Anticancer activity of the supercritical extract of Brazilian green propolis and its active component, artepillin C: Bioinformatics and experimental analyses of its mechanisms of action.

Propolis, a resinous substance collected by honeybees by mixing their saliva with plant sources, including tree bark and leaves and then mixed with secreted beeswax, possesses a variety of bioactivities. Whereas caffeic acid phenethyl ester (CAPE) has been recognized as a major bioactive ingredient in New Zealand propolis, Brazilian green propolis, on the other hand, possesses artepillin C (ARC). In this study, we report that, similar to CAPE, ARC docks into and abrogates mortalin-p53 complexes, causing the activation of p53 and the growth arrest of cancer cells. Cell viability assays using ARC and green propolis-supercritical extract (GPSE) revealed higher cytotoxicity in the latter, supported by nuclear translocation and the activation of p53. Furthermore, in vivo tumor suppression assays using nude mice, we found that GPSE and its conjugate with γ cyclodextrin (γCD) possessed more potent anticancer activity than purified ARC. GPSE­Î³CD may thus be recommended as a natural, effective and economic anticancer amalgam.

Supramolecular cyclodextrin-based metal-organic frameworks as efficient carrier for anti-inflammatory drugs.

Drug delivery systems have been used to reduce adverse effects and improve the efficacy of therapies. Drug carriers have been developed over the years, but they have limitations. γ-cyclodextrin-based metal-organic frameworks (γ-CD-MOF) have significant advantages due to their biocompatibility and environmental safety, besides crystallinity and porosity. Herein, γ-CD-MOFs were synthesised with different metals as nodes and investigated. Uniform mesoporous γ-CD-MOFs were obtained and showed an absence of toxicity in HepG2 and Caco-2 cells. The longer controlled release was verified for γ-CD-MOFs, with a maximum of 62% released in 12 h. An inflammation experiment was performed in mice and activity equivalent to the positive control was verified. γ-KCD-MOFs and γ-NaCD-MOFs reached activity after 6 h of administration, however this happened after 24 h in γ-FeCD-MOFs, being more effective than the positive control. Considering the ability for drug entrapment, easy preparation and controlled release, this class of material allows potential applications in drug delivery systems.

Evaluation of the effects of intra-arterial sugammadex and dexmedetomidine: an experimental study / Avaliação dos efeitos de sugamadex e dexmedetomidina intra-arterial: estudo experimental

Abstract Background: Intra-arterial injection of medications may cause acute and severe ischemia and result in morbidity and mortality. There is no information in the literature evaluating the arterial endothelial effects of sugammadex and dexmedetomidine. The hypothesis of our study is that sugammadex and dexmedetomidine will cause histological changes in arterial endothelial structure when administered intra-arterially. Methods: Rabbits were randomly divided into 4 groups. Group Control (n = 7); no intervention performed. Group Catheter (n = 7); a cannula inserted in the central artery of the ear, no medication was administered. Group Sugammadex (n = 7); rabbits were given 4 mg/kg sugammadex into the central artery of the ear, and Group Dexmedetomidine (n = 7); rabbits were given 1 µg/kg dexmedetomidine into the central artery of the ear. After 72 h, the ears were amputated and histologically investigated. Results: There was no significant difference found between the control and catheter groups in histological scores. The endothelial damage, elastic membrane and elastic fiber damage, smooth muscle hypertrophy and connective tissue increase scores in the dexmedetomidine and sugammadex groups were significantly higher than both the control and the catheter groups (p < 0.05). There was no significant difference found between the dexmedetomidine and sugammadex groups in histological scores. Conclusion: Administration of sugammadex and dexmedetomidine to rabbits by intra-arterial routes caused histological arterial damage. To understand the histological changes caused by sugammadex and dexmedetomidine more clearly, more experimental research is needed.

Resumo Justificativa: A injeção intra-arterial de medicamentos pode causar isquemia aguda e grave e resultar em morbidade e mortalidade. Não há informações na literatura que avaliem os efeitos endoteliais arteriais de sugamadex e dexmedetomidina. A hipótese de nosso estudo foi que dexmedetomidina e sugamadex causariam alterações histológicas na estrutura endotelial arterial quando administrados por via intra-arterial. Método: Os coelhos foram randomicamente divididos em quatro grupos: grupo controle (n = 7), sem intervenção; grupo cateter (n = 7), uma cânula foi inserida na artéria central da orelha e medicamentos não foram administrados; grupo sugamadex (n = 7), receberam 4 mg/kg de sugamadex na artéria central da orelha; grupo dexmedetomidina (n = 7), receberam 1 µg/kg de dexmedetomidina na artéria central da orelha. Após 72 horas, as orelhas foram amputadas e histologicamente examinadas. Resultados: Não houve diferença significativa entre os grupos controle e cateter referente aos escores histológicos. Os escores do dano causado ao endotélio e à membrana e fibra elásticas, da hipertrofia do músculo liso e do aumento do tecido conjuntivo foram significativamente maiores nos grupos dexmedetomidina e sugamadex do que nos grupos controle e cateter (p < 0,05). Não houve diferença significativa entre os grupos dexmedetomidina e sugamadex nos escores histológicos. Conclusão: A administração de sugamadex e dexmedetomidina a coelhos por via intra-arterial causou danos arteriais histológicos. Para entender as alterações histológicas causadas por sugamadex e dexmedetomidina com mais clareza, estudos experimentais adicionais são necessários.

Evaluation of the effects of intra-arterial sugammadex and dexmedetomidine: an experimental study.

BACKGROUND: Intra-arterial injection of medications may cause acute and severe ischemia and result in morbidity and mortality. There is no information in the literature evaluating the arterial endothelial effects of sugammadex and dexmedetomidine. The hypothesis of our study is that sugammadex and dexmedetomidine will cause histological changes in arterial endothelial structure when administered intra-arterially. METHODS: Rabbits were randomly divided into 4 groups. Group Control (n=7); no intervention performed. Group Catheter (n=7); a cannula inserted in the central artery of the ear, no medication was administered. Group Sugammadex (n=7); rabbits were given 4mg/kg sugammadex into the central artery of the ear, and Group Dexmedetomidine (n=7); rabbits were given 1µg/kg dexmedetomidine into the central artery of the ear. After 72h, the ears were amputated and histologically investigated. RESULTS: There was no significant difference found between the control and catheter groups in histological scores. The endothelial damage, elastic membrane and elastic fiber damage, smooth muscle hypertrophy and connective tissue increase scores in the dexmedetomidine and sugammadex groups were significantly higher than both the control and the catheter groups (p<0.05). There was no significant difference found between the dexmedetomidine and sugammadex groups in histological scores. CONCLUSION: Administration of sugammadex and dexmedetomidine to rabbits by intra-arterial routes caused histological arterial damage. To understand the histological changes caused by sugammadex and dexmedetomidine more clearly, more experimental research is needed.

The effect of sugammadex on postoperative cognitive function and recovery / O efeito de sugamadex sobre a função cognitiva e recuperação no pós-operatório

Abstract Background and objective: Sugammadex is the first selective relaxant binding agent. When compared with neostigmine, following sugammadex administration patients wake earlier and have shorter recovery times. In this study, we hypothesized that fast and clear awakening in patients undergoing general anesthesia has positive effects on cognitive functions in the early period after operation. Methods: Approved by the local ethical committee, 128 patients were enrolled in this randomized, prospective, controlled, double-blind study. Patients were allocated to either Sugammadex group (Group S) or the Neostigmine group (Group N). The primary outcome of the study was early postoperative cognitive recovery as measured by the Montreal Cognitive Assessment (MoCA) and Mini Mental State Examination (MMSE). After baseline assessment 12-24 h before the operation. After the operation, when the Modified Aldrete Recovery Score was ≥9 the MMSE and 1 h later the MoCA tests were repeated. Results: Although there was a reduction in MoCA and MMSE scores in both Group S and Group N between preoperative and postoperative scores, there was no statistically significant difference in the slopes (p > 0.05). The time to reach TOF 0.9 was 2.19 min in Group S and 6.47 min in Group N (p < 0.0001). Recovery time was 8.26 min in Group S and 16.93 min in Group N (p < 0.0001). Conclusion: We showed that the surgical procedure and/or accompanying anesthetic procedure may cause a temporary or permanent regression in cognitive function in the early postoperative period. However, better cognitive performance could not be proved in the Sugammadex compared to the Neostigmine.

Resumo Justificativa e objetivo: Sugamadex é o primeiro agente de ligação relaxante seletivo. Após a administração de sugamadex, os tempos de despertar e de recuperação dos pacientes são menores, em comparação com neostigmina. Neste estudo, a hipótese foi que um despertar mais rápido e claro dos pacientes submetidos à anestesia geral tem efeitos positivos sobre as funções cognitivas no pós-operatório imediato. Métodos: Após a aprovação do Comitê de Ética local, 128 pacientes foram incluídos neste estudo prospectivo, randômico, controlado e duplo-cego. Os pacientes foram designados para o grupo sugamadex (Grupo S) ou grupo neostigmina (Grupo N). O desfecho primário do estudo foi a recuperação cognitiva no pós-operatório imediato, de acordo com a mensuração da Avaliação de Montreal da Função Cognitiva (MoCA) e com o Mini Exame do Estado Mental (MMSE), após a avaliação inicial 12-24 h antes da operação. Após a operação, quando o escore de recuperação de Aldrete modificado era ≥ 9, o teste MMSE e, uma hora depois, o teste MoCA foram repetidos. Resultados: Embora tenha havido uma redução nos escores de MoCA e MMSE tanto no Grupo S quanto no Grupo N, entre os escores pré- e pós-operatório não houve diferença estatisticamente significativa nas reduções (p > 0,05). O tempo para atingir TOF 0,9 foi de 2,19 min no Grupo S e de 6,47 min no Grupo N (p < 0,0001). O tempo de recuperação foi de 8,26 min no Grupo S e de 16,93 min no Grupo N (p < 0,0001) Conclusão: Mostramos que o procedimento cirúrgico e/ou procedimento anestésico de acompanhamento pode causar uma regressão temporária ou permanente da função cognitiva no pós-operatório imediato. No entanto, um desempenho cognitivo melhor não pode ser provado no grupo sugamadex em comparação com o grupo neostigmina.

The effect of sugammadex on postoperative cognitive function and recovery.

BACKGROUND AND OBJECTIVE: Sugammadex is the first selective relaxant binding agent. When compared with neostigmine, following sugammadex administration patients wake earlier and have shorter recovery times. In this study, we hypothesized that fast and clear awakening in patients undergoing general anesthesia has positive effects on cognitive functions in the early period after operation. METHODS: Approved by the local ethical committee, 128 patients were enrolled in this randomized, prospective, controlled, double-blind study. Patients were allocated to either Sugammadex group (Group S) or the Neostigmine group (Group N). The primary outcome of the study was early postoperative cognitive recovery as measured by the Montreal Cognitive Assessment (MoCA) and Mini Mental State Examination (MMSE). After baseline assessment 12-24h before the operation. After the operation, when the Modified Aldrete Recovery Score was ≥9 the MMSE and 1h later the MoCA tests were repeated. RESULTS: Although there was a reduction in MoCA and MMSE scores in both Group S and Group N between preoperative and postoperative scores, there was no statistically significant difference in the slopes (p>0.05). The time to reach TOF 0.9 was 2.19min in Group S and 6.47min in Group N (p<0.0001). Recovery time was 8.26min in Group S and 16.93min in Group N (p<0.0001). CONCLUSION: We showed that the surgical procedure and/or accompanying anesthetic procedure may cause a temporary or permanent regression in cognitive function in the early postoperative period. However, better cognitive performance could not be proved in the Sugammadex compared to the Neostigmine.

Effect of magnesium sulphate on sugammadex reversal time for neuromuscular blockade: a randomised controlled study.

Magnesium potentiates neuromuscular blockade. Sugammadex reverses rocuronium-induced blockade. The aim of this study was to determine the effect of pre-treatment with magnesium sulphate on sugammadex reversal time for neuromuscular blockade. Seventy-three patients were randomly assigned to receive magnesium sulphate (40 mg.kg(-1) ) or saline intravenously. After anaesthetic induction, continuous train-of-four monitoring was performed and rocuronium was administered (0.6 mg.kg(-1) ). When a second twitch appeared, the patients received sugammadex (2 mg.kg(-1) ). The median (IQR [range]) reversal time of moderate neuromuscular blockade to a train-of-four ratio of 0.9 facilitated by sugammadex was 115 (93-177.5 [68-315]) s in the magnesium group and 120 (105-140 [70-298]) s in the saline group (p = 0.79). The median (IQR [range]) clinical duration was 45 (35.5-53 [22-102]) min in the magnesium group and 37 (31-43 [19-73]) min in the saline group (p = 0.031). Pre-treatment with magnesium did not significantly affect sugammadex reversal time of moderate neuromuscular blockade induced by rocuronium.

Impact of cyclodextrins on postprandial glycemia: evaluation in experimental animal model using the real-time continuous glucose monitoring system.

The impact of cyclodextrins (CDs) on postprandial glycemic response employing the real-time continuous glucose monitoring system (RT-CGMS) was investigated. For this purpose, α-CD, ß-CD, γ-CD, HP-ß-CD, curdlan, and dextrin at doses of 10 and 100 mg/kg were orally administered in rats. The RT-CGMS was efficient to evaluate the impact of CDs on postprandial glycemia. The results showed that α-CD, ß-CD, dextrin, and curdlan did not reduce the glycemic response after the administration of starch. In contrast, the HP-ß-CD (100 mg/kg) attenuated the rise in glycemia. Moreover, the γ-CD blunts the postprandial glycemic excursion at doses of 10 and 100 mg/kg. Therefore, γ-CD could attenuate the rise in glycemia promoted by oral administration of starch. Considering that the treatment of postprandial hyperglycemia is necessary to prevent type 2 diabetes, this study opens the perspective of better control of postprandial glycemia by the addition of γ-CD in food.

Comparison of effects of sugammadex and neostigmine on QTc prolongation in rabbits under general anesthesia.

PURPOSE: To compare the effects of sugammadex and neostigmine, used to antagonize the effects of rocuronium, on the QTc interval. METHODS: This study used 10 adult New Zealand white rabbits of 2.5-3.5 kg randomly divided into two groups: sugammadex group (Group S, n:5) and neostigmine group (Group N, n:5). For general anesthesia administering 2 mg/kg iv propofol and 1 mcg/kg iv fentanyl, 0.6 mg/kg iv rocuronium was given. Later to provide reliable airway for all experimental animals V-Gel Rabbit was inserted. The rabbits were manually ventilated by the same anesthetist. After the V-Gel Rabbit was inserted at 2, 5, 10, 20, 25, 27, 30 and 40 minutes measurements were repeated and recorded. At 25 minutes after induction Group N rabbits were given 0.05 mg/kg iv neostigmine + 0.01 mg/kg iv atropine. Group S were administered 2 mg/kg iv sugammadex. RESULTS: Comparing the QTc interval in the rabbits in Group S and Group N, in the 25th, 27th and 30th minute after muscle relaxant antagonist was administered the QTc interval in the neostigmine group rabbits was significantly increased (p<0.05). CONCLUSION: While sugammadex, administered to antagonize the effect of rocuronium, did not significantly affect the QTc interval, neostigmine+atropine proloned the QTc interval.

Comparison of effects of sugammadex and neostigmine on QTc prolongation in rabbits under general anesthesia

PURPOSE: To compare the effects of sugammadex and neostigmine, used to antagonize the effects of rocuronium, on the QTc interval. METHODS: This study used 10 adult New Zealand white rabbits of 2.5-3.5 kg randomly divided into two groups: sugammadex group (Group S, n:5) and neostigmine group (Group N, n:5). For general anesthesia administering 2 mg/kg iv propofol and 1 mcg/kg iv fentanyl, 0.6 mg/kg iv rocuronium was given. Later to provide reliable airway for all experimental animals V-Gel Rabbit was inserted. The rabbits were manually ventilated by the same anesthetist. After the V-Gel Rabbit was inserted at 2, 5, 10, 20, 25, 27, 30 and 40 minutes measurements were repeated and recorded. At 25 minutes after induction Group N rabbits were given 0.05 mg/kg iv neostigmine + 0.01 mg/kg iv atropine. Group S were administered 2 mg/kg iv sugammadex. RESULTS: Comparing the QTc interval in the rabbits in Group S and Group N, in the 25th, 27th and 30th minute after muscle relaxant antagonist was administered the QTc interval in the neostigmine group rabbits was significantly increased (p<0.05). CONCLUSION: While sugammadex, administered to antagonize the effect of rocuronium, did not significantly affect the QTc interval, neostigmine+atropine proloned the QTc interval. .

In vitro evaluation of antimicrobial features of sugammadex.

BACKGROUND: Drugs administered by intravenous routes may be contaminated during several stages of production or preparation. Sugammadex is a modified gamma cyclodextrin. While research into the antibacterial effects of varieties of cyclodextrin is available, there are no studies focusing on the antibacterial effects of sugammadex. This study investigates the in vitro antimicrobial activity of sugammadex. MATERIALS AND METHODS: The in vitro antimicrobial activity of sugammadex was investigated using the broth microdilution method. The pH of the test solution was determined using a pH meter. The test microorganisms included Staphylococcus aureus ATCC 29213, Enterococcus fecalis ATCC 29212, Escherichia coli ATCC 25922 and Pseudomonas aeruginosa ATCC 27853. In the second phase of the study 100mg/mL sugammadex (50µg) was contaminated with test microorganisms (50µg), including S. aureus ATCC 29213, E. fecalis ATCC 29212, E. coli ATCC 25922 and P. aeruginosa ATCC 27853, left to incubate for 24h and then the bacterial production in sugammadex was evaluated. RESULTS: The pH of the test solutions ranged between 7.25 and 6.97. Using the microdilution method, sugammadex had no antibacterial effect on S. aureus, E. fecalis, E. coli and P. aeruginosa at any concentration. In the second phase of the study bacterial production was observed after 24h in 100mg/mL sugammadex contaminated with the test microorganisms S. aureus, E. fecalis, E. coli and P. aeruginosa. CONCLUSIONS: Sugammadex had no antimicrobial effect on the test microorganisms, S. aureus, E. fecalis, E. coli and P. aeruginosa. Care should be taken that sterile conditions are maintained in the preparation of sugammadex; that the same sugammadex preparation not be used for more than one patient; and that storage conditions are adhered to after sugammadex is put into the injector.

Avaliação in vitro das características antimicrobianas de sugamadex / In vitro evaluation of antimicrobial features of sugammadex / Evaluación in vitro de las características antimicrobianasdel sugammadex

Justificativa e objetivo: os medicamentos administrados por via intravenosa podem ser contaminados durante as várias fases de produção ou preparação. Sugamadex é uma gama-ciclodextrina modificada. Embora muitas pesquisas sobre os efeitos antibacterianos de uma variedade de ciclodextrinas estejam disponíveis, não há estudos dos efeitos antibacterianos de sugamadex. Este estudo investigou a atividade antimicrobiana in vitro de sugamadex. Materiais e métodos: a atividade antimicrobiana in vitro de sugamadex foi investigada pelo método de microdiluição em meio de cultura. O pH da solução de ensaio foi determinado com o uso de um medidor de pH. Os microrganismos-teste analisados incluíram Staphylococcus aureus ATCC 29213, Enterococcus fecalis ATCC 29212, Escherichia coli ATCC 25922 e Pseudomonas aeruginosa ATCC 27853. Na segunda fase do estudo, 100 mg/mL de sugamadex (50 μg) foram contaminados com microrganismos-teste (50 μg), incluindo S. aureus ATCC 29213, E. fecalis ATCC 29212, E. coli ATCC 25922 e P. aeruginosa ATCC 27853, incubados por 24 horas e, em seguida, a produção bacteriana foi avaliada. Resultados: o pH das soluções da análise variaram entre 7,25 e 6,97. Com o uso do método de microdiluição, sugamadex não apresentou efeito antibacteriano contra S. aureus, E. fecalis, E. coli e P. aeruginosa em qualquer concentração. Na segunda fase do estudo, a produção bacteriana foi observada após 24 horas em 100 mg/mL de sugamadex contaminados com os microrganismos-teste S. aureus, E. fecalis, E. coli e P. aeruginosa. .

Background: Drugs administered by intravenous routes may be contaminated during several stages of production or preparation. Sugammadex is a modified gamma cyclodextrin. While research into the antibacterial effects of varieties of cyclodextrin is available, there are no studies focusing on the antibacterial effects of sugammadex. This study investigates the in vitro antimicrobial activity of sugammadex. Materials and methods: The in vitro antimicrobial activity of sugammadex was investigated using the broth microdilution method. The pH of the test solution was determined using a pH meter. The test microorganisms included Staphylococcus aureus ATCC 29213, Enterococcus fecalis ATCC 29212, Escherichia coli ATCC 25922 and Pseudomonas aeruginosa ATCC 27853. In the second phase of the study 100 mg/mL sugammadex (50 μg) was contaminated with test microorganisms (50 μg), including S. aureus ATCC 29213, E. fecalis ATCC 29212, E. coli ATCC 25922 and P. aeruginosa ATCC 27853, left to incubate for 24 h and then the bacterial production in sugammadex was evaluated. Results: The pH of the test solutions ranged between 7.25 and 6.97. Using the microdilution method, sugammadex had no antibacterial effect on S. aureus, E. fecalis, E. coli and P. aeruginosa at any concentration. In the second phase of the study bacterial production was observed after 24 h in 100 mg/mL sugammadex contaminated with the test microorganisms S. aureus, E. fecalis, E. coli and P. aeruginosa. Conclusions: Sugammadex had no antimicrobial effect on the test microorganisms, S. aureus, E. fecalis, E. coli and P. aeruginosa. Care should be taken that sterile conditions are maintained in the preparation of sugammadex; that the same sugammadex preparation not be used for more than one patient; and that storage conditions are adhered to after sugammadex is put into the injector. .

Justificación y objetivo: Los medicamentos administrados por vía intravenosa pueden ser contaminados durante las diversas fases de producción o preparación. El sugammadex es una gamaciclodextrina modificada. Aunque estén disponibles muchas investigaciones sobre los efectos antibacterianos de una variedad de ciclodextrinas, no existen estudios de los efectos antibacterianos del sugammadex. Este estudio investigó la actividad antimicrobiana in vitro del sugammadex. Materiales y métodos: La actividad antimicrobiana in vitro del sugammadex fue investigada por el método de microdilución en medio de cultivo. El pH de la solución de ensayo fue determinado usando un medidor de pH. Los microorganismos testados analizados incluyeron Staphylococcus aureus (S. aureus) (ATCC 29213), Enterococcus faecalis (E. faecalis) (ATCC 29212), Escherichia coli (E. coli) (ATCC 25922) y Pseudomonas aeruginosa (P. aeruginosa) (ATCC 27853). En la segunda fase del estudio, se contaminaron 100 mg/mL de sugammadex (50 µg) con microorganismos testados (50 µg), incluyendo S. aureus (ATCC 29213), E. faecalis (ATCC 29212), E. coli (ATCC 25922) y P. aeruginosa (ATCC 27853), incubados durante 24 h e inmediatamente se calculóla producción bacteriana. Resultados: El pH de las soluciones del análisis varió entre 7,25 y 6,97. Usando el métodode microdilución, el sugammadex no tuvo ningún efecto antibacteriano contra S. aureus, E. faecalis, E. coli y P. aeruginosa en ninguna concentración. En la segunda fase del estudio, la producción bacteriana fue observada después de 24 h en 100 mg/mL de sugammadex contaminados con los microorganismos testados S. aureus, E. faecalis, E. coli y P. aeruginosa. Conclusiones: El sugammadex no presentó ningún efecto antimicrobiano sobre los microorganismos testados S. aureus, E. faecalis, E. coli y P. aeruginosa. ...

Uso del sugammadex para la reversión del bloqueo neuromuscular de larga duración con rocuronio: bolos vs infusión continua / Use of sugammadex for reversal of neuromuscular blockade of long duration with rocuronium: bolus vs continuous infusion

Introducción: El bloqueo neuromuscular residual es causa de complicaciones postoperatorias. Objetivo: Identificar la eficacia del sugammadex para revertir el bloqueo neuromuscular con rocuronio, en procederes de larga duración, cuando éste se administra en forma de bolos versus infusión continua. Método: Se realizó un estudio descriptivo exploratorio en una serie de 10 pacientes para tratamiento quirúrgico de más de dos horas, de forma electiva con anestesia general en el Hospital General Universitario de Alicante, España, entre los meses de noviembre y diciembre del 2010. La inducción y el mantenimiento del bloqueo neuromuscular se realizaron mediante bolos (B) o infusión continua (IC), quedando los pacientes divididos en dos grupos. Se compararon los grupos según el tiempo de recuperación mediante la prueba de U-Mann Whitney. Resultados: Existió homogeneidad entre los grupos en cuanto a edad, peso corporal y estado físico según la ASA II û III. La mediana del tiempo quirúrgico para el grupo B fue de 3:55 horas versus 4:20 horas en el grupo de infusión continua. Para alcanzar el cociente T4/T1 > 90%, la mediana del tiempo de recuperación fue de 75.0 minutos para el grupo IC, mientras en el grupo que se utilizaron bolos se observó un tiempo de 140.0 minutos; las diferencias entre ambos grupos resultaron ser estadísticamente significativas (p = 0,008). Conclusiones: La reversión del bloqueo neuromuscular de larga duración inducido por rocuronio fue más rápida cuando el sugammadex se administró en infusión continua en nuestro grupo de pacientes. (AU)

Uso del sugammadex para la reversión del bloqueo neuromuscular de larga duración con rocuronio: bolos vs infusión continua / Use of sugammadex for reversal of neuromuscular blockade of long duration with rocuronium: bolus vs continuous infusion

Introducción: El bloqueo neuromuscular residual es causa de complicaciones postoperatorias. Objetivo: Identificar la eficacia del sugammadex para revertir el bloqueo neuromuscular con rocuronio, en procederes de larga duración, cuando éste se administra en forma de bolos versus infusión continua. Método: Se realizó un estudio descriptivo exploratorio en una serie de 10 pacientes para tratamiento quirúrgico de más de dos horas, de forma electiva con anestesia general en el Hospital General Universitario de Alicante, España, entre los meses de noviembre y diciembre del 2010. La inducción y el mantenimiento del bloqueo neuromuscular se realizaron mediante bolos (B) o infusión continua (IC), quedando los pacientes divididos en dos grupos. Se compararon los grupos según el tiempo de recuperación mediante la prueba de U-Mann Whitney. Resultados: Existió homogeneidad entre los grupos en cuanto a edad, peso corporal y estado físico según la ASA II – III. La mediana del tiempo quirúrgico para el grupo B fue de 3:55 horas versus 4:20 horas en el grupo de infusión continua. Para alcanzar el cociente T4/T1 > 90%, la mediana del tiempo de recuperación fue de 75.0 minutos para el grupo IC, mientras en el grupo que se utilizaron bolos se observó un tiempo de 140.0 minutos; las diferencias entre ambos grupos resultaron ser estadísticamente significativas (p = 0,008). Conclusiones: La reversión del bloqueo neuromuscular de larga duración inducido por rocuronio fue más rápida cuando el sugammadex se administró en infusión continua en nuestro grupo de pacientes.

SUGAMADEX: novos horizontes para a reversão do bloqueio neuromuscular / SUGAMMADEX: new horizons for the reversal of neuromuscular blockade

O sugamadex é uma droga nova e revolucionária desenvolvida como antagonista seletivo dos agentes bloqueadores neuromusculares (ABNM) esteroides (rocurônio > vecurônio ¼ pancurônio). O medicamento é uma y-ciclodextrina modificada e hidrossolúvel que forma um composto estável com o ABNM na razão de 1:1. Ele se liga ao ABNM livre no plasma, criando um gradiente de concentração que desloca o ABNM dos receptores nicotínicos na junção neuromuscular, levando à reversão completa e duradoura do BNM. O sugamadex não se liga às proteínas ou a qualquer outro receptor no organismo, o que lhe confere ótimo perfil de tolerância. O sugamadex pode ser usado na reversão do BNM profundo, promovendo recuperação mais rápida em relação à succinilcolina. Seu emprego pode diminuir a necessidade de monitorização do BNM, a incidência de bloqueio residual e ainda evitar os efeitos adversos causados pelos anticolinesterásicos e anticolinérgicos. Entretanto, também há limitações em relação à utilização 00 sugamadex. Ele impede o uso dos AB- NMs esteroides durante 24 horas, caso seja necessário novo BNM, e pode aumentar o risco do emprego desnecessário e indiscriminado dos ABNMs. Além disso, faltam dados da sua utilização em alguns grupos populacionais e de seu uso em larga escala. Por fim, deve-se considerar também o fator econômico, visto que se trata de uma droga nova e de valor ainda elevado no mercado...

Sugammadex is a novel and unique compaund designed as a selective antaganist ot steroidal neuromuscular blaeking agents (NMBA) (rocuronium>vecuronium¼pancuronium). The drug is a modified water-saluble y-cyclodextrin that forms a stable complex at a 1:1 ratio with the NMBA. It combines with the NMBA creating a concentration gradient favoring the movement ot the NMBA from the nicotine receptors ot the neuromuscular junction leading to the complete and lasting reversal af the neuromuscular blockade (NMB). Sugamadex does not bind to plasma proteins or any other receptors system in the body what provides him a great tolerance profile. Sugamadex can be used in the reversal af deep neuromuscular blockade with a faster recovery time in relation to succinylcholine. Its use can diminish the necessity af monitoring af the NMB, the incidence ot residual blockade and still prevent the adverse effects caused by the antiecholinesterase and anticholinergic drugs. However, there are limitatians regarding the use af Sugammadex. It hinders the use ot the steroidal NMBA during 24 hours if a new NMB must be restablished and it can increase the risk ot unnecessary and indiscriminate use af the NMBA. Mareaver, there is a laek ot data regarding the its use in some population groups and in large scale. Final/y, the economic factor must be also considered, since it is a new drug with a still raised value in market...