balsalazide indications/contra

Stem definitionDrug idCAS RN
phenylazosalicylic acid derivatives antibacterial 284 80573-04-2

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • balsalazide
  • balsalazide disodium
  • balsalazide sodium
a mesalamine 5-aminosalicylate prodrug; 99% of ingested drug remains intact through the stomach and is delivered to and activated in the colon; used for inflammatory bowel disease, ulcerative colitis and radiation-induced proctosigmoiditis but avoided in patients with known hypersensitivity reaction to salicylates or mesalamine
  • Molecular weight: 357.32
  • Formula: C17H15N3O6
  • CLOGP: 3.32
  • LIPINSKI: 0
  • HAC: 9
  • HDO: 4
  • TPSA: 148.65
  • ALOGS: -3.76
  • ROTB: 7

Drug dosage:

DoseUnitRoute
6.75 g O

Approvals:

DateAgencyCompanyOrphan
July 18, 2000 FDA SALIX PHARMS

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
Myocarditis 58.36 41.36 10 108 2153 3383588

Pharmacologic Action:

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SourceCodeDescription
ATC A07EC04 ALIMENTARY TRACT AND METABOLISM
ANTIDIARRHEALS, INTESTINAL ANTIINFLAMMATORY/ANTIINFECTIVE AGENTS
INTESTINAL ANTIINFLAMMATORY AGENTS
Aminosalicylic acid and similar agents
FDA EPC N0000175781 Aminosalicylate
FDA Chemical/Ingredient N0000005760 Aminosalicylic Acids
MeSH PA D000700 Analgesics
MeSH PA D018712 Analgesics, Non-Narcotic
MeSH PA D000893 Anti-Inflammatory Agents
MeSH PA D000894 Anti-Inflammatory Agents, Non-Steroidal
MeSH PA D018501 Antirheumatic Agents
MeSH PA D005765 Gastrointestinal Agents
MeSH PA D018373 Peripheral Nervous System Agents
MeSH PA D018689 Sensory System Agents
CHEBI has role CHEBI:50266 prodrug
CHEBI has role CHEBI:35475 non-steroidal anti-inflammatory drug
CHEBI has role CHEBI:49201 anti-ulcer drug
CHEBI has role CHEBI:55324 gastrointestinal drug

Drug Use (View source of the data)

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DiseaseRelationSNOMED_IDDOID
Ulcerative colitis indication 64766004 DOID:8577
Kidney disease contraindication 90708001 DOID:2527
Pyloric obstruction contraindication 244815007 DOID:3122

Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation levelDissociation constantType (acidic/basic)
pKa1 2.28 acidic
pKa2 4.08 acidic
pKa3 11.45 acidic
pKa4 12.18 acidic

Orange Book patent data (new drug applications)

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Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
1.1GM GIAZO VALEANT PHARMS INTL N022205 Feb. 3, 2012 RX TABLET ORAL 6197341 March 13, 2018 TREATMENT OF MILDLY TO MODERATELY ACTIVE ULCERATIVE COLITIS IN MALE PATIENTS
1.1GM GIAZO VALEANT PHARMS INTL N022205 Feb. 3, 2012 RX TABLET ORAL 9192616 Aug. 2, 2026 TREATMENT OF MILDLY TO MODERATELY ACTIVE ULCERATIVE COLITIS IN MALE PATIENTS
750MG COLAZAL VALEANT PHARMS INTL N020610 July 18, 2000 RX CAPSULE ORAL 7452872 Aug. 24, 2026 TREATMENT OF ULCERATIVE COLITIS
750MG COLAZAL VALEANT PHARMS INTL N020610 July 18, 2000 RX CAPSULE ORAL 7625884 Aug. 24, 2026 TREATMENT OF ULCERATIVE COLITIS
1.1GM GIAZO VALEANT PHARMS INTL N022205 Feb. 3, 2012 RX TABLET ORAL 7452872 Aug. 24, 2026 TREATMENT OF MILDLY TO MODERATELY ACTIVE ULCERATIVE COLITIS IN MALE PATIENTS
1.1GM GIAZO VALEANT PHARMS INTL N022205 Feb. 3, 2012 RX TABLET ORAL 7625884 Aug. 24, 2026 TREATMENT OF MILDLY TO MODERATELY ACTIVE ULCERATIVE COLITIS IN MALE PATIENTS
1.1GM GIAZO VALEANT PHARMS INTL N022205 Feb. 3, 2012 RX TABLET ORAL 8497256 June 23, 2031 TREATMENT OF MILDLY TO MODERATELY ACTIVE ULCERATIVE COLITIS IN MALE PATIENTS

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Prostaglandin G/H synthase 1 Enzyme INHIBITOR WOMBAT-PK CHEMBL
Prostaglandin G/H synthase 2 Enzyme INHIBITOR WOMBAT-PK CHEMBL
Arachidonate 5-lipoxygenase Enzyme INHIBITOR CHEMBL CHEMBL
Peroxisome proliferator-activated receptor gamma Nuclear hormone receptor AGONIST CHEMBL CHEMBL

External reference:

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IDSource
4021231 VUID
N0000148675 NUI
C0052940 UMLSCUI
D02715 KEGG_DRUG
1XL6BJI034 UNII
150399-21-6 SECONDARY_CAS_RN
DB01014 DRUGBANK_ID
4021231 VANDF
420306005 SNOMEDCT_US
420557005 SNOMEDCT_US
N0000005718 NDFRT
N0000148675 NDFRT
d04700 MMSL
18747 RXNORM
007156 NDDF
6335412 PUBCHEM_CID
CHEMBL1200760 ChEMBL_ID
CHEMBL1201346 ChEMBL_ID
5221 INN_ID
C038637 MESH_SUPPLEMENTAL_RECORD_UI
DB00244 DRUGBANK_ID
CHEBI:267413 CHEBI

Pharmaceutical products:

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ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
Balsalazide Disodium HUMAN PRESCRIPTION DRUG LABEL 1 0054-0079 CAPSULE 750 mg ORAL ANDA 16 sections
Balsalazide Disodium HUMAN PRESCRIPTION DRUG LABEL 1 42291-157 CAPSULE 750 mg ORAL ANDA 16 sections
Balsalazide Disodium HUMAN PRESCRIPTION DRUG LABEL 1 49884-367 TABLET 1.10 g ORAL ANDA 17 sections
Balsalazide Disodium HUMAN PRESCRIPTION DRUG LABEL 1 50268-102 CAPSULE 750 mg ORAL ANDA 17 sections
Balsalazide Disodium HUMAN PRESCRIPTION DRUG LABEL 1 54868-6137 CAPSULE 750 mg ORAL ANDA 17 sections
COLAZAL HUMAN PRESCRIPTION DRUG LABEL 1 55154-6775 CAPSULE 750 mg ORAL NDA 17 sections
Balsalazide Disodium HUMAN PRESCRIPTION DRUG LABEL 1 60429-952 CAPSULE 750 mg ORAL ANDA 16 sections
Balsalazide Disodium HUMAN PRESCRIPTION DRUG LABEL 1 60505-2575 CAPSULE 750 mg ORAL ANDA 16 sections
Colazal HUMAN PRESCRIPTION DRUG LABEL 1 65649-101 CAPSULE 750 mg ORAL NDA authorized generic 16 sections
GIAZO HUMAN PRESCRIPTION DRUG LABEL 1 65649-102 TABLET, FILM COATED 1.10 g ORAL NDA 17 sections
Balsalazide Disodium HUMAN PRESCRIPTION DRUG LABEL 1 68084-799 CAPSULE 750 mg ORAL ANDA 18 sections
balsalazide disodium HUMAN PRESCRIPTION DRUG LABEL 1 68682-750 CAPSULE 750 mg ORAL NDA authorized generic 16 sections