Development and potential clinical impairment of ultra-short-acting neuromuscular blocking agents

British Journal of Anaesthesia

Volumn 107, Issue SUPPL. 1, 2011, Pages

  Lien, C A ^a  

^a WEILL CORNELL MEDICAL COLLEGE   (United States)

Author keywords

CW 002; isoquinolines; neuromuscular block; neuromuscular blocking agents; olefins

Indexed keywords

ATRACURIUM; CISATRACURIUM; CW 002; CYSTEINE; DOXACURIUM; EDROPHONIUM; GANTACURIUM; MIVACURIUM; NEOSTIGMINE; NEUROMUSCULAR BLOCKING AGENT; PANCURONIUM; PYRIDOSTIGMINE; ROCURONIUM; SUGAMMADEX; SUXAMETHONIUM; TUBOCURARINE CHLORIDE; UNCLASSIFIED DRUG; VECURONIUM;

ARTICLE; DOSE RESPONSE; DRUG ANTAGONISM; DRUG CLEARANCE; DRUG DOSE INCREASE; DRUG ELIMINATION; DRUG HALF LIFE; DRUG MECHANISM; DRUG METABOLISM; DRUG POTENCY; HUMAN; MUSCLE STRENGTH; NEUROMUSCULAR BLOCKING; NEUROMUSCULAR FUNCTION; NONHUMAN; PRIORITY JOURNAL;

EID: 83455233763     PISSN: 00070912     EISSN: 14716771     Source Type: Journal    
DOI: 10.1093/bja/aer341     Document Type: Article

References (79)

1. Chestnut RJ, Healy TE, Harper NJ, Faragher EB. Suxamethonium- the relation between dose and response. Anaesthesia 1989; 44: 14-8
2. Szalados JE, Donati F, Bevan DR. Effect of d-tubocurarine pretreatment on succinylcholine twitch augmentation and neuromuscular blockade. Anesth Analg 1990; 71: 55-9 (Pubitemid 20380570)
3. Bevan DR. Neuromuscular blocking drugs: onset and intubation. J Clin Anesth 1997; 9: 36S-9S
4. Bowman WC, Rodger IW, Houston J, Marshall RJ, McIndewar I. Structure:action relationships among some desacetoxy analogues of pancuronium and vecuronium in the anesthetized cat. Anesthesiology 1988; 69: 57-62
5. Kopman AF. Pancuronium, gallamine, and d-tubocurarine compared: is speed of onset inversely related to drug potency? Anesthesiology 1989; 70: 915-20 (Pubitemid 19148493)
6. Kopman AF, Klewicka MM, Kopman DJ, Neuman GG. Molar potency is predictive of the speed of onset of neuromuscular block for agents of intermediate, short, and ultrashort duration. Anesthesiology 1999; 90: 425-31 (Pubitemid 29071510)
7. Donati F, Meistelman C. A kinetic-dynamic model to explain the relationship between high potency and slow onset time for neuromuscular blocking drugs. J Pharmacokinet Biopharm 1991; 19: 537-52
8. Ostergaard D, Jensen FS, Jensen E, Skovgaard LT, Viby-Mogensen J. Mivacurium-induced neuromuscular blockade in patients with atypical plasma cholinesterase. Acta Anaesthesiol Scand 1993; 37: 314-8 (Pubitemid 23199806)
9. Hickey DR, O'Connor JP, Donati F. Comparison of atracurium and succinylcholine for electroconvulsive therapy in a patient with atypical plasma cholinesterase. Can J Anaesth 1987; 34: 280-3 (Pubitemid 17077515)
10. Koscielniak-Nielsen ZJ, Bevan JC, Popovic V, Baxter MR, Donati F, Bevan DR. Onset of maximum neuromuscular block following succinylcholine or vecuronium in four age groups. Anesthesiology 1993; 79: 229-34 (Pubitemid 23224833)
11. Magorian T, Flannery KB, Miller RD. Comparison of rocuronium, succinylcholine, and vecuronium for rapid-sequence induction of anesthesia in adult patients. Anesthesiology 1993; 79: 913-8 (Pubitemid 23339048)
12. Booij LH, Knape HT. The neuromuscular blocking effect of Org 9426. A new intermediately-acting steroidal non-depolarising muscle relaxant in man. Anaesthesia 1991; 46: 341-3
13. Basta SJ, Savarese JJ, Ali HH, et al. Clinical pharmacology of doxacurium chloride. A new long-acting nondepolarizing muscle relaxant. Anesthesiology 1988; 69: 478-86
14. Belmont MR, Lien CA, Quessy S, et al. The clinical neuromuscular pharmacology of 51W89 in patients receiving nitrous oxide/ opioid/barbiturate anesthesia. Anesthesiology 1995; 82: 1139-45
15. Chen BB, Nyhan DP, Blanck TJ. Hemodynamic effects and onset time of increasing doses of vecuronium in patients undergoing myocardial revascularization. J Cardiothorac Vasc Anesth 1991; 5: 569-73
16. Kaufman JA, Dubois MY, Chen JC, Lea DE. Pharmacodynamic effects of vecuronium: a dose response study. J Clin Anesth 1989; 1: 434-9
17. Lien CA, Schmith VD, Belmont MR, Abalos A, Kisor DF, Savarese JJ. Pharmacokinetics of cisatracurium in patients receiving nitrous oxide/opioid/barbiturate anesthesia. Anesthesiology 1996; 84: 300-8 (Pubitemid 26053829)
18. Moss J, Rosow CE, Savarese JJ, Philbin DM, Kniffen KJ. Role of histamine in the hypotensive action of d-tubocurarine in humans. Anesthesiology 1981; 55: 19-25 (Pubitemid 11085512)
19. Basta SJ, Savarese JJ, Ali HH, Moss J, Gionfriddo M. Histamine-releasing potencies of atracurium, dimethyl tubocurarine and tubocurarine. Br J Anaesth 1983; 55(Suppl. 1): 105S-6S (Pubitemid 13060966)
20. Denman WT, Goudsouzian NG, Gelb C. Comparison of neuromuscular, cardiovascular, and histamine-releasing properties of doxacurium and pipecuronium. J Clin Anesth 1996; 8: 113-8 (Pubitemid 26073974)
21. Lien CA, Belmont MR, Abalos A, et al. The cardiovascular effects and histamine-releasing properties of 51W89 in patients receiving nitrous oxide/opioid/barbiturate anesthesia. Anesthesiology 1995; 82: 1131-8
22. Beecher HK, Todd DP. A study of the deaths associated with anesthesia and surgery: based on a study of 599,548 anesthesias in ten institutions 1948-1952, inclusive. Ann Surg 1954; 140: 2-35
23. Arbous MS, Meursing AE, van Kleef JW, et al. Impact of anesthesia management characteristics on severe morbidity and mortality. Anesthesiology 2005; 102: 257-68; quiz 491-2
24. Ali HH, Utting JE, Gray TC. Quantitative assessment of residual antidepolarizing block. I. Br J Anaesth 1971; 43: 473-7
25. Ali HH, Utting JE, Gray TC. Quantitative assessment of residual antidepolarizing block. II. Br J Anaesth 1971; 43: 478-85
26. Kopman AF, Yee PS, Neuman GG. Relationship of the train-of-four fade ratio to clinical signs and symptoms of residual paralysis in awake volunteers. Anesthesiology 1997; 86: 765-71 (Pubitemid 27174715)
27. Berg H, Roed J, Viby-Mogensen J, et al. Residual neuromuscular block is a risk factor for postoperative pulmonary complications. A prospective, randomised, and blinded study of postoperative pulmonary complications after atracurium, vecuronium and pancuronium. Acta Anaesthesiol Scand 1997; 41: 1095-103
28. Eriksson LI, Sato M, Severinghaus JW. Effect of a vecuronium-induced partial neuromuscular block on hypoxic ventilatory response. Anesthesiology 1993; 78: 693-9 (Pubitemid 23110043)
29. 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: 130-7
30. 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: 977-84 (Pubitemid 30180973)
31. Eikermann M, Vogt FM, Herbstreit F, et al. The predisposition to inspiratory upper airway collapse during partial neuromuscular blockade. Am J Respir Crit Care Med 2007; 175: 9-15 (Pubitemid 46105303)
32. Herbstreit F, Peters J, Eikermann M. Impaired upper airway integrity by residual neuromuscular blockade: increased airway collapsibility and blunted genioglossus muscle activity in response to negative pharyngeal pressure. Anesthesiology 2009; 110: 1253-60
33. Fruergaard K, Viby-Mogensen J, Berg H, el-Mahdy AM. Tactile evaluation of the response to double burst stimulation decreases, but does not eliminate, the problem of postoperative residual paralysis. Acta Anaesthesiol Scand 1998; 42: 1168-74 (Pubitemid 28516993)
34. Viby-Mogensen J, Jensen NH, Engbaek J, Ording H, Skovgaard LT, Chraemmer-Jorgensen B. Tactile and visual evaluation of the response to train-of-four nerve stimulation. Anesthesiology 1985; 63: 440-3 (Pubitemid 16236061)
35. Naguib M, Kopman AF, Lien CA, Hunter JM, Lopez A, Brull SJ. A survey of current management of neuromuscular block in the United States and Europe. Anesth Analg 2010; 111: 110-9
36. 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: 1042-8 (Pubitemid 36520189)
37. Murphy GS, Szokol JW, Marymont JH, et al. Intraoperative acceleromyographic monitoring reduces the risk of residual neuromuscular blockade and adverse respiratory events in the postanesthesia care unit. Anesthesiology 2008; 109: 389-98
38. 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: 1035-43 (Pubitemid 27469300)
39. Proost JH, Eriksson LI, Mirakhur RK, Roest G, Wierda JM. Urinary, biliary and faecal excretion of rocuronium in humans. Br J Anaesth 2000; 85: 717-23
40. Fisher DM, Canfell PC, Fahey MR, et al. Elimination of atracurium in humans: contribution of Hofmann elimination and ester hydrolysis versus organ-based elimination. Anesthesiology 1986; 65: 6-12 (Pubitemid 16098086)
41. Hughes R, Chapple DJ. The pharmacology of atracurium: a new competitive neuromuscular blocking agent. Br J Anaesth 1981; 53: 31-44 (Pubitemid 11210926)
42. Murphy GS, Szokol JW, Marymont JH, Avram MJ, Vender JS, Rosengart TK. Impact of shorter-acting neuromuscular blocking agents on fast-track recovery of the cardiac surgical patient. Anesthesiology 2002; 96: 600-6 (Pubitemid 34193499)
43. Bevan DR, Smith CE, Donati F. Postoperative neuromuscular blockade: a comparison between atracurium, vecuronium, and pancuronium. Anesthesiology 1988; 69: 272-6
44. Kirkegaard H, Heier T, Caldwell JE. Efficacy of tactile-guided reversal from cisatracurium-induced neuromuscular block. Anesthesiology 2002; 96: 45-50 (Pubitemid 34032480)
45. Bevan DR, Donati F, Kopman AF. Reversal of neuromuscular blockade. Anesthesiology 1992; 77: 785-805
46. Beemer GH, Bjorksten AR, Dawson PJ, Dawson RJ, Heenan PJ, Robertson BA. Determinants of the reversal time of competitive neuromuscular block by anticholinesterases. Br J Anaesth 1991; 66: 469-75
47. Bevan JC, Collins L, Fowler C, et al. Early and late reversal of rocuronium and vecuronium with neostigmine in adults and children. Anesth Analg 1999; 89: 333-9 (Pubitemid 29367712)
48. Caldwell JE. Reversal of residual neuromuscular block with neostigmine at one to four h after a single intubating dose of vecuronium. Anesth Analg 1995; 80: 1168-74
49. 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: 293-9 (Pubitemid 19112772)
50. Eikermann M, Fassbender P, Malhotra A, et al. Unwarranted administration of acetylcholinesterase inhibitors can impair genioglossus and diaphragm muscle function. Anesthesiology 2007; 107: 621-9 (Pubitemid 47480569)
51. McCaul C, Tobin E, Boylan JF, McShane AJ. Atracurium is associated with postoperative residual curarization. Br J Anaesth 2002; 89: 766-9 (Pubitemid 35277229)
52. Kirkegaard-Nielsen H, Severinsen IK, Pedersen HS, Lindholm P. Factors predicting atracurium reversal time. Acta Anaesthesiol Scand 1999; 43: 834-41 (Pubitemid 29408950)
53. Kim KS, Lew SH, Cho HY, Cheong MA. Residual paralysis induced by either vecuronium or rocuronium after reversal with pyridostigmine. Anesth Analg 2002; 95: 1656-60, table of contents (Pubitemid 35423956)
54. Katz RL. Clinical neuromuscular pharmacology of pancuronium. Anesthesiology 1971; 34: 550-6
55. Howardy-Hansen P, Rasmussen JA, Jensen BN. Residual curarization in the recovery room: atracurium versus gallamine. Acta Anaesthesiol Scand 1989; 33: 167-9 (Pubitemid 19055227)
56. Donati F, McCarroll SM, Antzaka C, McCready D, Bevan DR. Dose- response curves for edrophonium, neostigmine, and pyridostigmine after pancuronium and d-tubocurarine. Anesthesiology 1987; 66: 471-6 (Pubitemid 17051497)
57. Viby-Mogensen J. Postoperative residual curarization and evidence-based anaesthesia. Br J Anaesth 2000; 84: 301-3 (Pubitemid 30114121)
58. Tramer MR, Fuchs-Buder T. Omitting antagonism of neuromuscular block: effect on postoperative nausea and vomiting and risk of residual paralysis.Asystematic review. Br JAnaesth 1999; 82: 379-86 (Pubitemid 29112540)
59. Fuchs-Buder T, Meistelman C, Alla F, Grandjean A, Wuthrich Y, Donati F. Antagonism of low degrees of atracurium-induced neuromuscular blockade: dose-effect relationship for neostigmine. Anesthesiology 2010; 112: 34-40
60. Kopman AF, Eikermann M. Antagonism of non-depolarising neuromuscular block: current practice. Anaesthesia 2009; 64(Suppl. 1): 22-30
61. Herbstreit F, Zigrahn D, Ochterbeck C, Peters J, Eikermann M. Neostigmine/glycopyrrolate administered after recovery from neuromuscular block increases upper airway collapsibility by decreasing genioglossus muscle activity in response to negative pharyngeal pressure. Anesthesiology 2010; 113: 1280-8
62. Caldwell JE, Miller RD. Clinical implications of sugammadex. Anaesthesia 2009; 64(Suppl. 1): 66-72
63. Puhringer FK, Rex C, Sielenkamper AW, et al. Reversal of profound, high-dose rocuronium-induced neuromuscular blockade by sugammadex at two different time points: an international, multicenter, randomized, dose-finding, safety assessor-blinded, phase II trial. Anesthesiology 2008; 109: 188-97
64. Gijsenbergh F, Ramael S, Houwing N, van Iersel T. First human exposure of Org 25969, a novel agent to reverse the action of rocuronium bromide. Anesthesiology 2005; 103: 695-703 (Pubitemid 41415517)
65. Duvaldestin P, Kuizenga K, Saldien V, et al. A randomized, dose-response study of sugammadex given for the reversal of deep rocuronium- or vecuronium-induced neuromuscular blockade under sevoflurane anesthesia. Anesth Analg 2010; 110: 74-82
66. 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)
67. Epemolu O, Mayer I, Hope F, Scullion P, Desmond P. Liquid chromatography/ mass spectrometric bioanalysis of a modified gammacyclodextrin (Org 25969) and Rocuronium bromide (Org 9426) in guinea pig plasma and urine: its application to determine the plasma pharmacokinetics of Org 25969. Rapid Commun Mass Spectrom 2002; 16: 1946-52
68. Savarese JJ, Kitz RJ. Does clinical anesthesia need new neuromuscular blocking agents? Anesthesiology 1975; 42: 236-9
69. Boros EE, Bigham EC, Boswell GE, et al. Bis- and mixedtetrahydroisoquinolinium chlorofumarates: new ultra-shortacting nondepolarizing neuromuscular blockers. J Med Chem 1999; 42: 206-9 (Pubitemid 29069854)
70. Samano V, Ray JA, Thompson JB, et al. Synthesis of ultra-short-acting neuromuscular blocker GW 0430: a remarkably stereo- and regioselective synthesis of mixed tetrahydroisoquinolinium chlorofumarates. Org Lett 1999; 1: 1993-6
71. Savarese JJ, McGilvra JD, Sunaga H, et al. Rapid chemical antagonism of neuromuscular blockade by L-cysteine adduction to and inactivation of the olefinic (double-bonded) isoquinolinium diester compounds gantacurium (AV430A), CW 002, and CW 011. Anesthesiology 2010; 113: 58-73
72. Savarese JJ, Belmont MR, Hashim MA, et al. Preclinical pharmacology of GW280430A (AV430A) in the rhesus monkey and in the cat: a comparison with mivacurium. Anesthesiology 2004; 100: 835-45 (Pubitemid 38392570)
73. Belmont MR, Lien CA, Tjan J, et al. Clinical pharmacology of GW280430A in humans. Anesthesiology 2004; 100: 768-73 (Pubitemid 38392561)
74. Cronnelly R, Morris RB, Miller RD. Edrophonium: duration of action and atropine requirement in humans during halothane anesthesia. Anesthesiology 1982; 57: 261-6 (Pubitemid 12031853)
75. Heerdt PM, Kang R, The A, Hashim M, Mook RJ Jr, Savarese JJ. Cardiopulmonary effects of the novel neuromuscular blocking drug GW280430A (AV430A) in dogs. Anesthesiology 2004; 100: 846-51 (Pubitemid 38392571)
76. Sunaga H, Zhang Y, Savarese JJ, Emala CW. Gantacurium andCW002 do not potentiate muscarinic receptor-mediated airway smooth muscle constriction in guinea pigs. Anesthesiology 2010; 112: 892-9
77. Lien CA, Savard P, Belmont M, Sunaga H, Savarese JJ. Fumarates: unique nondepolarizing neuromuscular blocking agents that are antagonized by cysteine. J Crit Care 2009; 24: 50-7
78. Sunaga H, Malhotra JK, Yoon E, Savarese JJ, Heerdt PM. Cysteine reversal of the novel neuromuscular blocking drug CW002 in dogs: pharmacodynamics, acute cardiovascular effects, and preliminary toxicology. Anesthesiology 2010; 112: 900-9
79. Heerdt PM, Malhotra JK, Pan BY, Sunaga H, Savarese JJ. Pharmacodynamics and cardiopulmonary side effects of CW002, a cysteine-reversible neuromuscular blocking drug in dogs. Anesthesiology 2010; 112: 910-6