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Description

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.

CNS Activity

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency
3.69 nM [IC50]

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
MIVACRON

Cmax

ValueDoseCo-administeredAnalytePopulation
504 ng/mL
0.15 mg/kg single, intravenous
MIVACURIUM, CIS-CIS- plasma
Homo sapiens
2198 ng/mL
0.15 mg/kg single, intravenous
MIVACURIUM, CIS-TRANS- plasma
Homo sapiens
4486 ng/mL
0.15 mg/kg single, intravenous
MIVACURIUM, TRANS-TRANS- plasma
Homo sapiens

AUC

ValueDoseCo-administeredAnalytePopulation
1.295 μg × min/mL
0.15 mg/kg single, intravenous
MIVACURIUM, CIS-CIS- plasma
Homo sapiens
1.178 μg × min/mL
0.15 mg/kg single, intravenous
MIVACURIUM, CIS-TRANS- plasma
Homo sapiens
2.932 μg × min/mL
0.15 mg/kg single, intravenous
MIVACURIUM, TRANS-TRANS- plasma
Homo sapiens

T1/2

ValueDoseCo-administeredAnalytePopulation
28.5 min
0.15 mg/kg single, intravenous
MIVACURIUM, CIS-CIS- plasma
Homo sapiens
2 min
0.15 mg/kg single, intravenous
MIVACURIUM, CIS-TRANS- plasma
Homo sapiens
2.4 min
0.15 mg/kg single, intravenous
MIVACURIUM, TRANS-TRANS- plasma
Homo sapiens

Doses

AEs

PubMed

Sample Use Guides

In Vivo Use Guide
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
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.
Definition References