Details
| Stereochemistry | MIXED |
| Molecular Formula | C58H80N2O14.2HO |
| Molecular Weight | 1063.2755 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 2 / 4 |
| E/Z Centers | 1 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
[OH-].[OH-].COC1=CC(C[C@H]2C3=CC(OC)=C(OC)C=C3CC[N+]2(C)CCCOC(=O)CC\C=C\CCC(=O)OCCC[N+]4(C)CCC5=CC(OC)=C(OC)C=C5[C@H]4CC6=CC(OC)=C(OC)C(OC)=C6)=CC(OC)=C1OC
InChI
InChIKey=FXHLWQXSTCTSDZ-VBBWHNEHSA-L
InChI=1S/C58H80N2O14.2H2O/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;2*1H2/q+2;;/p-2/b14-13+;;/t45-,46+,59?,60?;;
Mivacurium chloride (Mivacron) is a new benzylisoquinolinium choline-like diester neuromuscular blocking drug with an onset of action at equipotent doses that is comparable to atracurium and vecuronium but slower than succinylcholine. MIVACRON (a mixture of three stereoisomers) binds competitively to cholinergic receptors on the
motor end-plate to antagonize the action of acetylcholine, resulting in a block of neuromuscular
transmission. This action is antagonized by acetylcholinesterase inhibitors, such as neostigmine. MIVACRON is a short-acting neuromuscular blocking agent indicated for inpatients and outpatients,
as an adjunct to general anesthesia, to facilitate tracheal intubation and to provide skeletal muscle
relaxation during surgery or mechanical ventilation.
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
| 3.69 nM [IC50] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | MIVACRON Approved UseMIVACRON is a short-acting neuromuscular blocking agent indicated for inpatients and outpatients, as an adjunct to general anesthesia, to facilitate tracheal intubation and to provide skeletal muscle relaxation during surgery or mechanical ventilation. Launch Date1992 |
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
504 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9054251/ |
0.15 mg/kg single, intravenous dose: 0.15 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered: |
MIVACURIUM, CIS-CIS- plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
2198 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9054251/ |
0.15 mg/kg single, intravenous dose: 0.15 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered: |
MIVACURIUM, CIS-TRANS- plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
4486 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9054251/ |
0.15 mg/kg single, intravenous dose: 0.15 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered: |
MIVACURIUM, TRANS-TRANS- plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
1.295 μg × min/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9054251/ |
0.15 mg/kg single, intravenous dose: 0.15 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered: |
MIVACURIUM, CIS-CIS- plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
1.178 μg × min/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9054251/ |
0.15 mg/kg single, intravenous dose: 0.15 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered: |
MIVACURIUM, CIS-TRANS- plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
2.932 μg × min/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9054251/ |
0.15 mg/kg single, intravenous dose: 0.15 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered: |
MIVACURIUM, TRANS-TRANS- plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
28.5 min EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9054251/ |
0.15 mg/kg single, intravenous dose: 0.15 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered: |
MIVACURIUM, CIS-CIS- plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
2 min EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9054251/ |
0.15 mg/kg single, intravenous dose: 0.15 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered: |
MIVACURIUM, CIS-TRANS- plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
2.4 min EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9054251/ |
0.15 mg/kg single, intravenous dose: 0.15 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered: |
MIVACURIUM, TRANS-TRANS- plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
Doses
| Dose | Population | Adverse events |
|---|---|---|
0.2 mg/kg single, intravenous Recommended Dose: 0.2 mg/kg Route: intravenous Route: single Dose: 0.2 mg/kg Sources: Page: p.12 |
unhealthy Health Status: unhealthy Condition: Skeletal muscle relaxation during surgery Sources: Page: p.12 |
Other AEs: Anaphylactic reaction... Other AEs: Anaphylactic reaction (grade 3-5) Sources: Page: p.12 |
AEs
| AE | Significance | Dose | Population |
|---|---|---|---|
| Anaphylactic reaction | grade 3-5 | 0.2 mg/kg single, intravenous Recommended Dose: 0.2 mg/kg Route: intravenous Route: single Dose: 0.2 mg/kg Sources: Page: p.12 |
unhealthy Health Status: unhealthy Condition: Skeletal muscle relaxation during surgery Sources: Page: p.12 |
PubMed
| Title | Date | PubMed |
|---|---|---|
| The effect of mivacurium pretreatment on intra-ocular pressure changes induced by suxamethonium. | 1998 May |
|
| Suxamethonium and mivacurium sensitivity from pregnancy-induced plasma cholinesterase deficiency. | 1998 Nov |
|
| Organophosphorus pesticide-induced butyrylcholinesterase inhibition and potentiation of succinylcholine toxicity in mice. | 1999 |
|
| Intubation conditions and postoperative myalgia in outpatient dental surgery: a comparison of succinylcholine with mivacurium. | 2000 Apr |
|
| Is succinylcholine after pretreatment with d-tubocurarine and lidocaine contraindicated for outpatient anesthesia? | 2000 Aug |
|
| Nondepolarizing neuromuscular blockers inhibit the serotonin-type 3A receptor expressed in Xenopus oocytes. | 2000 Feb |
|
| The cardiovascular effects of mivacurium in hypertensive patients. | 2002 Aug |
|
| [Plasma cholinesterase variations as a result of prolonged neuromuscular blockade. Review and problems encountered in two cases of prolonged neuromuscular blockade after muscle relaxation with succinylcholine as compared to mivacurium]. | 2002 Feb |
|
| Prevention of succinylcholine-induced fasciculation and myalgia: a meta-analysis of randomized trials. | 2005 Oct |
|
| Unexpected prolonged paralysis after mivacurium in a patient with Bamforth syndrome. | 2006 Aug |
|
| Distinct pharmacologic properties of neuromuscular blocking agents on human neuronal nicotinic acetylcholine receptors: a possible explanation for the train-of-four fade. | 2006 Sep |
|
| Fresh frozen plasma transfusion for reversal of prolonged post-anaesthesia apnoea. | 2008 Apr |
Sample Use Guides
Adults
Initial Doses
Doses of 0.15 mg/kg administered over 5 to 15 seconds, 0.20 mg/kg administered over 30 seconds,
or 0.25 mg/kg administered in divided doses (0.15 mg/kg followed in 30 seconds by 0.10 mg/kg) are
recommended for facilitation of tracheal intubation for most patients
Route of Administration:
Intravenous
In Vitro Use Guide
Curator's Comment: Left atrial preparations were stimulated by electrical field stimulation using a bipolar platinum electrode, and the effects of cumulative concentrations of nondepolarizing neuromuscular blocking agents on the developed force in the presence and absence of propranolol (10(-8) M) and desipramine (10(-7) M) were recorded.
The left or right atria of rats were removed and suspended in organ baths. Mivacurium was added cumulatively (10(-9)-10(-5) M) in the presence and absence of the nonselective β-blocker propranolol (10(-8) M) and the noradrenaline reuptake inhibitor desipramine (10(-7) M), and heart rate changes were recorded in spontaneously beating right atria. Mivacurium increased developed force in a dose-dependent manner; the increases were significant at 10(-5) M concentration for mivacurium.
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135390842
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FM8VA7ORPP
Created by
admin on Fri Dec 15 15:36:25 GMT 2023 , Edited by admin on Fri Dec 15 15:36:25 GMT 2023
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ACTIVE MOIETY
SUBSTANCE RECORD
