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

Stem definition	Drug id	CAS RN
beta-adrenoreceptor antagonists	356	63659-18-7

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: betaxolol (+/-)-Betaxolol betaxolol hydrochloride betaxolol HCl	A cardioselective beta-1-adrenergic antagonist with no partial agonist activity. Molecular weight: 307.43 Formula: C18H29NO3 CLOGP: 2.32 LIPINSKI: 0 HAC: 4 HDO: 2 TPSA: 50.72 ALOGS: -4.01 ROTB: 11 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

betaxolol
(+/-)-Betaxolol
betaxolol hydrochloride
betaxolol HCl

A cardioselective beta-1-adrenergic antagonist with no partial agonist activity.

Molecular weight: 307.43
Formula: C18H29NO3
CLOGP: 2.32
LIPINSKI: 0
HAC: 4
HDO: 2
TPSA: 50.72
ALOGS: -4.01
ROTB: 11

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
20	mg	O

ADMET properties:

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Property	Value	Reference
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
MRTD (Maximum Recommended Therapeutic Daily Dose)	2.17 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
t_half (Half-life)	17 hours	Lombardo F, Berellini G, Obach RS
EoM (Fraction excreted unchanged in urine)	15 %	Benet LZ, Broccatelli F, Oprea TI
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
fu (Fraction unbound in plasma)	0.40 %	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
Aug. 30, 1985	FDA	ALCON

FDA Adverse Event Reporting System (Female)

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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	82.59	27.78	27	3206	9331	63476458
Limb injury	65.65	27.78	30	3203	25447	63460342
Dental restoration failure	64.90	27.78	14	3219	973	63484816
Angioplasty	60.10	27.78	14	3219	1378	63484411
Nasal discharge discolouration	58.13	27.78	15	3218	2256	63483533
Fall	55.81	27.78	83	3150	392251	63093538
Stevens-Johnson syndrome	53.85	27.78	26	3207	24924	63460865
Transient ischaemic attack	51.73	27.78	29	3204	37724	63448065
Peripheral vascular disorder	51.57	27.78	17	3216	6018	63479771
Fungal infection	49.64	27.78	28	3205	36846	63448943

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FDA Adverse Event Reporting System (Male)

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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	43.49	25.02	26	1094	61009	34894802
Wrong drug	40.21	25.02	6	1114	79	34955732
Splenic rupture	37.94	25.02	9	1111	1532	34954279
Gastrointestinal ischaemia	34.50	25.02	6	1114	214	34955597
Cardiac disorder	27.16	25.02	17	1103	43109	34912702

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FDA Adverse Event Reporting System (Geriatric)

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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	75.19	22.86	27	4082	12195	79728084
Limb injury	67.11	22.86	32	4077	29496	79710783
Dental restoration failure	64.77	22.86	14	4095	970	79739309
Fall	61.16	22.86	98	4011	487531	79252748
Angioplasty	60.90	22.86	15	4094	1848	79738431
Nasal discharge discolouration	56.39	22.86	15	4094	2506	79737773
Haemorrhage	52.71	22.86	41	4068	91077	79649202
Transient ischaemic attack	52.25	22.86	33	4076	52662	79687617
Peripheral vascular disorder	50.36	22.86	18	4091	8012	79732267
Crepitations	46.49	22.86	18	4091	9999	79730280

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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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
CHEBI has role	CHEBI:35530	beta-adrenergic blockers
CHEBI has role	CHEBI:35674	antihypertensive drugs
CHEBI has role	CHEBI:66991	sympatholytic drug
FDA EPC	N0000175556	beta-Adrenergic Blocker
FDA MoA	N0000000161	Adrenergic beta-Antagonists
MeSH PA	D018663	Adrenergic Agents
MeSH PA	D018674	Adrenergic Antagonists

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

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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

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	9.19	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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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
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

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External reference:

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ID	Source
001859	NDDF
004743	NDDF
142144	RXNORM
2369	PUBCHEM_CID
31545	MMSL
349900007	SNOMEDCT_US
387195001	SNOMEDCT_US
4018588	VANDF
4019633	VUID
4019633	VANDF

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
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	HUMAN PRESCRIPTION DRUG LABEL	1	17478-705	SOLUTION/ DROPS	5 mg	OPHTHALMIC	ANDA	19 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	HUMAN PRESCRIPTION DRUG LABEL	1	60429-753	TABLET, FILM COATED	10 mg	ORAL	ANDA	12 sections

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