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).
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.
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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