Sugammadex CCC

Reviewed and revised 27 January 2014

CLASS

  • modified cyclodextrin

MECHANISM OF ACTION

  • selective relaxant binding agent for reversal of the aminosteroid NMBDs rocuronium, vecuronium and pancuronium
  • gamma-cyclodextrin component has a hydrophilic exterior and hydrophobic core that traps the aminosteroid ring
  • complex is pH- and temperature-independent and very stable
  • Two phase reversal: encapsulation in bloodstream followed by elimination of the complexes renally

PHARMACEUTICS

  • 200mg in 2 mL or 500mg in 5 mL
  • clear colourless solution
  • photosensitive and must be stored protected from ambient light at <30C
  • shelf life of 3 years
  • 200 mg costs Aus$170

DOSE

  • guided by degree of neuromuscular blockade and NMBD to be reversed
  • no published dose recommendations for pancuronium
  • onset is slower for vecuronium than for rocuronium
  • Shallow block (TOF = 2): 2 mg/kg
  • Deep block  (PTC = 1 to 2) 4 mg/kg
  • Immediate rescue reversal: 16 mg/kg (dose not known for vecuronium) — recovery of first TOF to 90% takes mean 4.4 min following 1.2 mg/kg rocuronium (despite a 3 minute delay in administration!)

INDICATIONS

  1. selective reversal of neuromuscular blockade by the aminosteroid NMBD rocuronium; vecuronium and pancuronium

CONTRA-INDICATIONS

  • not recommended if severe renal dysfunction or dialysis (although efficacy is maintained and can be removed by hemodialysis)

ADVERSE EVENTS

<1%, well tolerated

  • hypotension
  • cough
  • altered taste
  • hypersensitivity reactions

PHARMACOKINETICS

  • Absorption – IV
  • Distribution – Protein binding < 1%, Volume of distribution at steady state 18 L
  • Metabolism – nil
  • Elimination – renal, t1/2 = 100 minutes, Plasma clearance 120 mL/minute

INTERACTIONS

  • none known to be clinically significant
  • theoretical risk of displacement interactions (e.g. flucloxacillin) leading to release of bound aminosteroid NMBDs or capture interactions (e.g. oral contraceptives, cortisone, atropine, verapamil) leading to decreased efficacy of another drug
  • potential role in treatment of hypersensitivity reactions due to aminosteroids (but may also bind steroids given as therapy!)

OTHER INFORMATION

  • reversal is independent of the intensity of neuromuscular blockade prior to sugammadex administration — even deep neuromuscular blockade can be predictably and reliably reversed
  • sourcing the drug, dose calculation and preparation may lead to substantial delays in administration in the ‘can’t intubate, can’t ventilate’ scenario
  • rocuronium reversal (1.2 mg/kg) with sugammadex (16 mg/kg) is faster than suxamethonium (1.5mg/kg) reversal by approximately 2 minutes

References and Links

LITFL

Journal articles

  • Karalapillai D, Kaufman M, Weinberg L. Sugammadex. Crit Care Resusc. 2013 Mar;15(1):57-62. PMID: 23432503.

CCC 700 6

Critical Care

Compendium

Chris is an Intensivist and ECMO specialist at the Alfred ICU in Melbourne. He is also the Innovation Lead for the Australian Centre for Health Innovation at Alfred Health and Clinical Adjunct Associate Professor at Monash University. He is a co-founder of the Australia and New Zealand Clinician Educator Network (ANZCEN) and is the Lead for the ANZCEN Clinician Educator Incubator programme. He is on the Board of Directors for the Intensive Care Foundation and is a First Part Examiner for the College of Intensive Care Medicine. He is an internationally recognised Clinician Educator with a passion for helping clinicians learn and for improving the clinical performance of individuals and collectives.

After finishing his medical degree at the University of Auckland, he continued post-graduate training in New Zealand as well as Australia’s Northern Territory, Perth and Melbourne. He has completed fellowship training in both intensive care medicine and emergency medicine, as well as post-graduate training in biochemistry, clinical toxicology, clinical epidemiology, and health professional education.

He is actively involved in in using translational simulation to improve patient care and the design of processes and systems at Alfred Health. He coordinates the Alfred ICU’s education and simulation programmes and runs the unit’s education website, INTENSIVE.  He created the ‘Critically Ill Airway’ course and teaches on numerous courses around the world. He is one of the founders of the FOAM movement (Free Open-Access Medical education) and is co-creator of litfl.com, the RAGE podcast, the Resuscitology course, and the SMACC conference.

His one great achievement is being the father of two amazing children.

On Twitter, he is @precordialthump.

| INTENSIVE | RAGE | Resuscitology | SMACC

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