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
S (Water solubility) 21 mg/mL Bocci G, Oprea TI, Benet LZ

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 102.64 44.66 74 1713 272530 63214705
Bradycardia 102.60 44.66 47 1740 73180 63414055
Neuromuscular block prolonged 102.37 44.66 17 1770 525 63486710
Hyperthermia malignant 95.05 44.66 17 1770 817 63486418
Cardiac arrest 89.22 44.66 46 1741 92499 63394736
Anaphylactic shock 81.37 44.66 29 1758 23604 63463631
Blood pressure decreased 58.79 44.66 31 1756 64991 63422244
Arteriospasm coronary 58.68 44.66 15 1772 3953 63483282
Anaphylactic reaction 52.72 44.66 29 1758 66071 63421164
Delayed recovery from anaesthesia 51.38 44.66 10 1777 761 63486474
Neuromuscular blockade 46.91 44.66 8 1779 290 63486945

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 148.00 27.96 34 2580 2143 34952174
Anaphylactic reaction 72.16 27.96 39 2575 32262 34922055
Neuromuscular block prolonged 63.11 27.96 13 2601 488 34953829
Cardiac arrest 60.46 27.96 53 2561 96106 34858211
Hypotension 53.93 27.96 74 2540 221575 34732742
Fear 48.92 27.96 21 2593 10455 34943862
Renal injury 41.22 27.96 19 2595 11176 34943141
Post procedural complication 37.83 27.96 18 2596 11370 34942947
Injury 35.39 27.96 21 2593 20666 34933651
Anhedonia 34.73 27.96 15 2599 7570 34946747
Bradycardia 34.70 27.96 35 2579 75383 34878934
Emotional distress 33.11 27.96 18 2596 15008 34939309
Ventricular tachycardia 32.96 27.96 22 2592 26557 34927760
Blood creatine phosphokinase increased 32.77 27.96 27 2587 44830 34909487
Drug interaction 32.02 27.96 59 2555 225887 34728430
Renal impairment 29.84 27.96 36 2578 94477 34859840
Metabolic acidosis 29.24 27.96 25 2589 43655 34910662
Unevaluable event 28.92 27.96 22 2592 32568 34921749
Ventricular fibrillation 28.45 27.96 19 2595 22935 34931382
Serotonin syndrome 28.39 27.96 18 2596 19915 34934402
Urine analysis abnormal 28.04 27.96 9 2605 1992 34952325

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 215.47 27.81 46 4267 2871 79737204
Hypotension 122.73 27.81 134 4179 440183 79299892
Neuromuscular block prolonged 121.70 27.81 24 4289 1006 79739069
Cardiac arrest 117.46 27.81 87 4226 172009 79568066
Anaphylactic reaction 113.10 27.81 65 4248 83678 79656397
Bradycardia 98.01 27.81 71 4242 135486 79604589
Anaphylactic shock 89.14 27.81 42 4271 35954 79704121
Fear 81.32 27.81 34 4279 21952 79718123
Renal injury 68.77 27.81 28 4285 16899 79723176
Anaesthetic complication 67.82 27.81 18 4295 2841 79737234
Delayed recovery from anaesthesia 66.92 27.81 16 4297 1657 79738418
Blood pressure decreased 62.64 27.81 48 4265 99418 79640657
Procedural complication 61.05 27.81 21 4292 7962 79732113
Arteriospasm coronary 60.58 27.81 20 4293 6696 79733379
Drug interaction 59.35 27.81 91 4222 415092 79324983
Ventricular tachycardia 57.74 27.81 33 4280 41902 79698173
Anhedonia 54.95 27.81 23 4290 14875 79725200
Chemical peritonitis 54.23 27.81 10 4303 291 79739784
Unevaluable event 54.04 27.81 35 4278 55550 79684525
Post procedural complication 53.47 27.81 26 4287 23803 79716272
Tachycardia 52.54 27.81 56 4257 177712 79562363
Respiratory acidosis 50.59 27.81 20 4293 11180 79728895
Renal impairment 48.92 27.81 51 4262 157732 79582343
Injury 47.90 27.81 37 4276 77459 79662616
Multiple organ dysfunction syndrome 46.79 27.81 44 4269 120202 79619873
Serotonin syndrome 45.36 27.81 29 4284 44998 79695077
Ventricular fibrillation 43.61 27.81 25 4288 31901 79708174
Emotional distress 43.41 27.81 27 4286 39942 79700133
Respiratory failure 43.18 27.81 51 4262 180860 79559215
Metabolic acidosis 39.60 27.81 34 4279 82495 79657580
Shock 38.86 27.81 26 4287 43522 79696553
Rhabdomyolysis 38.70 27.81 37 4276 103094 79636981
Extrasystoles 36.15 27.81 14 4299 7405 79732670
Hyperthermia 35.48 27.81 18 4295 18019 79722056
Bronchospasm 35.38 27.81 20 4293 24839 79715236
Ventricular extrasystoles 33.98 27.81 18 4295 19686 79720389
Blood creatine phosphokinase increased 33.28 27.81 28 4285 66062 79674013
Haemodynamic instability 33.19 27.81 17 4296 17365 79722710
Renal failure 32.84 27.81 47 4266 200921 79539154
Carcinoid crisis 31.61 27.81 7 4306 516 79739559
Neuromuscular blockade 30.89 27.81 7 4306 573 79739502
Tryptase increased 30.07 27.81 7 4306 646 79739429

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
FDA EPC N0000175720 Nondepolarizing Neuromuscular Blocker
FDA PE N0000175732 Neuromuscular Nondepolarizing Blockade
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

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 0409-1632 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 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 0703-2914 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 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 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 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 63323-781 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 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 67457-438 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 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