Keyword
Sugammadex
Definition
selective relaxant-binding agent, modified gamma-cyclodextrin
Structure & Mechanism
- hollow truncated cone or doughnut with an 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 NM blocking action and restrains the drug in ECF.
Indication
Reversal of neuromuscular blockade induced by steroidal neuromuscular blocking drugs (rocuronium, vecuronium, pancuronium).
Excretion
eliminated unchanged via the kidneys.
Dose
- Immediate reversal : 16.0 mg/kg
- Administration of 16.0 mg/kg sugammadex 3 minutes following a bolus dose of 1.2 mg/kg rocuronium bromide provides a median time to recovery of the T4/T1 ratio to 0.9 of approximately 1.5 minutes (see CLINICAL TRIALS).
- There are no data to recommend the use of sugammadex for immediate reversal following vecuronium-induced blockade
- routine reversal
- A dose of 4.0 mg/kg sugammadex is recommended if recovery has reached 1 – 2 post-tetanic counts (PTC) following rocuronium- or vecuronium-induced blockade.
- A dose of 2.0 mg/kg sugammadex is recommended, if spontaneous recovery has occurred up to the reappearance of T2 following rocuronium- or vecuronium-induced blockade.
Rocuronium recovery time(min) from the administration of sugammadex (2mg/kg at appearance of T2) until the recovery of train-of-four ratios as indicated in patients with and without renal failure