Details of the Drug

General Information of Drug (ID: DM473VD)

Drug Name
Mivacurium
Synonyms
Mivacron; Chlorure de mivacurium; Chlorure de mivacurium [French]; Cloruro de mivacurio; Cloruro de mivacurio [Spanish]; MIVACURIUM CHLORIDE; Mivacurii chloridum; Mivacurii chloridum [Latin]; BW B109OU dichloride; BWB109OU; BW-B1090U; BW-B109OU; MIVACRON IN DEXTROSE 5% IN PLASTIC CONTAINER; Mivacron (TN); Mivacurium chloride(USAN/INN); Mivacurium chloride [USAN:INN:BAN]; Bis[3-[(1R)-6,7-dimethoxy-2-methyl-1-[(3,4,5-trimethoxyphenyl)methyl]-3,4-dihydro-1H-isoquinolin-2-ium-2-yl]propyl] (E)-oct-4-enedioate; Bis[3-[(1R)-6,7-dimethoxy-2-methyl-1-[(3,4,5-trimethoxyphenyl)methyl]-3,4-dihydro-1H-isoquinolin-2-ium-2-yl]propyl] (E)-oct-4-enedioate dichloride; (R)-1,2,3,4-Tetrahydro-2-(3-hydroxypropyl)-6,7-dimethoxy-2-methyl-1-(3,4,5-trimethoxybenzyl)isoquinolinium chloride, (E)-4-octenedioate (2:1)
Indication
Disease Entry ICD 11 Status REF
Anaesthesia 9A78.6 Approved [1]
Therapeutic Class
Neuromuscular Nondepolarizing Agents
Affected Organisms
Humans and other mammals
ATC Code
M03AC10: Mivacurium
M03AC: Other quaternary ammonium compounds
M03A: MUSCLE RELAXANTS, PERIPHERALLY ACTING AGENTS
M03: MUSCLE RELAXANTS
M: MUSCULO-SKELETAL SYSTEM
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 4 Molecular Weight (mw) 1029.3
Logarithm of the Partition Coefficient (xlogp) 8.7
Rotatable Bond Count (rotbonds) 30
Hydrogen Bond Donor Count (hbonddonor) 0
Hydrogen Bond Acceptor Count (hbondacc) 14
ADMET Property
Clearance
The drug present in the plasma can be removed from the body at the rate of 5.2 mL/min/kg [2]
Half-life
The concentration or amount of drug in body reduced by one-half in 1.7 - 2.6 minutes (in healthy young adults administered 0.1 to 0.25 mg/kg mivacurium) [2]
Metabolism
The drug is metabolized via the enzymatic hydrolysis catalyzed by plasma cholinesterase []
MRTD
The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 0.22724 micromolar/kg/day [3]
Unbound Fraction
The unbound fraction of drug in plasma is 0.7% [2]
Vd
Fluid volume that would be required to contain the amount of drug present in the body at the same concentration as in the plasma 0.27 L/kg [2]
Chemical Identifiers
Formula
C58H80N2O14+2
IUPAC Name
bis[3-[(1R)-6,7-dimethoxy-2-methyl-1-[(3,4,5-trimethoxyphenyl)methyl]-3,4-dihydro-1H-isoquinolin-2-ium-2-yl]propyl] (E)-oct-4-enedioate
Canonical SMILES
C[N+]1(CCC2=CC(=C(C=C2[C@H]1CC3=CC(=C(C(=C3)OC)OC)OC)OC)OC)CCCOC(=O)CC/C=C/CCC(=O)OCCC[N+]4(CCC5=CC(=C(C=C5[C@H]4CC6=CC(=C(C(=C6)OC)OC)OC)OC)OC)C
InChI
InChI=1S/C58H80N2O14/c1-59(25-21-41-35-47(63-3)49(65-5)37-43(41)45(59)29-39-31-51(67-7)57(71-11)52(32-39)68-8)23-17-27-73-55(61)19-15-13-14-16-20-56(62)74-28-18-24-60(2)26-22-42-36-48(64-4)50(66-6)38-44(42)46(60)30-40-33-53(69-9)58(72-12)54(34-40)70-10/h13-14,31-38,45-46H,15-30H2,1-12H3/q+2/b14-13+/t45-,46-,59?,60?/m1/s1
InChIKey
ILVYCEVXHALBSC-OTBYEXOQSA-N
Cross-matching ID
PubChem CID
5281042
ChEBI ID
CHEMBL6958
CAS Number
133814-19-4
UNII
77D66S9Q93
DrugBank ID
DB01226
TTD ID
D0OB2M
Drug ADMET Endpoint Profile (DAE)NEW Click to Jump to the Detailed DAE Information of This Drug

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Neuronal acetylcholine receptor alpha-2 (CHRNA2) TTF4E0J ACHA2_HUMAN Antagonist [4]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Disease Different from Mivacurium (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Paromomycin DM1AGXN Major Additive neuromuscular blocking effects by the combination of Mivacurium and Paromomycin. Amoebiasis [1A36] [5]
Fosphenytoin DMOX3LB Moderate Increased metabolism of Mivacurium caused by Fosphenytoin mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [6]
Levobetaxolol DMSREPX Moderate Additive neuromuscular blocking effects by the combination of Mivacurium and Levobetaxolol. Glaucoma [9C61] [7]
Lincomycin DMVTHER Moderate Additive neuromuscular blocking effects by the combination of Mivacurium and Lincomycin. Gram-positive bacterial infection [1B74-1F40] [8]
Penbutolol DM4ES8F Moderate Additive neuromuscular blocking effects by the combination of Mivacurium and Penbutolol. Hypertension [BA00-BA04] [9]
Nebivolol DM7F1PA Moderate Additive neuromuscular blocking effects by the combination of Mivacurium and Nebivolol. Hypertension [BA00-BA04] [9]
Metoclopramide DMFA5MY Moderate Additive neuromuscular blocking effects by the combination of Mivacurium and Metoclopramide. Nausea/vomiting [MD90] [10]
Dexamethasone DMMWZET Moderate Additive neuromuscular blocking effects by the combination of Mivacurium and Dexamethasone. Rheumatoid arthritis [FA20] [11]
Vecuronium DMP0UK2 Moderate Additive neuromuscular blocking effects by the combination of Mivacurium and Vecuronium. Tonus and reflex abnormality [MB47] [12]
Plazomicin DMKMBES Major Additive neuromuscular blocking effects by the combination of Mivacurium and Plazomicin. Urinary tract infection [GC08] [5]
⏷ Show the Full List of 10 DDI Information of This Drug

References

1 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7243).
2 Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds
3 Estimating the safe starting dose in phase I clinical trials and no observed effect level based on QSAR modeling of the human maximum recommended daily dose
4 Pharmacological characteristics of the inhibition of nondepolarizing neuromuscular blocking agents at human adult muscle nicotinic acetylcholine receptor. Anesthesiology. 2009 Jun;110(6):1244-52.
5 Burkett L, Bikhazi GB, Thomas KC Jr, Rosenthal DA, Wirta MG, Foldes FF "Mutual potentiation of the neuromuscular effects of antibiotics and relaxants." Anesth Analg 58 (1979): 107-15. [PMID: 571233]
6 Liberman BA, Norman P, Hardy BG "Pancuronium-phenytoin interaction: a case of decreased duration of neuromuscular blockade." Int J Clin Pharmacol Ther Toxicol 26 (1988): 371-4. [PMID: 3220609]
7 Harrah MD, Way WL, Katzung BG "The interaction of d-tubocurarine with antiarrhythmic drugs." Anesthesiology 33 (1970): 406-10. [PMID: 5512329]
8 Alahdal O, Bevan DR "Clindamycin-induced neuromuscular blockade." Can J Anaesth 42 (1995): 614-7. [PMID: 7553999]
9 Chapple DJ, Clark JS, Hughes R "Interaction between atracurium and drugs used in anaesthesia." Br J Anaesth 55 Suppl 1 (1983): s17-22. [PMID: 6688011]
10 Multum Information Services, Inc. Expert Review Panel.
11 Agencia Espaola de Medicamentos y Productos Sanitarios Healthcare "Centro de informacion online de medicamentos de la AEMPS - CIMA.".
12 Pandit SK, Ferres CJ, Gibson FM, Mirakhur RK "Time course of action of combinations of vecuronium and pancuronium." Anaesthesia 41 (1986): 151-4. [PMID: 2869710]