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
March 9, 2000 EMA Novartis Europharm Limited

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 236.65 21.58 178 6062 198865 63283917
Eye irritation 222.55 21.58 83 6157 21888 63460894
Intraocular pressure increased 194.58 21.58 55 6185 6023 63476759
Eye pain 105.65 21.58 56 6184 33798 63448984
Ocular hyperaemia 91.12 21.58 46 6194 25098 63457684
Glaucoma 84.75 21.58 40 6200 18865 63463917
Blindness 70.81 21.58 37 6203 21662 63461120
Hyperaesthesia 65.22 21.58 27 6213 9331 63473451
Visual acuity reduced 56.70 21.58 32 6208 21794 63460988
Cataract 56.55 21.58 46 6194 57007 63425775
Dental restoration failure 55.72 21.58 14 6226 973 63481809
Vision blurred 55.37 21.58 56 6184 91868 63390914
Bradycardia 50.41 21.58 48 6192 73179 63409603
Corneal opacity 49.31 21.58 12 6228 731 63482051
Nasal discharge discolouration 48.36 21.58 15 6225 2256 63480526
Conjunctival hyperaemia 47.67 21.58 15 6225 2364 63480418
Toxic epidermal necrolysis 44.74 21.58 29 6211 25305 63457477
Foreign body sensation in eyes 44.41 21.58 14 6226 2220 63480562
Floppy iris syndrome 44.04 21.58 8 6232 114 63482668
Visual impairment 41.19 21.58 46 6194 84400 63398382
Punctate keratitis 41.06 21.58 10 6230 611 63482171
Encephalitis 40.43 21.58 19 6221 8861 63473921
Product container issue 38.84 21.58 12 6228 1781 63481001
Device deposit issue 38.79 21.58 6 6234 29 63482753
Wound haemorrhage 38.77 21.58 13 6227 2503 63480279
Phlebitis 35.67 21.58 16 6224 6708 63476074
Catheter site pain 34.14 21.58 14 6226 4721 63478061
Hypotonia 33.65 21.58 17 6223 9268 63473514
Fungal infection 32.92 21.58 28 6212 36846 63445936
Visual field defect 32.86 21.58 15 6225 6546 63476236
Epigastric discomfort 32.39 21.58 15 6225 6765 63476017
Corneal oedema 32.37 21.58 10 6230 1483 63481299
Middle insomnia 31.38 21.58 18 6222 12625 63470157
Eye discharge 30.81 21.58 14 6226 6049 63476733
Eye disorder 30.62 21.58 22 6218 22663 63460119
Corneal disorder 30.46 21.58 10 6230 1804 63480978
Ulcerative keratitis 30.21 21.58 11 6229 2699 63480083
Product delivery mechanism issue 29.82 21.58 7 6233 365 63482417
Visual acuity reduced transiently 29.36 21.58 6 6234 163 63482619
Ulcer 27.87 21.58 22 6218 26085 63456697
Eye pruritus 27.27 21.58 19 6221 18652 63464130
Endophthalmitis 27.19 21.58 11 6229 3581 63479201
Poor venous access 23.85 21.58 16 6224 14769 63468013
Duodenal ulcer haemorrhage 23.78 21.58 9 6231 2458 63480324
Intraocular pressure test abnormal 23.50 21.58 5 6235 166 63482616
Deep anterior chamber of the eye 22.61 21.58 3 6237 3 63482779
Eyelid margin crusting 22.48 21.58 7 6233 1065 63481717
Ocular discomfort 22.22 21.58 10 6230 4223 63478559

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 270.63 20.98 114 2970 46583 34907264
Intraocular pressure increased 183.71 20.98 50 3034 5333 34948514
Eye irritation 77.43 20.98 28 3056 7533 34946314
Corneal oedema 57.68 20.98 15 3069 1336 34952511
Visual acuity reduced 51.03 20.98 26 3058 16123 34937724
Ocular hyperaemia 49.97 20.98 23 3061 11429 34942418
Eye pain 49.42 20.98 24 3060 13438 34940409
Ureteric injury 43.56 20.98 7 3077 51 34953796
Corneal disorder 42.94 20.98 11 3073 923 34952924
Corneal erosion 39.89 20.98 7 3077 91 34953756
Pyelitis 38.59 20.98 7 3077 111 34953736
Foreign body sensation in eyes 36.80 20.98 9 3075 625 34953222
Punctate keratitis 35.78 20.98 8 3076 375 34953472
Glaucoma 33.68 20.98 15 3069 6897 34946950
Vision blurred 32.21 20.98 29 3055 45934 34907913
Intraocular pressure decreased 28.28 20.98 5 3079 68 34953779
Hypersensitivity 25.30 20.98 29 3055 61006 34892841
Conjunctival hyperaemia 24.96 20.98 9 3075 2393 34951454
Visual impairment 23.92 20.98 22 3062 35780 34918067
Myalgia 22.29 20.98 32 3052 84078 34869769
Pyroglutamate increased 21.32 20.98 5 3079 290 34953557

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 279.65 18.27 79 7345 9126 79727838
Eye irritation 105.23 18.27 47 7377 20634 79716330
Visual acuity reduced 86.56 18.27 46 7378 29423 79707541
Eye pain 76.13 18.27 46 7378 37532 79699432
Punctate keratitis 71.88 18.27 17 7407 969 79735995
Ocular hyperaemia 68.94 18.27 39 7385 28167 79708797
Corneal oedema 68.40 18.27 20 7404 2600 79734364
Glaucoma 67.08 18.27 34 7390 19727 79717237
Blindness 63.37 18.27 37 7387 28346 79708618
Corneal disorder 62.07 18.27 18 7406 2273 79734691
Hyperaesthesia 59.68 18.27 27 7397 12195 79724769
Conjunctival hyperaemia 58.14 18.27 20 7404 4393 79732571
Dental restoration failure 56.52 18.27 14 7410 970 79735994
Visual field defect 53.95 18.27 23 7401 9022 79727942
Vision blurred 53.03 18.27 57 7367 105841 79631123
Bradycardia 47.89 18.27 61 7363 135496 79601468
Nasal discharge discolouration 47.61 18.27 15 7409 2506 79734458
Cataract 47.15 18.27 42 7382 62078 79674886
Endophthalmitis 43.89 18.27 18 7406 6410 79730554
Corneal opacity 41.38 18.27 11 7413 1009 79735955
Device deposit issue 37.48 18.27 6 7418 40 79736924
Ureteric injury 36.49 18.27 7 7417 144 79736820
Floppy iris syndrome 35.77 18.27 8 7416 355 79736609
Corneal erosion 35.41 18.27 8 7416 372 79736592
Dyspnoea 35.17 18.27 165 7259 856860 78880104
Catheter site pain 33.10 18.27 14 7410 5382 79731582
Wound haemorrhage 33.07 18.27 13 7411 4148 79732816
Phlebitis 32.33 18.27 16 7408 8814 79728150
Fungal infection 31.22 18.27 28 7396 41720 79695244
Epigastric discomfort 30.99 18.27 15 7409 7881 79729083
Pyelitis 30.77 18.27 7 7417 336 79736628
Encephalitis 29.70 18.27 18 7406 14742 79722222
Toxic epidermal necrolysis 29.64 18.27 28 7396 44553 79692411
Middle insomnia 28.29 18.27 18 7406 16051 79720913
Visual acuity reduced transiently 26.75 18.27 6 7418 270 79736694
Hypotonia 26.68 18.27 16 7408 12854 79724110
Ulcer 26.24 18.27 22 7402 29950 79707014
Foreign body sensation in eyes 25.43 18.27 9 7415 2148 79734816
Intraocular pressure test abnormal 24.66 18.27 5 7419 138 79736826
Visual impairment 24.27 18.27 36 7388 92095 79644869
Ulcerative keratitis 24.06 18.27 10 7414 3679 79733285
Flat anterior chamber of eye 24.04 18.27 5 7419 157 79736807
Iridocyclitis 24.02 18.27 10 7414 3694 79733270
Erythema of eyelid 23.89 18.27 9 7415 2561 79734403
Intraocular pressure decreased 23.46 18.27 5 7419 177 79736787
Medication error 22.82 18.27 30 7394 68612 79668352
Conjunctival scar 22.58 18.27 5 7419 212 79736752
Fall 22.23 18.27 97 7327 487532 79249432
Poor venous access 21.67 18.27 16 7408 18133 79718831
Deep anterior chamber of the eye 21.55 18.27 3 7421 6 79736958
Asthenia 21.24 18.27 99 7325 511590 79225374
Oral mucosal discolouration 20.12 18.27 5 7419 351 79736613
Keratic precipitates 20.02 18.27 5 7419 358 79736606
Corneal infection 19.99 18.27 4 7420 103 79736861
Eye pruritus 19.89 18.27 16 7408 20554 79716410
Small intestinal haemorrhage 19.70 18.27 9 7415 4154 79732810
Hyphaema 19.69 18.27 6 7418 898 79736066
Panic attack 19.61 18.27 17 7407 24199 79712765
Eye discharge 19.36 18.27 10 7414 6024 79730940
Haemoglobin decreased 18.59 18.27 54 7370 222065 79514899

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 | Suggest Off label Use Form| |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
108836002 SNOMEDCT_US
386925003 SNOMEDCT_US
4021097 VANDF
007497 NDDF

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 26 sections
SIMBRINZA HUMAN PRESCRIPTION DRUG LABEL 2 0065-4147 SUSPENSION/ DROPS 10 mg OPHTHALMIC NDA 26 sections
Azopt HUMAN PRESCRIPTION DRUG LABEL 1 0078-0722 SUSPENSION/ DROPS 10 mg OPHTHALMIC NDA 27 sections
Azopt HUMAN PRESCRIPTION DRUG LABEL 1 0078-0722 SUSPENSION/ DROPS 10 mg OPHTHALMIC NDA 27 sections
Azopt HUMAN PRESCRIPTION DRUG LABEL 1 0078-0722 SUSPENSION/ DROPS 10 mg OPHTHALMIC NDA 27 sections
SIMBRINZA HUMAN PRESCRIPTION DRUG LABEL 2 0078-0904 SUSPENSION/ DROPS 10 mg OPHTHALMIC NDA 26 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 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 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