Sugammadex

Question 1

What are the uses of sugammadex?

Answer 1

• reversal of neuromuscular blockade caused by vecuronium or rocuronium
• can be used confidently to reverse effects , even following an intubating dose of roc

Question 2

What is the MOA of sugammadex?

Answer 2

• ring-like structure enables drug to encapsulate rocuronium and vecuronium in it’s lipophilic core
• the active site of muscle relaxant is bound to carboxyl groups in the cyclodextrin so can’t interact with ACh receptors at the NMJ
• causes reversal of neuromuscular blockade

Question 3

What is the absorption/distribution of sugammadex?

Answer 3

• biologically inactive
• no protein binding
• half life 1.8 hrs

Question 4

What are the CVS effects of sugammadex?

Answer 4

• CVS stable
• avoids need to give anticholinesterase and antimuscarinic to reverse neuromuscular blockade, with their attendant SEs

Question 5

What is the affinity for sugammadex?

Answer 5

Rocuronium > vecuronium > pancuronium (pancuronium is not licensed for reversal with this)

Produces rapid reversal because encapsulating the muscle relaxant in the plasma creates a concentration gradient between plasma and NMJ - causes roc/vec to diffuse away from NMJ into plasma

Question 6

What is sugammadex?

Answer 6

Modified gamma cyclodextrin

Clear colourless solution 100mg/ml in 2ml or 5ml vials

Question 7

What is the dose of sugammadex?

Answer 7

• moderate block: 2 twitches 2mg/kg
• deep block: 1-2 post tetanic count = 4mg/kg
• immediate reversal from RSI = 16mg/kg

Question 8

What is the metabolism and excretion of sugammadex?

Answer 8

• both cyclodextrin-aminosteroid complex and cyclodextrin excreted in urine