Selective relaxant binding agents for reversal of neuromuscular blockade

Current Opinion in Pharmacology

Volumn 7, Issue 3, 2007, Pages 298-302

  Bom, Anton ^a   Epemolu, Ola ^a   Hope, Frank ^a   Rutherford, Samantha ^a   Thomson, Karen ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ACETYLCHOLINE; CHOLINESTERASE INHIBITOR; CYCLODEXTRIN; EDROPHONIUM; MUSCARINIC RECEPTOR BLOCKING AGENT; NEOSTIGMINE; NEUROMUSCULAR BLOCKING AGENT; NICOTINIC RECEPTOR; PLACEBO; ROCURONIUM; SODIUM CHLORIDE; SUGAMMADEX; VECURONIUM;

ANESTHESIA INDUCTION; ANESTHETIC RECOVERY; BINDING AFFINITY; CLINICAL TRIAL; CONCENTRATION (PARAMETERS); DRUG CLEARANCE; DRUG DISTRIBUTION; DRUG DOSE COMPARISON; DRUG ELIMINATION; DRUG HALF LIFE; DRUG SAFETY; DRUG SELECTIVITY; DRUG TOLERABILITY; ENCAPSULATION; GUINEA PIG; HUMAN; IN VITRO STUDY; IN VIVO STUDY; MONKEY; MUSCLE CONTRACTION; NERVE ENDING; NERVE STIMULATION; NEUROMUSCULAR BLOCKING; NEUROMUSCULAR SYNAPSE; NONHUMAN; PHRENIC NERVE; PRIORITY JOURNAL; REVIEW; UNSPECIFIED SIDE EFFECT;

ANIMALS; CLINICAL TRIALS; CYCLODEXTRINS; HUMANS; NEUROMUSCULAR BLOCKADE; NEUROMUSCULAR NONDEPOLARIZING AGENTS;

EID: 34248366126     PISSN: 14714892     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.coph.2006.11.009     Document Type: Review

References (17)

1. Griffith H.R., and Johnson G.E. The use of curare in general anesthesia. Anesthesiology 3 (1942) 418-420
2. Organon laboratories Ltd (Bom A, Muir A, Rees DC): Use of chemical chelators as reversal agents for drug-induced neuromuscular block. Patent Application 2001; WO-00112202.
3. Bom A., Bradley M., Cameron K., Clark J.K., Van Egmond J., Feilden H., MacLean E.J., Muir A.W., Palin R., Rees D.C., and Zhang M.Q. A novel concept of reversing neuromuscular block: chemical encapsulation of rocuronium bromide by a cyclodextrin-based synthetic host. Angew Chem Int Ed Engl 41 (2002) 266-270
4. Adam J.M., Bennett D.J., Bom A., Clark J.K., Feilden H., Hutchinson E.J., Palin R., Prosser A., Rees D.C., Rosair G.M., et al. Cyclodextrin-derived host molecules as reversal agents for the neuromuscular blocker rocuronium bromide: synthesis and structure-activity relationships. J Med Chem 45 (2002) 1806-1816
5. Organon laboratories Ltd (Zhang M-Q, Palin R, Bennett JD): 6-Mercapto-cyclodextrin derivatives: reversal agents for drug-induced neuromuscular block. Patent Application 2001; WO-00140316.
6. De Boer H.D., van Egmond J., van de Pol F., Bom A., and Booij L.H. Sugammadex, a new reversal agent for neuromuscular block induced by rocuronium in the anaesthetized Rhesus monkey. Br J Anaesth 96 (2006) 473-479
7. De Boer H.D., van Egmond J., van de Pol F., Bom A., and Booij L.H. Reversal of profound rocuronium neuromuscular blockade by sugammadex in anesthetized Rhesus monkeys. Anesthesiology 104 (2006) 718-723
8. Epemolu O., Bom A., Hope F., and Mason R. Reversal of neuromuscular blockade and simultaneous increase in plasma rocuronium concentration after the intravenous infusion of the novel reversal agent Org 25969. Anesthesiology 99 (2003) 632-637
9. Gijsenbergh F., Ramael S., Houwing N., and van Iersel T. First human exposure of Org 25969, a novel agent to reverse the action of rocuronium bromide. Anesthesiology 103 (2005) 695-703. This report summarises the results obtained from Phase I clinical trials in conscious and anaesthetised healthy male volunteers.
10. Sorgenfrei I.F., Norrild K., Larsen P.B., Stensballe J., Ostergaard D., Prins M.E., and Viby-Mogensen J. Reversal of rocuronium-induced neuromuscular block by the selective relaxant binding agent sugammadex: a dose-finding and safety study. Anesthesiology 104 (2006) 667-674. A Phase II clinical study showing clear dose-dependent reversal of rocuronium-induced neuromuscular blockade.
11. Shields M., Giovannelli M., Mirakhur R.K., Moppett I., Adams J., and Hermens Y. Org 25969 (sugammadex), a selective relaxant binding agent for antagonism of prolonged rocuronium-induced neuromuscular block. Br J Anaesth 96 (2006) 36-43. A Phase II clinical study showing the effect of sugammadex against prolonged and profound blockade.
12. Vanacker B.F., Vermeyen K.M., Struys M.M.R.F., Rietbergen H., Vandermeersch E., Saldien V., Kalmar A.F., and Prins M.E. Reversal of rocuronium-induced neuromuscular block with the novel drug sugammadex is equally effective under maintenance anesthesia with propofol or sevoflurane. Anesth & Analg 104 (2007) 563-568
13. Sacan O., White P.F., Tufanogullari B., and Klein K. Sugammadex reversal of rocuronium-induced blockade: a comparison with neostigmine-glycopyrrolate and edrophonium-atropine. Anesth & Analg 104 (2007) 569-574
14. Groudine S.B., Soto R., Lien C., Drover D., and Roberts K. 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 (2007) 555-562
15. Eleveld D.J., Kuizenga K., Proost J.H., and Wierda J.M.K.H. A temporary decrease in twitch response during reversal of rocuronium-induced muscle relaxation with a small dose of sugammadex. Anesth & Analg 104 (2007) 582-584
16. Naguib M. Sugammadex: another milestone in clinical neuromuscular pharmacology. Anesth & Analg 104 (2007) 575-581
17. Miller R.D. Sugammadex: an opportunity to change the practice of Anesthesiology. Anesth & Analg 104 (2007) 477-478