mivacurium 🐶 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 1822 133814-19-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • mivacurium
  • mivacurium chloride
An isoquinoline derivative that is used as a short-acting non-depolarizing agent.
  • Molecular weight: 1029.28
  • Formula: C58H80N2O14
  • CLOGP: 2.54
  • LIPINSKI: 2
  • HAC: 16
  • HDO: 0
  • TPSA: 144.90
  • ALOGS: -7.53
  • ROTB: 30
  • Status: OFM
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

PropertyValueReference
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.23 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) 0.27 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 5.20 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.70 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 0.83 hours Lombardo F, Berellini G, Obach RS

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 -0.180 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 16.711 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 0.617 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 5.321 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 28.660 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 60.820 % High 1
herg hERG pIC50 4.581 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 2.958 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 54.576 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 21.630 % High 1
kinase-safety-class ACVR2A,ACVR2B,AKT3,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,GSK3B,ITK,JAK2,MAP2K6,MAP3K21,MAP3K7,MAPK10,MAPK7,MAPK9,MAPKAPK2,MTOR,NTRK2,PAK4,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TTK 45
kinase-selectivity-class AXL,DDR1,EIF2AK3,EPHB4,ERBB2,GRK2,PDK4,PIK3CB,PRKDC,SIK2,TEK,TTK 12
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 2.483 High 1
mh-clint Mouse hepatocyte intrinsic clearance 29.785 High 1
mppb Mouse plasma protein binding (% unbound) 36.050 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 5.495 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 68.930 % High 1
rh-clint Rat hepatocyte intrinsic clearance 27.290 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 75.210 % High 1
rppb Rat plasma protein binding (% unbound) 49.710 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 881.049 uM High 1

Approvals:

DateAgencyCompanyOrphan
Jan. 22, 1992 FDA ABBVIE

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC M03AC10 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
FDA EPC N0000175720 Nondepolarizing Neuromuscular Blocker
FDA PE N0000175732 Neuromuscular Nondepolarizing Blockade

Related Drugs by ATC class:

M03AC Other quaternary ammonium compounds 10 drugs
atracuriumcisatracuriumdoxacuriumfazadiniumgallaminehexafluroniumpancuroniumpipecuroniumrocuroniumvecuronium

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
End stage renal disease contraindication 46177005 DOID:784
Burn injury contraindication 48333001
Disorder of cardiovascular system contraindication 49601007 DOID:1287
Acute nephropathy contraindication 58574008
Myasthenia gravis contraindication 91637004 DOID:437
Disease of liver contraindication 235856003 DOID:409
Carcinomatosis contraindication 307593001
Deficiency of cholinesterase contraindication 360607009




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

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 WOMBAT-PK CHEMBL
Neuronal acetylcholine receptor subunit alpha-2 Ion channel WOMBAT-PK

External reference:

IDSource
4020541 VUID
N0000179194 NUI
D00763 KEGG_DRUG
4020276 VANDF
4020541 VANDF
C0066621 UMLSCUI
CHEBI:6958 CHEBI
CHEMBL1182833 ChEMBL_ID
CHEMBL984 ChEMBL_ID
D000077590 MESH_DESCRIPTOR_UI
DB01226 DRUGBANK_ID
7243 IUPHAR_LIGAND_ID
106861-44-3 SECONDARY_CAS_RN
77D66S9Q93 UNII
5281042 PUBCHEM_CID
30077 RXNORM
5125 MMSL
d00951 MMSL
003640 NDDF
013417 NDDF
108446009 SNOMEDCT_US
108447000 SNOMEDCT_US
372493004 SNOMEDCT_US
6226 INN_ID

Pharmaceutical products:

None