vecuronium 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | 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 µM/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
S (Water solubility) 21 mg/mL Bocci G, Oprea TI, Benet LZ

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 0.512 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 6.855 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 8.128 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 3.228 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 66.250 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 49.880 % High 1
herg hERG pIC50 4.554 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 2.228 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 14.521 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 61.700 % High 1
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 4.207 High 1
mh-clint Mouse hepatocyte intrinsic clearance 43.853 High 1
mppb Mouse plasma protein binding (% unbound) 46.440 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 4.721 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 58.100 % High 1
rh-clint Rat hepatocyte intrinsic clearance 96.383 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 85.220 % High 1
rppb Rat plasma protein binding (% unbound) 55.050 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 893.305 uM High 1

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
Hypotension 123.74 42.46 82 1986 325315 90301064
Cardiac arrest 123.62 42.46 56 2012 104879 90521500
Anaphylactic reaction 123.40 42.46 53 2015 87471 90538908
Bradycardia 115.64 42.46 50 2018 83797 90542582
Neuromuscular block prolonged 102.78 42.46 17 2051 635 90625744
Hyperthermia malignant 97.48 42.46 18 2050 1280 90625099
Anaphylactic shock 90.31 42.46 32 2036 31585 90594794
Blood pressure decreased 66.65 42.46 33 2035 74862 90551517
Arteriospasm coronary 58.20 42.46 15 2053 5035 90621344
Delayed recovery from anaesthesia 56.69 42.46 11 2057 1019 90625360
Neuromuscular blockade 53.87 42.46 9 2059 357 90626022
Drug interaction 50.09 42.46 45 2023 276408 90349971
Acute postoperative sialadenitis 45.30 42.46 6 2062 45 90626334
Ventricular tachycardia 44.98 42.46 18 2050 24690 90601689
Fear 44.31 42.46 16 2052 16606 90609773
Respiratory acidosis 42.49 42.46 13 2055 8106 90618273

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 145.12 28.72 34 2807 2624 42615870
Anaphylactic reaction 93.62 28.72 49 2792 42694 42575800
Cardiac arrest 80.73 28.72 63 2778 109257 42509237
Neuromuscular block prolonged 61.86 28.72 13 2828 606 42617888
Hypotension 54.83 28.72 76 2765 257555 42360939
Delayed recovery from anaesthesia 53.63 28.72 13 2828 1156 42617338
Fear 50.32 28.72 21 2820 10944 42607550
Renal injury 41.63 28.72 19 2822 12261 42606233
Blood creatine phosphokinase increased 40.28 28.72 30 2811 48308 42570186
Bradycardia 38.09 28.72 37 2804 85447 42533047
Post procedural complication 38.07 28.72 18 2823 12572 42605922
Ventricular tachycardia 37.61 28.72 24 2817 30136 42588358
Tachycardia 36.40 28.72 39 2802 101048 42517446
Anhedonia 36.29 28.72 15 2826 7625 42610869
Injury 36.15 28.72 21 2820 22295 42596199
Metabolic acidosis 34.14 28.72 28 2813 51830 42566664
Emotional distress 33.89 28.72 18 2823 16075 42602419
Ventricular fibrillation 30.37 28.72 21 2820 30102 42588392
Unevaluable event 30.17 28.72 22 2819 34266 42584228
Drug interaction 29.81 28.72 59 2782 266940 42351554
Hyperthermia 29.14 28.72 15 2826 12559 42605935

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 217.98 29.49 47 4739 3853 110580660
Anaphylactic reaction 191.54 29.49 95 4691 114205 110470308
Cardiac arrest 173.36 29.49 107 4679 196646 110387867
Hypotension 146.45 29.49 144 4642 523705 110060808
Neuromuscular block prolonged 122.45 29.49 24 4762 1223 110583290
Bradycardia 115.47 29.49 76 4710 155441 110429072
Delayed recovery from anaesthesia 108.71 29.49 24 4762 2191 110582322
Anaphylactic shock 95.64 29.49 46 4740 51500 110533013
Fear 86.89 29.49 34 4752 23159 110561354
Ventricular tachycardia 81.92 29.49 41 4745 49968 110534545
Drug interaction 73.79 29.49 99 4687 500084 110084429
Anaesthetic complication 72.43 29.49 19 4767 3587 110580926
Renal injury 72.09 29.49 28 4758 18685 110565828
Blood pressure decreased 70.52 29.49 50 4736 115041 110469472
Tachycardia 66.16 29.49 64 4722 226581 110357932
Procedural complication 64.58 29.49 21 4765 8384 110576129
Unevaluable event 59.17 29.49 35 4751 59192 110525321
Anhedonia 59.13 29.49 23 4763 15405 110569108
Arteriospasm coronary 58.99 29.49 20 4766 9080 110575433
Chemical peritonitis 56.33 29.49 10 4776 295 110584218
Post procedural complication 56.21 29.49 26 4760 26632 110557881
Respiratory acidosis 54.36 29.49 21 4765 13805 110570708
Respiratory failure 53.97 29.49 56 4730 215276 110369237
Rhabdomyolysis 53.11 29.49 43 4743 120358 110464155
Blood creatine phosphokinase increased 52.41 29.49 35 4751 73042 110511471
Shock 51.78 29.49 31 4755 53557 110530956
Renal impairment 50.84 29.49 51 4735 188394 110396119
Multiple organ dysfunction syndrome 50.28 29.49 46 4740 151664 110432849
Metabolic acidosis 49.09 29.49 38 4748 99706 110484807
Serotonin syndrome 48.96 29.49 31 4755 59122 110525391
Ventricular fibrillation 48.15 29.49 27 4759 41286 110543227
Renal failure 46.43 29.49 53 4733 226521 110357992
Emotional distress 46.09 29.49 27 4759 44820 110539693
Bronchospasm 44.29 29.49 23 4763 30216 110554297
Myoglobinuria 42.44 29.49 10 4776 1218 110583295
Neuromuscular blockade 41.74 29.49 9 4777 735 110583778
Hyperthermia 39.47 29.49 19 4767 21253 110563260
Acute postoperative sialadenitis 38.53 29.49 6 4780 77 110584436
Haemodynamic instability 38.15 29.49 19 4767 22869 110561644
Extrasystoles 37.63 29.49 14 4772 8304 110576209
Myopathy 36.59 29.49 19 4767 24941 110559572
Therapeutic product effect prolonged 36.45 29.49 8 4778 710 110583803
Ventricular extrasystoles 35.40 29.49 18 4768 22623 110561890
Necrotising myositis 32.88 29.49 9 4777 1993 110582520
Carcinoid crisis 32.75 29.49 7 4779 548 110583965
Hypoxia 31.19 29.49 33 4753 129482 110455031
Propofol infusion syndrome 30.60 29.49 9 4777 2580 110581933

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
MeSH PA D003473 Neuromuscular Nondepolarizing Agents
MeSH PA D009465 Neuromuscular Agents
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018678 Cholinergic Agents
MeSH PA D018680 Cholinergic Antagonists
MeSH PA D018733 Nicotinic Antagonists
FDA EPC N0000175720 Nondepolarizing Neuromuscular Blocker
FDA PE N0000175732 Neuromuscular Nondepolarizing Blockade
CHEBI has role CHEBI:48878 nicotinic antagonist
CHEBI has role CHEBI:51371 muscle relaxant
CHEBI has role CHEBI:51372 neuromuscular agent
CHEBI has role CHEBI:88188 drug allergen

Related Drugs by ATC class:

M03AC Other quaternary ammonium compounds 10 drugs
atracuriumcisatracuriumdoxacuriumfazadiniumgallaminehexafluroniummivacuriumpancuroniumpipecuroniumrocuronium

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




🐶 Veterinary Drug Use

None

🐶 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
86029-43-8 SECONDARY_CAS_RN
4018512 VANDF
4019968 VANDF
C0242531 UMLSCUI
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
CHEBI:9940 CHEBI
5100 INN_ID

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 23360-160 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 1 mg INTRAVENOUS ANDA 20 sections
Vecuronium Bromide HUMAN PRESCRIPTION DRUG LABEL 1 25021-685 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 1 mg INTRAVENOUS ANDA 24 sections
Vecuronium Bromide HUMAN PRESCRIPTION DRUG LABEL 1 25021-686 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 1 mg INTRAVENOUS ANDA 24 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 51662-1547 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 10 mg INTRAVENOUS ANDA 12 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 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
Vecuronium Bromide HUMAN PRESCRIPTION DRUG LABEL 1 71288-744 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 10 mg INTRAVENOUS ANDA 23 sections
Vecuronium Bromide HUMAN PRESCRIPTION DRUG LABEL 1 71288-745 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 20 mg INTRAVENOUS ANDA 23 sections
Vecuronium Bromide HUMAN PRESCRIPTION DRUG LABEL 1 81565-206 INJECTION, POWDER, FOR SOLUTION 10 mg INTRAVENOUS ANDA 21 sections
Vecuronium Bromide HUMAN PRESCRIPTION DRUG LABEL 1 83301-0056 INJECTION 10 mg INTRAVENOUS ANDA 21 sections
Vecuronium Bromide HUMAN PRESCRIPTION DRUG LABEL 1 83301-0057 INJECTION 20 mg INTRAVENOUS ANDA 21 sections