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Pantoprazole
Clinical data
Trade namesProtonix
AHFS/Drugs.comMonograph
MedlinePlusa601246
License data
Pregnancy
category
  • AU: B3
Routes of
administration		Oral and intravenous
ATC code
Legal status
Legal status
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability77%
MetabolismHepatic (CYP3A4)
Elimination half-life1-2 hours
ExcretionRenal
Identifiers
  • (RS)-6-(Difluoromethoxy)-2-[(3,4-dimethoxypyridin-2-yl)methylsulfinyl]-1H-benzo[d]imidazole
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
Chemical and physical data
FormulaC16H15F2N3O4S
Molar mass383.371 g/mol g·mol−1
3D model (JSmol)
  • FC(F)Oc3cc1c(nc(n1)S(=O)Cc2nccc(OC)c2OC)cc3
  • InChI=1S/C16H15F2N3O4S/c1-23-13-5-6-19-12(14(13)24-2)8-26(22)16-20-10-4-3-9(25-15(17)18)7-11(10)21-16/h3-7,15H,8H2,1-2H3,(H,20,21) checkY
  • Key:IQPSEEYGBUAQFF-UHFFFAOYSA-N checkY
  (verify)

Pantoprazole is a proton pump inhibitor drug that inhibits gastric acid secretion. It was initially marketed under the brand name Protonix and is now available as a generic. Pantoprazole is indicated 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]. Pantoprazole works on gastric parietal cells to irreversibly inhibit (H+/K+)-ATPase function and suppress the production of gastric acid[1][2]. Some common adverse reactions from pantoprazole use in adults include: headache, diarrhea, nausea, abdominal pain, vomiting, flatulence, dizziness, and arthralgia (>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 (more than 3 years of use), and low magnesium (usually after one year of treatment)[1][3].

Medical uses

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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]. Initial treatment is generally of eight weeks' duration, after which another eight-week course of treatment may be considered if necessary.[4] It can be used as a maintenance therapy for long-term use after initial response is obtained, but there has not been any controlled studies that study 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.[5] When treating H. pylori ulcers, pantoprazole is given twice daily,[6] in contrast to gastroesophageal reflux disease, where it is usually given once daily.[4] Typical treatment courses for H. pylori range from 10 to 14 days.[6] It can also be used for long term treatment of Zollinger-Ellison syndrome. [1]

Use in Special Populations

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Pregnancy:

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U.S.A Pregnancy Category B: In reproductive studies performed on rats and rabbits, there have been no evidence of impaired development/harm when used. Dosages given to these animals were up to 88 times the recommended human dose in rats, and 16 times the recommended human dose in rabbits[1].

Breast feeding:

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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 should take into consideration the risk and benefit of continuing the therapy for the mother, and child[1].

Pediatric Use:

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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]

Geriatric Use:

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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

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  • Infection: Stomach acid plays a role in killing ingested bacteria. Use of pantoprazole may increase the chance of developing infections such as pneumonia, particularly in hospitalized patients.[7]

Common

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  • Gastrointestinal: abdominal pain (6%), diarrhea (9%), flatulence (4%), nausea (7%), vomiting (4%)[1]
  • Neurologic: headache (12%), dizziness (3%), [1]
  • Neuromuscular and Skeletal: arthralgia (3%)[1]

Rare

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  • Gastrointestinal: constipation, dry mouth, Hepatitis[1]
  • Hematologic: Leukopenia, thrombocytopenia[1]
  • Immunologic: Stevens–Johnson syndrome, toxic epidermal necrolysis[1]
  • Metabolic: elevated creatinine kinase, elevated triglycerides, elevated Liver enzymes (AST/ALT), Edema[1]
  • Musculoskeletal: Muscle disorders, bone fracture and infection, Clostridium difficile infection, osteoporosis-related hip fracture, rhabdomyolysis[1]
  • Renal: interstitial nephritis[8]
  • Nutrition: may reduce the absorption of important nutrients, vitamins and minerals, as well as medications, leaving users at increased risk for pneumonia[9]. During long-term use, hypomagnesia has been observed in patients on medications like Pantoprazole.[3]
  • Cardiovascular: increase in a chemical that suppresses the production of nitric oxide by 25% in humans, which has proven to relax and protect arteries and veins, causes blood vessels to constrict, a development that could lead to a number of cardiovascular problems if continued for a prolonged time[9]

 Long-term Use

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  • Osteoporosis and bone fracture have been observed in patients on high-dose and/or long term (over 1 year) prescription proton pump inhibitors.[10]
  • Hypomagnesia has been observed in patients on medications like Pantoprazole when taken for longer periods of time (generally 1 year or more, although cases have been reported with regimens as short as 3 months), [11]

Interactions

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Pharmacology

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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 to last for up to 24 hours and longer.[1]

Pantoprazole is metabolized in the liver by the cytochrome P450 system.[12] 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. Generally inactive at the acidic pH of stomach, thus it is usually given with a prokinetic drug. Pantoprazole binds irreversibly to H+K+ATPase (proton pumps) and suppresses the secretion of acid. As it binds irreversibly to the pumps, new pumps have to be made before acid production can be resumed. The drug's plasma half-life is about 2 hours.[13]

See also

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References

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  1. ^ a b c d e f g h i j k l m n o p q r s t u v w "Prescribing Info". Protonix package insert. Retrieved November 3 2015. {{cite web}}: Check date values in: |accessdate= (help)
  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. S2CID 46962618.
  3. ^ a b 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.
  4. ^ a b Katz, Philip O; Gerson, Lauren B; Vela, Marcelo F (19 February 2013). "Guidelines for the Diagnosis and Management of Gastroesophageal Reflux Disease". The American Journal of Gastroenterology. 108 (3): 308–328. doi:10.1038/ajg.2012.444. PMID 23419381. S2CID 8198975.
  5. ^ Dammann, HG; Fölsch, UR; Hahn, EG; von Kleist, DH; Klör, HU; Kirchner, T; Strobel, S; Kist, M (March 2000). "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. PMID 10672051. S2CID 32184484.
  6. ^ a b Chey, WD; Wong, BC; Practice Parameters Committee of the American College of, Gastroenterology (August 2007). "American College of Gastroenterology guideline on the management of Helicobacter pylori infection". The American Journal of Gastroenterology. 102 (8): 1808–25. PMID 17608775.
  7. ^ 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. PMC 4214881. PMID 25164323.
  8. ^ 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 2645468. PMID 19255077.
  9. ^ a b [Dr. John Cooke, chair of Methodist Hospital's cardiovascular services] [Houston Chronicle Health Zone dated Thursday, July 11, 2013 chron.com/refluxmeds] (Journal: Circulation)
  10. ^ 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.
  11. ^ 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.
  12. ^ 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. PMID 8930576. S2CID 24171788.
  13. ^ Sachs G, Shin JM, Hunt R (December 2010). "Novel approaches to inhibition of gastric acid secretion". Curr Gastroenterol Rep. 12 (6): 437–47. doi:10.1007/s11894-010-0149-5. PMC 2974194. PMID 20924727.{{cite journal}}: CS1 maint: multiple names: authors list (link)
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Category:Proton pump inhibitors Category:Benzimidazoles Category:Sulfoxides Category:Wyeth Category:Phenol ethers Category:Organofluorides Category:Pyridines

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