brinzolamide

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Property	Description	Value
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

Date	Agency	Company
April 1, 1998	FDA	ALCON PHARMS LTD
Oct. 8, 2002	PMDA	ALCON JAPAN
March 9, 2000	EMA	Novartis Europharm Limited

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
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

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	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

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	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

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

Description:

Drug dosage:

ADMET properties:

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Approvals:

FDA Adverse Event Reporting System (Female)

FDA Adverse Event Reporting System (Male)

FDA Adverse Event Reporting System (Geriatric)

FDA Adverse Event Reporting System (Pediatric)

Pharmacologic Action:

Related Drugs by ATC class:

Drug Use | Suggest Off label Use Form| |View source of the data|

🐶 Veterinary Drug Use

🐶 Veterinary products

Acid dissociation constants calculated using MoKa v3.0.0

Orange Book patent data (new drug applications)

Orange Book exclusivity data (new drug applications)

Bioactivity Summary:

External reference:

Pharmaceutical products:

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 (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

Disease	Relation	SNOMED_ID	DOID
Ocular hypertension	indication	4210003	DOID:9282
Open-angle glaucoma	indication	84494001	DOID:1067
Acute nephropathy	contraindication	58574008

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	Enzyme		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	Enzyme		Q31FD6_HYDCU		Ki	8.38	CHEMBL
Carbonate dehydratase	Enzyme		B2V8E3_SULSY		Ki	7.91	CHEMBL

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
9451Z89515	INXIGHT DRUGS

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
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

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	8.31	acidic
pKa2	7.75	Basic