isoprenaline indications/contra

Stem definitionDrug idCAS RN
bronchodilators, phenethylamine derivatives 1499 7683-59-2

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • isoprenaline
  • isoproterenol
  • isoproterenol hydrochloride
  • DL-Isoproterenol
  • isoprenalin
  • isoprenaline sulfate
  • DL-isoprenaline hydrochloride
  • isoproterenol sulfate
  • isoproterenol HCl
  • DL-isoprenaline HCl
Isopropyl analog of EPINEPHRINE; beta-sympathomimetic that acts on the heart, bronchi, skeletal muscle, alimentary tract, etc. It is used mainly as bronchodilator and heart stimulant.
  • Molecular weight: 211.26
  • Formula: C11H17NO3
  • CLOGP: 0.15
  • LIPINSKI: 0
  • HAC: 4
  • HDO: 4
  • TPSA: 72.72
  • ALOGS: -1.56
  • ROTB: 4

Drug dosage:

DoseUnitRoute
90 mg O
90 mg P
0.64 mg Inhal.aerosol
10 mg Inhal.solution
40 mg O

Approvals:

DateAgencyCompanyOrphan
March 9, 1956 FDA

FDA Adverse Event Reporting System

None

Pharmacologic Action:

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SourceCodeDescription
ATC C01CA02 CARDIOVASCULAR SYSTEM
CARDIAC THERAPY
CARDIAC STIMULANTS EXCL. CARDIAC GLYCOSIDES
Adrenergic and dopaminergic agents
ATC R03AB02 RESPIRATORY SYSTEM
DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
ADRENERGICS, INHALANTS
Non-selective beta-adrenoreceptor agonists
ATC R03CB01 RESPIRATORY SYSTEM
DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
ADRENERGICS FOR SYSTEMIC USE
Non-selective beta-adrenoreceptor agonists
ATC R03AK02 RESPIRATORY SYSTEM
DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
ADRENERGICS, INHALANTS
Adrenergics in combination with corticosteroids or other drugs, excl. anticholinergics
ATC R03CB51 RESPIRATORY SYSTEM
DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
ADRENERGICS FOR SYSTEMIC USE
Non-selective beta-adrenoreceptor agonists
CHEBI has role CHEBI:35522 beta-adrenergic agonist
CHEBI has role CHEBI:35523 bronchodilator agent
CHEBI has role CHEBI:38147 cardiotonic drug
CHEBI has role CHEBI:35524 sympathomimetic agent
MeSH PA D018663 Adrenergic Agents
MeSH PA D000322 Adrenergic Agonists
MeSH PA D000318 Adrenergic beta-Agonists
MeSH PA D018927 Anti-Asthmatic Agents
MeSH PA D001337 Autonomic Agents
MeSH PA D001993 Bronchodilator Agents
MeSH PA D002316 Cardiotonic Agents
MeSH PA D002317 Cardiovascular Agents
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018373 Peripheral Nervous System Agents
MeSH PA D020011 Protective Agents
MeSH PA D019141 Respiratory System Agents
MeSH PA D013566 Sympathomimetics

Drug Use (View source of the data)

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DiseaseRelationSNOMED_IDDOID
Hypovolemic shock indication 39419009
Low cardiac output syndrome indication 44088000
Common cold indication 82272006 DOID:10459
Atrioventricular block indication 233917008 DOID:0050820
Cardiac arrest indication 410429000 DOID:0060319
Syncope due to Heart Block indication
Thick Bronchial Secretions indication
Tachyarrhythmia contraindication 6285003
Myocardial infarction contraindication 22298006 DOID:5844
Hyperthyroidism contraindication 34486009 DOID:7998
Hypertensive disorder contraindication 38341003 DOID:10763
Diabetes mellitus contraindication 73211009 DOID:9351
Angina pectoris contraindication 194828000
Chronic myocardial ischemia contraindication 413844008 DOID:3393
Disorder of coronary artery contraindication 414024009
Digitalis Toxicity with AV Conduction Defects contraindication
Atrioventricular Conduction Defect contraindication
Tachycardia due to Digitalis Toxicity contraindication

Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.97 acidic
pKa2 12.82 acidic
pKa3 13.92 acidic
pKa4 8.94 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 AGONIST EC50 9 WOMBAT-PK CHEMBL
Beta-2 adrenergic receptor GPCR AGONIST EC50 9.80 WOMBAT-PK CHEMBL
Beta-3 adrenergic receptor GPCR AGONIST EC50 8.50 WOMBAT-PK
Arachidonate 15-lipoxygenase Enzyme IC50 5.75 DRUG MATRIX
Beta-2 adrenergic receptor GPCR Ki 6.87 CHEMBL
Beta-1 adrenergic receptor GPCR IC50 6.22 CHEMBL
Beta-2 adrenergic receptor GPCR IC50 6 CHEMBL
Beta-2 adrenergic receptor GPCR Kd 6.48 CHEMBL
Beta-2 adrenergic receptor GPCR EC50 7.54 CHEMBL
Beta-3 adrenergic receptor Unclassified AGONIST Ki 5.30 IUPHAR
Beta-3 adrenergic receptor Unclassified AGONIST Ki 5.30 IUPHAR

External reference:

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IDSource
536 IUPHAR_LIGAND_ID
4019793 VUID
N0000147882 NUI
C0022245 UMLSCUI
D01390 KEGG_DRUG
CHEMBL434 ChEMBL_ID
DB01064 DRUGBANK_ID
3779 PUBCHEM_CID
6054 RXNORM
372781009 SNOMEDCT_US
57845006 SNOMEDCT_US
d00697 MMSL
4019793 VANDF
N0000006336 NDFRT
N0000147882 NDFRT
001778 NDDF
925FX3X776 UNII
6078-56-4 SECONDARY_CAS_RN
CHEBI:64317 CHEBI
CHEMBL1711 ChEMBL_ID
CHEMBL1160723 ChEMBL_ID
CHEMBL1200447 ChEMBL_ID
D007545 MESH_DESCRIPTOR_UI
4201 INN_ID
5FW PDB_CHEM_ID

Pharmaceutical products:

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ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
Isuprel HUMAN PRESCRIPTION DRUG LABEL 1 0187-4330 INJECTION, SOLUTION 0.20 mg INTRAVENOUS NDA 12 sections
Isuprel HUMAN PRESCRIPTION DRUG LABEL 1 0409-1442 INJECTION, SOLUTION 0.20 mg INTRAVENOUS EXPORT ONLY 12 sections
Isoproterenol Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 14789-011 INJECTION, SOLUTION 0.20 mg INTRAMUSCULAR ANDA 12 sections
Isoproterenol Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 14789-015 INJECTION, SOLUTION 0.20 mg INTRAMUSCULAR ANDA 12 sections