bretylium indications/contra

Stem definitionDrug idCAS RN
394 61-75-6

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • bretylium
  • bretylium tosilate
  • bretylan
  • bretylate
  • bretylium tosylate
An agent that blocks the release of adrenergic transmitters and may have other actions. It was formerly used as an antihypertensive agent, but is now proposed as an anti-arrhythmic.
  • Molecular weight: 243.17
  • Formula: C11H17BrN
  • CLOGP: -1.25
  • LIPINSKI: 0
  • HAC: 1
  • HDO: 0
  • TPSA:
  • ALOGS: -6.26
  • ROTB: 3

Drug dosage:

None

Approvals:

DateAgencyCompanyOrphan
March 6, 1986 FDA INTL MEDICATION

FDA Adverse Event Reporting System

None

Pharmacologic Action:

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SourceCodeDescription
ATC C01BD02 CARDIOVASCULAR SYSTEM
CARDIAC THERAPY
ANTIARRHYTHMICS, CLASS I AND III
Antiarrhythmics, class III
MeSH PA D018663 Adrenergic Agents
MeSH PA D018674 Adrenergic Antagonists
MeSH PA D000889 Anti-Arrhythmia Agents
MeSH PA D000959 Antihypertensive Agents
MeSH PA D002317 Cardiovascular Agents
MeSH PA D018377 Neurotransmitter Agents

Drug Use (View source of the data)

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DiseaseRelationSNOMED_IDDOID
Ventricular arrhythmia indication 44103008
Ventricular fibrillation indication 71908006
Life-Threatening Ventricular Tachycardia indication
Prevention of Ventricular Fibrillation indication
Orthostatic hypotension contraindication 28651003
Low cardiac output syndrome contraindication 44088000
Sinus bradycardia contraindication 49710005
Aortic valve stenosis contraindication 60573004 DOID:1712
Pulmonary hypertension contraindication 70995007 DOID:6432
Kidney disease contraindication 90708001 DOID:2527
Cardiac arrest off-label use 410429000 DOID:0060319

Acid dissociation constants calculated using MoKa v3.0.0

None

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
Sodium-dependent noradrenaline transporter Transporter SUBSTRATE CHEMBL CHEMBL
Beta-2 adrenergic receptor GPCR WOMBAT-PK
Beta-1 adrenergic receptor GPCR WOMBAT-PK

External reference:

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IDSource
4019638 VUID
N0000171583 NUI
C0054040 UMLSCUI
7130 IUPHAR_LIGAND_ID
D00645 KEGG_DRUG
78ZP3YR353 UNII
927 INN_ID
2431 PUBCHEM_CID
4019638 VANDF
N0000147731 NDFRT
N0000171583 NDFRT
004448 NDDF
d00005 MMSL
19685 RXNORM
372774002 SNOMEDCT_US
56230001 SNOMEDCT_US
CHEMBL1095292 ChEMBL_ID
CHEMBL1199080 ChEMBL_ID
D001950 MESH_DESCRIPTOR_UI
C045166 MESH_SUPPLEMENTAL_RECORD_UI
DB01158 DRUGBANK_ID
59-41-6 SECONDARY_CAS_RN

Pharmaceutical products:

None