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You are in Home >> Resources >> Pharmacology >> Neuromuscular blockade and reversal
Sugammadex Created: 22/2/2010Updated: 30/11/2011
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Neuromuscular Blockade Reversal
Sugammadex 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.1–12
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
Key features of Sugammadex
Unique mode of action (first-in-class SRBA)2 Rapid reversal from any depth* of rocuronium- or vecuronium-induced neuromuscular blockade 3,4,11,12
Significantly faster speed of reversal versus neostigmine 3,4,11,12 Generally well tolerated. Safety and tolerability studied in ~1700 patients 1,2,5,13–15 Low risk of residual blockade1 Dosing for multiple situations (e.g. immediate, moderate and deep block reversal)1
Mode of Action
Sugammadex 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
Pharmacokinetic Properties of Bridion
Please consult the sugammadex Summary of Product Characteristics for more detailed information.1
Distribution Sugammadex has a steady-state volume of distribution of approximately 11–14 litres. Neither sugammadex nor the complex of sugammadex and rocuronium bind to plasma proteins or erythrocytes. When given as an intravenous bolus dose of 1–16 mg/kg, sugammadex exhibits linear kinetics.1
Metabolism
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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
Recommended Adult Doses of Bridion
The 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
Body weight (kg) Recommended dose
mg ml
30 60 0.6
35 70 0.7
40 80 0.8
45 90 0.9
50 100 1.0
55 110 1.1
60 120 1.2
65 130 1.3
70 140 1.4
75 150 1.5
80 160 1.6
85 170 1.7
90 180 1.8
95 190 1.9
100 200 2.0*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
Body weight (kg) Recommended dose
mg ml
30 120 1.2
35 140 1.4
40 160 1.6
45 180 1.8
50 200 2.0
55 220 2.2
60 240 2.4
65 260 2.6
70 280 2.8
75 300 3.0
80 320 3.2
85 340 3.4
90 360 3.6
95 380 3.8
100 400 4.0*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
Body weight (kg) Recommended dose
mg ml
30 480 4.8
35 560 5.6
40 640 6.4
45 720 7.2
50 800 8.0
55 880 8.8
60 960 9.6
65 1040 10.4
70 1120 11.2
75 1200 12.0
80 1280 12.8
85 1360 13.6
90 1440 14.4
95 1520 15.2
100 1600 16.0*All volumes given have been rounded to the nearest practical volume.
References
1. 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): 575–581.
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): 816–824.
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 13–17, 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): 1020–1025.
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): 913–918.
8. McCourt KC, Salmela L, Mirakhur RK, et al. Comparison of rocuronium and suxamethonium for use during rapid sequence induction of anaesthesia. Anaesthesia 1998: 53 (9): 867–871.
9. Andrews JJ, Kumar N, van den Brom RH, Olkkola KT, Roest GJ, Wright PM. A large simple randomized trial of rocuronium versus succinylcholine in rapid-sequence induction of anaesthesia along with propofol. Acta Anaesthesiol Scand 1999:43(1): 4–8.
10. Perry J, Lee JS, Sillberg VA, Wells GA. Rocuronium versus succinylcholine for rapid sequence induction intubation. Cochrane Database Syst Rev 2008 16;(2):CD002788.
11. Blobner M, Eriksson L, Scholz J, Hillebrand H, Pompei L. Sugammadex (2.0 mg/kg) reverses shallow rocuronium-induced neuromuscular blockade significantly faster compared with neostigmine (50 µg/kg). Eur J Anaesthesiol 2007;24(Suppl. 39):125 [Abstract 9AP7-10]
12. Alvarez-Gómez JA, Wattwill M, Vanacker B, Lora-Tamayo JI, Khünl-Brady KS. Reversal of vecuronium-induced shallow neuromuscular blockade is significantly faster with sugammadex compared with neostigmine. Eur J Anaesthesiol 2007;24(Suppl. 39):124–25 [Abstract 9AP7-8].
13. McDonagh DL, Benedict PE, Kovac AL, Drover DR, Brister NW. Efficacy and safety of sugammadex for reversal of rocuronium-induced neuromuscular blockade in adults and elderly patients. Poster presented at the Annual Meeting of the American Society of Anesthesiologists, October 13–17, 2007; San Francisco, California, USA.
14. Amao R, Zornow MH, McTaggart Cowan R, Cheng DCH, Allard M. Sugammadex safely reverses rocuronium-induced blockade in patients with pulmonary disease. Poster presented at the Annual Meeting of the American Society of Anesthesiologists, October 13–17, 2007; San Francisco, California, USA.
15. Dahl V, Pendeville PE, Hollmann MW, et al. Safety and efficacy of sugammadex for the reversal of rocuronium-induced neuromuscular blockade in cardiac patients undergoing noncardiac surgery. Eur J Anaesthesiol 2009 May 18. [Epub ahead of print].
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