/ana.24262. PMID 25164323.
  6. Ricketson, Jeffrey; Kimel, Gil; Spence, James; Weir, Rene (2009-03-03). "Acute allergic interstitial nephritis after use of pantoprazole". Canadian Medical Association Journal. 180 (5): 535–538. doi:10.1503/cmaj.080456. ISSN 0820-3946. PMC 2645468Freely accessible. PMID 19255077.
  7. [Dr. John Cooke, chair of Methodist Hospital's cardiovascular services] [Houston Chronicle Health Zone dated Thursday, July 11, 2013 chron.com/refluxmeds] (Journal: Circulation)
  8. Research, Center for Drug Evaluation and. "Postmarket Drug Safety Information for Patients and Providers - FDA Drug Safety Communication: Possible increased risk of fractures of the hip, wrist, and spine with the use of proton pump inhibitors". www.fda.gov. Retrieved 2015-11-03.
  9. Meyer, U A (1996). "Metabolic interactions of the proton-pump inhibitors lansoprazole, omeprazole and pantoprazole with other drugs". European journal of gastroenterology & hepatology. 8 (Suppl 1): S21–25. doi:10.1097/00042737-199610001-00005.
  10. Sachs, George; Shin, Jai Moo; Hunt, Richard (2010-10-06). "Novel Approaches to Inhibition of Gastric Acid Secretion". Current Gastroenterology Reports. 12 (6): 437–447. doi:10.1007/s11894-010-0149-5. ISSN 1522-8037. PMC 2974194Freely accessible. PMID 20924727.
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