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

Stem definitionDrug idCAS RN
sympathomimetic, phenethyl derivatives 1101 709-55-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • ethyl adrianol
  • etilefrine
  • ethylphenylephrine
  • etiladrianol
  • etilefrin
  • N-Ethylnorphenylephrine
  • dl-Etilefrin
  • etilefrine hydrochloride
  • etilefrine HCl
A phenylephrine-related beta-1 adrenergic and alpha adrenergic agonist used as a cardiotonic and antihypotensive agent.
  • Molecular weight: 181.24
  • Formula: C10H15NO2
  • CLOGP: 0.44
  • LIPINSKI: 0
  • HAC: 3
  • HDO: 3
  • TPSA: 52.49
  • ALOGS: -1.12
  • ROTB: 4

Drug dosage:

DoseUnitRoute
50 mg O
50 mg P

ADMET properties:

PropertyValueReference
MRTD (Maximum Recommended Therapeutic Daily Dose) 3.94 ยตM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 55 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 2.10 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 14 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.77 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 2.20 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Jan. 1, 1929 YEAR INTRODUCED

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
Postoperative adhesion 45.24 44.54 6 195 370 63488451

FDA Adverse Event Reporting System (Male)

None

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
Postoperative adhesion 42.18 35.70 6 326 468 79743588

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC C01CA01 CARDIOVASCULAR SYSTEM
CARDIAC THERAPY
CARDIAC STIMULANTS EXCL. CARDIAC GLYCOSIDES
Adrenergic and dopaminergic agents
ATC C01CA51 CARDIOVASCULAR SYSTEM
CARDIAC THERAPY
CARDIAC STIMULANTS EXCL. CARDIAC GLYCOSIDES
Adrenergic and dopaminergic agents
MeSH PA D018663 Adrenergic Agents
MeSH PA D000322 Adrenergic Agonists
MeSH PA D000316 Adrenergic alpha-Agonists
MeSH PA D058665 Adrenergic beta-1 Receptor Agonists
MeSH PA D000318 Adrenergic beta-Agonists
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 D013566 Sympathomimetics
MeSH PA D014662 Vasoconstrictor Agents

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

None




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 10.15 acidic
pKa2 13.78 acidic
pKa3 8.83 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 AGONIST SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE

External reference:

IDSource
N0000166808 NUI
D01573 KEGG_DRUG
943-17-9 SECONDARY_CAS_RN
C0015116 UMLSCUI
CHEBI:91518 CHEBI
CHEMBL86882 ChEMBL_ID
DB08985 DRUGBANK_ID
D005039 MESH_DESCRIPTOR_UI
3306 PUBCHEM_CID
2229 INN_ID
ZB6F8MY53V UNII
235960 RXNORM
004352 NDDF
004353 NDDF
734508002 SNOMEDCT_US
96255000 SNOMEDCT_US

Pharmaceutical products:

None