vecuronium Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
neuromuscular blocking agents with rigid structure 2811 50700-72-6

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • vecuronium hydrobromide
  • vecuronium citrate
  • vecuronium maleate
  • vecuronium hydrochloride
  • vecuronium HCl
  • Org NC 45
  • vecuronium
  • vecuronium bromide
Monoquaternary homolog of PANCURONIUM. A non-depolarizing neuromuscular blocking agent with shorter duration of action than pancuronium. Its lack of significant cardiovascular effects and lack of dependence on good kidney function for elimination as well as its short duration of action and easy reversibility provide advantages over, or alternatives to, other established neuromuscular blocking agents.
  • Molecular weight: 557.84
  • Formula: C34H57N2O4
  • CLOGP: 4.33
  • LIPINSKI: 1
  • HAC: 6
  • HDO: 0
  • TPSA: 55.84
  • ALOGS: -7.50
  • ROTB: 6

  • Status: OFP

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

Drug dosage:

None

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 3 Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 20 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.16 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 0 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 0.30 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 4.50 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.25 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 1.40 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
April 30, 1984 FDA ORGANON USA INC

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
ATC M03AC03 MUSCULO-SKELETAL SYSTEM
MUSCLE RELAXANTS
MUSCLE RELAXANTS, PERIPHERALLY ACTING AGENTS
Other quaternary ammonium compounds
FDA PE N0000175732 Neuromuscular Nondepolarizing Blockade
FDA EPC N0000175720 Nondepolarizing Neuromuscular Blocker
MeSH PA D018678 Cholinergic Agents
MeSH PA D018680 Cholinergic Antagonists
MeSH PA D009465 Neuromuscular Agents
MeSH PA D009466 Neuromuscular Blocking Agents
MeSH PA D003473 Neuromuscular Nondepolarizing Agents
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018733 Nicotinic Antagonists
MeSH PA D018373 Peripheral Nervous System Agents
CHEBI has role CHEBI:48878 nicotinic antagonist
CHEBI has role CHEBI:51372 neuromuscular agent
CHEBI has role CHEBI:51371 muscle relaxant

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Muscle relaxation, function indication 11977004
General anesthesia indication 50697003
Skeletal Muscle Relaxation for Endotracheal Intubation indication
Cirrhosis of liver contraindication 19943007 DOID:5082
Obstruction of bile duct contraindication 30144000
Eaton-Lambert syndrome contraindication 56989000 DOID:0050214
Myasthenia gravis contraindication 91637004 DOID:437
Disorder of electrolytes contraindication 237840007
Morbid obesity contraindication 238136002 DOID:11981
Neuromyopathy contraindication 255522009 DOID:440

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.58 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
Acetylcholine receptor Ion channel ANTAGONIST IC50 7.82 WOMBAT-PK CHEMBL
Neuronal acetylcholine receptor; alpha2/beta4 Ion channel WOMBAT-PK
Neuronal acetylcholine receptor; alpha4/beta4 Ion channel WOMBAT-PK
Solute carrier family 22 member 2 Transporter IC50 5.46 CHEMBL
Multidrug and toxin extrusion protein 2 Transporter IC50 4.60 CHEMBL
Multidrug and toxin extrusion protein 1 Transporter IC50 5.72 CHEMBL
Neuronal acetylcholine receptor; alpha4/beta2 Ion channel WOMBAT-PK
Acetylcholine receptor; alpha1/beta1/delta/gamma Ion channel IC50 7.09 CHEMBL

External reference:

IDSource
4018512 VUID
N0000146834 NUI
C0042435 UMLSCUI
D00767 KEGG_DRUG
7E4PHP5N1D UNII
5100 INN_ID
86085000 SNOMEDCT_US
4019968 VANDF
013413 NDDF
7979 MMSL
71535 RXNORM
372883002 SNOMEDCT_US
d00399 MMSL
CHEMBL1200629 ChEMBL_ID
DB01339 DRUGBANK_ID
CHEBI:9940 CHEBI
CHEMBL1201219 ChEMBL_ID
D014673 MESH_DESCRIPTOR_UI
39765 PUBCHEM_CID
4002 IUPHAR_LIGAND_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Vecuronium Bromide HUMAN PRESCRIPTION DRUG LABEL 1 0143-9232 INJECTION, POWDER, FOR SOLUTION 20 mg INTRAVENOUS ANDA 12 sections
Vecuronium Bromide HUMAN PRESCRIPTION DRUG LABEL 1 0143-9234 INJECTION, POWDER, FOR SOLUTION 10 mg INTRAVENOUS ANDA 12 sections
Vecuronium Bromide HUMAN PRESCRIPTION DRUG LABEL 1 0409-1632 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 1 mg INTRAVENOUS ANDA 12 sections
Vecuronium Bromide HUMAN PRESCRIPTION DRUG LABEL 1 0409-1634 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 1 mg INTRAVENOUS ANDA 12 sections
Vecuronium Bromide HUMAN PRESCRIPTION DRUG LABEL 1 0703-2914 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 10 mg INTRAVENOUS ANDA 12 sections
Vecuronium Bromide HUMAN PRESCRIPTION DRUG LABEL 1 0703-2925 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 20 mg INTRAVENOUS ANDA 12 sections
Vecuronium bromide HUMAN PRESCRIPTION DRUG LABEL 1 23360-160 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 1 mg INTRAVENOUS ANDA 13 sections
vecuronium bromide HUMAN PRESCRIPTION DRUG LABEL 1 47335-931 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 1 mg INTRAVENOUS ANDA 12 sections
vecuronium bromide HUMAN PRESCRIPTION DRUG LABEL 1 47335-932 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 1 mg INTRAVENOUS ANDA 12 sections
VECURONIUM BROMIDE HUMAN PRESCRIPTION DRUG LABEL 1 51662-1475 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 1 mg INTRAVENOUS ANDA 13 sections
VECURONIUM BROMIDE HUMAN PRESCRIPTION DRUG LABEL 1 55150-235 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 10 mg INTRAVENOUS ANDA 12 sections
VECURONIUM BROMIDE HUMAN PRESCRIPTION DRUG LABEL 1 55150-236 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 20 mg INTRAVENOUS ANDA 12 sections
Vecuronium Bromide HUMAN PRESCRIPTION DRUG LABEL 1 63323-781 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 1 mg INTRAVENOUS ANDA 13 sections
Vecuronium Bromide HUMAN PRESCRIPTION DRUG LABEL 1 63323-782 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 1 mg INTRAVENOUS ANDA 13 sections
VECURONIUM BROMIDE HUMAN PRESCRIPTION DRUG LABEL 1 67457-438 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 1 mg INTRAVENOUS ANDA 13 sections
VECURONIUM BROMIDE HUMAN PRESCRIPTION DRUG LABEL 1 67457-475 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 1 mg INTRAVENOUS ANDA 13 sections
Vecuronium Bromide HUMAN PRESCRIPTION DRUG LABEL 1 68083-139 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 1 mg INTRAVENOUS ANDA 12 sections
Vecuronium Bromide HUMAN PRESCRIPTION DRUG LABEL 1 68083-140 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 1 mg INTRAVENOUS ANDA 12 sections