Update on neuromuscular pharmacology

Abstract

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.

Sugammadex: A Cyclodextrin‐Based Novel Formulation and Marketing Story

“…The doses used have been as high as 32 mg/kg, which is considerably more than the usual doses of 2 to 4 mg/kg. There is one case of "hypersensitivity reaction" in one volunteer that resulted in discontinuation of administration of sugammadex but did not require any treatment [7]. Six volunteers also showed possible hypersensitivity after 32 mg/kg [7].…”

“…Most modern neuromuscular blocking drugs available today belong to one of two classes: the benzyl isoquinolines (atracurium, cisatracurium, mivacurium, doxacurium) and the steroid-based (rocuronium, vecuronium, pancuronium). Development of chlorofumarates (gantacurium), which have a short duration of action and can be antagonized by cysteine, is under way [6,7]. Rocuronium and vecuronium are devoid of cardiovascular effects and have become very popular in anesthesia.…”

“…There is one case of "hypersensitivity reaction" in one volunteer that resulted in discontinuation of administration of sugammadex but did not require any treatment [7]. Six volunteers also showed possible hypersensitivity after 32 mg/kg [7]. Other volunteers were anesthetized and received rocuronium or vecuronium followed by sugammadex.…”

“…Side effects may be masked when a general anesthetic is given. However, it was observed that although volunteers appeared to have an adequate depth of anesthesia before sugammadex was injected, signs of light anesthesia (such as movement, coughing, and grimacing) were often observed after sugammadex [7]. This probably has little clinical significance because sugammadex is intended to be given at the end of anesthesia and surgery.…”

“…In mid-2008, the U.S. Food and Drug Administration (FDA) ruled that the drug was "not approvable," based on a few mild cases of hypersensitivity or allergy seen in volunteers [7]. The FDA required more clinical and safety data.…”