betaxolol 🐶 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 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

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
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
Choking 46.94 27.78 18 3215 9861 63475928
Crepitations 46.80 27.78 17 3216 8023 63477766
Phlebitis 45.89 27.78 16 3217 6708 63479081
Epigastric discomfort 45.76 27.78 16 3217 6764 63479025
Haemorrhage 43.54 27.78 31 3202 60991 63424798
Catheter site pain 43.13 27.78 14 3219 4721 63481068
Eye irritation 38.84 27.78 20 3213 21951 63463838
Glaucoma 38.68 27.78 19 3214 18886 63466903
Encephalitis 38.01 27.78 15 3218 8865 63476924
Urinary retention 35.43 27.78 21 3212 30280 63455509
Sputum discoloured 35.16 27.78 17 3216 16330 63469459
Pulmonary congestion 34.13 27.78 17 3216 17401 63468388
Middle insomnia 32.90 27.78 15 3218 12628 63473161
Acquired haemophilia 32.27 27.78 8 3225 1023 63484766
Muscular weakness 31.77 27.78 35 3198 122318 63363471
Coronary artery disease 31.62 27.78 20 3213 32357 63453432
Poor venous access 30.66 27.78 15 3218 14770 63471019
Cardiac failure congestive 30.37 27.78 30 3203 92403 63393386
Bradycardia 30.27 27.78 27 3206 73200 63412589
Status epilepticus 30.24 27.78 15 3218 15218 63470571
Panic attack 30.16 27.78 17 3216 22314 63463475
Vascular resistance systemic 29.31 27.78 4 3229 15 63485774
Blindness 27.90 27.78 16 3217 21683 63464106

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
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

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
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
Fungal infection 46.09 22.86 28 4081 41720 79698559
Choking 43.19 22.86 18 4091 12083 79728196
Phlebitis 41.45 22.86 16 4093 8814 79731465
Catheter site pain 41.17 22.86 14 4095 5382 79734897
Epigastric discomfort 39.54 22.86 15 4094 7881 79732398
Bradycardia 38.69 22.86 41 4068 135516 79604763
Glaucoma 37.66 22.86 19 4090 19742 79720537
Eye irritation 36.84 22.86 19 4090 20662 79719617
Sputum discoloured 35.94 22.86 19 4090 21724 79718555
Panic attack 34.03 22.86 19 4090 24197 79716082
Wound 31.14 22.86 34 4075 116145 79624134
Encephalitis 30.51 22.86 15 4094 14745 79725534
Wrong drug 29.87 22.86 6 4103 290 79739989
Splenic rupture 29.61 22.86 9 4100 2420 79737859
Pulmonary congestion 29.45 22.86 18 4091 27082 79713197
Middle insomnia 29.31 22.86 15 4094 16054 79724225
Vascular resistance systemic 29.26 22.86 4 4105 15 79740264
Poor venous access 27.59 22.86 15 4094 18134 79722145
Acquired haemophilia 27.29 22.86 8 4101 1903 79738376
Asthma 26.98 22.86 34 4075 135061 79605218
Gastrointestinal ischaemia 26.77 22.86 6 4103 491 79739788
Cardiac failure congestive 25.56 22.86 34 4075 142368 79597911
Urinary retention 25.41 22.86 22 4087 56608 79683671
Muscular weakness 25.28 22.86 36 4073 160693 79579586

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




🐶 Veterinary Drug Use

None

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

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Betoptic S HUMAN PRESCRIPTION DRUG LABEL 1 0065-0246 SUSPENSION/ DROPS 2.80 mg OPHTHALMIC NDA 25 sections
Betoptic S HUMAN PRESCRIPTION DRUG LABEL 1 0065-0246 SUSPENSION/ DROPS 2.80 mg OPHTHALMIC NDA 25 sections
Betoptic S HUMAN PRESCRIPTION DRUG LABEL 1 0065-0246 SUSPENSION/ DROPS 2.80 mg OPHTHALMIC NDA 25 sections
Betoptic S HUMAN PRESCRIPTION DRUG LABEL 1 0078-0729 SUSPENSION/ DROPS 2.80 mg OPHTHALMIC NDA 25 sections
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 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
Betaxolol Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 61314-245 SOLUTION/ DROPS 5.60 mg OPHTHALMIC NDA authorized generic 19 sections