|Systematic (IUPAC) name|
|Licence data||US FDA:|
|Routes||Oral and intravenous|
|Mol. mass||383.371 g/mol|
|(what is this?)|
Pantoprazole is used for short-term treatment of erosion and ulceration of the oesophagus caused by gastroesophageal reflux disease. Initial treatment is generally of eight weeks' duration, after which another eight week course of treatment may be considered if necessary. It can be used as a maintenance therapy for long term use after initial response is obtained.
Antacid preparations such as pantoprazole work by suppressing the acid-mediated breakdown of proteins. This leads to an elevated risk of developing food and drug allergies due to undigested proteins passing into the gastrointestinal tract where sensitisation occurs. It is unclear whether this risk occurs with short-term or only long-term use.
- Gastrointestinal: Abdominal pain (3%), diarrhea (4%), flatulence (4%)
- Neurologic: Headache (5%)
- Gastrointestinal: Atrophic gastritis, clostridium difficile diarrhea
- Hematologic: Thrombocytopenia (less than 1%)
- Immunologic: Stevens-Johnson syndrome, toxic epidermal necrolysis
- Musculoskeletal: Muscle disorders, bone fracture and infection, Clostridium difficile, osteoporosis-related, hip fracture, rhabdomyolysis
- Renal: Interstitial nephritis (rare)
- Nutrition: May reduce the absorption of important nutrients, vitamins and minerals, as well as medications, leaving users at increased risk for pneumonia.
- Cardiovascular: Increase in a chemical that suppresses the production of nitric oxide by 25% in humans, which have 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 period of time.
Pantoprazole is metabolized in the liver by the cytochrome P450 system. 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. Pantoprazole is relatively free of drug interactions; however, it may alter the absorption of other medications that depend on the amount of acid in the stomach, such as ketoconazole or digoxin. Generally inactive at acidic pH of stomach, thus it is usually given with a pro kinetic 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.
- Bioavailability: (oral, delayed release tablets), approximately 77%
- Effect of food: (oral, delayed-release tablets), AUC and Cmax no effect, Tmax variable, absorption delayed, no net effect
- Effect of food: (oral, for-delayed-release suspension), administer 30 minutes before a meal
- Tmax, Oral, delayed-release suspension: 2 to 2.5 h
- Tmax, Oral, delayed-release tablets: 2.5 h
- Tmax, Oral, delayed-release tablets: 1.5 to 2 hours (pediatrics)
- Protein binding: about 98% to primarily albumin
- Vd, extensive metabolizers (IV): approximately 11 L to 23.6 L
- Vd, pediatrics (oral): 0.21 to 0.43 L/kg.
- Hepatic; cytochrome P450 CYP2C19; minor metabolism from CYP3A4, 2D6, and 2C9
- Fecal: (oral or IV, normal metabolizers), 18%
- Renal: (oral or IV, normal metabolizers), approximately 71%, none as unchanged
- Dialyzable: no (hemodialysis)
- Total body clearance: (IV) 7.6 to 14 L/hour.
- Total body clearance: (oral, pediatrics) 0.18 to 2.08 L/h/kg
Elimination Half Life
- Oral or IV, 1 hour
- Oral or IV, slow metabolizers, 3.5 to 10 hours
- Pediatrics, 0.7 to 5.34 hours
Pantoprazole was developed by Altana (owned by Nycomed) and was licensed in the USA to Wyeth (which was taken over by Pfizer). It was initially marketed under the brand name Protonix by Wyeth-Ayerst Laboratories and now is available as a generic. It is available by prescription in delayed-release tablets. It is also available for intravenous use.
On 24 December 2007, Teva Pharmaceutical released an AB-rated generic alternative to Protonix. This was followed by generic equivalents from Sun Pharma and Kudco Pharma. Wyeth sued all three for patent infringement and launched its own generic version of Protonix with Nycomed.
Pantoprazole is available from a range of international suppliers under brand names including Pantazone, Pantop-D, Pantasan, Pantrol, Prazolin, Pantochem, Pansev, Pantec, Somac, API, Tecta, Protium, Pantodac, Perizole, Pansped, Percazole, Astropan, Fenix, Pantecta, Pantoloc, Controloc, Somac, Tecta, Protium, Inipomp, Eupantol, Pantozol, Pantodac, Perizole, Pansped, Zurcazol, Protonex, Pantup,Pantomed, TopZole, Nolpaza, Controloc, UXL-D, Pantid, Pantogen, Pantpas, Proton and Prazolin.
Notice the polonovski reaction.
- Pali-Schöll I, Jensen-Jarolim E (April 2011). "Anti-acid medication as a risk factor for food allergy". Allergy 66 (4): 469–77. doi:10.1111/j.1398-9995.2010.02511.x. PMID 21121928.
- [Dr. John Cooke, chair of Methodist Hospital's cardiovascular services] [Houston Chronicle Health Zone dated Thursday, July 11, 2013 chron.com/refluxmeds] (Journal: Circulation)
- 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.
- Steinijans, V. W.; Huber, R.; Hartmann, M.; Zech, K.; Bliesath, H.; Wurst, W.; Radtke, H. W. (1996). "Lack of pantoprazole drug interactions in man: An updated review". International Journal of Clinical Pharmacology and Therapeutics 34 (6): 243–262. PMID 8793611.
- 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.
- Teva Announces Launch Of Generic Protonix Tablets
- Rubenstein, Sarah (29 January 2008). "Wyeth Plans Generic Protonix; Litigation With Teva to Continue". The Wall Street Journal. p. D9. Retrieved 25 October 2009.
- "Nycomed and Wyeth announce launch of an own generic version of PROTONIX - lawsuit to defend patent continues". Retrieved 25 October 2009.[dead link]
- IntelliPharmaCeutics Press Release
- Kohl, B.; Sturm, E.; Senn-Bilfinger, J.; Simon, W. A.; Krueger, U.; Schaefer, H.; Rainer, G.; Figala, V.; Klemm, K. (1992). "(H+, K+)-ATPase inhibiting 2-[(2-pyridylmethyl)sulfinyl]benzimidazoles. 4. A novel series of dimethoxypyridyl-substituted inhibitors with enhanced selectivity. The selection of pantoprazole as a clinical candidate". Journal of Medicinal Chemistry 35 (6): 1049–57. doi:10.1021/jm00084a010. PMID 1313110.