Reversal of neuromuscular blockade: Current concepts & future developments

Journal of Anaesthesiology Clinical Pharmacology

Volumn 25, Issue 4, 2009, Pages 403-412

  Hogg, Rosemary M G ^a   Mirakhur, Rajinder K ^a  

^a QUEEN'S UNIVERSITY BELFAST   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

ACETYLCHOLINESTERASE; AMINOGLYCOSIDE; ATROPINE; CALCIUM CHANNEL BLOCKING AGENT; CHOLINESTERASE INHIBITOR; CYCLODEXTRIN DERIVATIVE; EDROPHONIUM; ETOMIDATE; FLUCLOXACILLIN; FUSIDIC ACID; GLYCOPYRRONIUM BROMIDE; MAGNESIUM SULFATE; NEOSTIGMINE; NEUROMUSCULAR BLOCKING AGENT; ORAL CONTRACEPTIVE AGENT; PANCURONIUM; PLACEBO; PROPOFOL; PYRIDOSTIGMINE; ROCURONIUM; SEVOFLURANE; STEROID; SUGAMMADEX; SUXAMETHONIUM; TOREMIFENE; VECURONIUM;

AMNESIA; ANESTHESIA; BRADYCARDIA; BRONCHIAL MUSCLE TONE; BRONCHOSPASM; CLINICAL PRACTICE; CLINICAL TRIAL; COGNITION; COUGHING; DRUG ANTAGONISM; DRUG DISTRIBUTION; DRUG EFFICACY; DRUG ELIMINATION; DRUG HALF LIFE; DRUG HYPERSENSITIVITY; DRUG MECHANISM; DRUG MEGADOSE; DRUG SAFETY; DRUG TOLERABILITY; DYSGEUSIA; ENZYME INHIBITION; GROUPS BY AGE; HALLUCINATION; HEART DISEASE; HUMAN; HYPOTENSION; HYPOXEMIA; KIDNEY DISEASE; LUNG COMPLICATION; LUNG DISEASE; MUSCLE TONE; NEUROMUSCULAR BLOCKING; NEUROMUSCULAR FUNCTION; NEUROMUSCULAR SYNAPSE; NONHUMAN; OBESITY; REVIEW; SALIVATION; SIDE EFFECT; SMOOTH MUSCLE TONE; STRUCTURE ACTIVITY RELATION; SURGERY; TACHYCARDIA; UPPER RESPIRATORY TRACT OBSTRUCTION;

EID: 70350448420     PISSN: 09709185     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Review

References (99)

1. Griffith HR, Johnson GE. The use of curare in general anaesthesia. Anesthesiology 1942; 3: 418-420
2. Gray TC. d-Tubocurarine chloride. Proc R Soc Med 1948: 41; 559-568
3. Hunter JM. New neuromuscular blocking drugs. N Engl J Med 1995; 332: 1691-1699
4. Bowman WC. Neuromuscular block. Br J Pharmacol 2006; 147: S277-86.
5. Heier T, Caldwell JE, Sessler DI, Miller RD. Mild intraoperative hypothermia increases duration of action and spontaneous recovery of vecuronium blockade during nitrous oxide-isoflurane anesthesia in humans. Anesthesiology 1991: 74: 815-819
6. McCarthy GJ, Elliott P, Mirakhur RK, Cooper R, Sharpe TDE, Clarke RSJ. Onset and duration of action of vecuronium in the elderly: comparison with adults. Acta Anaesthesiol Scand 1992; 36: 383-386
7. Lowry DW, Mirakhur RK, McCarthy GJ, Carroll MT, McCourt KC. Neuromuscular effects of rocuronium during sevoflurane, isoflurane and intravenous anesthesia. Anesth Analg 1998; 87: 936-940 (Pubitemid 28455498)
8. Yamauchi M, Takahashi H, Iwasaki H, Namiki A. Respiratory acidosis prolongs, while alkalosis shortens, the duration and recovery time of vecuronium in humans. J Clin Anesth 2002; 14: 98-101. (Pubitemid 34275461)
9. Caldwell JE. Reversal of residual neuromuscular block with neostigmine at 1 to 4 hours after a single intubating dose of vecuronium. Anesth Analg 1995; 80: 1168-1174
10. Debaene B, Plaud B, Dilly MP, Donati F. Residual paralysis in the PACU after a single intubating dose of nondepolarizing muscle relaxant with an intermediate duration of action. Anesthesiology 2003; 98:1042-1048 (Pubitemid 36520189)
11. Miller RD. Antagonism of neuromuscular blockade. Anesthesiology 1976; 44: 318.
12. Wachtel RE. Comparison of anticholinesterases and their effects on acetylcholine-activated ion channels. Anesthesiology 1990; 72: 496-503. (Pubitemid 20095367)
13. Bevan DR Donati F, Kopman AR. Reversal of neuro-muscular blockade. Anesthesiology 1992; 77: 785-802.
14. Booij LH. Neuromuscular transmission and its pharmacological blockade. Part 3: Continuous infusion of relaxants and reversal and monitoring of relaxation. Pharm World Sci 1997; 19: 35-44.
15. Mirakhur RK, McCarthy GJ. Basic pharmacology of reversal agents. Anesthesiol Clin North America 1993; 11: 237-250
16. Mirakhur RK. Antagonism of neuromuscular blockade, in Bailliere's Clinical Anaesthesiology, Muscle Relaxants, eds Goldhill DR and Flynn PJ, Bailliere Tindall, London, 1994; 8: 461-481
17. Caldwell JE. Clinical limitations of acetylcholinesterase antagonists. J Crit Care 2009; 24: 21-28
18. Cronnelly R, Morris B, Miller RD. Edrophonium: Duration of action & atropine requirement in humans during halothane anaesthesia. Anesthesiology 1982; 57: 261-266 (Pubitemid 12031853)
19. Blitt CD, Moon BJ, Kartchner CD. Duration of action of neostigmine in man. Can Anaesth Soc J 1976; 23: 80-84
20. Young WL, Matteo RS, Omstein E. Duration of action of neostigmine and pyridostigmine in the elderly. Anesth Analg 1988; 67: 775-778
21. Morris RB, Cronnelly R, Miller RD, Stanski DR, Fahey MR. Pharmacokinetics of edrophonium and neostigmine when antagonizing d-tubocurarine neuromuscular blockade in man. Anesthesiology 1981; 54: 399-402. (Pubitemid 11156398)
22. McCoy EP, Mirakhur RK, Maddineni VR, Loan PB. Connolly F. Administration of rocuronium. (Org 9426) by continuous infusion and its reversibility with anticholinesterases. Anaesthesia 1994; 49: 940-945
23. Shorten GD, Ali HH, Goudsouzian NG. Neostigmine and edrophonium antagonism of moderate neuromuscular block induced by pancuronium or tubocurarine. Br J Anaesth 1993; 70: 160-162 (Pubitemid 23042088)
24. Jones JE, Hunter JM, Utting JE. Use o neostigmine in the antagonism of residual neuromuscular blockade produced by vecuronium. Br J Anaesth 1987; 59: 1454-1458 (Pubitemid 17159348)
25. Magorian TT, Lynam DP, Caldwell JE, Miller RD. Can early administration of neostigmine, in single or repeated doses, alter the course of neuromuscular recovery from a vecuronium-induced neuromuscular blockade? Anesthesiology 1990; 73: 410-414
26. Pratt CI. Bronchospasm after neostigmine. Anaesthesia 1988; 43: 248.
27. Simpson KH, Smith RJ, Davies LF. Comparison of the effects of atropine and glycopyrrolate on cognitive function following general anaesthesia. Br J Anaesth 1987; 59: 966-969
28. Mirakhur RK, Dundee JW. Glycopyrrolate: pharmacology and clinical use. Anaesthesia 1983; 38: 1195-1204
29. Saitoh Y, Hattori H, Sanbe N, Nakajima H, Akatu M, Murakawa M. Reversal of vecuronium with neostigmine in patients with diabetes mellitus. Anaesthesia 2004; 59: 750-754 (Pubitemid 39136669)
30. Kim J, Mangold J. Sensitivity to both vecuronium and neostigmine in a sero-negative myasthenic patient. Br J Anaesth 1989; 63: 497-500. (Pubitemid 19254193)
31. Suzuki T, Masaki G, Ogawa S. Neostigmine-induced reversal of vecuronium in normal weight, overweight & obese female patients. Br J Anaesth 2006; 97: 160-163 (Pubitemid 44295699)
32. Fawcett JW, Stone JP. Recurarization in the recovery room following the use of magnesium sulphate. Br J Anaesth 2003; 91: 435-438
33. Van Poorten JF, Dhasmana KM, Kuypers RSM, Erdmann W. Verapamil & reversal of vecuronium neuro-muscular blockade. Anesth Analg 1984; 63: 155-157 (Pubitemid 14181768)
34. Jones RM, Cashman JN, Casson WR, Broadbent MP. Verapamil potentiation of neuromuscular blockade: failure of reversal with neostigmine but prompt reversal with edrophonium. Anesth Analg 1985; 64: 1021-1025
35. Hasfurther DL, Bailey PL. Failure of neuromuscular blockade reversal after rocuronium in a patient who received oral neomycin. Can J Anesth 1996; 43: 617-620
36. Payne JP, Hughes R, Al Azawi S. Neuromuscular block by neostigmine in the anaesthetized man. Br J Anaesth 1982; 52: 69-76. (Pubitemid 10203717)
37. Goldhill DR, Wainwright AP, Stuart CS, Flynn PJ. Neostigmine after spontaneous recovery from neuromuscular blockade. Effect on depth of blockade monitored with train-of-four and tetanic stimuli. Anaesthesia 1989; 44: 293-299
38. Yost CS. Maestrone E. Clinical concentrations of edrophonium enhance desensitization of the nicotinic acetylcholine receptor. Anesth Analg. 1994; 78:520-526 (Pubitemid 24079377)
39. Eikermann M, Zaremba S, Malhotra A, Jordan AS, Rosow C, Chamberlin NL. Neostigmine but not sugammadex impairs upper airway dilator muscle activity and breathing. Br J Anaesth 2008; 101: 344-349
40. Hayes AH, Mirakhur RK, Breslin DS, Reid JE, McCourt KC. Postoperative residual block after intermediate acting neuromuscular blocking drugs. Anaesthesia 2001; 56: 312-318
41. Grayling M, Sweeney BP. Recovery from neuromuscular blockade: a survey of practice. Anaesthesia 2007; 62: 806-809
42. Eriksson LI. Sato M. Severinghaus JW . Effect of a vecuronium-induced partial neuromuscular block on hypoxic ventilatory response. Anesthesiology 1993; 78: 693-699 (Pubitemid 23110043)
43. Eriksson LI, Sundman E, Olsson R et al. Functional assessment of the pharynx at rest and during swallowing in partially paralyzed humans: simultaneous videomanometry and mechanomyography of awake human volunteers. Anesthesiology 1997; 87: 1035-1043 (Pubitemid 27469300)
44. Sundman E. Witt H. Olsson R. Ekberg O. Kuylenstierna R. Eriksson LI. The incidence and mechanisms of pharyngeal and upper esophageal dysfunction in partially paralyzed humans: pharyngeal videoradiography and simultaneous manometry after atracurium. Anesthesiology 2000; 92: 977-984 (Pubitemid 30180973)
45. Berg H. Roed J. Viby-Mogensen J. et al. Residual neuromuscular block is a risk factor for postoperative pulmonary complications. A prospective, randomised, & blinded study of postoperative pulmonary complications after atracurium, vecuronium and pancuronium. Acta Anaesthesiol Scand 1997; 41: 1095-1103 (Pubitemid 27454134)
46. Murphy GS. Szokol JW. Marymont JH. Greenberg SB. Avram MJ. Vender JS. Residual neuromuscular blockade and critical respiratory events in the postanesthesia care unit. Anesth Analg 2008; 107: 130-137
47. Booij LHDJ. Cyclodextrins and the emergence of sugammadex. Anaesthesia 2009; 64 (Suppl 1): 31-37
48. Loftsson T, Masson M. Cyclodextrins in topical drug formulations: theory and practice. Int J Pharm 2001; 225: 15-30. (Pubitemid 32728196)
49. Szetjtli J. Past, present and future of cyclodextrin research. Pure Appl Chem 2004; 76: 1825-1845
50. Loftsson T, Duchene D. Cyclodextrins & their pharmaceutical applications. Int J Pharm 2007; 329: 1-11.
51. Brewster ME. Loftsson T. Cyclodextrins as pharmaceutical solubilizers. Adv Drug Deliv Rev 2007; 59: 645-666
52. Challa R, Ahula A, Ali J, Khar RK. Cyclodextrins in drug delivery: an updated review. AAPS Pharma Sci Tech 2005; 6: S329-57. (Pubitemid 41631739)
53. Zhang M-Q. Drug-specific cyclodextrins: the future of rapid neuromuscular block reversal? Drugs Future 2003; 28: 347-354
54. Tayal G, Kundra S, Grewal A. Sugammadex- new neuromuscular block reversal. J Anaesth Clin Pharmacol 2008; 24: 211-214 (Pubitemid 351845564)
55. Bom A, Bradley M, Cameron K. A novel concept of reversing neuromuscular block: chemical encapsulation of rocuronium bromide by a cyclodextrin-based synthetic host. Angew Chem Int Ed Engl 2002; 41: 266-270 (Pubitemid 34126377)
56. Adam JM, Bennett DJ, Bom A, et al. Cyclodextrin-derived host molecules as reversal agents for the neuromuscular blocker rocuronium bromide: synthesis and structure-activity relationships. J Med Chem 2002; 45: 1806-1816 (Pubitemid 34415376)
57. Tarver GJ, Grove SJA, Buchanan K, et al. 2-O-substituted cyclodextrins as reversal agents for the neuromuscular blocker rocuronium bromide. Bioorg Med Chem 2002; 10: 1819-1827 (Pubitemid 34286374)
58. Booij LHDJ, van Egmond J, Driessen JJ, de Boer HD. In vivo animal studies with sugammadex. Anaesthesia. 2009; 64 (Suppl 1): 38-44.
59. Gijsenbergh F, Ramael S, Houwing N, evan Iersel T. First human exposure of Org 25969. A novel agent to reverse the action of rocuronium bromide. Anesthesiology 2005; 103: 695-703.
60. Sorgenfrei IF, Norrild K, Larsen PB, et al. Reversal of rocuronium-induced neuromuscular block by the selective relaxant binding agent sugammadex: a dose finding and safety study. Anesthesiology 2007; 104: 667-674
61. Sparr HJ, Vermeyen KM, Beaufort AM et al. Early reversal of profound rocuronium-induced neuromuscular blockade by sugammadex in a randomized multicenter study: efficacy, safety and pharmacokinetics. Anesthesiology 2007; 106: 935-943 (Pubitemid 46684059)
62. Staals LM, Snoek MJ, Driessen JJ, Flockton E, Heeringa M, Hunter JM. Multicentre, parallel-group, comparative trial evaluating the efficacy and safety of sugammadex in patients with end-stage renal failure or normal renal function. Br J Anaesth 2008; 101: 492-497
63. Smeets J, Ploeger B, Strougo A, Liefaard L, Kerbusch T. A mechanism-based pharmacokinetic model describing the interaction between sugammadex and rocuronium in patients with normal and impaired renal function. PAGE 17 (2008) Abstr 1276 [www.pagemeeting. org/?abstract=1276].
64. Bom A, Mason R, McIndewar I. Org 25969 causes rapid reversal of rocuronium-induced neuromuscular block, independent of acid-base status. Anesthesiology 2002; 96: A1009.
65. Bom A, van Egmond J, Hope F, et al. Rapid reversal of rocuronium induced neuromuscular block by Org 25969 is independent of renal perfusion. Anesthesiology 2003; 99: A1158.
66. Mason R, Bom A. Org 25969 causes selective reversal of neuromuscular block induced by steroidal NMBAs in anesthetized guinea pigs. Eur J Anaesthesiol 2001; 18: 100.
67. de Boer HD, van Egmond J, van de Pol F, Bom A, Booij LHDJ. Sugammadex, a new reversal agent for neuro-muscular block induced by rocuronium in the anaesthetized Rhesus monkey. Br J Anaesth 2006; 96: 473-479
68. Blobner M, Eriksson L, Scholz J, Hillebrand H, Pompei L. Sugammadex (2mg/kg) significantly faster reverses shallow rocuronium-induced neuromuscular blockade compared with neostigmine (50 ìg/kg). Eur J Anaesthesiol 2007; 24 (Suppl 39): 125-126
69. Suy K, Morias K, Cammu G, Hans P, van Duijnhoven WGF. Effective reversal of moderate rocuronium- or vecuronium-induced neuromuscular block with sugammadex, a selective relaxant binding agent. Anesthesiology 2007; 106: 283-288 (Pubitemid 46185173)
70. Pühringer F, Blaszyk M, Gammu G, Sparr H, Heeringa M. Sugammadex achieves fast recovery from shallow neuromuscular blockade induced by rocuronium or vecuronium: dose-response studies. Eur J Anaesthesiol 2007; 24 (Suppl 39): 111.
71. Shields M, Giovannelli M, Mirakhur RK, Moppett I, Adams J, Hermens Y. Org 25969 (sugammadex), a selective relaxant binding agent for antagonism of prolonged rocuronium-induced neuromuscular block. Br J Anaesth 2006; 96: 36-43. (Pubitemid 43124528)
72. de Boer HD, Driessen JJ, Marcus MAE, Kerkkamp H, Heeringa M, Klimek M. Reversal of rocuronium-induced (1.2 mg/kg) profound neuromuscular block by sugammadex. Anesthesiology 2007; 107: 239-244
73. de Boer HD, van Egmond J, Marcus M, Schouten P, Smeets J, Driessen JJ. Pharmacokinetics of high doses of the selective relaxant binding agent sugammadex, administered shortly after profound rocuronium-induced neuromuscular block. Eur J Anaesthesiol 2006; 23 (Suppl 37): 143.
74. Groudine SB, Soto R, Lien C, Drover D, Roberts K. Randomised, dose finding, phase II study of the selective relaxant binding drug, sugammadex, capable of safely reversing profound rocuronium-induced neuromuscular block. Anesth Analg 2007; 104: 555-562 (Pubitemid 46309872)
75. Duvaldestin P, Kuizenga K, Kjaer CC, Saldieen V, Debaene B. Sugammadex achieves fast recovery from profound neuromuscular blockade induced by rocuronium or vecuronium: a dose response study. Eur J Anaesthesiol 2007; 24 (Suppl 39): 123.
76. Alvarez-Gomez JA, Wattwil M, Vanacker B, Lora-Tamayo JI, Khunl-Brady KS. Reversal of vecuronium-induced shallow neuromuscular blockade is significantly faster with sugammadex compared with neostigmine. Eur J Anaesthesiol 2007; 24 (Suppl 39): 124-125
77. Jones RK, Caldwell JE, Brull S, Soto R. Reversal of profound rocuronium-induced blockade with sugammadex: a randomized comparison with neostigmine. Anesthesiology 2008; 109: 816-824
78. Lemmens HJM, El-Orbany M, Berry J, Martin G. Sugammadex reverses profound vecuronium blockade more rapidly than neostigmine. Anesthesiology 2007; 107: A1578.
79. Vanacker BF, Vermeyen KM, Struys MMRF et al. Reversal of rocuronium-induced neuromuscular block with the novel drug sugammadex is equally effective under maintenance anesthesia with propofol or sevoflurane. Anesth Analg 2007; 104: 563-568
80. Rex C, Wagner S, Spies C et al. Reversal of neuromuscular blockade by sugammadex after continuous infusion of rocuronium in patients randomized to sevoflurane or propofol maintenance anesthesia. Anesthesiology 2009; 111: 30-35
81. Pühringer F K, Rex C, Sielenkamber AW et al. Reversal of profound, high dose rocuronium-induced neuromuscular blockade by sugammadex at two different time points. An international multicenter, randomised, dose finding, safety assessor-blinded, phase II trial. Anesthesiology 2008; 109: 188-197
82. McCourt KC. Salmela L. Mirakhur RK et al. Comparison of rocuronium and suxamethonium for use during rapid sequence induction of anaesthesia. Anaesthesia 1998; 53: 867-871 (Pubitemid 28431593)
83. Lee C, Jahr JS, Candiotti KA, Warriner B, Zornow M, Naguib M. Reversal of profound neuromuscular block by sugammadex administered three minutes after rocuronium: a comparison with spontaneous recovery from succinylcholine. Anesthesiology 2009; 110: 1020-1025
84. Dahl V, Pendeville PE, Hollman MW et al. Reversal of rocuronium induced blockade by sugammadex in cardiac patients. Anesthesiology 2007; 107: A1581.
85. De Kam P-J, van Kuijk J, Smeets J, et al. 2007. Single IV sugammaedx doses up to 32 mg/kg are not associated with QT/QTc prolongation. Anesthesiology 2007; 107: A1580.
86. Cammu G, De Kam PJ, Demeyer I et al. Safety and tolerability of single intravenous doses of sugammadex administered simultaneously with rocuronium or vecuronium in healthy volunteers. Br J Anaesth 2008; 100: 373-379 (Pubitemid 351773650)
87. Amao R, Zornow MH, Cowan MR, et al. 2007. Sugammadex safely reverses rocuronium-induced blockade in patients with pulmonary disease. Anesthesiology 2007; 107: A1582.
88. Flockton EA, Mastronardi P, Hunter JM et al. Reversal of rocuronium-induced neuromuscular block with sugammadex is faster than reversal of cisatracurium-induced block with neostigmine. Br J Anaesthesia 2008; 100: 622-630 (Pubitemid 351774353)
89. Hartman J, Smeets JMW, deZwart MAH, Peters SMA. In-vitro dialysability of sugammadex (Org 25969), a selective relaxant binding agent for reversal of neuromuscular block induced by rocuronium. Eur J Anaesthesiol 2006; 26 (Suppl 37): 144.
90. Monk TG, Rietbergen H, Woo T. Obesity has no clinically relevant impact upon recovery time following administration of sugammadex. Anesthesiology 2008; 109: A682.
91. Plaud B, Meretoja O, Hofmockel R et al. Reversal of Rocuronium-induced Neuromuscular blockade with sugammadex in pediatric and adult surgical patients. Anesthesiology 2009; 110: 284-294
92. McDonagh DL, Benedict PE, Kovac AL, et al. Safety of sugammadex for reversal of rocuronium-induced blockade in elderly patients. Anesthesiology 2007; 107: A1583.
93. Plaud B, van Heumen E, Zweirs A. Sugammadex is well tolerated for the reversal of rocuronium or vecuronium induced neuromuscular blockade in a pooled analysis of events in 10 placebo controlled trials. Eur J Anaesthesiol. 2008; 25 (Suppl 44): 9AP3-3.
94. http://www.fda.gov/ohrms/dockets/ac/08/slides/2008- 4346s1-01-Schering- Plough-corebackup.pdf
95. http://www.emea.europa.eu/humandocs/PDFs/EPAR/ bridion/H-885-PI-en.pdf
96. Benumof JL, Dagg R, Benumof R. Critical desaturation will occur before return to an unparalyzed state following 1 mg/kg intravenous succinylcholine. Anesthesiology 1997; 87: 979-982 (Pubitemid 27456253)
97. Hayes AH, Breslin DS, Mirakhur RK, Reid JE, O'Hare RA. Frequency of haemoglobin desaturation with the use of succinylcholine during rapid sequence induction of anaesthesia. Acta Anaesthesiol Scand 2001; 45: 746-749
98. Williams NE, Calvey TN, Chan K. Clearance of neostigmine from the circulation during antagonism of neuromuscular block. Br J Anaesth 1978; 50: 1065-1067 (Pubitemid 9066351)
99. Cronnelly R, Stanski DR, Miller RD, Sheiner LB. Pyridostigmine kinetics with and without renal function. Clin Pharm Ther 1980; 28: 78-81. (Pubitemid 10090689)