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Mivacurium (chloride) Sale

(Synonyms: 二氯美维库铵) 目录号 : GC44209

An antagonist of nAChRs and muscarinic M2 and M3 receptors

Mivacurium (chloride) Chemical Structure

Cas No.:106861-44-3

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产品描述

Mivacurium is an antagonist of nicotinic acetylcholine receptors (nAChRs) and muscarinic M2 and M3 receptors (ED50s = 0.08, 0.3, and 0.1 mg/kg for ex vivo human skeletal muscle nAChRs, guinea pig cardiac M2 receptors, and guinea pig bronchial M3 receptors, respectively). It inhibits acetylcholine-induced activation of neuronal nAChRs (IC50s = 69.04, 3.71, 1.52, and 2.90 for human α3β2-, α3β4-, α4β2-, and α7-containing nAChRs expressed in Xenopus oocytes). Mivacurium also inhibits adult human muscular α1β1εδ-containing nAChRs (IC50 = 3.69 nM in Xenopus oocytes expressing the human recombinant receptor). In vivo, mivacurium inhibits bradycardia and bronchoconstriction induced by vagal stimulation or acetylcholine in guinea pigs. It also induces neuromuscular blockade (ED95 = 80 μg/kg) in sheep with a more rapid onset time than atracurium and vecuronium . Formulations containing mivacurium have been used for pediatric anesthesia.

Chemical Properties

Cas No. 106861-44-3 SDF
别名 二氯美维库铵
Canonical SMILES O=C(OCCC[N+]1(C)CCC(C=C(OC)C(OC)=C2)=C2[C@H]1CC3=CC(OC)=C(OC)C(OC)=C3)CC/C=C/CCC(OCCC[N+]4(C)[C@H](CC5=CC(OC)=C(OC)C(OC)=C5)C(C=C(OC)C(OC)=C6)=C6CC4)=O.[Cl-].[Cl-]
分子式 C58H80N2O14•2Cl 分子量 1100.2
溶解度 DMSO: Soluble,Water: Soluble 储存条件 Store at -20°C
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1 mM 0.9089 mL 4.5446 mL 9.0893 mL
5 mM 0.1818 mL 0.9089 mL 1.8179 mL
10 mM 0.0909 mL 0.4545 mL 0.9089 mL
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Research Update

Mivacurium chloride--a comparative profile

Acta Anaesthesiol Scand Suppl 1995;106:23-5.PMID:8533540DOI:10.1111/j.1399-6576.1995.tb04304.x.

Mivacurium is a new nondepolarizing muscle relaxant of the benzylisoquinoline type. Its short duration of action is due to rapid breakdown by plasma cholinesterase. The dose of Mivacurium which produces 95% inhibition of twitch response (ED95) is between 60 and 80 micrograms/kg. Thus, Mivacurium is 0.8 times and four times as potent as vecuronium and atracurium, respectively. With 2-3 x ED95, tracheal intubation can be accomplished within 2.5 min of intravenous injection. The ensuing DUR25% (time from injection to 25% recovery of control twitch tension) is twice as long as with suxamethonium and about half as long as with equipotent doses of atracurium or vecuronium. For muscle relaxation during long surgical procedures, Mivacurium has been used as a continuous infusion. The average 6-min recovery index after infusion of Mivacurium is particularly favourable for flexible control of muscle paralysis, whereas the recovery indices after infusion of atracurium or vecuronium are 15-30 min. In conclusion, Mivacurium will close the pharmacodynamic gap between suxamethonium and the nondepolarizing muscle relaxants of intermediate duration of action. It will probably also be a suitable alternative to suxamethonium in elective cases.

Mivacurium chloride

Nurse Anesth 1992 Dec;3(4):173-82.PMID:1290779doi

This brief review summarizes the major research to date involving the clinical use of Mivacurium in adults and children. The principle focal points are the pharmacokinetic and pharmacodynamic characteristics of the drug and the side effects that have been commonly observed with its clinical use. Comparisons and contrasts with vecuronium, atracurium, and succinylcholine are made. Particular attention is focused on dosages, infusion rates, recovery characteristics, and individual patient variability.

Clinical pharmacology of Mivacurium chloride: a review

J Clin Anesth 1992 Mar-Apr;4(2):153-63.PMID:1373287DOI:10.1016/0952-8180(92)90034-x.

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. Its clinical duration (injection-25% recovery and injection-95% recovery) is twice that of succinylcholine but one-half to one-third that of atracurium and vecuronium. Mivacurium is easy to use as a continuous infusion and when used this way its recovery characteristics are unchanged. It is readily antagonized by anticholinesterase drugs. The ED95 in adults under narcotic-based anesthesia is 0.07-0.08 mg/kg. At twice the ED95 (0.15 mg/kg) onset time is about 2 to 3 minutes, duration to 25% recovery is 15 to 20 minutes, and 5-95% recovery time about 14 minutes. The mean infusion rate in adults is 6 micrograms/kg/min (range 2-15) with a 5-95% recovery time of 14 minutes. Enflurane and isoflurane require a 20-30% decrease in dosage; halothane, enflurane, and isoflurane prolong the duration of Mivacurium 25-30%. The ED95 in children 2 to 12 years of age is slightly higher (0.09-0.11 mg/kg) with a faster onset and shorter duration. In these young patients, a dose of 0.2 mg/kg has an onset comparable to succinylcholine. Being chemically related to atracurium, Mivacurium may cause histamine release. When administered rapidly at doses of 0.2 mg/kg or greater in adults, histamine release and transient hypotension have been observed. Doses of 0.2 mg/kg or higher are not recommended by the manufacturer. Mivacurium is metabolized by plasma cholinesterase. In vitro, the rate is about 70% that of succinylcholine. In patients with normal or slightly less than normal plasma cholinesterase activity, no prolonged durations of action have been observed. In patients heterozygous for the atypical gene and at a dose of 0.2 mg/kg, 50% prolongation has been shown. Those individuals homozygous for the atypical gene are exquisitely sensitive to Mivacurium and have a markedly prolonged blockade that is readily reversible. In these patients and those with acquired deficiencies, Mivacurium should not be used. The duration of action in elderly patients is comparable to that in the young, while in prerenal transplant patients, its duration is prolonged by about 50%, and in prehepatic transplant patients, duration of block is increased threefold. Mivacurium possesses the advantages of short duration, unchanged recovery characteristics following infusions (without phase II block or tachyphylaxis), and precise control.(ABSTRACT TRUNCATED AT 250 WORDS)

Comparative Analysis of the Anesthesia Effect of Cisatracurium Besylate and Mivacurium chloride Otolaryngology Surgery

Evid Based Complement Alternat Med 2022 Jul 18;2022:6192409.PMID:35899229DOI:10.1155/2022/6192409.

Objective: The aim is to investigate and compare the anesthesia effect of cisatracurium besylate and Mivacurium chloride otolaryngology surgery. Materials and methods: 108 patients who underwent ENT surgery under general anesthesia in our hospital from November 2021 to March 2022 were recruited for retrospective analysis, in which patients in the experimental group A were anesthetized with cisatracurium besylate and patients in the experimental group B were anesthetized with Mivacurium, and the anesthetic effects and recovery of the two groups were compared and analyzed. Results: There was no significant difference in mean arterial pressure, heart rate, and pulse oximetry levels between the two groups at the six time points of admission, anesthesia induction, intubation, end of operation, recovery of consciousness, and extubation (all P > 0.05). The train of four stimulation values at end of operation, recovery of consciousness, and extubation were significantly higher than those of the experimental group A (all P > 0.05). The recovery time of self-consciousness, extubation time, and eye-opening time of the experimental group B were significantly shorter than those of the experimental group A, and the occurrence of agitation was significantly less than that of the experimental group A (all P > 0.05). The total incidence of adverse conditions in the experimental group B was significantly lower than that in the experimental group A (P > 0.05). Conclusion: Compared with cisatracurium besylate in otolaryngology surgery, Mivacurium chloride anesthesia offers a promising route with respect to less impact on hemodynamics, faster postoperative recovery, absence of the accumulation of neuromuscular blockade, less adverse reactions, and higher safety.

Mivacurium chloride and myotonic dystrophy

Br J Anaesth 1995 Oct;75(4):498-9.PMID:7488498DOI:10.1093/bja/75.4.498.

We describe the successful use of the short-acting, non-depolarizing neuromuscular blocking agent, Mivacurium, in a patient with myotonic dystrophy. Increased sensitivity to Mivacurium was demonstrated using train-of-four monitoring, with a single dose of Mivacurium providing adequate block for 90 min of surgery. Spontaneous recovery appeared prolonged with a recovery index (25-75% T1) of 10 min and a recovery time (5-95% T1) of 30 min. The use of reversal agents and anticholinergic agents was avoided.