2-O-Substituted Cyclodextrins as Reversal Agents for the Neuromuscular Blocker Rocuronium Bromide

Tarver, Gary J.; Grove, Simon J. A.; Buchanan, Kirsteen; Bom, A.; Cooke, Andrew; Rutherford, Samantha; Zhang, Ming Qiang

doi:10.1016/s0968-0896(02)00026-3

Cited by 37 publications

(22 citation statements)

References 10 publications

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“…The bradycardia observed in three P. expansa was attributed to the use of neostigmine, which has muscarinic side effects 14 , and not to rocuronium, since this drug exerts minimal action upon the cardiovascular system 12 . This finding was reinforced by the satisfactory response to the administration of atropine.…”

Section: Discussionmentioning

confidence: 95%

“…Loss of pupillary reflex occurred basically in G2, and can be explained by two hypotheses: excessively deep degree of neuromuscular blockage due to an excessive dosage, which would inactivate this reflex 4 , or a muscarinic side effect of neostigmine 10,14 . Handling was directly affected by the dose, which is consistent with what was reported for T. carolina major 7 .…”

Section: Discussionmentioning

confidence: 99%

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The use of rocuronium in giant Amazon turtle Podocnemis expansa (Schweigger, 1812) (Testudines, Podocnemididae)

et al. 2009

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Purpose: To determine whether rocuronium would provide safe, short-term immobilization in Podocnemis expansa. Methods: Twenty P. expansa, weighing on average 1.59 ± 0.28 kg, were subjected to two protocols: G1 0.25 mg/kg IM of rocuronium and 0.07 mg/kg IM of neostigmine, while G2 received 0.50 mg/kg IM of rocuronium and 0.07 mg/kg IM of neostigmine. The drugs were applied, respectively, in the left and right thoracic members. Assessments were made of the anesthetic parameters of respiratory frequency, heartbeat, righting reflex, cloacal relaxation, palpebral and pupilar reflexes, easy handling, muscle relaxation, locomotion, response to pain stimuli in the right thoracic members, pelvic members and tail, ambient humidity and temperature. Results: They were not found statistical differences between the dosages for the majority of the assessments. G1 was as efficient as G2. A consistent neuromuscular blockade effect was recorded 12 ± 4.21 minutes in G1 and G2. All the animals were recovered in 150 minutes. Conclusions: Administration of rocuronium at dose of 0.25 to 0.5 mg/kg IM is a safe and effective adjunct to clinical proceedings or pre-anesthetics in P. expansa. Because rocuronium does not provide any analgesic or sedative effects, the duration of neuromuscular blockade without anesthesia should be minimized to avoid undue stress. Key words: Anesthetics. Neuromuscular Blocking Agents. Reptiles. RESUMOObjetivo: Determinar se o rocurônio promove imobilização segura e de curta duração em Podocnemis expansa. Métodos: Vinte P. expansa com média de peso 1,59 ± 0,28 kg, foram submetidas a dois protocolos: G1 recebeu rocurônio 0,25 mg/kg IM e neostigmina 0,07 mg/kg IM enquanto G2 rocurônio 0,50 mg/kg IM e neostigmina 0,07 mg/kg IM, aplicados no membro torácico esquerdo e direito, respectivamente. Observaram-se os parâmetros anestésicos: freqüência respiratória e cardíaca, reflexo de endireitamento, relaxamento do esfíncter da cloaca, reflexo palpebral e pupilar, facilidade de manipulação, relaxamento muscular, locomoção, resposta aos estímulos dolorosos no membro torácico direito, nos membros pelvinos e na cauda, temperatura e umidade ambiental. Resultados: Não foram encontradas diferenças estatísticas entre as doses para a maioria dos parâmetros e o G1 foi tão eficiente quanto o G2. Um bloqueio neuromuscular consistente foi observado aos 12 ± 4,21 minutos tanto no G1 como no G2. A recuperação de todos os animais ocorreu em até 150 minutos. Conclusões: Administração de rocurônio nas doses 0,25 e 0,50 mg/kg IM é segura e efetiva para os procedimentos clínicos ou pré-anestésicos em P. expansa. Como o rocurônio não produz efeitos sedativos ou analgésicos, a duração do bloqueio neuromuscular sem anestesia deverá ser minimizado para evitar estresse.

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Section: Discussionmentioning

confidence: 95%

Section: Discussionmentioning

confidence: 99%

The use of rocuronium in giant Amazon turtle Podocnemis expansa (Schweigger, 1812) (Testudines, Podocnemididae)

et al. 2009

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“…Cyclodextrins are not metabolized following IV administration and are excreted by the kidneys. While cyclodextrins as a chemical class are not universally nontoxic, some cyclodextrins used pharmacologically appear to be safe [37][38][39][40].…”

Section: Cyclodextrinsmentioning

confidence: 99%

Sugammadex: the first selective binding reversal agent for neuromuscular block

Kovac

2009

Journal of Clinical Anesthesia

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“…16,[54][55][56] Cyclodextrins are cyclic dextrose units joined through 1-4 glycosyl bonds, and are produced from starch or starch derivates using cyclodextrin glycosyltransferase. The three most common cyclodextrins consist of six, seven, or eight cyclic oligosaccharides and are named α-, β-, or γ-cyclodextrin, respectively.…”

Section: Sugammadex Pharmacologymentioning

confidence: 99%

“…Because of the intermolecular (van der Waals) forces, the thermodynamic (hydrogen) bonds, and the hydrophobic interactions, sugammadex forms very tight complexes at a 1:1 ratio with steroidal neuromuscular blocking agents (rocuronium  vecuronium  pancuronium). 16,[54][55][56] The sugammadex-rocuronium complex has a very high association rate (an association constant of 10 7 M -1 as determined by isothermal titration calorimetry) and a very low dissociation rate. It is estimated that only one out of every 25 million sugammadex-rocuronium complexes dissociates.…”

Section: Sugammadex Pharmacologymentioning

confidence: 99%

Selective reversal of muscle relaxation in general anesthesia: focus on sugammadex

Naguib¹

2009

DDDT

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Despite the significant improvements in the pharmacology of muscle relaxants in the past six decades, the search for the ideal muscle relaxant continues, mainly because of the incomplete efficacy and persistent side effects associated with their antagonism. Clinical concerns remain about the residual paralysis and hemodynamic side effects associated with the classic pharmacologic reversal agents, the acetylcholinesterase inhibitors. Although the development of the "ideal muscle relaxant" remains illusory, pharmacologic advancements hold promise for improved clinical care and patient safety. Recent clinical advances include the development of short-acting nondepolarizing muscle relaxant agents that have fast onset and a very rapid metabolism that allows reliable and complete recovery; and the development of selective, "designer" reversal agents that are specific for a single drug or class of drugs. This article reviews recent developments in the pharmacology of these selective reversal agents: plasma cholinesterases, cysteine, and sugammadex. Although each of the selective reversal agents is specific in its substrate, the clinical use of the combination of muscle relaxant with its specific reversal agent will allow much greater intraoperative titrating ability, decreased side effect profile, and may result in a decreased incidence of postoperative residual paralysis and improved patient safety.

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2-O-Substituted Cyclodextrins as Reversal Agents for the Neuromuscular Blocker Rocuronium Bromide

Cited by 37 publications

References 10 publications

The use of rocuronium in giant Amazon turtle Podocnemis expansa (Schweigger, 1812) (Testudines, Podocnemididae)

The use of rocuronium in giant Amazon turtle Podocnemis expansa (Schweigger, 1812) (Testudines, Podocnemididae)

Sugammadex: the first selective binding reversal agent for neuromuscular block

Selective reversal of muscle relaxation in general anesthesia: focus on sugammadex

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