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

Stem definitionDrug idCAS RN
1571 1477-40-3

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • levomethadyl acetate hydrochloride
  • levacetylmethadol
  • levomethadyl acetate
  • levomethadyl
  • orlaam
  • levomethadyl acetate HCl
  • levacetylmethadol hydrochloride
  • Molecular weight: 353.51
  • Formula: C23H31NO2
  • CLOGP: 4.59
  • LIPINSKI: 0
  • HAC: 3
  • HDO: 0
  • TPSA: 29.54
  • ALOGS: -5.30
  • ROTB: 9

  • Status: OFM

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

PropertyValueReference
MRTD (Maximum Recommended Therapeutic Daily Dose) 11.32 ยตM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
Vd (Volume of distribution) 8.30 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 5.40 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.20 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 18 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Jan. 7, 1997 EMA
July 9, 1993 FDA ROXANE

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC N07BC03 NERVOUS SYSTEM
OTHER NERVOUS SYSTEM DRUGS
DRUGS USED IN ADDICTIVE DISORDERS
Drugs used in opioid dependence
MeSH PA D000700 Analgesics
MeSH PA D000701 Analgesics, Opioid
MeSH PA D002491 Central Nervous System Agents
MeSH PA D002492 Central Nervous System Depressants
MeSH PA D009294 Narcotics
MeSH PA D018373 Peripheral Nervous System Agents
MeSH PA D018689 Sensory System Agents
CHEBI has role CHEBI:35482 narcotic analgesic
CHEBI has role CHEBI:50137 mu-opioid receptor antagonists

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Opioid dependence indication 75544000 DOID:2559




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 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
Mu-type opioid receptor GPCR AGONIST WOMBAT-PK CHEMBL
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 5.66 CHEMBL

External reference:

IDSource
4020836 VUID
N0000179426 NUI
D00840 KEGG_DRUG
43033-72-3 SECONDARY_CAS_RN
14019-10-4 SECONDARY_CAS_RN
4020836 VANDF
4020848 VANDF
CHEBI:6441 CHEBI
CHEMBL1514 ChEMBL_ID
CHEMBL1200817 ChEMBL_ID
7212 IUPHAR_LIGAND_ID
3175 INN_ID
DB01227 DRUGBANK_ID
R3B637Y991 UNII
15130 PUBCHEM_CID
218943 RXNORM
3114 MMSL
4973 MMSL
d03187 MMSL
004753 NDDF
004754 NDDF
007409 NDDF
108375002 SNOMEDCT_US
108378000 SNOMEDCT_US
409482006 SNOMEDCT_US
D008692 MESH_DESCRIPTOR_UI
C3536876 UMLSCUI

Pharmaceutical products:

None