brinzolamide 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | 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

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2B,AXL,BRAF,BTK,CAMK2D,CDK5,CDK9,DYRK1B,EIF2AK3,ERBB2,GRK2,ITK,MAP3K21,MAPK7,MAPKAPK2,NTRK2,PDK1,PDK2,PDK4,PIK3CB,PIK3CD,PRKDC,STK33,TEK 24
kinase-selectivity-class AXL,GRK2,MAP2K6,PDK1,TEK 5
pfas-class PFAS structural alert (1 = True, 0 = False) 0

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
Eye irritation 231.25 20.55 91 7200 33887 90587269
Intraocular pressure increased 215.48 20.55 59 7232 7034 90614122
Treatment failure 201.44 20.55 178 7113 303750 90317406
Toxic epidermal necrolysis 159.70 20.55 69 7222 32459 90588697
Eye pain 142.50 20.55 70 7221 44098 90577058
Glaucoma 121.80 20.55 50 7241 20705 90600451
Epidermal necrosis 112.05 20.55 28 7263 2333 90618823
Rash papular 102.56 20.55 44 7247 20311 90600845
Ocular hyperaemia 95.55 20.55 49 7242 33749 90587407
Haemoglobin decreased 95.44 20.55 89 7202 161867 90459289
Visual acuity reduced 81.17 20.55 39 7252 23371 90597785
Blindness 73.59 20.55 38 7253 26530 90594626
Conjunctival hyperaemia 71.92 20.55 21 7270 3148 90618008
Hyperaesthesia 66.94 20.55 27 7264 10675 90610481
Cataract 65.82 20.55 51 7240 72041 90549115
Corneal opacity 64.91 20.55 15 7276 896 90620260
Vision blurred 63.73 20.55 60 7231 110233 90510923
Bradycardia 63.15 20.55 53 7238 83794 90537362
Dental restoration failure 61.25 20.55 15 7276 1149 90620007
Punctate keratitis 56.15 20.55 13 7278 783 90620373
Rash erythematous 54.99 20.55 44 7247 65060 90556096
Encephalitis 52.58 20.55 23 7268 11111 90610045
Nasal discharge discolouration 52.16 20.55 16 7275 2837 90618319
Visual impairment 49.42 20.55 57 7234 132308 90488848
Wound haemorrhage 47.87 20.55 15 7276 2852 90618304
Floppy iris syndrome 45.64 20.55 8 7283 114 90621042
Corneal oedema 44.92 20.55 13 7278 1888 90619268
Foreign body sensation in eyes 41.79 20.55 14 7277 3286 90617870
Device deposit issue 41.12 20.55 6 7285 23 90621133
Phlebitis 40.53 20.55 17 7274 7413 90613743
Product container issue 38.89 20.55 12 7279 2169 90618987
Catheter site pain 38.10 20.55 15 7276 5564 90615592
Eye disorder 37.96 20.55 25 7266 27365 90593791
Ulcerative keratitis 37.29 20.55 13 7278 3440 90617716
Epigastric discomfort 36.93 20.55 16 7275 7552 90613604
Visual field defect 34.47 20.55 15 7276 7151 90614005
Fungal infection 34.25 20.55 28 7263 42633 90578523
Hypotonia 33.53 20.55 17 7274 11409 90609747
Middle insomnia 32.65 20.55 19 7272 16732 90604424
Corneal disorder 31.26 20.55 10 7281 2032 90619124
Ocular discomfort 29.56 20.55 13 7278 6357 90614799
Ulcer 29.42 20.55 23 7268 32859 90588297
Macular oedema 29.37 20.55 12 7279 4897 90616259
Eye discharge 29.35 20.55 14 7277 8244 90612912
Product delivery mechanism issue 28.94 20.55 7 7284 509 90620647
Visual acuity reduced transiently 28.79 20.55 6 7285 221 90620935
Intraocular pressure test abnormal 28.76 20.55 6 7285 222 90620934
Endophthalmitis 26.50 20.55 11 7280 4674 90616482
Eye pruritus 25.31 20.55 20 7271 29007 90592149
Duodenal ulcer haemorrhage 25.22 20.55 9 7282 2547 90618609
Poor venous access 25.07 20.55 17 7274 19510 90601646
Keratomileusis 24.08 20.55 5 7286 181 90620975
Short stature 23.88 20.55 7 7284 1063 90620093
Dry eye 23.39 20.55 26 7265 57905 90563251
Deep anterior chamber of the eye 23.21 20.55 3 7288 3 90621153
Erythema of eyelid 23.03 20.55 9 7282 3274 90617882
Conjunctival scar 23.02 20.55 4 7287 54 90621102
Eye swelling 22.98 20.55 19 7272 29367 90591789
Panic attack 22.63 20.55 18 7273 26347 90594809
Small intestinal haemorrhage 22.42 20.55 8 7283 2263 90618893
Iridocyclitis 22.08 20.55 9 7282 3652 90617504
Dyspnoea 21.86 20.55 133 7158 880822 89740334
Heart rate decreased 21.57 20.55 24 7267 53481 90567675
Oral mucosal discolouration 20.71 20.55 5 7286 361 90620795

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 242.82 20.43 115 3592 62509 42555119
Intraocular pressure increased 212.19 20.43 58 3649 6375 42611253
Eye irritation 84.03 20.43 33 3674 11285 42606343
Visual acuity reduced 70.09 20.43 33 3674 17517 42600111
Corneal oedema 60.61 20.43 16 3691 1532 42616096
Eye pain 52.95 20.43 27 3680 17003 42600625
Ocular hyperaemia 48.73 20.43 25 3682 15938 42601690
Foreign body sensation in eyes 42.85 20.43 11 3696 944 42616684
Vision blurred 42.33 20.43 36 3671 53663 42563965
Corneal disorder 41.72 20.43 11 3696 1048 42616580
Corneal opacity 41.60 20.43 10 3697 655 42616973
Punctate keratitis 40.17 20.43 9 3698 432 42617196
Corneal erosion 38.18 20.43 7 3700 120 42617508
Glaucoma 37.57 20.43 17 3690 8231 42609397
Ureteric injury 37.04 20.43 6 3701 47 42617581
Pyelitis 36.65 20.43 7 3700 151 42617477
Conjunctival hyperaemia 33.55 20.43 12 3695 3164 42614464
Corneal infection 32.97 20.43 5 3702 24 42617604
Intraocular pressure decreased 26.94 20.43 5 3702 92 42617536
Iridocyclitis 25.82 20.43 9 3698 2202 42615426
Cataract 25.08 20.43 21 3686 30583 42587045
Hypersensitivity 24.80 20.43 31 3676 72339 42545289
Cystoid macular oedema 23.59 20.43 7 3700 1026 42616602
Choroidal detachment 23.15 20.43 6 3701 534 42617094
Visual impairment 22.52 20.43 23 3684 43090 42574538
Visual field defect 21.92 20.43 10 3697 4928 42612700
Hyphaema 21.44 20.43 6 3701 714 42616914
Pyroglutamate increased 21.06 20.43 5 3702 310 42617318
Erythema of eyelid 21.00 20.43 7 3700 1496 42616132
Myalgia 20.76 20.43 33 3674 96047 42521581

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 315.69 18.98 89 9649 10787 110568774
Eye pain 150.75 18.98 78 9660 50021 110529540
Eye irritation 114.97 18.98 57 9681 33395 110546166
Toxic epidermal necrolysis 114.75 18.98 68 9670 56659 110522902
Visual acuity reduced 111.10 18.98 55 9683 32118 110547443
Epidermal necrosis 102.42 18.98 28 9710 3022 110576539
Blindness 101.90 18.98 54 9684 36305 110543256
Vision blurred 93.68 18.98 83 9655 128939 110450622
Glaucoma 91.37 18.98 43 9695 22474 110557087
Rash papular 85.89 18.98 44 9694 27595 110551966
Conjunctival hyperaemia 84.52 18.98 28 9710 5803 110573758
Corneal oedema 83.18 18.98 24 9714 3149 110576412
Punctate keratitis 74.54 18.98 18 9720 1186 110578375
Ocular discomfort 74.10 18.98 28 9710 8505 110571056
Haemoglobin decreased 74.08 18.98 100 9638 248627 110330934
Corneal opacity 73.86 18.98 18 9720 1233 110578328
Ocular hyperaemia 71.44 18.98 44 9694 39242 110540319
Amaurosis fugax 71.32 18.98 20 9718 2370 110577191
Corneal disorder 60.83 18.98 18 9720 2579 110576982
Dental restoration failure 60.12 18.98 15 9723 1132 110578429
Visual field defect 59.39 18.98 25 9713 10047 110569514
Bradycardia 56.43 18.98 69 9669 155448 110424113
Hyperaesthesia 56.30 18.98 27 9711 14700 110564861
Haemorrhagic stroke 51.86 18.98 25 9713 13764 110565797
Cataract 51.51 18.98 48 9690 79437 110500124
Nasal discharge discolouration 48.92 18.98 16 9722 3185 110576376
Rash erythematous 46.56 18.98 46 9692 81786 110497775
Iridocyclitis 44.27 18.98 17 9721 5391 110574170
Endophthalmitis 40.65 18.98 18 9720 8169 110571392
Wound haemorrhage 39.16 18.98 15 9723 4723 110574838
Dyspnoea 38.19 18.98 195 9543 1106677 109472884
Photophobia 37.28 18.98 25 9713 25746 110553815
Encephalitis 36.55 18.98 22 9716 18817 110560744
Floppy iris syndrome 36.42 18.98 8 9730 346 110579215
Urinary tract disorder 36.11 18.98 15 9723 5829 110573732
Catheter site pain 34.69 18.98 15 9723 6431 110573130
Phlebitis 34.48 18.98 17 9721 9824 110569737
Intraocular pressure test abnormal 34.22 18.98 7 9731 214 110579347
Corneal erosion 34.01 18.98 8 9730 471 110579090
Macular oedema 33.58 18.98 15 9723 6951 110572610
Generalised oedema 33.34 18.98 25 9713 30679 110548882
Epigastric discomfort 32.86 18.98 16 9722 8999 110570562
Corneal infection 32.16 18.98 6 9732 112 110579449
Hypotonia 32.14 18.98 19 9719 15726 110563835
Ureteric injury 31.01 18.98 6 9732 137 110579424
Syncope 30.72 18.98 60 9678 202476 110377085
Device deposit issue 30.53 18.98 6 9732 149 110579412
Visual impairment 29.71 18.98 47 9691 134381 110445180
Pyelitis 29.61 18.98 7 9731 421 110579140
Foreign body sensation in eyes 29.16 18.98 11 9727 3323 110576238
Somnolence 28.13 18.98 73 9665 297376 110282185
Fall 27.90 18.98 116 9622 603366 109976195
Fungal infection 27.85 18.98 28 9710 50778 110528783
Haematemesis 27.79 18.98 30 9708 59078 110520483
Middle insomnia 27.54 18.98 19 9719 20483 110559078
Erythema of eyelid 27.44 18.98 11 9727 3904 110575657
Visual acuity reduced transiently 26.20 18.98 6 9732 314 110579247
Conjunctival scar 25.63 18.98 6 9732 346 110579215
Dizziness 25.39 18.98 125 9613 698068 109881493
Ulcerative keratitis 25.35 18.98 11 9727 4755 110574806
Keratomileusis 24.16 18.98 5 9733 162 110579399
Head discomfort 24.10 18.98 17 9721 18983 110560578
Flat anterior chamber of eye 24.04 18.98 5 9733 166 110579395
Intraocular pressure decreased 23.49 18.98 5 9733 186 110579375
Hyphaema 23.02 18.98 7 9731 1100 110578461
Ulcer 22.25 18.98 23 9715 43093 110536468
Asthenia 22.01 18.98 119 9619 688880 109890681
Iris adhesions 21.89 18.98 6 9732 653 110578908
Deep anterior chamber of the eye 21.72 18.98 3 9735 6 110579555
Presyncope 21.57 18.98 24 9714 48863 110530698
Choroidal detachment 20.95 18.98 6 9732 766 110578795
Coma 20.45 18.98 37 9701 117832 110461729
Corneal exfoliation 20.39 18.98 3 9735 11 110579550
Poor venous access 20.25 18.98 17 9721 24505 110555056
Oral mucosal discolouration 20.11 18.98 5 9733 372 110579189
Corneal epithelium defect 19.96 18.98 6 9732 906 110578655
Panic attack 19.75 18.98 18 9720 28922 110550639
Xerophthalmia 19.72 18.98 6 9732 945 110578616
Small intestinal haemorrhage 19.28 18.98 9 9729 4609 110574952

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 (carbonic anhydrase) inhibitor
CHEBI has role CHEBI:35674 antihypertensive agent
CHEBI has role CHEBI:39456 antiglaucoma drug
MeSH PA D002257 Carbonic Anhydrase Inhibitors
MeSH PA D004791 Enzyme Inhibitors

Related Drugs by ATC class:

S01EC Carbonic anhydrase inhibitors 4 drugs
acetazolamidedichlorphenamidedorzolamidemethazolamide

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 Enzyme Ki 6.93 CHEMBL
Carbonic anhydrase 2 Enzyme Ki 6.90 CHEMBL
Carbonic anhydrase Enzyme Ki 7.50 CHEMBL
Carbonic anhydrase, alpha family Enzyme 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
9451Z89515 INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
SIMBRINZA HUMAN PRESCRIPTION DRUG LABEL 2 0065-4147 SUSPENSION/ DROPS 10 mg OPHTHALMIC NDA 25 sections
BRINZOLAMIDE HUMAN PRESCRIPTION DRUG LABEL 1 0574-4012 SUSPENSION/ DROPS 10 mg OPHTHALMIC ANDA 25 sections
Brinzolamide HUMAN PRESCRIPTION DRUG LABEL 1 0591-2127 SUSPENSION/ DROPS 10 mg OPHTHALMIC ANDA 26 sections
Brinzolamide HUMAN PRESCRIPTION DRUG LABEL 1 0781-6014 SUSPENSION/ DROPS 10 mg OPHTHALMIC NDA authorized generic 25 sections
BRINZOLAMIDE HUMAN PRESCRIPTION DRUG LABEL 1 24208-464 SUSPENSION/ DROPS 10 mg OPHTHALMIC ANDA 25 sections
Azopt HUMAN PRESCRIPTION DRUG LABEL 1 66758-085 SUSPENSION/ DROPS 10 mg OPHTHALMIC NDA 25 sections
BRINZOLAMIDE HUMAN PRESCRIPTION DRUG LABEL 1 68682-464 SUSPENSION/ DROPS 10 mg OPHTHALMIC ANDA 24 sections
BRINZOLAMIDE HUMAN PRESCRIPTION DRUG LABEL 1 72162-2201 SUSPENSION/ DROPS 10 mg OPHTHALMIC ANDA 25 sections