pantoprazole indications/contra

Stem definitionDrug idCAS RN
antiulcer, benzimidazole derivatives 2054 102625-70-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • pantoprazole
  • pantozol
  • pantoprazole sodium
  • controloc control
  • pantoprazole sodium hydrate
  • pantoprazole sodium sesquihydrate
Pantoprazole sodium is a proton pump inhibitor (PPI) that suppresses the final step in gastric acid production by covalently binding to the (H+, K+)-ATPase enzyme system at the secretory surface of the gastric parietal cell. This effect leads to inhibition of both basal and stimulated gastric acid secretion, irrespective of the stimulus. The binding to the (H+, K+)-ATPase results in a duration of antisecretory effect that persists longer than 24 hours.
  • Molecular weight: 383.37
  • Formula: C16H15F2N3O4S
  • CLOGP: 2.11
  • LIPINSKI: 0
  • HAC: 7
  • HDO: 1
  • TPSA: 86.33
  • ALOGS: -2.89
  • ROTB: 7

Drug dosage:

DoseUnitRoute
40 mg O
40 mg P

Approvals:

DateAgencyCompanyOrphan
Feb. 2, 2000 FDA WYETH PHARMS INC

FDA Adverse Event Reporting System

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MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Hypomagnesaemia 994.97 23.60 223 5726 3479 3376431
Drug interaction 582.92 23.60 270 5679 46542 3333368
Hypocalcaemia 574.28 23.60 157 5792 5664 3374246
Drug hypersensitivity 569.48 23.60 245 5704 35435 3344475
Hyponatraemia 454.14 23.60 173 5776 18186 3361724
Suicide attempt 386.93 23.60 148 5801 15699 3364211
Acute kidney injury 368.11 23.60 202 5747 49481 3330429
Drug ineffective 335.20 23.60 261 5688 115829 3264081
Diarrhoea 335.06 23.60 250 5699 104098 3275812
Vomiting 313.11 23.60 226 5723 89305 3290605
Nausea 303.57 23.60 258 5691 129387 3250523
Tubulointerstitial nephritis 299.99 23.60 89 5860 4297 3375613
Agranulocytosis 287.36 23.60 90 5859 5222 3374688
Toxic epidermal necrolysis 283.93 23.60 86 5863 4459 3375451
Hypokalaemia 263.45 23.60 108 5841 13697 3366213
Subacute cutaneous lupus erythematosus 259.39 23.60 49 5900 299 3379611
Drug reaction with eosinophilia and systemic symptoms 256.16 23.60 91 5858 7804 3372106
Pruritus 254.81 23.60 156 5793 46677 3333233
Thrombocytopenia 248.60 23.60 139 5810 35129 3344781
Dyspnoea 224.32 23.60 197 5752 102737 3277173
Stevens-Johnson syndrome 223.23 23.60 79 5870 6693 3373217
Hypotension 222.02 23.60 146 5803 49368 3330542
Drug screen positive 217.95 23.60 58 5891 1870 3378040
Gastrooesophageal reflux disease 194.52 23.60 83 5866 11608 3368302
Asthenia 184.94 23.60 146 5803 65519 3314391
Abdominal pain 184.79 23.60 127 5822 46098 3333812
Drug screen false positive 183.66 23.60 40 5909 534 3379376
Product substitution issue 181.62 23.60 70 5879 7530 3372380
Condition aggravated 181.34 23.60 118 5831 39115 3340795
Leukopenia 179.56 23.60 86 5863 15737 3364173

Pharmacologic Action:

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SourceCodeDescription
ATC A02BC02 ALIMENTARY TRACT AND METABOLISM
DRUGS FOR ACID RELATED DISORDERS
DRUGS FOR PEPTIC ULCER AND GASTRO-OESOPHAGEAL REFLUX DISEASE (GORD)
Proton pump inhibitors
ATC A02BD04 ALIMENTARY TRACT AND METABOLISM
DRUGS FOR ACID RELATED DISORDERS
DRUGS FOR PEPTIC ULCER AND GASTRO-OESOPHAGEAL REFLUX DISEASE (GORD)
Combinations for eradication of Helicobacter pylori
ATC A02BD11 ALIMENTARY TRACT AND METABOLISM
DRUGS FOR ACID RELATED DISORDERS
DRUGS FOR PEPTIC ULCER AND GASTRO-OESOPHAGEAL REFLUX DISEASE (GORD)
Combinations for eradication of Helicobacter pylori
FDA EPC N0000175525 Proton Pump Inhibitor
MeSH PA D000897 Anti-Ulcer Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D005765 Gastrointestinal Agents
MeSH PA D054328 Proton Pump Inhibitors
CHEBI has role CHEBI:49201 anti-ulcer drug

Drug Use (View source of the data)

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DiseaseRelationSNOMED_IDDOID
Peptic ulcer indication 13200003 DOID:750
Erosive esophagitis indication 40719004
Zollinger-Ellison syndrome indication 53132006 DOID:0050782
Multiple endocrine adenomas indication 60549007
Gastroesophageal reflux disease indication 235595009 DOID:8534
Maintenance of Healing Erosive Esophagitis indication
Gastric Hypersecretory Conditions indication
Osteoporosis contraindication 64859006 DOID:11476
Pernicious anemia contraindication 84027009 DOID:13381
Fracture of bone contraindication 125605004
Hypomagnesemia contraindication 190855004
Upper gastrointestinal hemorrhage off-label use 37372002
Duodenal ulcer disease off-label use 51868009 DOID:1724
Gastric ulcer off-label use 397825006 DOID:10808
Pathological Gastric Hypersecretory Condition off-label use
Duodenal Ulcer due to H. Pylori off-label use
Prevention of NSAID-Induced Gastric Ulcer off-label use

Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.42 acidic
pKa2 3.58 Basic
pKa3 2.32 Basic

Orange Book patent data (new drug applications)

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Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 40MG BASE PROTONIX WYETH PHARMS INC N022020 Nov. 14, 2007 RX FOR SUSPENSION, DELAYED RELEASE ORAL 7550153 Sept. 30, 2024 EROSIVE ESOPHAGITIS, HYPERSECRETORY CONDITIONS INCLUDING ZOLLINGER-ELLISON SYNDROME, MAINTENANCE OF HEALING OF EROSIVE ESOPHAGITIS AND REDUCTION OF SYMPTOMS IN PATIENTS WITH GERD
EQ 40MG BASE PROTONIX WYETH PHARMS INC N022020 Nov. 14, 2007 RX FOR SUSPENSION, DELAYED RELEASE ORAL 7553498 Sept. 30, 2024 EROSIVE ESOPHAGITIS, HYPERSECRETORY CONDITIONS INCLUDING ZOLLINGER-ELLISON SYNDROME, MAINTENANCE OF HEALING OF EROSIVE ESOPHAGITIS AND REDUCTION OF SYMPTOMS IN PATIENTS WITH GERD
EQ 40MG BASE PROTONIX WYETH PHARMS INC N022020 Nov. 14, 2007 RX FOR SUSPENSION, DELAYED RELEASE ORAL 7838027 Sept. 30, 2024 EROSIVE ESOPHAGITIS, HYPERSECRETORY CONDITIONS INCLUDING ZOLLINGER-ELLISON SYNDROME, MAINTENANCE OF HEALING OF EROSIVE ESOPHAGITIS AND REDUCTION OF SYMPTOMS IN PATIENTS WITH GERD

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Potassium-transporting ATPase Transporter INHIBITOR CHEMBL CHEMBL
Solute carrier family 22 member 2 Transporter IC50 5.82 CHEMBL
Multidrug and toxin extrusion protein 2 Transporter IC50 4.36 CHEMBL
Multidrug and toxin extrusion protein 1 Transporter IC50 5.55 CHEMBL
Sodium/potassium-transporting ATPase subunit alpha-1 Transporter WOMBAT-PK
Fatty acid synthase Enzyme Ki 5.39 CHEMBL
Indoleamine 2,3-dioxygenase 2 Enzyme IC50 4.90 CHEMBL
Potassium-transporting ATPase Enzyme IC50 6 SCIENTIFIC LITERATURE

External reference:

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IDSource
DB00213 DRUGBANK_ID
4021208 VUID
N0000148654 NUI
C0081876 UMLSCUI
7260 IUPHAR_LIGAND_ID
D02593 KEGG_DRUG
6871619Q5X UNII
164579-32-2 SECONDARY_CAS_RN
4021208 VANDF
130104 MMSL
N0000007399 NDFRT
N0000148654 NDFRT
006006 NDDF
d04514 MMSL
40790 RXNORM
317317009 SNOMEDCT_US
395821003 SNOMEDCT_US
CHEMBL1502 ChEMBL_ID
4679 PUBCHEM_CID
CHEMBL1200408 ChEMBL_ID
C064276 MESH_SUPPLEMENTAL_RECORD_UI
6548 INN_ID
CHEBI:7915 CHEBI

Pharmaceutical products:

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ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
Protonix HUMAN PRESCRIPTION DRUG LABEL 1 0008-0841 TABLET, DELAYED RELEASE 40 mg ORAL NDA 20 sections
Protonix HUMAN PRESCRIPTION DRUG LABEL 1 0008-0843 TABLET, DELAYED RELEASE 20 mg ORAL NDA 20 sections
Protonix HUMAN PRESCRIPTION DRUG LABEL 1 0008-0844 GRANULE, DELAYED RELEASE 40 mg ORAL NDA 20 sections
Protonix HUMAN PRESCRIPTION DRUG LABEL 1 0008-0923 INJECTION, POWDER, FOR SOLUTION 40 mg INTRAVENOUS NDA 18 sections
Protonix HUMAN PRESCRIPTION DRUG LABEL 1 0008-0941 INJECTION, POWDER, FOR SOLUTION 40 mg INTRAVENOUS NDA 18 sections
Protonix HUMAN PRESCRIPTION DRUG LABEL 1 0008-2001 INJECTION, POWDER, FOR SOLUTION 40 mg INTRAVENOUS NDA 18 sections
Protonix HUMAN PRESCRIPTION DRUG LABEL 1 0008-4001 INJECTION, POWDER, FOR SOLUTION 40 mg INTRAVENOUS NDA 18 sections
Pantoprazole Sodium HUMAN PRESCRIPTION DRUG LABEL 1 0093-0011 TABLET, DELAYED RELEASE 20 mg ORAL ANDA 18 sections
Pantoprazole Sodium HUMAN PRESCRIPTION DRUG LABEL 1 0093-0012 TABLET, DELAYED RELEASE 40 mg ORAL ANDA 18 sections
Pantoprazole Sodium HUMAN PRESCRIPTION DRUG LABEL 1 0143-9284 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 40 mg INTRAVENOUS NDA 17 sections
Pantoprazole Sodium HUMAN PRESCRIPTION DRUG LABEL 1 0143-9300 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 40 mg INTRAVENOUS NDA 17 sections
Pantoprazole Sodium HUMAN PRESCRIPTION DRUG LABEL 1 0378-6688 TABLET, DELAYED RELEASE 20 mg ORAL ANDA 18 sections
Pantoprazole Sodium HUMAN PRESCRIPTION DRUG LABEL 1 0378-6689 TABLET, DELAYED RELEASE 40 mg ORAL ANDA 18 sections
Pantoprazole Sodium HUMAN PRESCRIPTION DRUG LABEL 1 0615-7629 TABLET, DELAYED RELEASE 40 mg ORAL ANDA 17 sections
Pantoprazole Sodium HUMAN PRESCRIPTION DRUG LABEL 1 0615-7916 TABLET, DELAYED RELEASE 20 mg ORAL ANDA 18 sections
Pantoprazole Sodium HUMAN PRESCRIPTION DRUG LABEL 1 0615-7998 TABLET, DELAYED RELEASE 40 mg ORAL ANDA 18 sections
Pantoprazole Sodium HUMAN PRESCRIPTION DRUG LABEL 1 0904-6474 TABLET, DELAYED RELEASE 40 mg ORAL ANDA 18 sections
Pantoprazole Sodium HUMAN PRESCRIPTION DRUG LABEL 1 13668-429 TABLET, DELAYED RELEASE 40 mg ORAL ANDA 18 sections
PANTOPRAZOLE SODIUM HUMAN PRESCRIPTION DRUG LABEL 1 16590-635 TABLET, DELAYED RELEASE 20 mg ORAL NDA 18 sections
PROTONIX HUMAN PRESCRIPTION DRUG LABEL 1 16590-939 TABLET, DELAYED RELEASE 20 mg ORAL NDA 19 sections
Protonix HUMAN PRESCRIPTION DRUG LABEL 1 21695-108 TABLET, DELAYED RELEASE 40 mg ORAL NDA 17 sections
Pantoprazole Sodium HUMAN PRESCRIPTION DRUG LABEL 1 21695-771 TABLET, DELAYED RELEASE 40 mg ORAL ANDA 17 sections
PANTOPRAZOLE SODIUM HUMAN PRESCRIPTION DRUG LABEL 1 31722-712 TABLET, DELAYED RELEASE 20 mg ORAL ANDA 19 sections
PANTOPRAZOLE SODIUM HUMAN PRESCRIPTION DRUG LABEL 1 31722-713 TABLET, DELAYED RELEASE 40 mg ORAL ANDA 19 sections
Pantoprazole sodium HUMAN PRESCRIPTION DRUG LABEL 1 33342-019 TABLET, DELAYED RELEASE 20 mg ORAL ANDA 19 sections
Pantoprazole sodium HUMAN PRESCRIPTION DRUG LABEL 1 33342-020 TABLET, DELAYED RELEASE 40 mg ORAL ANDA 19 sections
Pantoprazole Sodium HUMAN PRESCRIPTION DRUG LABEL 1 33358-536 TABLET, DELAYED RELEASE 20 mg ORAL ANDA 17 sections
PANTOPRAZOLE SODIUM HUMAN PRESCRIPTION DRUG LABEL 1 35356-622 TABLET, DELAYED RELEASE 40 mg ORAL ANDA 17 sections
PANTOPRAZOLE SODIUM HUMAN PRESCRIPTION DRUG LABEL 1 35356-768 TABLET, DELAYED RELEASE 20 mg ORAL ANDA 17 sections
Pantoprazole Sodium HUMAN PRESCRIPTION DRUG LABEL 1 42043-370 TABLET, DELAYED RELEASE 20 mg ORAL ANDA 18 sections