betaxolol ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
beta-adrenoreceptor antagonists 356 63659-18-7

Description:

MoleculeDescription

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:

DoseUnitRoute
20 mg O

ADMET properties:

PropertyValueReference
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 ยตM/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

Approvals:

DateAgencyCompanyOrphan
Aug. 30, 1985 FDA ALCON

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
Limb injury 57.97 25.12 25 2335 20225 50582539
Stevens-Johnson syndrome 56.25 25.12 25 2335 21727 50581037
Hyperaesthesia 48.00 25.12 17 2343 8156 50594608
Transient ischaemic attack 46.92 25.12 25 2335 32185 50570579
Fall 46.75 25.12 67 2293 334865 50267899
Angioplasty 46.68 25.12 11 2349 1244 50601520
Haemorrhage 39.95 25.12 27 2333 53414 50549350
Peripheral vascular disorder 38.40 25.12 13 2347 5454 50597310
Crepitations 36.76 25.12 13 2347 6206 50596558
Choking 36.34 25.12 14 2346 8484 50594280
Acquired haemophilia 34.03 25.12 8 2352 895 50601869
Bradycardia 33.22 25.12 26 2334 64400 50538364
Glaucoma 31.09 25.12 15 2345 15671 50587093
Status epilepticus 30.19 25.12 14 2346 13392 50589372
Fungal infection 29.46 25.12 18 2342 29947 50572817
Urinary retention 29.04 25.12 17 2343 26173 50576591
Asthma 27.74 25.12 27 2333 89310 50513454
Cardiac failure congestive 27.13 25.12 26 2334 84356 50518408
Sputum discoloured 27.12 25.12 13 2347 13382 50589382
Low density lipoprotein increased 26.65 25.12 10 2350 5636 50597128
Pulmonary congestion 25.52 25.12 13 2347 15234 50587530

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
Wrong drug 41.01 26.56 6 823 79 29573619
Splenic rupture 34.36 26.56 8 821 1438 29572260

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
Limb injury 63.06 20.60 28 3081 23477 64472146
Fall 54.04 20.60 82 3027 416744 64078879
Transient ischaemic attack 48.98 20.60 29 3080 44153 64451470
Angioplasty 48.05 20.60 12 3097 1673 64493950
Haemorrhage 44.26 20.60 34 3075 79317 64416306
Hyperaesthesia 44.07 20.60 17 3092 9997 64485626
Peripheral vascular disorder 38.02 20.60 14 3095 7247 64488376
Crepitations 36.85 20.60 14 3095 7901 64487722
Wound 36.70 20.60 30 3079 76447 64419176
Bradycardia 36.21 20.60 36 3073 118183 64377440
Choking 32.97 20.60 14 3095 10524 64485099
Wrong drug 31.58 20.60 6 3103 232 64495391
Asthma 31.01 20.60 30 3079 95195 64400428
Glaucoma 30.02 20.60 15 3094 16333 64479290
Acquired haemophilia 29.12 20.60 8 3101 1612 64494011
Sputum discoloured 28.76 20.60 15 3094 17841 64477782
Fungal infection 26.70 20.60 18 3091 34233 64461390
Splenic rupture 26.64 20.60 8 3101 2211 64493412
Low density lipoprotein increased 23.27 20.60 10 3099 7730 64487893
Cardiac failure congestive 23.23 20.60 30 3079 130550 64365073
Pulmonary congestion 22.16 20.60 14 3095 23866 64471757
Urinary retention 20.89 20.60 18 3091 49183 64446440

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
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 beta-adrenergic blockers
CHEBI has role CHEBI:35674 antihypertensive drugs
CHEBI has role CHEBI:66991 sympatholytic drug
MeSH PA D018663 Adrenergic Agents
MeSH PA D018674 Adrenergic Antagonists
MeSH PA D058671 Adrenergic beta-1 Receptor Antagonists
MeSH PA D000319 Adrenergic beta-Antagonists
MeSH PA D000959 Antihypertensive Agents
MeSH PA D002317 Cardiovascular Agents
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018373 Peripheral Nervous System Agents
MeSH PA D013565 Sympatholytics

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

DiseaseRelationSNOMED_IDDOID
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




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.19 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
Beta-1 adrenergic receptor GPCR ANTAGONIST Kd 8.80 WOMBAT-PK CHEMBL
Beta-2 adrenergic receptor GPCR Kd 7.20 WOMBAT-PK
Beta-2 adrenergic receptor GPCR Kd 6.98 CHEMBL
Beta-2 adrenergic receptor GPCR IC50 6.18 CHEMBL
Beta-1 adrenergic receptor GPCR Kd 8.53 CHEMBL
Beta-1 adrenergic receptor GPCR Kd 8.76 CHEMBL

External reference:

IDSource
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
001859 NDDF
004743 NDDF
349900007 SNOMEDCT_US
387195001 SNOMEDCT_US
409276006 SNOMEDCT_US
4018588 VANDF
4019633 VANDF

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Betoptic S HUMAN PRESCRIPTION DRUG LABEL 1 0065-0246 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 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
Betaxolol HUMAN PRESCRIPTION DRUG LABEL 1 60429-754 TABLET, FILM COATED 20 mg ORAL ANDA 12 sections
Betaxolol Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 61314-245 SOLUTION/ DROPS 5.60 mg OPHTHALMIC NDA authorized generic 19 sections