betaxolol indications/contra

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

Drug dosage:

DoseUnitRoute
20 mg O

Approvals:

DateAgencyCompanyOrphan
Aug. 30, 1985 FDA ALCON

FDA Adverse Event Reporting System

None

Pharmacologic Action:

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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 agents1)
ATC S01ED52 SENSORY ORGANS
OPHTHALMOLOGICALS
ANTIGLAUCOMA PREPARATIONS AND MIOTICS
Beta blocking agents1)
FDA EPC N0000175556 beta-Adrenergic Blocker
MeSH PA D018663 Adrenergic Agents
MeSH PA D018674 Adrenergic Antagonists
MeSH PA D058671 Adrenergic beta-1 Receptor Antagonists
MeSH PA D000319 Adrenergic beta-Antagonists
CHEBI has role CHEBI:66991 sympatholytic agent
CHEBI has role CHEBI:35530 beta-adrenergic antagonist
CHEBI has role CHEBI:35674 antihypertensive agent
MeSH PA D000959 Antihypertensive Agents
MeSH PA D001337 Autonomic Agents
MeSH PA D002317 Cardiovascular Agents
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018373 Peripheral Nervous System Agents
MeSH PA D013565 Sympatholytics

Drug Use (View source of the data)

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DiseaseRelationSNOMED_IDDOID
Ocular hypertension indication 4210003 DOID:9282
Hypertensive disorder indication 38341003 DOID:10763
Open-angle glaucoma indication 84494001 DOID:1067
Bronchospasm contraindication 4386001
Psoriasis contraindication 9014002 DOID:8893
Complete atrioventricular block contraindication 27885002
Acute cerebrovascular insufficiency contraindication 29322000
Depressive disorder contraindication 35489007 DOID:2848
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:2527
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 DOID:9993
Raynaud's phenomenon contraindication 266261006
Pregnancy, function contraindication 289908002
Pheochromocytoma contraindication 302835009
Acute exacerbation of asthma contraindication 708038006
Malignant glaucoma off-label use 10100008
Aphakic glaucoma off-label use 15374009
Secondary glaucoma off-label use 95717004

Acid dissociation constants calculated using MoKa v3.0.0

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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:

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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 IC50 6.18 CHEMBL
Beta-2 adrenergic receptor GPCR Kd 6.98 CHEMBL
Beta-1 adrenergic receptor GPCR Kd 8.76 CHEMBL

External reference:

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IDSource
DB00195 DRUGBANK_ID
549 IUPHAR_LIGAND_ID
4019633 VUID
N0000147726 NUI
C0005320 UMLSCUI
D00598 KEGG_DRUG
CHEMBL423 ChEMBL_ID
6X97D2XT0O UNII
63659-19-8 SECONDARY_CAS_RN
4019633 VANDF
N0000006532 NDFRT
N0000147726 NDFRT
1520 RXNORM
349900007 SNOMEDCT_US
409276006 SNOMEDCT_US
d00176 MMSL
004743 NDDF
2369 PUBCHEM_CID
CHEBI:3082 CHEBI
CHEMBL1691 ChEMBL_ID
4530 INN_ID
D015784 MESH_DESCRIPTOR_UI

Pharmaceutical products:

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ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
Betoptic S HUMAN PRESCRIPTION DRUG LABEL 1 0065-0246 SUSPENSION/ DROPS 2.80 mg OPHTHALMIC NDA 17 sections
Betaxolol HUMAN PRESCRIPTION DRUG LABEL 1 10135-623 TABLET, FILM COATED 10 mg ORAL ANDA 12 sections
Betaxolol HUMAN PRESCRIPTION DRUG LABEL 1 10135-624 TABLET, FILM COATED 20 mg ORAL ANDA 12 sections
BETAXOLOL HYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 10702-013 TABLET, COATED 10 mg ORAL ANDA 11 sections
BETAXOLOL HYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 10702-014 TABLET, COATED 20 mg ORAL ANDA 11 sections
Betaxolol HUMAN PRESCRIPTION DRUG LABEL 1 17478-705 SOLUTION/ DROPS 5 mg OPHTHALMIC ANDA 12 sections
Betaxolol HUMAN PRESCRIPTION DRUG LABEL 1 24658-700 TABLET, FILM COATED 10 mg ORAL ANDA 11 sections
Betaxolol HUMAN PRESCRIPTION DRUG LABEL 1 24658-701 TABLET, FILM COATED 20 mg ORAL ANDA 11 sections
Betaxolol HUMAN PRESCRIPTION DRUG LABEL 1 42806-038 TABLET, FILM COATED 10 mg ORAL ANDA 11 sections
Betaxolol HUMAN PRESCRIPTION DRUG LABEL 1 42806-039 TABLET, FILM COATED 20 mg ORAL ANDA 11 sections
Betaxolol HUMAN PRESCRIPTION DRUG LABEL 1 54868-4932 TABLET, FILM COATED 10 mg ORAL ANDA 11 sections
Betaxolol HUMAN PRESCRIPTION DRUG LABEL 1 60429-753 TABLET, FILM COATED 10 mg ORAL ANDA 11 sections
Betaxolol HUMAN PRESCRIPTION DRUG LABEL 1 60429-754 TABLET, FILM COATED 20 mg ORAL ANDA 11 sections
Betaxolol Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 61314-245 SOLUTION/ DROPS 5.60 mg OPHTHALMIC NDA authorized generic 14 sections