vecuronium ๐Ÿถ Veterinary Use | 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 ยตM/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)

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
Neuromuscular block prolonged 99.85 44.94 17 1735 494 50602878
Hypotension 98.64 44.94 74 1678 235395 50367977
Hyperthermia malignant 93.59 44.94 17 1735 722 50602650
Bradycardia 92.96 44.94 45 1707 64381 50538991
Cardiac arrest 81.86 44.94 45 1707 83606 50519766
Anaphylactic shock 80.02 44.94 29 1723 20126 50583246
Arteriospasm coronary 57.89 44.94 15 1737 3387 50599985
Blood pressure decreased 57.16 44.94 31 1721 55878 50547494
Anaphylactic reaction 52.56 44.94 29 1723 54026 50549346
Delayed recovery from anaesthesia 49.60 44.94 10 1742 739 50602633
Neuromuscular blockade 45.47 44.94 8 1744 282 50603090

FDA Adverse Event Reporting System (Male)

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
Hyperthermia malignant 152.06 31.29 34 2361 1750 29570382
Anaphylactic reaction 72.20 31.29 38 2357 27535 29544597
Hypotension 53.89 31.29 72 2323 194282 29377850
Fear 49.29 31.29 21 2374 9483 29562649
Cardiac arrest 46.41 31.29 45 2350 85546 29486586
Renal injury 41.47 31.29 19 2376 10183 29561949
Post procedural complication 38.04 31.29 18 2377 10371 29561761
Injury 35.46 31.29 21 2374 19025 29553107
Anhedonia 34.34 31.29 15 2380 7185 29564947
Blood creatine phosphokinase increased 33.23 31.29 27 2368 40617 29531515
Emotional distress 33.09 31.29 18 2377 13877 29558255
Ventricular tachycardia 32.17 31.29 21 2374 22553 29549579
Renal impairment 31.91 31.29 36 2359 81297 29490835

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
Hyperthermia malignant 216.14 31.52 46 4033 2413 64492240
Hypotension 118.06 31.52 132 3947 380842 64113811
Anaphylactic reaction 112.97 31.52 64 4015 68600 64426053
Cardiac arrest 94.57 31.52 78 4001 153986 64340667
Neuromuscular block prolonged 89.95 31.52 19 4060 958 64493695
Anaphylactic shock 86.66 31.52 41 4038 30287 64464366
Bradycardia 83.46 31.52 65 4014 118154 64376499
Fear 79.03 31.52 34 4045 20137 64474516
Renal injury 67.05 31.52 28 4051 15401 64479252
Anaesthetic complication 66.87 31.52 18 4061 2561 64492092
Delayed recovery from anaesthesia 65.88 31.52 16 4063 1512 64493141
Blood pressure decreased 62.09 31.52 48 4031 86151 64408502
Arteriospasm coronary 61.56 31.52 20 4059 5445 64489208
Ventricular tachycardia 56.43 31.52 32 4047 34233 64460420
Procedural complication 55.98 31.52 20 4059 7245 64487408
Injury 53.50 31.52 37 4042 55955 64438698
Anhedonia 53.33 31.52 23 4056 13683 64480970
Chemical peritonitis 53.25 31.52 10 4069 274 64494379
Post procedural complication 52.33 31.52 26 4053 21327 64473326
Unevaluable event 52.12 31.52 35 4044 50454 64444199
Respiratory acidosis 50.04 31.52 20 4059 9835 64484818
Renal impairment 48.91 31.52 51 4028 134966 64359687
Tachycardia 46.30 31.52 52 4027 149527 64345126
Drug interaction 45.93 31.52 82 3997 362001 64132652
Multiple organ dysfunction syndrome 45.40 31.52 43 4036 101370 64393283
Serotonin syndrome 44.83 31.52 29 4050 39253 64455400
Ventricular fibrillation 43.97 31.52 24 4055 23836 64470817
Emotional distress 42.10 31.52 27 4052 36011 64458642
Rhabdomyolysis 35.63 31.52 36 4043 91690 64402963
Extrasystoles 35.50 31.52 14 4065 6644 64488009
Shock 33.56 31.52 24 4055 38216 64456437
Metabolic acidosis 33.49 31.52 31 4048 70927 64423726
Ventricular extrasystoles 33.32 31.52 18 4061 17511 64477142
Haemodynamic instability 33.14 31.52 17 4062 14895 64479758
Blood creatine phosphokinase increased 32.42 31.52 28 4051 58530 64436123

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC M03AC03 MUSCULO-SKELETAL SYSTEM
MUSCLE RELAXANTS
MUSCLE RELAXANTS, PERIPHERALLY ACTING AGENTS
Other quaternary ammonium compounds
CHEBI has role CHEBI:48878 nicotinic antagonists
CHEBI has role CHEBI:51371 muscle relaxants
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
FDA EPC N0000175720 Nondepolarizing Neuromuscular Blocker
FDA PE N0000175732 Neuromuscular Nondepolarizing Blockade

Drug Use | Suggest Off label Use Form| |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




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 8.58 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
Muscarinic acetylcholine receptor M2 GPCR IC50 9.30 CHEMBL
Muscarinic acetylcholine receptor M3 GPCR IC50 9.60 CHEMBL
Muscarinic acetylcholine receptor M4 GPCR IC50 9.80 CHEMBL
Muscarinic acetylcholine receptor M5 GPCR IC50 9.70 CHEMBL
Solute carrier family 22 member 2 Transporter IC50 5.46 CHEMBL
Multidrug and toxin extrusion protein 1 Transporter IC50 5.72 CHEMBL
Multidrug and toxin extrusion protein 2 Transporter IC50 4.60 CHEMBL
Neuronal acetylcholine receptor; alpha2/beta4 Ion channel WOMBAT-PK
Neuronal acetylcholine receptor; alpha4/beta2 Ion channel WOMBAT-PK
Neuronal acetylcholine receptor; alpha4/beta4 Ion channel WOMBAT-PK
Muscarinic acetylcholine receptor M1 GPCR IC50 9.90 CHEMBL
Acetylcholine receptor; alpha1/beta1/delta/gamma Ion channel IC50 7.09 CHEMBL

External reference:

IDSource
4018512 VUID
N0000146834 NUI
D00767 KEGG_DRUG
4018512 VANDF
4019968 VANDF
C0242531 UMLSCUI
CHEBI:9940 CHEBI
CHEMBL1201219 ChEMBL_ID
CHEMBL1201027 ChEMBL_ID
CHEMBL1200629 ChEMBL_ID
DB01339 DRUGBANK_ID
4002 IUPHAR_LIGAND_ID
5438723848 UNII
39765 PUBCHEM_CID
11153 RXNORM
5668 MMSL
6443 MMSL
7979 MMSL
d00399 MMSL
002408 NDDF
013413 NDDF
372883002 SNOMEDCT_US
86085000 SNOMEDCT_US
87472002 SNOMEDCT_US
D014673 MESH_DESCRIPTOR_UI
5100 INN_ID
86029-43-8 SECONDARY_CAS_RN

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Vecuronium Bromide HUMAN PRESCRIPTION DRUG LABEL 1 0143-9232 INJECTION, POWDER, FOR SOLUTION 20 mg INTRAVENOUS ANDA 21 sections
Vecuronium Bromide HUMAN PRESCRIPTION DRUG LABEL 1 0143-9234 INJECTION, POWDER, FOR SOLUTION 10 mg INTRAVENOUS ANDA 21 sections
Vecuronium Bromide Human prescription drug label 1 0409-1632 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 1 mg INTRAVENOUS ANDA 13 sections
Vecuronium Bromide Human prescription drug label 1 0409-1634 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 1 mg INTRAVENOUS ANDA 13 sections
Vecuronium Bromide HUMAN PRESCRIPTION DRUG LABEL 1 0703-2914 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 10 mg INTRAVENOUS ANDA 24 sections
Vecuronium Bromide HUMAN PRESCRIPTION DRUG LABEL 1 0703-2925 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 20 mg INTRAVENOUS ANDA 24 sections
Vecuronium bromide HUMAN PRESCRIPTION DRUG LABEL 1 23360-160 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 1 mg INTRAVENOUS ANDA 20 sections
vecuronium bromide Human Prescription Drug Label 1 47335-931 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 1 mg INTRAVENOUS ANDA 20 sections
vecuronium bromide Human Prescription Drug Label 1 47335-932 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 1 mg INTRAVENOUS ANDA 20 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 23 sections
VECURONIUM BROMIDE Human Prescription Drug Label 1 55150-235 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 10 mg INTRAVENOUS ANDA 23 sections
VECURONIUM BROMIDE Human Prescription Drug Label 1 55150-236 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 20 mg INTRAVENOUS ANDA 23 sections
VECURONIUM BROMIDE Human Prescription Drug Label 1 55150-236 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 20 mg INTRAVENOUS ANDA 23 sections
Vecuronium Bromide Human Prescription Drug Label 1 63323-781 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 1 mg INTRAVENOUS ANDA 20 sections
Vecuronium Bromide Human Prescription Drug Label 1 63323-781 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 1 mg INTRAVENOUS ANDA 20 sections
Vecuronium Bromide Human Prescription Drug Label 1 63323-782 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 1 mg INTRAVENOUS ANDA 20 sections
VECURONIUM BROMIDE HUMAN PRESCRIPTION DRUG LABEL 1 67457-438 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 1 mg INTRAVENOUS ANDA 20 sections
VECURONIUM BROMIDE HUMAN PRESCRIPTION DRUG LABEL 1 67457-475 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 1 mg INTRAVENOUS ANDA 20 sections
Vecuronium Bromide Human Prescription Drug Label 1 68083-139 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 1 mg INTRAVENOUS ANDA 20 sections
Vecuronium Bromide Human Prescription Drug Label 1 68083-140 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 1 mg INTRAVENOUS ANDA 20 sections