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Pantoprazole

Generic Name
Pantoprazole
Brand Names
Protonix, Somac Control, Tecta, Pantozol Control, Controloc Control
Drug Type
Small Molecule
Chemical Formula
C16H15F2N3O4S
CAS Number
102625-70-7
Unique Ingredient Identifier
D8TST4O562

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 amoxicillin, clarithromycin, and metronidazole, for example. Its efficacy is considered similar to other medications within the PPI class including omeprazole, esomeprazole, lansoprazole, dexlansoprazole, and rabeprazole. 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 the stimulus. As the binding of pantoprazole to the (H+, K+)-ATPase enzyme is irreversible and new enzyme needs to be expressed in order to resume acid secretion, pantoprazole's duration of antisecretory effect persists longer than 24 hours. Due to their good safety profile and as several PPIs are available over the counter without a prescription, their current use in North America is widespread. Long term use of PPIs such as pantoprazole have been associated with possible adverse effects, however, including increased susceptibility to bacterial infections (including gastrointestinal C. difficile), reduced absorption of micronutrients including iron and B12, and an increased risk of developing hypomagnesemia and hypocalcemia which may contribute to osteoporosis and bone fractures later in life. PPIs such as pantoprazole have also been shown to inhibit the activity of dimethylarginine dimethylaminohydrolase (DDAH), an enzyme necessary for cardiovascular health. DDAH inhibition causes a consequent accumulation of the nitric oxide synthase inhibitor asymmetric dimethylarginie (ADMA), which is thought to cause the association of PPIs with increased risk of cardiovascular events in patients with unstable coronary syndromes. Pantoprazole doses should be slowly lowered, or tapered, before discontinuing as rapid discontinuation of PPIs such as pantoprazole may cause a rebound effect and a short term increase in hypersecretion.

Background

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 amoxicillin, clarithromycin, and metronidazole, for example. Its efficacy is considered similar to other medications within the PPI class including omeprazole, esomeprazole, lansoprazole, dexlansoprazole, and rabeprazole. 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 the stimulus. As the binding of pantoprazole to the (H+, K+)-ATPase enzyme is irreversible and new enzyme needs to be expressed in order to resume acid secretion, pantoprazole's duration of antisecretory effect persists longer than 24 hours. Due to their good safety profile and as several PPIs are available over the counter without a prescription, their current use in North America is widespread. Long term use of PPIs such as pantoprazole have been associated with possible adverse effects, however, including increased susceptibility to bacterial infections (including gastrointestinal C. difficile), reduced absorption of micronutrients including iron and B12, and an increased risk of developing hypomagnesemia and hypocalcemia which may contribute to osteoporosis and bone fractures later in life. PPIs such as pantoprazole have also been shown to inhibit the activity of dimethylarginine dimethylaminohydrolase (DDAH), an enzyme necessary for cardiovascular health. DDAH inhibition causes a consequent accumulation of the nitric oxide synthase inhibitor asymmetric dimethylarginie (ADMA), which is thought to cause the association of PPIs with increased risk of cardiovascular events in patients with unstable coronary syndromes. Pantoprazole doses should be slowly lowered, or tapered, before discontinuing as rapid discontinuation of PPIs such as pantoprazole may cause a rebound effect and a short term increase in hypersecretion.

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 esophagitis, as an alternative to oral medication in patients who are unable to continue taking pantoprazole delayed-release tablets. Safety and efficacy of pantoprazole injection as the initial treatment of patients having GERD with a history of erosive esophagitis have not been demonstrated at this time. Pathological Hypersecretion Associated with Zollinger-Ellison Syndrome Pantoprazole for injection is indicated for the treatment of pathological hypersecretory conditions associated with Zollinger-Ellison Syndrome or other neoplastic conditions. Pantoprazole delayed-release oral suspension: Short-Term Treatment of erosive esophagitis associated with gastroesophageal reflux disease (GERD) Indicated in adults and pediatric patients five years of age and above for the short-term treatment (up to 8 weeks) in the healing and symptomatic relief of erosive esophagitis. For adult patients who have not healed after 8 weeks of treatment, an additional 8-week course of pantoprazole may be considered. Safety of treatment beyond 8 weeks in pediatric patients has not been determined. Maintenance of healing of erosive esophagitis Indicated for maintenance of healing of erosive esophagitis and reduction in relapse rates of daytime and nighttime heartburn symptoms in adult patients with GERD. Pathological hypersecretory conditions including Zollinger-Ellison syndrome Indicated for the long-term treatment of the above conditions.

Associated Conditions

  • Erosive Esophagitis
  • GERD With Erosive Esophagitis
  • Gastro-esophageal Reflux Disease (GERD)
  • Healing
  • Heartburn
  • Helicobacter Pylori Infection
  • Stress Ulcers
  • Zollinger-Ellison Syndrome
  • Conditions where a reduction of gastric acid secretion is required
  • Pathological hypersecretory conditions

FDA Approved Products

Pantoprazole
Manufacturer:Preferred Pharmaceuticals Inc.
Route:ORAL
Strength:20 mg in 1 1
Approved: 2023/08/15
NDC:68788-8505
PANTOPRAZOLE SODIUM
Manufacturer:RPK Pharmaceuticals, Inc.
Route:ORAL
Strength:20 mg in 1 1
Approved: 2022/07/21
NDC:53002-1700
Pantoprazole Sodium
Manufacturer:Mylan Pharmaceuticals Inc.
Route:ORAL
Strength:20 mg in 1 1
Approved: 2022/03/28
NDC:0378-6688
Pantoprazole Sodium
Manufacturer:Preferred Pharmaceuticals Inc.
Route:ORAL
Strength:40 mg in 1 1
Approved: 2023/11/01
NDC:68788-6326
Pantoprazole Sodium
Manufacturer:Golden State Medical Supply, Inc.
Route:ORAL
Strength:40 mg in 1 1
Approved: 2024/03/29
NDC:51407-613

Singapore Approved Products

CONTROLOC IV INJECTION 40 mg/vial
Manufacturer:Takeda GmBH, Hikma Farmaceutica (Portugal), S.A., Patheon Italia S.P.A., Wasserburger Arzneimittelwerk GmbH
Form:INJECTION
Strength:40 mg/vial
Online:Yes
Approved: 1999/10/07
Approval:SIN11165P
PANTOBEX DELAYED RELEASE TABLET 40MG
Manufacturer:Beximco Pharmaceuticals Limited
Form:TABLET, DELAYED RELEASE
Strength:40 mg
Online:Yes
Approved: 2022/09/01
Approval:SIN16590P
CONTROLOC TABLET 20 mg
Manufacturer:Takeda GmbH
Form:ENTERIC COATED TABLET
Strength:20 mg
Online:Yes
Approved: 1999/10/07
Approval:SIN11170P
PANTONEX DR-40 TABLET 40MG
Manufacturer:IPCA LABORATORIES LIMITED
Form:TABLET, DELAYED RELEASE
Strength:40 mg
Online:Yes
Approved: 2013/12/23
Approval:SIN14467P
PANTIN 40 PANTOPRAZOLE GASTRO-RESISTANT TABLETS 40 MG
Manufacturer:Hetero Labs Limited
Form:TABLET, ENTERIC COATED
Strength:40.0 mg
Online:Yes
Approved: 2016/07/04
Approval:SIN15041P

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