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      Effects of rocuronium and vecuronium on initial rundown of endplate potentials in the isolated phrenic nerve diaphragm preparation of rats

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          Abstract

          Rocuronium and vecuronium, two non-depolarizing neuromuscular blockers, have been widely used in surgery procedures. However, their electrophysiological properties need to be more widely explored. We examined the effects of rocuronium and vecuronium on initial rundown of endplate potential amplitudes in the non-uniform stretched muscle preparation of the rat isolated phrenic nerve diaphragm. More specifically, the endplate potentials were recorded with one microelectrode from a single endplate. The effects of rocuronium or vecuronium each at 4 concentrations (0.5 ×, l ×, 2 ×, 4 × EC95; EC95 = concentration of the drug required to produce the inhibitory effect by 95%) on the amplitude of endplate potentials and its rundown were observed. Treatment of the isolated rat phrenic nerve-diaphragm preparation with rocuronium (2.5–20 μg/ml) or vecuronium (0.5–4 μg/ml) decreased the amplitude of endplate potentials and inhibited its rundown in a concentration-dependent manner. At the concentration (2.5 μg/ml for rocuronium and 0.5 μg/ml for vecuronium) that did not alter the endplate potential amplitude, the onset of reduced endplate potential rundown was 3 and 5 min after administration of rocuronium or vecuronium, respectively. The results suggest that rocuronium and vecuronium block the neuromuscular junction presynaptically and that rocuronium does it faster than vecuronium.

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          Rocuronium (ORG 9426) neuromuscular blockade at the adductor muscles of the larynx and adductor pollicis in humans.

          The effects of rocuronium, 0.25 or 0.5 mg.kg-1, were measured simultaneously on the adductor muscles of the larynx and adductor pollicis in 14 adult patients. Anaesthesia was induced and maintained with propofol and fentanyl. Tracheal intubation was performed without muscle relaxants. The recurrent laryngeal and ulnar nerves were both stimulated supramaximally, at the notch of the thyroid cartilage and at the wrist respectively, using train-of-four stimulation. The laryngeal response was evaluated by measuring the pressure change in the cuff of a tracheal tube positioned between the vocal cords. Onset time, intensity of blockade and duration of action were less at the larynx than at the adductor pollicis. After rocuronium, 0.25 mg.kg-1, the onset time (interval between injection and maximal T1 blockade) was 1.6 +/- 0.1 min and 3.0 +/- 0.3 min (mean +/- SEM) at the laryngeal muscles and adductor pollicis, respectively (P less than 0.01 between muscles). Maximum blockade was 37 +/- 8% and 69 +/- 8%, respectively (P less than 0.05), and time to 90% T1 recovery was 7 +/- 1 min and 20 +/- 4 min, respectively (P less than 0.05). With 0.5 mg.kg-1, the onset time was also more rapid at the vocal cords (1.4 +/- 0.1 min) than at the adductor pollicis (2.4 +/- 0.2 min, P less than 0.001). Maximum blockade was 77 +/- 5% and 98 +/- 1%, respectively (P less than 0.01), and time to 90% T1 recovery was 22 +/- 3 min and 37 +/- 4 min, respectively (P less than 0.01).(ABSTRACT TRUNCATED AT 250 WORDS)
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            Current concepts in neuromuscular transmission.

            The neuromuscular junction (NMJ) is structured and powered to transduce electrical activity from the distal nerve terminal of a motor neurone via the neuromuscular cleft to the post-junctional muscle membrane to ultimately generate muscle contraction. Our understanding of this complex function has expanded over many years, and the NMJ has served as a prototype for how different synapses operate in the peripheral and central nervous systems. The NMJ has a presynaptic part which is synonymous with the distal nerve ending, being responsible for neurotransmitter synthesis, packaging into vesicles, and subsequent vesicle transportation to active release sites where vesicle docking, fusion, and release of acetylcholine and other co-released transmitters finally take place. The synaptic cleft, filled with large molecular complexes that guarantee ultrastructural NMJ arrangement and signal transduction, allows for rapid diffusion and degradation of the neurotransmitter. The postsynaptic part consists of a folded muscle membrane into which nicotinic acetylcholine receptors (nAChRs) directly opposite the presynaptic active release sites are mounted and fixed by a cytoskeleton. This specialized postsynaptic region is closely associated with the perijunctional zone where a high density of sodium channels promote and amplify the signal in order to guarantee the propagation of the electrical activity to generate muscle contraction. The transduction process is maintained at load (i.e. high stimulus frequency) by a presynaptic mechanism allowing for sustained transmitter release over time at high demand. This positive feedback mechanism relies on neuronal nAChRs present on the distal nerve terminal, whereas the continuation of the transduction process at the postsynaptic part relies on the classical muscle type nAChR. In this review, we will focus on recent findings of potential clinical importance that will advance our understanding of the effects of neuromuscular blocking agents and neuromuscular monitoring and also our management of disorders of the neuromuscular system within anaesthesia and intensive care.
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              Prejunctional and postjunctional cholinoceptors at the neuromuscular junction.

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                Author and article information

                Contributors
                junlinavy@yahoo.com.cn
                junlinavy@yahoo.com.cn
                hzhang@hsc.wvu.edu
                Journal
                Springerplus
                Springerplus
                SpringerPlus
                Springer International Publishing AG (Cham )
                2193-1801
                11 April 2013
                11 April 2013
                2013
                : 2
                : 155
                Affiliations
                [1 ]Department of Anesthesiology, Navy General Hospital of PLA, Beijing, 100037 China
                [2 ]Departments of Behavioral Medicine & Psychiatry and Physiology & Pharmacology, West Virginia University Health Sciences Center, Morgantown, WV 26506 USA
                Article
                216
                10.1186/2193-1801-2-155
                3639353
                23641322
                7c5de1f5-52fe-476a-8a8f-9ec201ab5a8e
                © Li et al.; licensee Springer. 2013

                This article is published under license to BioMed Central Ltd. This is an Open Access article distributed under the terms of the Creative Commons Attribution License ( http://creativecommons.org/licenses/by/2.0), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

                History
                : 23 December 2012
                : 4 April 2013
                Categories
                Research
                Custom metadata
                © The Author(s) 2013

                Uncategorized
                rocuronium,vecuronium,motor endplate,neuromuscular junction,diaphragm
                Uncategorized
                rocuronium, vecuronium, motor endplate, neuromuscular junction, diaphragm

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