brinzolamide 🐶 Veterinary Use | 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
Oct. 8, 2002 PMDA ALCON JAPAN

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
Treatment failure 300.64 19.99 178 4689 137459 50462798
Eye irritation 198.31 19.99 71 4796 17069 50583188
Intraocular pressure increased 187.23 19.99 52 4815 5464 50594793
Eye pain 107.08 19.99 53 4814 28396 50571861
Ocular hyperaemia 89.02 19.99 42 4825 20250 50580007
Glaucoma 73.53 19.99 34 4833 15652 50584605
Visual acuity reduced 59.78 19.99 32 4835 20107 50580150
Cataract 58.29 19.99 43 4824 47257 50553000
Vision blurred 57.96 19.99 53 4814 78594 50521663
Corneal opacity 45.88 19.99 11 4856 643 50599614
Visual impairment 44.51 19.99 43 4824 68232 50532025
Blindness 44.51 19.99 25 4842 17244 50583013
Floppy iris syndrome 44.35 19.99 8 4859 112 50600145
Foreign body sensation in eyes 43.26 19.99 13 4854 1798 50598459
Conjunctival hyperaemia 41.47 19.99 13 4854 2069 50598188
Product container issue 37.33 19.99 11 4856 1421 50598836
Punctate keratitis 37.18 19.99 9 4858 548 50599709
Hypotonia 36.15 19.99 17 4850 8117 50592140
Hyperaesthesia 36.07 19.99 17 4850 8156 50592101
Visual field defect 35.01 19.99 15 4852 5764 50594493
Eye discharge 33.37 19.99 14 4853 5109 50595148
Corneal oedema 33.31 19.99 10 4857 1377 50598880
Ulcerative keratitis 32.05 19.99 11 4856 2322 50597935
Eye pruritus 31.90 19.99 18 4849 12516 50587741
Corneal disorder 31.75 19.99 10 4857 1616 50598641
Product delivery mechanism issue 31.07 19.99 7 4860 311 50599946
Visual acuity reduced transiently 30.24 19.99 6 4861 143 50600114
Bradycardia 30.16 19.99 34 4833 64392 50535865
Endophthalmitis 29.65 19.99 11 4856 2905 50597352
Eyelid margin crusting 25.31 19.99 7 4860 721 50599536
Eye disorder 25.25 19.99 18 4849 18721 50581536
Duodenal ulcer haemorrhage 25.11 19.99 9 4858 2157 50598100
Intraocular pressure test abnormal 24.57 19.99 5 4862 136 50600121
Product quality issue 23.09 19.99 21 4846 30837 50569420
Deep anterior chamber of the eye 22.67 19.99 3 4864 3 50600254
Small intestinal haemorrhage 22.33 19.99 8 4859 1915 50598342

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
Treatment failure 289.23 21.78 114 2678 36825 29534910
Intraocular pressure increased 186.19 21.78 50 2742 4739 29566996
Eye irritation 74.61 21.78 26 2766 5872 29565863
Corneal oedema 59.18 21.78 15 2777 1127 29570608
Visual acuity reduced 51.39 21.78 26 2766 14850 29556885
Eye pain 51.29 21.78 24 2768 11571 29560164
Ocular hyperaemia 47.00 21.78 21 2771 9106 29562629
Pyelitis 39.01 21.78 7 2785 97 29571638
Corneal disorder 38.74 21.78 10 2782 807 29570928
Foreign body sensation in eyes 37.42 21.78 9 2783 544 29571191
Punctate keratitis 36.19 21.78 8 2784 332 29571403
Glaucoma 35.10 21.78 15 2777 5842 29565893
Vision blurred 33.90 21.78 29 2763 40147 29531588
Intraocular pressure decreased 28.37 21.78 5 2787 62 29571673
Hypersensitivity 27.11 21.78 29 2763 52874 29518861
Corneal erosion 26.63 21.78 5 2787 90 29571645
Visual impairment 24.14 21.78 21 2771 29687 29542048
Conjunctivitis 21.97 21.78 12 2780 7986 29563749

FDA Adverse Event Reporting System (Geriatric)

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 275.86 19.53 76 5780 8226 64484650
Visual acuity reduced 91.26 19.53 46 5810 27095 64465781
Eye pain 79.11 19.53 44 5812 31581 64461295
Eye irritation 78.22 19.53 35 5821 15821 64477055
Corneal oedema 71.12 19.53 20 5836 2323 64490553
Punctate keratitis 69.17 19.53 16 5840 849 64492027
Ocular hyperaemia 66.48 19.53 35 5821 22529 64470347
Corneal disorder 60.15 19.53 17 5839 2010 64490866
Vision blurred 59.98 19.53 56 5800 90260 64402616
Glaucoma 58.75 19.53 29 5827 16319 64476557
Visual field defect 56.84 19.53 23 5833 8123 64484753
Conjunctival hyperaemia 49.20 19.53 17 5839 3882 64488994
Cataract 48.66 19.53 39 5817 51223 64441653
Endophthalmitis 47.49 19.53 18 5838 5347 64487529
Blindness 42.75 19.53 26 5830 21993 64470883
Corneal opacity 38.11 19.53 10 5846 895 64491981
Floppy iris syndrome 36.38 19.53 8 5848 337 64492539
Hyperaesthesia 33.71 19.53 17 5839 9997 64482879
Pyelitis 32.14 19.53 7 5849 282 64492594
Bradycardia 31.78 19.53 46 5810 118173 64374703
Hypotonia 29.11 19.53 16 5840 11196 64481680
Visual acuity reduced transiently 28.12 19.53 6 5850 219 64492657
Corneal erosion 26.34 19.53 6 5850 297 64492579
Visual impairment 26.27 19.53 33 5823 74044 64418832
Ulcerative keratitis 26.00 19.53 10 5846 3087 64489789
Intraocular pressure test abnormal 25.11 19.53 5 5851 129 64492747
Eye pruritus 24.70 19.53 15 5841 12644 64480232
Flat anterior chamber of eye 24.25 19.53 5 5851 154 64492722
Intraocular pressure decreased 23.98 19.53 5 5851 163 64492713
Foreign body sensation in eyes 23.52 19.53 8 5848 1741 64491135
Iridocyclitis 22.63 19.53 9 5847 3036 64489840
Erythema of eyelid 22.60 19.53 8 5848 1960 64490916
Corneal infection 21.84 19.53 4 5852 65 64492811
Deep anterior chamber of the eye 21.63 19.53 3 5853 6 64492870
Somnolence 21.41 19.53 53 5803 203592 64289284
Eye discharge 21.23 19.53 10 5846 5074 64487802
Keratic precipitates 21.03 19.53 5 5851 299 64492577
Small intestinal haemorrhage 20.63 19.53 9 5847 3824 64489052

FDA Adverse Event Reporting System (Pediatric)

None

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 MoA N0000000235 Carbonic Anhydrase Inhibitors
FDA EPC N0000175517 Carbonic Anhydrase Inhibitor
CHEBI has role CHEBI:23018 EC 4.2.1.1 inhibitor
CHEBI has role CHEBI:39456 antiglaucoma agent
MeSH PA D002257 Carbonic Anhydrase Inhibitors
MeSH PA D004791 Enzyme Inhibitors

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




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

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 1 Enzyme Ki 8.52 CHEMBL
Carbonic anhydrase 4 Enzyme Ki 5.40 CHEMBL
Carbonic anhydrase 9 Enzyme Ki 7.44 CHEMBL
Carbonic anhydrase 12 Enzyme Ki 8.52 CHEMBL
Carbonic anhydrase 5A, mitochondrial Enzyme Ki 7.30 CHEMBL
Carbonic anhydrase 5B, mitochondrial Enzyme Ki 7.52 CHEMBL
Carbonic anhydrase 7 Enzyme Ki 8.55 CHEMBL
Carbonic anhydrase 6 Enzyme Ki 9.05 CHEMBL
Carbonic anhydrase 14 Enzyme Ki 7.62 CHEMBL
Carbonic anhydrase 13 Enzyme Ki 7.96 CHEMBL
Carbonic anhydrase Enzyme Ki 6.68 CHEMBL
Carbonic anhydrase 13 Enzyme Ki 8 CHEMBL
Carbonic anhydrase 4 Enzyme Ki 7.35 CHEMBL
Carbonic anhydrase 15 Enzyme Ki 7.21 CHEMBL
Carbonic anhydrase Enzyme Ki 6.94 CHEMBL
Carbonic anhydrase Enzyme Ki 8.52 CHEMBL
Probable transmembrane carbonic anhydrase (Carbonate dehydratase) (Carbonic dehydratase); Transmembrane carbonic anhydrase Enzyme Ki 6.70 CHEMBL
Carbonic anhydrase Enzyme Ki 5.36 CHEMBL
Alpha carbonic anhydrase Enzyme Ki 7.32 CHEMBL
Carbonic anhydrase Enzyme Ki 6.77 CHEMBL
Carbonic anhydrase 2 Enzyme Ki 7.06 CHEMBL
Astrosclerin-3 Enzyme Ki 6.56 CHEMBL
Beta-carbonic anhydrase 1 Enzyme Ki 6.08 CHEMBL
Delta carbonic anhydrase Unclassified Ki 6.93 CHEMBL
Carbonic anhydrase 2 Enzyme Ki 6.90 CHEMBL
Carbonic anhydrase Enzyme Ki 7.50 CHEMBL
Carbonic anhydrase, alpha family Unclassified Ki 8.38 CHEMBL
Carbonate dehydratase Enzyme Ki 7.91 CHEMBL

External reference:

IDSource
4021097 VUID
N0000148553 NUI
D00652 KEGG_DRUG
194881 RXNORM
C0673966 UMLSCUI
CHEBI:3176 CHEBI
BZ1 PDB_CHEM_ID
CHEMBL220491 ChEMBL_ID
DB01194 DRUGBANK_ID
C111827 MESH_SUPPLEMENTAL_RECORD_UI
68844 PUBCHEM_CID
6797 IUPHAR_LIGAND_ID
7532 INN_ID
9451Z89515 UNII
11638 MMSL
234032 MMSL
4298 MMSL
007497 NDDF
108836002 SNOMEDCT_US
386925003 SNOMEDCT_US
4021097 VANDF

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Azopt HUMAN PRESCRIPTION DRUG LABEL 1 0065-0275 SUSPENSION/ DROPS 10 mg OPHTHALMIC NDA 25 sections
SIMBRINZA HUMAN PRESCRIPTION DRUG LABEL 2 0065-4147 SUSPENSION/ DROPS 10 mg OPHTHALMIC NDA 24 sections
Azopt HUMAN PRESCRIPTION DRUG LABEL 1 0078-0722 SUSPENSION/ DROPS 10 mg OPHTHALMIC NDA 25 sections
SIMBRINZA HUMAN PRESCRIPTION DRUG LABEL 2 0078-0904 SUSPENSION/ DROPS 10 mg OPHTHALMIC NDA 26 sections
Brinzolamide HUMAN PRESCRIPTION DRUG LABEL 1 0591-2127 SUSPENSION/ DROPS 10 mg OPHTHALMIC ANDA 24 sections
Brinzolamide HUMAN PRESCRIPTION DRUG LABEL 1 0781-6014 SUSPENSION/ DROPS 10 mg OPHTHALMIC NDA authorized generic 24 sections
Brinzolamide HUMAN PRESCRIPTION DRUG LABEL 1 0781-6014 SUSPENSION/ DROPS 10 mg OPHTHALMIC NDA authorized generic 24 sections
BRINZOLAMIDE HUMAN PRESCRIPTION DRUG LABEL 1 24208-464 SUSPENSION/ DROPS 10 mg OPHTHALMIC ANDA 24 sections
Brinzolamide HUMAN PRESCRIPTION DRUG LABEL 1 63629-8793 SUSPENSION/ DROPS 10 mg OPHTHALMIC NDA authorized generic 23 sections
Brinzolamide HUMAN PRESCRIPTION DRUG LABEL 1 63629-8793 SUSPENSION/ DROPS 10 mg OPHTHALMIC NDA authorized generic 23 sections
BRINZOLAMIDE HUMAN PRESCRIPTION DRUG LABEL 1 68682-464 SUSPENSION/ DROPS 10 mg OPHTHALMIC ANDA 24 sections