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

Stem definitionDrug idCAS RN
neuromuscular blocking agents with rigid structure 2052 15500-66-0

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • pancuronium bromide
  • bromurex
  • pancuronium
  • pancuronium dibromide
A bis-quaternary steroid that is a competitive nicotinic antagonist. As a neuromuscular blocking agent it is more potent than CURARE but has less effect on the circulatory system and on histamine release.
  • Molecular weight: 572.87
  • Formula: C35H60N2O4
  • CLOGP: 1.21
  • LIPINSKI: 1
  • HAC: 6
  • HDO: 0
  • TPSA: 52.60
  • ALOGS: -8.32
  • 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) 67 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.17 ┬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) 0.20 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 1.50 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.09 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 1.90 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Oct. 24, 1972 FDA

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
ATC M03AC01 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:48873 cholinergic antagonist
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
Asthenia contraindication 13791008
Disorder of lung contraindication 19829001 DOID:850
Renal failure syndrome contraindication 42399005 DOID:1074
Body fluid retention contraindication 43498006
Decreased cardiac function contraindication 43650005
Acidosis contraindication 51387008
Kidney disease contraindication 90708001 DOID:557
Myasthenia gravis contraindication 91637004 DOID:437
Disease of liver contraindication 235856003 DOID:409
Disorder of electrolytes contraindication 237840007
Carcinomatosis contraindication 307593001
Hypoxia contraindication 389086002
Obesity contraindication 414916001 DOID:9970
Complete Biliary Obstruction contraindication

Acid dissociation constants calculated using MoKa v3.0.0

None

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 8.20 WOMBAT-PK CHEMBL
Neuronal acetylcholine receptor; alpha4/beta2 Ion channel IC50 8.26 WOMBAT-PK
Acetylcholine receptor; alpha1/beta1/delta/gamma Ion channel IC50 7.09 CHEMBL

External reference:

IDSource
4018513 VUID
N0000178946 NUI
C0030311 UMLSCUI
D00492 KEGG_DRUG
350064000 SNOMEDCT_US
4019874 VANDF
7883 RXNORM
373738000 SNOMEDCT_US
d00330 MMSL
013421 NDDF
CHEMBL185073 ChEMBL_ID
CHEMBL1200757 ChEMBL_ID
U9LY9Y75X2 UNII
2489 INN_ID
DB01337 DRUGBANK_ID
CHEBI:7907 CHEBI
D010197 MESH_DESCRIPTOR_UI
441289 PUBCHEM_CID
4001 IUPHAR_LIGAND_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Pancuronium Bromide HUMAN PRESCRIPTION DRUG LABEL 1 0409-4646 INJECTION, SOLUTION 1 mg INTRAVENOUS ANDA 12 sections