brinzolamide indications/contra

Stem definitionDrug idCAS RN
396 138890-62-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • AL-4862
  • brinzolamide
  • azopt
an antiglaucoma agent
  • Molecular weight: 383.50
  • Formula: C12H21N3O5S3
  • CLOGP: 0.33
  • LIPINSKI: 0
  • HAC: 8
  • HDO: 2
  • TPSA: 118.80
  • ALOGS: -2.73
  • ROTB: 7

Drug dosage:

DoseUnitRoute
0.20 ml None

Approvals:

DateAgencyCompanyOrphan
April 1, 1998 FDA ALCON PHARMS LTD

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
Intraocular pressure increased 276.28 43.59 48 501 2374 3382936
Ocular hyperaemia 222.07 43.59 45 504 5108 3380202
Eye irritation 212.83 43.59 42 507 4157 3381153
Vision blurred 139.42 43.59 40 509 19549 3365761
Eye pain 130.72 43.59 30 519 6017 3379293
Glaucoma 101.08 43.59 21 528 2635 3382675
Visual acuity reduced 94.37 43.59 25 524 8989 3376321
Eye allergy 79.32 43.59 11 538 114 3385196
Punctate keratitis 71.87 43.59 11 538 235 3385075
Conjunctival hyperaemia 69.32 43.59 13 536 957 3384353
Corneal oedema 68.65 43.59 12 537 594 3384716
Eye pruritus 67.00 43.59 15 534 2656 3382654
Dizziness 64.87 43.59 33 516 76479 3308831
Drug ineffective 62.35 43.59 37 512 116053 3269257
Hypersensitivity 59.33 43.59 23 526 27877 3357433
Dyspnoea 58.34 43.59 34 515 102900 3282410
Corneal disorder 56.20 43.59 10 539 548 3384762
Foreign body sensation in eyes 49.23 43.59 9 540 574 3384736
Lacrimation increased 48.14 43.59 12 537 3356 3381954
Dry mouth 47.64 43.59 15 534 9807 3375503
Fatigue 46.77 43.59 30 519 107210 3278100

Pharmacologic Action:

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SourceCodeDescription
ATC S01EC04 SENSORY ORGANS
OPHTHALMOLOGICALS
ANTIGLAUCOMA PREPARATIONS AND MIOTICS
Carbonic anhydrase inhibitors
ATC S01EC54 SENSORY ORGANS
OPHTHALMOLOGICALS
ANTIGLAUCOMA PREPARATIONS AND MIOTICS
Carbonic anhydrase inhibitors
FDA EPC N0000175517 Carbonic Anhydrase Inhibitor
MeSH PA D002257 Carbonic Anhydrase Inhibitors
MeSH PA D004791 Enzyme Inhibitors
CHEBI has role CHEBI:39456 antiglaucoma drug

Drug Use (View source of the data)

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DiseaseRelationSNOMED_IDDOID
Ocular hypertension indication 4210003 DOID:9282
Open-angle glaucoma indication 84494001 DOID:1067
Acute nephropathy contraindication 58574008

Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.31 acidic
pKa2 7.75 Basic

Orange Book patent data (new drug applications)

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Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
1% SIMBRINZA NOVARTIS PHARMS CORP N204251 April 19, 2013 RX SUSPENSION/DROPS OPHTHALMIC 6316441 Dec. 7, 2019 REDUCTION OF ELEVATED INTRAOCULAR PRESSURE IN PATIENTS WITH OPEN ANGLE GLAUCOMA OR OCULAR HYPERTENSION

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Carbonic anhydrase 2 Enzyme INHIBITOR Ki 9.90 CHEMBL CHEMBL
Carbonic anhydrase 12 Enzyme Ki 8.52 CHEMBL
Carbonic anhydrase 4 Enzyme Ki 5.40 CHEMBL
Carbonic anhydrase 13 Enzyme Ki 7.96 CHEMBL
Carbonic anhydrase 5A, mitochondrial Enzyme Ki 7.30 CHEMBL
Carbonic anhydrase 14 Enzyme Ki 7.62 CHEMBL
Carbonic anhydrase 7 Enzyme Ki 8.55 CHEMBL
Carbonic anhydrase 9 Enzyme Ki 7.44 CHEMBL
Carbonic anhydrase 1 Enzyme Ki 8.52 CHEMBL
Carbonic anhydrase 5B, mitochondrial Enzyme Ki 7.52 CHEMBL
Carbonic anhydrase 6 Enzyme Ki 9.05 CHEMBL
Carbonic anhydrase 13 Enzyme Ki 8 CHEMBL
Alpha carbonic anhydrase Unclassified Ki 7.32 CHEMBL
Probable transmembrane carbonic anhydrase (Carbonate dehydratase) (Carbonic dehydratase); Transmembrane carbonic anhydrase Enzyme Ki 6.70 CHEMBL
Astrosclerin-3 Unclassified Ki 6.56 CHEMBL
Beta-carbonic anhydrase 1 Enzyme Ki 6.08 CHEMBL
Carbonic anhydrase Unclassified Ki 6.77 CHEMBL
Delta carbonic anhydrase Unclassified Ki 6.93 CHEMBL
Carbonic anhydrase Enzyme Ki 6.94 CHEMBL
Carbonic anhydrase Enzyme Ki 6.68 CHEMBL
Carbonic anhydrase 15 Enzyme Ki 7.21 CHEMBL
Carbonic anhydrase Enzyme Ki 8.52 CHEMBL
Carbonic anhydrase 2 Enzyme Ki 6.90 CHEMBL
Carbonic anhydrase 4 Enzyme Ki 7.35 CHEMBL
Carbonic anhydrase Unclassified Ki 7.50 CHEMBL
Carbonic anhydrase Enzyme Ki 5.36 CHEMBL

External reference:

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IDSource
4021097 VUID
N0000148553 NUI
C0673966 UMLSCUI
6797 IUPHAR_LIGAND_ID
D00652 KEGG_DRUG
4298 MMSL
194881 RXNORM
4021097 VANDF
108836002 SNOMEDCT_US
386925003 SNOMEDCT_US
N0000148553 NDFRT
N0000004426 NDFRT
007497 NDDF
9451Z89515 UNII
7532 INN_ID
CHEMBL220491 ChEMBL_ID
68844 PUBCHEM_CID
DB01194 DRUGBANK_ID
C111827 MESH_SUPPLEMENTAL_RECORD_UI
CHEBI:3176 CHEBI
BZ1 PDB_CHEM_ID

Pharmaceutical products:

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ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
Azopt HUMAN PRESCRIPTION DRUG LABEL 1 0065-0275 SUSPENSION/ DROPS 10 mg OPHTHALMIC NDA 16 sections
SIMBRINZA HUMAN PRESCRIPTION DRUG LABEL 2 0065-4147 SUSPENSION/ DROPS 10 mg OPHTHALMIC NDA 16 sections