A Novel Concept of Reversing Neuromuscular Block: Chemical Encapsulation of Rocuronium Bromide by a Cyclodextrin-Based Synthetic Host

Bom, A.; Bradley, Mark; Cameron, Ken; Clark, John K.; Egmond, J. van; Feilden, Helen; MacLean, Elizabeth J.; Muir, Alan W.; Palin, Ronald; Rees, David C.; Zhang, Ming‐Qiang

doi:10.1002/1521-3757(20020118)114:2<275::aid-ange275>3.0.co;2-a

Cited by 250 publications

(399 citation statements)

References 13 publications

Supporting

Mentioning

368

Contrasting

Unclassified

Order By: Relevance

“…First, the complexation of relaxant sugammadex and its breakdown into constituent molecules depends on the propensity of the two substances to associate and to dissociate. 2 Because sugammadex is more selective for rocuronium than for vecuronium (Ka = 1.79 × 10 7 mol/L and 5.72 × 10 6 mol/L, respectively), 8 the complexation is slower with vecuronium than with rocuronium. Second, because the Kd of vecuronium is 0.17 μM versus 0.055 μM for rocuronium, 8 higher relative sugammadex concentrations are required for complex formation with vecuronium compared with rocuronium.…”

supporting

confidence: 84%

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

et al. 2017

View full text Add to dashboard Cite

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.

show abstract

supporting

confidence: 84%

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

et al. 2017

View full text Add to dashboard Cite

show abstract

“…Briefly, sugammadex is a gamma-cyclodextrin, made up of a ring of eight sugars, to which negatively charged side chains were added for the purpose of binding rocuronium and other steroid-based neuromuscular blocking agents. 1,2 The first description of sugammadex appeared in the peer-reviewed literature in 2002. 2 Human trials are underway and the drug should reach market within one to three years.…”

mentioning

confidence: 99%

“…1,2 The first description of sugammadex appeared in the peer-reviewed literature in 2002. 2 Human trials are underway and the drug should reach market within one to three years.…”

mentioning

confidence: 99%

See 1 more Smart Citation

Sugammadex: an opportunity for more thinking or more cookbook medicine?

Donati

2007

Can J Anesth/J Can Anesth

View full text Add to dashboard Cite

“…More specifically, the crystallography services encompass protein crystallography from crystallisation to refined data [2]; small molecule crystallography [3]; wide-spread applications of powder diffraction; and small angle X-ray scattering measurements. We present here examples of work done using the service in all of these areas of scientific interest.…”

mentioning

confidence: 99%

Advances in X-ray optics: improving the performance of sealed-tube-based diffraction systems

Coetzee¹,

Schierbeek²,

Storm³

2004

Acta Cryst Sect A

View full text Add to dashboard Cite

New generation sensitive CCD detectors in combination with recent advances in X-ray optics, have brought problems that were traditionally intractable within scientific reach. With the addition of optics the intensity obtained from a standard sealed tube generator can be significantly increased over the traditional graphite monochromator. Monocapillary glass optics can easily be added to a system. These optics focus the beam, based on total external reflection of x-rays on smooth surfaces. Combining graded multilayer optics [1] with a sealed tube generator allows for the exclusion of a monochromator, since this optics will monochromate the beam. These optics can be configured for maximum parallelism of the beam (Göbel mirrors) or in a side-by-side Kirkpatrick-Baez scheme as conceived by Montel in the 1950's [2] to optimize flux density. This study reviews the advances in optics for Cu radiation, giving representative examples of samples which have been studied, using a sealed tube X-ray generator in combination with a sensitive CCD detector, combined with different optics. Typical results obtained on small crystals of organic molecules, absolute structure configuration of natural products and pharmaceuticals and the screening of proteins are presented. The Daresbury Synchrotron Radiation Source (SRS) provides state-of-the-art analytical techniques from infrared to hard X-ray wavelengths. The unique characteristics of synchrotron radiation are ideal for analytical problems that require high spatial or temporal resolution or problems that are simply intractable using conventional instruments.An increasing number of large-scale facilities exist worldwide, but are traditionally used by universities and higher education institutions for pure research and development. In recognition of the needs of commercial customers, Daresbury Laboratory established DARTS (Daresbury Analytical Research and Technology Service) [1]. DARTS offers unique services which can be tailored to the needs of the customer, allowing access to synchrotron analytical facilities and also the significant expertise and knowledge of staff on site. The analytical portfolio offered by the facility encompasses imaging, spectroscopic and structural characterisation techniques. DARTS also has links to conventional analytical houses for standard analyses should these be required prior to use of the synchrotron. The nature of problems and issues solved by DARTS is varied and includes: investigations of product failure and non-conformance, manufacturing issues, basic R&D and information used in expert witness legal cases.More specifically, the crystallography services encompass protein crystallography from crystallisation to refined data [2]; small molecule crystallography [3]; wide-spread applications of powder diffraction; and small angle X-ray scattering measurements. We present here examples of work done using the service in all of these areas of scientific interest.[1] www.darts.ac.uk [2] J

show abstract

A Novel Concept of Reversing Neuromuscular Block: Chemical Encapsulation of Rocuronium Bromide by a Cyclodextrin-Based Synthetic Host

Cited by 250 publications

References 13 publications

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

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

Sugammadex: an opportunity for more thinking or more cookbook medicine?

Advances in X-ray optics: improving the performance of sealed-tube-based diffraction systems

Contact Info

Product

Resources

About