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

Stem definition	Drug id	CAS RN
	396	138890-62-7

Description:

Molecule	Description
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

Molecule

Description

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:

Dose	Unit	Route
0.20	ml	None

ADMET properties:

None

Approvals:

Date	Agency	Company
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 term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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 term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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 term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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:

Source	Code	Description
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|

Disease	Relation	SNOMED_ID	DOID
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 level	Dissociation constant	Type (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:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Carbonic anhydrase 2	Enzyme	P00918	CAH2_HUMAN	INHIBITOR	Ki	9.90	CHEMBL	CHEMBL
Carbonic anhydrase 1	Enzyme	P00915	CAH1_HUMAN		Ki	8.52	CHEMBL
Carbonic anhydrase 4	Enzyme	P22748	CAH4_HUMAN		Ki	5.40	CHEMBL
Carbonic anhydrase 9	Enzyme	Q16790	CAH9_HUMAN		Ki	7.44	CHEMBL
Carbonic anhydrase 12	Enzyme	O43570	CAH12_HUMAN		Ki	8.52	CHEMBL
Carbonic anhydrase 5A, mitochondrial	Enzyme	P35218	CAH5A_HUMAN		Ki	7.30	CHEMBL
Carbonic anhydrase 5B, mitochondrial	Enzyme	Q9Y2D0	CAH5B_HUMAN		Ki	7.52	CHEMBL
Carbonic anhydrase 7	Enzyme	P43166	CAH7_HUMAN		Ki	8.55	CHEMBL
Carbonic anhydrase 6	Enzyme	P23280	CAH6_HUMAN		Ki	9.05	CHEMBL
Carbonic anhydrase 14	Enzyme	Q9ULX7	CAH14_HUMAN		Ki	7.62	CHEMBL
Carbonic anhydrase 13	Enzyme	Q8N1Q1	CAH13_HUMAN		Ki	7.96	CHEMBL
Carbonic anhydrase	Enzyme		CYNT_HELPY		Ki	6.68	CHEMBL
Carbonic anhydrase 13	Enzyme		CAH13_MOUSE		Ki	8	CHEMBL
Carbonic anhydrase 4	Enzyme		CAH4_BOVIN		Ki	7.35	CHEMBL
Carbonic anhydrase 15	Enzyme		CAH15_MOUSE		Ki	7.21	CHEMBL
Carbonic anhydrase	Enzyme		CAN_YEAST		Ki	6.94	CHEMBL
Carbonic anhydrase	Enzyme		CAN_CANAL		Ki	8.52	CHEMBL
Probable transmembrane carbonic anhydrase (Carbonate dehydratase) (Carbonic dehydratase); Transmembrane carbonic anhydrase	Enzyme		P96878_MYCTU		Ki	6.70	CHEMBL
Carbonic anhydrase	Enzyme		Q6FTL6_CANGA		Ki	5.36	CHEMBL
Alpha carbonic anhydrase	Enzyme		B5SU02_9CNID		Ki	7.32	CHEMBL
Carbonic anhydrase	Enzyme		C0IX24_9CNID		Ki	6.77	CHEMBL
Carbonic anhydrase 2	Enzyme		Q3I4V7_CRYNV		Ki	7.06	CHEMBL
Astrosclerin-3	Enzyme		A6YCJ1_9METZ		Ki	6.56	CHEMBL
Beta-carbonic anhydrase 1	Enzyme		MTCA1_MYCTU		Ki	6.08	CHEMBL
Delta carbonic anhydrase	Unclassified		Q5U9J1_THAWE		Ki	6.93	CHEMBL
Carbonic anhydrase 2	Enzyme		MTCA2_MYCTU		Ki	6.90	CHEMBL
Carbonic anhydrase	Enzyme		Q5TU56_ANOGA		Ki	7.50	CHEMBL
Carbonic anhydrase, alpha family	Unclassified		Q31FD6_HYDCU		Ki	8.38	CHEMBL
Carbonate dehydratase	Enzyme		B2V8E3_SULSY		Ki	7.91	CHEMBL

External reference:

ID	Source
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:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
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