Simulation of the reversal of neuromuscular block by sequestration of the free molecules of the muscle relaxant

Journal of Pharmacokinetics and Pharmacodynamics

Volumn 34, Issue 6, 2007, Pages 771-788

  Nigrovic, Vladimir ^a   Bhatt, Shashi B ^a   Amann, Anton ^b,c  

^a MEDICAL COLLEGE OF OHIO   (United States)

^b INNSBRUCK MEDICAL UNIVERSITY   (Austria)

^c ETH ZURICH   (Switzerland)

Author keywords

Nondepolarizing neuromuscular blocking drugs; Reversal agents; Sequestration; Simulation of neuromuscular block; Simulation of the reversal; Sugammadex

Indexed keywords

MUSCLE RELAXANT AGENT; POSTSYNAPTIC RECEPTOR; RECEPTOR BLOCKING AGENT; ROCURONIUM; SUGAMMADEX;

ARTICLE; DRUG RECEPTOR BINDING; MUSCLE TWITCH; NERVE ENDING; NEUROMUSCULAR BLOCKING; NEUROMUSCULAR TRANSMISSION; PHYSICAL CHEMISTRY; PRIORITY JOURNAL; SIMULATION;

ANIMALS; HUMANS; NEUROMUSCULAR BLOCKADE; NEUROMUSCULAR NONDEPOLARIZING AGENTS; SYNAPSES;

EID: 36448993317     PISSN: 1567567X     EISSN: None     Source Type: Journal    
DOI: 10.1007/s10928-007-9068-y     Document Type: Article

References (29)

1. Adam JM, Bennett DJ, Bom A, Clark JK, Feilden H, Hutchinson EJ, Palin R, Prosser A, Rees DC, Rosair GM, Stevenson D, Tarver GJ and Zhang MQ (2002). Cyclodextrin-derived host molecules as reversal agents for the neuromuscular blocker rocuronium bromide: synthesis and structure-activity relationships. J Med Chem 45: 1806-1816
2. Bom A, Bradley M, Cameron K, Clark JK, Van Egmond J, Feilden H, MacLean EJ, Muir AW, Palin R, Rees DC and Zhang M-Q (2002). A novel concept of reversing neuromuscular block: chemical encapsulation of rocuronium bromide by a cyclodextrin-based synthetic host. Angew Chem (Int Ed Engl) 41: 266-270
3. Cameron KS, Clark JK, Cooper A, Fielding L, Palin R, Rutherford SJ and Zhang MQ (2002). Modified gamma-cyclodextrins and their rocuronium complexes. Org Lett 4: 3403-3406
4. Cameron KS, Fielding L, Mason R, Muir AW, Rees DC, Thorn S and Zhang MQ (2002). Anionic cyclophanes as potential reversal agents of muscle relaxants by chemical chelation. Bioorg Med Chem Lett 12: 753-755
5. Tarver GJ, Grove SJ, Buchanan K, Bom A, Cooke A, Rutherford SJ and Zhang MQ (2002). 2-O-substituted cyclodextrins as reversal agents for the neuromuscular blocker rocuronium bromide. Bioorg Med Chem 10: 1819-1827
6. Epemolu O, Bom A, Hope F, Mason R (2003) Reversal of neuromuscular blockade and simultaneous increase in plasma rocuronium concentration after the intravenous infusion of the novel reversal agent Org 25969. Anesthesiology 99:632-637; discussion 636A
7. Hope F and Bom A (2001). Org 25969 reverses rocuronium-induced neuromuscular blockade in the cat without important haemodynamic effect. Eur J Anaesthesiol 18(Suppl 23): 99
8. Mason R and Bom A (2001). Org 25969 causes selective reversal of neuromuscular block induced by steroidal NMBs in anaesthetized giunea pigs. Eur J Anaesthesiol 18(Suppl 23): 100
9. Miller S and Bom A (2001). Org 25969 causes selective reversal of neuromuscular blockade induced by steroidal NMBs in the mouise hemi-diapgragm preparation. Eur J Anaesthesiol 18(Suppl 23): 100-101
10. Booij L, Bom A, van Egmont J and van de Pol F (2001). Neuromuscular blockade induced by steroidal NMBs can be rapidly reversed by Org 25969 in the anaesthetized monkey. Eur J Anaesthesiol 18(Suppl 23): 100
11. Bom A, Booij LH, de Boer HD, van Egmond J and van de Pol F (2006). Reversal of profound rocuronium neuromuscular blockade by sugammadex in anesthetized rhesus monkeys. Anesthesiology 104: 718-723
12. Gijsenbergh F, Ramael S, Houwing N and van Iersel T (2005). First human exposure of Org 25969, a novel agent to reverse the action of rocuronium bromide. Anesthesiology 103: 695-703
13. Shields M, Giovannelli M, Mirakhur RK, Moppett I, Adams J and Hermens Y (2006). Org 25969 (sugammadex), a selective relaxant binding agent for antagonism of prolonged rocuronium-induced neuromuscular block. Br J Anaesth 96: 36-43
14. Sorgenfrei IF, Norrild K, Larsen PB, Stensballe J, Ostergaard D, Prins ME and Viby-Mogensen J (2006). Reversal of rocuronium-induced neuromuscular block by the selective relaxant binding agent sugammadex: a dose-finding and safety study. Anesthesiology 104: 667-674
15. Suy K, Morias K, Cammu G, Hans P, Heeringa M, Demeyer I and van Duijnhoven WG F (2007). Effective reversal of moderate rocuronium- or vecuronium-induced neuromuscular block with sugammadex, a selective relaxant binding agent. Anesthesiology 106: 283-288
16. Groudine SB, Soto R, Lien C, Drover D and Roberts K (2007). A randomized, dose-finding, phase II study of the selective relaxant binding drug, Sugammadex, capable of safely reversing profound rocuronium-induced neuromuscular block. Anesth Analg 104: 555-562
17. Hunter JM and Flockton EA (2006). The doughnut and the hole: a new pharmacological concept for anaesthetists. Br J Anaesth 97: 123-126
18. Kopman AF (2006). Sugammadex: a revolutionary approach to neuromuscular antagonism. Anesthesiology 104: 631-633
19. Miller RD (2007). Sugammadex: an opportunity to change the practice of anesthesiology?. Anesth Analg 104: 477-478
20. Naguib M (2007). Sugammadex: another milestone in clinical neuromuscular pharmacology. Anesth Analg 104: 575-581
21. Bom A, Bradley M, Cameron K, Clark JK, Feilden H, MacLean EJ, Muir AW, Palin R, Rees DC, Zhang MQ and van Egmond J (2002). A novel concept of reversing neuromuscular block: chemical encapsulation of rocuronium bromide by a cyclodextrin-based synthetic host. Angew Chem Int Ed Engl 41: 266-270
22. Nigrovic V, Bhatt SB, Amann A (2006) First human exposure to Org 25969. Anesthesiology 105:427; author reply 427
23. Levitt DG (2003). The pharmacokinetics of the interstitial space in humans. BMC Clin Pharmacol 3: 3
24. Nigrovic V, Anton A and Bengez R (2004). Analysis of the pharmacodynamic parameters in a model for neuromuscular block. Med Sci Monit 10: BR468-BR476
25. Fambrough DM, Drachman DB and Satyamurti S (1973). Neuromuscular junction in myasthenia gravis: decreased acetylcholine receptors. Science 182: 293-295
26. Bhatt SB, Amann A and Nigrovic V (2006). Modeling of twitch fade based on slow interaction of nondepolarizing muscle relaxants with the presynaptic receptors. J Pharmacokinet Pharmacodyn 33: 461-483
27. Nigrovic V and Amann A (2003). Competition between acetylcholine and a nondepolarizing muscle relaxant for binding to the postsynaptic receptors at the motor end plate: simulation of twitch strength and neuromuscular block. J Pharmacokinet Pharmacodyn 30: 23-51
28. Kopman AF, Yee PS and Neuman GG (1997). Relationship of the train-of-four fade ratio to clinical signs and symptoms of residual paralysis in awake volunteers. Anesthesiology 86: 765-771
29. Bom A, Booij LH, de Boer HD, van Egmond J and van de Pol F (2006). Sugammadex, a new reversal agent for neuromuscular block induced by rocuronium in the anaesthetized Rhesus monkey. Br J Anaesth 96: 473-479