Sugamma.....something or other

The only reason I had heard of this prior to the SAQs in April was because one of my previous bosses, who I did regular lists with as an SHO, was fascinated by it and would discuss it regularly - amazing to think that even a couple of years later those 'discussions' would be useful to me! So what's all the fuss about?

Sugammadex (AKA 'The Molecular Condom' as described by gaussling)

Company

- Organon

Codenames

- Org 25969

- Modified γ-cyclodextrin

Structure

- Lipophilic core and hydrophilic periphery enabling the molecule to engulf and bind lipophilic molecules while maintaining aqueous solubility (8 negatively-charged thio ether extensions are situated at the 6th carbon position of each ring, thus extending the cavity size allowing greater encapsulation of the rocuronium molecule).

Mechanism of action

- The first selective relaxant binding agent - it forms very tight water-soluble complexes at a 1:1 ratio with aminosteroidal neuromuscular blocking drugs e.g. rocuronium, preventing them from binding to the ACh molecule and exerting muscular relaxation.

Uses

- Reversal of profound neuromuscular blockade without the need to inhibit acetylcholinesterase i.e. eliminating the autonomic/CVS effects of the more traditional acetylcholinesterase inhibitors(neostigmine) and the concomitant antimuscarinics (glycopyrrolate) that must be also administered. (Phase 3 trials)

- Elimination of the incomplete reversal experienced with use of traditional acetylcholinesterase inhibitors.

- Also, the rapid onset (and now reversal by Sugammadex) of action of rocuronium could make it a safer alternative to suxamethonium in rapid sequence inductions.

Pharmacodynamics/Pharmacokinetics

- No effects on other receptor systems in body i.e. biologically inactive

- Does not bind to plasma protein
- No renal excretion