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

Stem definitionDrug idCAS RN
neuromuscular blocking agents with rigid structure 2183 68399-58-6

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • pipecuronium
  • pipecuronium bromide
A piperazinyl androstane derivative which is a non-depolarizing neuromuscular blocking agent (NEUROMUSCULAR NONDEPOLARIZING AGENTS). It is used as a muscle relaxant during ANESTHESIA and surgical procedures.
  • Molecular weight: 602.90
  • Formula: C35H62N4O4
  • CLOGP: 0.63
  • LIPINSKI: 1
  • HAC: 8
  • HDO: 0
  • TPSA: 59.08
  • ALOGS: -6.85
  • ROTB: 6

  • Status: OFM

  • 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) 39 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.12 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
Vd (Volume of distribution) 0.35 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 3 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.98 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 1.90 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
June 26, 1990 FDA

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
ATC M03AC06 MUSCULO-SKELETAL SYSTEM
MUSCLE RELAXANTS
MUSCLE RELAXANTS, PERIPHERALLY ACTING AGENTS
Other quaternary ammonium compounds
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

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Muscle relaxation, function indication 11977004

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 4.95 Basic
pKa2 4.34 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 WOMBAT-PK CHEMBL
Neuronal acetylcholine receptor; alpha4/beta2 Ion channel WOMBAT-PK
Neuronal acetylcholine receptor; alpha2/beta4 Ion channel WOMBAT-PK
Neuronal acetylcholine receptor; alpha4/beta4 Ion channel WOMBAT-PK

External reference:

IDSource
4019895 VUID
N0000147980 NUI
C0071102 UMLSCUI
D00764 KEGG_DRUG
108455007 SNOMEDCT_US
4019895 VANDF
33742 RXNORM
373725008 SNOMEDCT_US
d00956 MMSL
013423 NDDF
CHEMBL1200722 ChEMBL_ID
R6ZTY81RE1 UNII
4645 INN_ID
52212-02-9 SECONDARY_CAS_RN
DB01338 DRUGBANK_ID
CHEBI:8230 CHEBI
CHEMBL1201206 ChEMBL_ID
D017300 MESH_DESCRIPTOR_UI
50192 PUBCHEM_CID

Pharmaceutical products:

None