Drug-specific cyclodextrins: The future of rapid neuromuscular block reversal

This is the authors' abstract. We don't add key points for this paper.

Chemical modification of /-cyclodextrin afforded Or-25969 that has a cavity dimension capable of forming a binary host-guest complex with the steroidal neuromuscular blocker rocuronium bromide with high affinity. In this complex. rocuronium is encapsulated inside the cavity of Or-25969. As a consequence, the neuromuscular blocking activity of rocuronium can be reversed by Org-25969. The reversal produced by 0rg - 25969 is more efficacious than the standard combination of acetylcholinesterase inhibitor and muscarinic receptor antagonist, e.g., neostigmine + atropine. Unlike neostigmine + atropine. Org-25969 does not interfere with the acetylcholine homeostasis. At the effective reversal dose (0.5 μmol/kg i.v.), Org-25969 produced negligible changes in hemodynamic parameters in anesthetized guinea pigs, cats and monkeys. Org-25969 is also effective in reversing profound block induced by 3 times the ED ( x ) of rocuronium in guinea pigs at a rate at least 3 times faster than neostigmine + atropine. Therefore, Org-25969 is also potentially useful for early or escape reversal of rocuronium, for instance, in a intubate, cannot ventilate situation.