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Update on neuromuscular pharmacology

Naguib, Mohameda; Brull, Sorin Jb

Current Opinion in Anaesthesiology: August 2009 - Volume 22 - Issue 4 - p 483–490
doi: 10.1097/ACO.0b013e32832b8cff
Drugs in anesthesia: Edited by Klaus T. Olkkola

Purpose of review: We review the efficacy and safety of gantacurium and AV002, two novel, investigational fumarate-based nondepolarizing neuromuscular blockers, as well as sugammadex and cysteine, two novel reversal drugs that have no acetylcholinesterase inhibition properties.

Recent findings: Gantacurium (with a pharmacodynamic profile similar to that of succinylcholine) and AV002 (with an intermediate duration of action) have shown efficacy in animals and, for gantacurium, in humans. Animal data have shown that exogenous administration of the amino acid cysteine accelerates the natural chemical degradation of both gantacurium and AV002 via the cysteine adduction pathway. Another reversal drug, sugammadex (a modified γ-cyclodextrin and the first selective relaxant binding agent), forms very tight complexes in a 1: 1 ratio with steroidal neuromuscular blocking agents.

Summary: In a multicenter phase-2 randomized controlled study in the European Union, the efficacy and safety of gantacurium were evaluated, but results have not yet been published. Sugammadex is currently available in the European Union, but the United States Food and Drug Administration has had concerns about its safety (hypersensitivity and allergic reactions) and has asked for additional safety data. It is hoped that the widespread use of sugammadex in the European Union will provide additional information.

aDepartment of Anesthesiology and Pain Medicine, The University of Texas M. D. Anderson Cancer Center, Houston, Texas, USA

bMayo Clinic College of Medicine, Jacksonville, Florida, USA

Correspondence to Dr Mohamed Naguib, MB, BCh, MSc, FFARCSI, MD, Department of Anesthesiology and Pain Medicine, Unit 409, The University of Texas M. D. Anderson Cancer Center, 1400 Holcombe Boulevard, Houston, TX 77030, USA Tel: +1 713 745 4948; fax: +1 713 792 7591; e-mail: Naguib@mdanderson.org

Disclosure: Dr Naguib has worked as a consultant on an ad hoc basis with Organon Pharmaceuticals (Roseland, New Jersey, USA) and Avera Pharmaceuticals (San Diego, California, USA).

© 2009 Lippincott Williams & Wilkins, Inc.