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Sugammadex

Created: 22/2/2010 Updated: 30/11/2011

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Neuromuscular Blockade ReversalSugammadex is a selective relaxant binding agent (SRBA) that provides rapid reversal from neuromuscular blockade induced by the nondepolarising neuromuscular blocking agents (NMBAs) rocuronium and vecuronium.1,2 Sugammadex enables rapid reversal from any depth of neuromuscular blockade, has no effect on the cholinergic nervous system, minimises the risk of residual paralysis and potentially offers a new alternative to suxamethonium for rapid sequence induction.112 First Selective Relaxant Binding Agent Sugammadex is a synthetic, modified gamma-cyclodextrin and is the first and only selective relaxant binding agent (SRBA).1,2 Sugammadex is a unique reversal agent because it encapsulates and then inactivates rocuronium and vecuronium rather than counteracting their effects. With this innovative mode of action, Bridion provides rapid reversal of neuromuscular blockade caused by these neuromuscular blocking agents.2

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Key features of SugammadexUnique mode of action (first-in-class SRBA)2 Rapid reversal from any depth* of rocuronium- or vecuronium-induced neuromuscular blockade Significantly faster speed of reversal versus neostigmine 3,4,11,12 Generally well tolerated. Safety and tolerability studied in ~1700 patients 1,2,5,1315 Low risk of residual blockade1 Dosing for multiple situations (e.g. immediate, moderate and deep block reversal) 1

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Mode of ActionSugammadex forms a complex with the neuromuscular blocking agents (NMBAs) rocuronium or vecuronium in the plasma. By forming complexes with these NMBAs, sugammadex reduces their ability to bind to nicotinic receptors in the neuromuscular junction and thereby reverses neuromuscular blockade.1 Upon injection of sugammadex, any rocuronium or vecuronium molecules present in the plasma are attracted to sugammadex via lipophilic interactions and are bound in a ratio of one sugammadex molecule to one molecule of the NMBA.1,2 This causes a concentration gradient and any remaining rocuronium or vecuronium molecules are attracted back into the plasma and become bound to free sugammadex molecules.2

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Pharmacokinetic Properties of BridionPlease consult the sugammadex Summary of Product Characteristics for more detailed information. 1 Distribution Sugammadex has a steady-state volume of distribution of approximately 1114 litres. Neither sugammadex nor the complex of sugammadex and rocuronium bind to plasma proteins or erythrocytes. When given as an intravenous bolus dose of 116 mg/kg, sugammadex exhibits linear kinetics.1

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Nausea and vomiting Neuroanaesthesia Obstetric Anaesthesia Regional anaesthesia Thromboelastometry Airway Equipment Breathing circuits Central venous access Depth of anaesthesia Laryngoscopes Medical Equipment Medical gases Monitoring & Physical principles Scavenging Simulators in Anaesthesia Temperature Ultrasound Vapourisers Ventilation Beta-blockers Inhalational agents Neuromuscular blockade and reversal Local anaesthetics Opioids Pharmacology Body weight (kg) Recommended dose mg 30 35 40 45 50 55 60 65 70 75 80 85 60 70 80 90 100 110 120 130 140 150 160 170 180 190 200 ml 0.6 0.7 0.8 0.9 1.0 1.1 1.2 1.3 1.4 1.5 1.6 1.7 1.8 1.9 2.0 Metabolism In preclinical and clinical studies no metabolites of sugammadex have been observed and only renal excretion of the unchanged product was observed as the route of elimination.1 Elimination The elimination half-life of sugammadex is 1.8 hours and the estimated rate of clearance from the plasma is 88 ml/min. Almost all (>90%) sugammadex is excreted within 24 hours of administration. 1

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Recommended Adult Doses of BridionThe recommended dose of sugammadex depends on the level of neuromuscular blockade to be reversed. The recommended dose, however, does not depend on the anaesthetic regimen being used. The tables below give recommended adult dosages for the reversal of rocuronium-induced neuromuscular blockade only. Please consult the sugammadex Summary of Product Characteristics for more detailed information on dosing and administration.1 Adult dosage guides (a) Reversal of shallow neuromuscular blockade induced by rocuronium* Use Bridion at a dose of 2 mg/kg (reversal likely within 1.2 and 1.5 minutes)5

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*All volumes given have been rounded to the nearest practical volume. (b) Reversal of profound neuromuscular blockade induced by rocuronium* Use Bridion at a dose of 4 mg/kg (reversal likely within 2.3 and 3.3 minutes) 5

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Ethics - articles and literature 65 Renal - articles and literature Haematology-articles and literature Neurosciences - Articles Metabolic - articles and literature Gastro - articles and literature Cardiac articles and literature *All volumes given have been rounded to the nearest practical volume. (c) Immediate reversal of neuromuscular blockade induced by rocuronium* Use Bridion at a dose of 16 mg/kg (reversal likely within 5.7 and 6.7 minutes)5 70 75 80 85 90 95 100 260 280 300 320 340 360 380 400 2.6 2.8 3.0 3.2 3.4 3.6 3.8 4.0

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rviews/jobs Body weight (kg) Recommended dose mg 30 35 40 45 50 55 60 65 70 75 80 85 90 95 100 480 560 640 720 800 880 960 1040 1120 1200 1280 1360 1440 1520 1600 ml 4.8 5.6 6.4 7.2 8.0 8.8 9.6 10.4 11.2 12.0 12.8 13.6 14.4 15.2 16.0

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References1. Bridion (Sugammadex) Summary of Product Characteristics available via the electronic Medicines Compendium. [Accessed July 2009]. 2. Naguib M. Sugammadex: another milestone in clinical neuromuscular pharmacology. Anesth Analg 2007; 104(3): 575581. 3. Jones KR, Caldwell JE, Brull SJ, Soto RG. Reversal of profound rocuronium-induced blockade with sugammadex: a randomized comparison with neostigmine.Anesthesiology 2008; 109(5): 816824. 4. Lemmens, HJM, El-Orbany MI, Berry J, Martin G. Sugammadex reverses profound vecuronium blockade more rapidly than neostigmine. Poster presented at the Annual Meeting of the American Society of Anesthesiologists, October 1317, 2007; San Francisco, California, USA. 5. Schering Plough. Data on file, 2008. 6. Lee C, Jahr JS, Candiotti K, et al. Reversal of profound neuromuscular block by sugammadex administered three minutes after rocuronium: a comparison with spontaneous recovery from succinylcholine. Anesthesiology 2009; 110(5): 10201025. 7. Magorian,T, Flannery KB, Miller RD. Comparison of rocuronium, succinylcholine, and vecuronium for rapid-sequence induction of anesthesia in adult patients. Anesthesiology 1993: 79 (5): 913918.

8. McCourt KC, Salmela L, Mirakhur RK, et al. Comparison of roc