brinzolamide Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

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

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.20 ml None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
April 1, 1998 FDA ALCON PHARMS LTD

FDA Adverse Event Reporting System (Female)

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
Eye irritation 377.52 41.68 71 590 3441 2353983
Ocular hyperaemia 293.76 41.68 59 602 3997 2353427
Intraocular pressure increased 289.68 41.68 50 611 1459 2355965
Eye pain 186.49 41.68 42 619 4849 2352575
Vision blurred 181.01 41.68 51 610 14617 2342807
Glaucoma 166.25 41.68 33 628 2062 2355362
Visual impairment 114.04 41.68 34 627 11721 2345703
Eye pruritus 103.08 41.68 23 638 2508 2354916
Product dropper issue 98.33 41.68 14 647 106 2357318
Eye allergy 89.29 41.68 13 648 117 2357307
Product quality issue 78.13 41.68 25 636 10804 2346620
Dry mouth 76.11 41.68 23 638 8230 2349194
Foreign body sensation in eyes 73.45 41.68 13 648 427 2356997
Corneal oedema 62.75 41.68 11 650 341 2357083
Cataract 61.08 41.68 18 643 5890 2351534
Drug ineffective 60.16 41.68 41 620 101583 2255841
Dry eye 58.75 41.68 16 645 3940 2353484
Punctate keratitis 56.45 41.68 9 652 154 2357270
Eyelid margin crusting 56.28 41.68 9 652 157 2357267
Dizziness 55.66 41.68 32 629 58633 2298791
Product residue present 55.48 41.68 12 649 1124 2356300
Liquid product physical issue 54.21 41.68 9 652 200 2357224
Somnolence 52.63 41.68 23 638 23462 2333962
Blindness 50.78 41.68 14 647 3604 2353820
Conjunctival hyperaemia 50.72 41.68 10 651 593 2356831
Hypersensitivity 46.09 41.68 21 640 23572 2333852
Erythema of eyelid 43.84 41.68 9 652 654 2356770
Eye swelling 43.70 41.68 13 648 4377 2353047
Product physical consistency issue 42.35 41.68 7 654 151 2357273

FDA Adverse Event Reporting System (Male)

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 252.54 57.45 43 369 1138 1745231
Eye irritation 178.98 57.45 33 379 1370 1744999
Ocular hyperaemia 167.14 57.45 33 379 1977 1744392
Vision blurred 129.50 57.45 35 377 8388 1737981
Eye pain 121.43 57.45 26 386 2305 1744064
Uveitis 79.49 57.45 16 396 1035 1745334
Foreign body sensation in eyes 77.06 57.45 12 400 171 1746198
Visual acuity reduced 72.98 57.45 19 393 3869 1742500
Corneal oedema 69.88 57.45 12 400 321 1746048
Visual impairment 68.56 57.45 20 392 6198 1740171
Glaucoma 66.88 57.45 14 398 1097 1745272
Punctate keratitis 59.83 57.45 9 403 100 1746269

Pharmacologic Action:

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)

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

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

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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:

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

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
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