Structure, conformation, and action of neuromuscular blocking drugs †

Lee, C.

doi:10.1093/bja/87.5.755

Cited by 53 publications

(30 citation statements)

References 74 publications

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“…2 The strategy of bivalent ligands has been successfully implemented for searching for acetylcholinesterase inhibitors. 8,9 Furthermore, many of them have been tested as antimalarial drugs. There are some examples in the literature of dimeric molecules acquiring properties that are completely different from those of the precursor molecules.…”

Section: Introductionmentioning

confidence: 99%

New quaternary ammonium camphor derivatives and their antiviral activity, genotoxic effects and cytotoxicity

Соколова

Yarovaya

Shernyukov

et al. 2013

Bioorganic & Medicinal Chemistry

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The synthesis and biological evaluation of a novel series of dimeric camphor derivatives are described. The resulting compounds were studied for their antiviral activity, cyto- and genotoxicity. Compounds 3a and 3d in which the quaternary nitrogen atoms are separated by the C5H10 and С9H18 aliphatic chain, exhibited the highest efficiency as an agent inhibiting the reproduction of the influenza virus A(H1N1)pdm09. The cytotoxicity data of compounds 3 and 4 revealed their moderate activity against malignant cell lines; compound 3f had the highest activity for the CEM-13 cells. These results show close agreement with the data of independent studies on toxicity of these compounds, in particular that the toxicity of compounds strongly depends on spacer length.

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Section: Introductionmentioning

confidence: 99%

New quaternary ammonium camphor derivatives and their antiviral activity, genotoxic effects and cytotoxicity

Соколова

Yarovaya

Shernyukov

et al. 2013

Bioorganic & Medicinal Chemistry

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“…13 These data, however, may not be valid for vecuronium. Because the neuromuscular potency of vecuronium is six times greater than that of rocuronium (ED 95 = 0.05 and 0.30 mg/kg, respectively) 1 and their molecular weight is similar (637 and 610 Da, respectively, http://www.scbt.com/datasheet-205880.html; accessed December 15, 2015), fewer vecuronium than rocuronium molecules produce similar degrees of neuromuscular block. To encapsulate 1.0 mg vecuronium 3.4 mg of sugammadex is necessary, and to encapsulate the intubating dose (e.g., 7.0 mg), 2.4 mg sugammadex is sufficient.…”

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confidence: 99%

Reversal of Vecuronium-induced Neuromuscular Blockade with Low-dose Sugammadex at Train-of-four Count of Four

et al. 2017

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Background Rocuronium-induced neuromuscular block that spontaneously recovered to a train-of-four count of four can be reversed with sugammadex 0.5 or 1.0 mg/kg. We investigated whether these doses of sugammadex can also reverse vecuronium at a similar level of block. Methods Sixty-five patients were randomly assigned, and 64 were analyzed in this controlled, superiority study. Participants received general anesthesia with propofol, sevoflurane, fentanyl, and vecuronium. Measurement of neuromuscular function was performed with acceleromyography (TOF-Watch-SX, Organon Teknika B.V., The Netherlands ). Once the block recovered spontaneously to four twitches in response to train-of-four stimulation, patients were randomly assigned to receive sugammadex 0.5, 1.0, or 2.0 mg/kg; neostigmine 0.05 mg/kg; or placebo. Time from study drug injection to normalized train-of-four ratio 0.9 and the incidence of incomplete reversal within 30 min were the primary outcome variables. Secondary outcome was the incidence of reparalysis (normalized train-of-four ratio less than 0.9). Results Sugammadex, in doses of 1.0 and 2.0 mg/kg, reversed a threshold train-of-four count of four to normalized train-of-four ratio of 0.9 or higher in all patients in 4.4 ± 2.3 min (mean ± SD) and 2.6 ± 1.6 min, respectively. Sugammadex 0.5 mg/kg reversed the block in 6.8 ± 4.1 min in 70% of patients (P < 0.0001 vs. 1.0 and 2.0 mg/kg), whereas neostigmine produced reversal in 11.3 ± 9.7 min in 77% of patients (P > 0.05 vs. sugammadex 0.5 mg/kg). The overall frequency of reparalysis was 18.7%, but this incidence varied from group to group. Conclusions Sugammadex 1.0 mg/kg, unlike 0.5 mg/kg, properly reversed a threshold train-of-four count of four vecuronium-induced block but did not prevent reparalysis.

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“…This type of anesthesia includes inhalational anesthesia [6] combined with intravenous administration of opioids [7], nondepolarizing M relaxation [8][9][10], and a continuous caudal epidural block [11].…”

Section: Discussionmentioning

confidence: 99%

Influence of anesthesia on the results of intraoperative diagnostic electromyostimulation in patients with anorectal malformation

Mixa

Škába

Kraus

et al. 2011

Journal of Pediatric Surgery

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Structure, conformation, and action of neuromuscular blocking drugs †

Cited by 53 publications

References 74 publications

New quaternary ammonium camphor derivatives and their antiviral activity, genotoxic effects and cytotoxicity

New quaternary ammonium camphor derivatives and their antiviral activity, genotoxic effects and cytotoxicity

Reversal of Vecuronium-induced Neuromuscular Blockade with Low-dose Sugammadex at Train-of-four Count of Four

Influence of anesthesia on the results of intraoperative diagnostic electromyostimulation in patients with anorectal malformation

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