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Chapter: Clinical Anesthesiology: Clinical Pharmacology: Cholinesterase Inhibitors & Other Pharmacologic Antagonists to Neuromuscular Blocking Agents

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Sugammadex

Sugammadex is a novel selective relaxant-binding agent that is currently available for clinical use in Europe.

SUGAMMADEX

Sugammadex is a novel selective relaxant-binding agent that is currently available for clinical use in Europe. It is a modified gamma-cyclodextrin (su refers to sugar, and gammadex refers to the struc-tural molecule gamma-cyclodextrin).

Physical Structure

Its three-dimensional structure resembles a hollow truncated cone or doughnut with a hydrophobic cavity and a hydrophilic exterior. Hydrophobic interactions trap the drug (eg, rocuronium) in the cyclodextrin cavity (doughnut hole),resulting in tight formation of a water-soluble guest–host complex in a 1:1 ratio. This terminates the neuromuscular blocking action and restrains the drug in extracellular fluid where it cannot interact with nicotinic acetylcholine receptors. Sugammadex is essentially eliminated unchanged via the kidneys.

Clinical Considerations

Sugammadex has been administered in doses of 4–8 mg/kg. With an injection of 8 mg/kg, given 3 min after administration of 0.6 mg/kg of rocuronium, recovery of TOF ratio to 0.9 was observed within 2 min. It produces rapid and effective reversal of both shallow and profound rocuronium-induced neuromuscular blockade in a consistent manner. Because of some concerns about hypersensitivity and allergic reactions, sugamma-dex has not yet been approved by the US Food and Drug Administration.

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