betaxolol

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Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	0.45 mg/mL	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	15 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	2.17 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	85 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution)	4.80 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	3.40 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.40 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	17 hours	Lombardo F, Berellini G, Obach RS

Property	Description	Value	Unit	Confidence	Similarity
kinase-safety-class	ACVR2A,ACVR2B,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,EIF2AK3,EPHB4,ERBB2,GRK2,IKBKB,ITK,JAK3,MAP2K6,MAPK7,NTRK2,PDK2,PDK4,PRKDC,TEK,TGFBR1,ZAP70	26
kinase-selectivity-class	CDK4,EIF2AK3	2
mdck-mdr1-bcrp-efflux	MDCK-MDR1-BCRP efflux ratio	0.610		High	1
pfas-class	PFAS structural alert (1 = True, 0 = False)	0
pld-class	Phospholipidosis risk class (1 = positive, 0 = negative)	1		Moderate	0.68
rat-kpuu-brain	Rat brain Kpuu	0.476	%	High	1

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
Stevens-Johnson syndrome	86.90	25.30	36	3764	29340	90595307
Hyperaesthesia	84.17	25.30	27	3773	10675	90613972
Dental restoration failure	71.00	25.30	15	3785	1149	90623498
Limb injury	65.11	25.30	30	3770	31478	90593169
Nasal discharge discolouration	62.49	25.30	16	3784	2837	90621810
Angioplasty	61.98	25.30	14	3786	1463	90623184
Status epilepticus	58.75	25.30	24	3776	18850	90605797
Fall	57.89	25.30	85	3715	481725	90142922
Peripheral vascular disorder	53.75	25.30	17	3783	6414	90618233
Transient ischaemic attack	53.35	25.30	29	3771	43147	90581500
Phlebitis	51.34	25.30	17	3783	7413	90617234
Epigastric discomfort	51.03	25.30	17	3783	7551	90617096
Fungal infection	50.90	25.30	28	3772	42633	90582014
Crepitations	48.42	25.30	17	3783	8835	90615812
Catheter site pain	47.68	25.30	15	3785	5564	90619083
Choking	46.89	25.30	18	3782	12015	90612632
Haemorrhage	45.37	25.30	31	3769	69338	90555309
Encephalitis	44.62	25.30	17	3783	11117	90613530
Glaucoma	40.50	25.30	19	3781	20736	90603911
Sopor	40.34	25.30	20	3780	24624	90600023
Coma	39.49	25.30	29	3771	72603	90552044
Skin laceration	39.30	25.30	20	3780	26015	90598632
Urinary retention	37.54	25.30	22	3778	37722	90586925
Eye irritation	36.98	25.30	21	3779	33957	90590690
Pulmonary congestion	35.50	25.30	17	3783	19416	90605231
Middle insomnia	34.75	25.30	16	3784	16735	90607912
Sputum discoloured	34.72	25.30	17	3783	20374	90604273
Coronary artery disease	34.50	25.30	20	3780	33603	90591044
Bradycardia	33.69	25.30	28	3772	83819	90540828
Cardiac failure congestive	33.66	25.30	30	3770	98664	90525983
Panic attack	33.37	25.30	18	3782	26347	90598300
Poor venous access	32.41	25.30	16	3784	19511	90605136
Ischaemic stroke	30.49	25.30	16	3784	22150	90602497
Blindness	30.48	25.30	17	3783	26551	90598096
Vascular resistance systemic	30.09	25.30	4	3796	15	90624632
Acute myocardial infarction	28.68	25.30	18	3782	34872	90589775
Acquired haemophilia	28.41	25.30	7	3793	1062	90623585
Acute kidney injury	28.01	25.30	49	3751	320338	90304309
Pulmonary oedema	25.49	25.30	21	3779	62059	90562588

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
Hypersensitivity	114.04	23.70	51	1204	72319	42547761
Cardiac disorder	94.99	23.70	40	1215	48892	42571188
Splenic rupture	48.76	23.70	11	1244	1636	42618444
Gastrointestinal ischaemia	39.41	23.70	7	1248	308	42619772
Wrong drug	36.62	23.70	6	1249	162	42619918
Shock haemorrhagic	24.01	23.70	11	1244	16231	42603849

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
Hyperaesthesia	75.28	23.03	27	4683	14700	110569889
Dental restoration failure	70.98	23.03	15	4695	1132	110583457
Limb injury	65.51	23.03	32	4678	37604	110546985
Angioplasty	62.89	23.03	15	4695	1956	110582633
Fall	62.15	23.03	100	4610	603382	109981207
Nasal discharge discolouration	60.41	23.03	16	4694	3185	110581404
Cardiac disorder	58.83	23.03	38	4672	76242	110508347
Haemorrhage	53.88	23.03	41	4669	106651	110477938
Peripheral vascular disorder	52.55	23.03	18	4692	8558	110576031
Transient ischaemic attack	52.13	23.03	33	4677	63949	110520640
Crepitations	48.44	23.03	18	4692	10817	110573772
Phlebitis	46.40	23.03	17	4693	9824	110574765
Fungal infection	45.92	23.03	28	4682	50778	110533811
Catheter site pain	45.31	23.03	15	4695	6431	110578158
Epigastric discomfort	44.09	23.03	16	4694	8999	110575590
Choking	42.64	23.03	18	4692	15092	110569497
Bradycardia	42.33	23.03	42	4668	155475	110429114
Splenic rupture	39.55	23.03	11	4699	2626	110581963
Glaucoma	38.73	23.03	19	4691	22498	110562091
Panic attack	37.00	23.03	20	4690	28920	110555669
Hypersensitivity	36.20	23.03	63	4647	403935	110180654
Encephalitis	35.74	23.03	17	4693	18822	110565767
Sputum discoloured	34.86	23.03	19	4691	27926	110556663
Eye irritation	34.30	23.03	20	4690	33432	110551157
Gastrointestinal ischaemia	33.04	23.03	7	4703	534	110584055
Stevens-Johnson syndrome	32.82	23.03	22	4688	46879	110537710
Status epilepticus	32.70	23.03	19	4691	31552	110553037
Coma	32.37	23.03	32	4678	117837	110466752
Middle insomnia	31.43	23.03	16	4694	20486	110564103
Pulmonary congestion	30.39	23.03	18	4692	30948	110553641
Vascular resistance systemic	30.03	23.03	4	4706	15	110584574
Cardiac failure congestive	29.13	23.03	34	4676	150966	110433623
Poor venous access	28.74	23.03	16	4694	24506	110560083
Wrong drug	28.49	23.03	6	4704	445	110584144
Ischaemic stroke	28.02	23.03	19	4691	41244	110543345
Urinary retention	27.11	23.03	23	4687	69660	110514929
Skin laceration	26.46	23.03	17	4693	33736	110550853
Sopor	25.23	23.03	17	4693	36529	110548060

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betaxolol 🐶 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	C07AB05	CARDIOVASCULAR SYSTEM BETA BLOCKING AGENTS BETA BLOCKING AGENTS Beta blocking agents, selective
ATC	S01ED02	SENSORY ORGANS OPHTHALMOLOGICALS ANTIGLAUCOMA PREPARATIONS AND MIOTICS Beta blocking agents
ATC	S01ED52	SENSORY ORGANS OPHTHALMOLOGICALS ANTIGLAUCOMA PREPARATIONS AND MIOTICS Beta blocking agents
FDA MoA	N0000000161	Adrenergic beta-Antagonists
FDA EPC	N0000175556	beta-Adrenergic Blocker
CHEBI has role	CHEBI:35530	β-adrenergic antagonist
CHEBI has role	CHEBI:35554	cardiovascular drug
CHEBI has role	CHEBI:35674	antihypertensive agent
CHEBI has role	CHEBI:39456	antiglaucoma drug
CHEBI has role	CHEBI:66991	sympatholytic agent
MeSH PA	D000319	Adrenergic beta-Antagonists
MeSH PA	D000959	Antihypertensive Agents
MeSH PA	D002317	Cardiovascular Agents
MeSH PA	D013565	Sympatholytics
MeSH PA	D018377	Neurotransmitter Agents
MeSH PA	D018663	Adrenergic Agents
MeSH PA	D018674	Adrenergic Antagonists
MeSH PA	D058671	Adrenergic beta-1 Receptor Antagonists

Disease	Relation	SNOMED_ID	DOID
Ocular hypertension	indication	4210003	DOID:9282
Hypertensive disorder	indication	38341003	DOID:10763
Open-angle glaucoma	indication	84494001	DOID:1067
Malignant glaucoma	off-label use	10100008
Aphakic glaucoma	off-label use	15374009
Secondary glaucoma	off-label use	95717004
Bronchospasm	contraindication	4386001
Psoriasis	contraindication	9014002	DOID:8893
Complete atrioventricular block	contraindication	27885002
Acute cerebrovascular insufficiency	contraindication	29322000
Depressive disorder	contraindication	35489007
Anaphylaxis	contraindication	39579001
Chronic heart failure	contraindication	48447003
Sinus bradycardia	contraindication	49710005
Acute nephropathy	contraindication	58574008
Diabetes mellitus	contraindication	73211009	DOID:9351
Pulmonary emphysema	contraindication	87433001
Cardiogenic shock	contraindication	89138009
Kidney disease	contraindication	90708001	DOID:557
Myasthenia gravis	contraindication	91637004	DOID:437
Second degree atrioventricular block	contraindication	195042002
Decompensated cardiac failure	contraindication	195111005
Asthma	contraindication	195967001	DOID:2841
Heart block	contraindication	233916004
Disease of liver	contraindication	235856003	DOID:409
Hypoglycemic disorder	contraindication	237630007
Raynaud's phenomenon	contraindication	266261006
Pregnancy, function	contraindication	289908002
Pheochromocytoma	contraindication	302835009
Acute exacerbation of asthma	contraindication	708038006

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Beta-1 adrenergic receptor	GPCR	P08588	ADRB1_HUMAN	ANTAGONIST	Kd	8.80	WOMBAT-PK	CHEMBL
Beta-2 adrenergic receptor	GPCR	P07550	ADRB2_HUMAN		Kd	7.20	WOMBAT-PK
Sigma non-opioid intracellular receptor 1	Membrane receptor	Q99720	SGMR1_HUMAN		Ki	6.61	CHEMBL
Transmembrane protein 97	Enzyme	Q5BJF2	TMM97_HUMAN		Ki	5.78	CHEMBL
Beta-2 adrenergic receptor	GPCR		ADRB2_CAVPO		Kd	6.98	CHEMBL
Beta-2 adrenergic receptor	GPCR		ADRB2_BOVIN		IC50	6.18	CHEMBL
Beta-1 adrenergic receptor	GPCR		ADRB1_RAT		Kd	8.53	CHEMBL
Beta-1 adrenergic receptor	GPCR		B0FL73_CAVPO		Kd	8.76	CHEMBL

ID	Source
4019633	VUID
N0000147726	NUI
D00598	KEGG_DRUG
63659-19-8	SECONDARY_CAS_RN
142144	RXNORM
C0005320	UMLSCUI
CHEBI:3082	CHEBI
CHEMBL423	ChEMBL_ID
CHEMBL1691	ChEMBL_ID
DB00195	DRUGBANK_ID
D015784	MESH_DESCRIPTOR_UI
2369	PUBCHEM_CID
549	IUPHAR_LIGAND_ID
4530	INN_ID
O0ZR1R6RZ2	UNII
31545	MMSL
4280	MMSL
d00176	MMSL
4018588	VANDF
4019633	VANDF
001859	NDDF
004743	NDDF
349900007	SNOMEDCT_US
387195001	SNOMEDCT_US
409276006	SNOMEDCT_US
O0ZR1R6RZ2	INXIGHT DRUGS

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Betoptic S	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0729	SUSPENSION/ DROPS	2.80 mg	OPHTHALMIC	NDA	25 sections
Betaxolol	HUMAN PRESCRIPTION DRUG LABEL	1	10135-623	TABLET, FILM COATED	10 mg	ORAL	ANDA	19 sections
Betaxolol	HUMAN PRESCRIPTION DRUG LABEL	1	10135-624	TABLET, FILM COATED	20 mg	ORAL	ANDA	19 sections
BETAXOLOL HYDROCHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	10702-013	TABLET, COATED	10 mg	ORAL	ANDA	12 sections
BETAXOLOL HYDROCHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	10702-014	TABLET, COATED	20 mg	ORAL	ANDA	12 sections
Betaxolol	HUMAN PRESCRIPTION DRUG LABEL	1	17478-705	SOLUTION/ DROPS	5 mg	OPHTHALMIC	ANDA	19 sections
Betaxolol	HUMAN PRESCRIPTION DRUG LABEL	1	24658-700	TABLET, FILM COATED	10 mg	ORAL	ANDA	17 sections
Betaxolol	HUMAN PRESCRIPTION DRUG LABEL	1	24658-701	TABLET, FILM COATED	20 mg	ORAL	ANDA	17 sections
Betaxolol	HUMAN PRESCRIPTION DRUG LABEL	1	42806-038	TABLET, FILM COATED	10 mg	ORAL	ANDA	17 sections
Betaxolol	HUMAN PRESCRIPTION DRUG LABEL	1	42806-039	TABLET, FILM COATED	20 mg	ORAL	ANDA	17 sections
Betaxolol	HUMAN PRESCRIPTION DRUG LABEL	1	54868-4932	TABLET, FILM COATED	10 mg	ORAL	ANDA	17 sections
Betaxolol Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	61314-245	SOLUTION/ DROPS	5.60 mg	OPHTHALMIC	NDA authorized generic	19 sections