True statement (s) about sugammadex:
B. Selectively binds to rocuroniumSugammadex Morgan 5th/23lSugammadex is a novel selective relaxant-binding agentIts three-dimensional structure resembles a hollow truncated cone or doughnut with a hydrophobic cavity and a hydrophilic exterior.Hydrophobic interactions trap the drug (e.g., 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 neuromuscular blocking action and restrains the drug in extracellular fluid where it cannot interact with nicotinic acetylcholine receptors.It is essentially eliminated unchanged via the kidneys.It produces rapid and effective reversal of both shallow and profound rocuronium-induced neuromuscular blockade in a consistent manner.* Barash 6th/Chap 20Sugammadex, previously called ORG 25969, leads to restoration of normal neuromuscular function not by interfering with acetylcholine, the nicotinic receptor or acetylcholinesterase, but by selectively binding to rocuronium, and to a lesser extent to vecuronium and pancuronium.Selective relaxant binding agent for reversal of neuromuscular blockade (NMB) induced by rocuronium or vecuronium in adults undergoing surgery"-reference.medscape.comThe compound is a cyclodextrin, made up of eight sugars arranged in a ring to make a center to accommodate the rocuronium molecule. Once bound, rocuronium is held in place by polar side chains attached to the ring.Because sugammadex does not bind to any known receptory it is devoid of major cardiovascular or other side effects.It does not bind neuromuscular blocking drugs that do not have a steroid nucleus.The benzylisoquinolines, such as atracurium, cisatracurium and mivacurium, and succinylcholine are unaffected by sugammadex.After injection of sugammadex, evidence suggests that binding of rocuronium to sugammadex in plasma leads to a marked decrease in free (unbound) rocuronium concentration, 153 leading to the establishment of a concentration gradient of rocuronium between the neuromuscular junction and plasma. This favors movement of rocuronium from neuromuscular junction to plasma, producing less neuromuscular block. Vecuronium has less affinity for sugammadex than rocuronium does, and pancuronium has less still.Sugammadex could also be used in the case of a failed intubation. If rocuronium 0.6 mg/kg was given, sugammadex 8 mg/kg might be effective as early as 3 minutes after rocuronium injection, and if the dose of rocuronium is doubled to 1.2 mg/ kg, one might need 16 mg/kg of sugammadex. The availability of sugammadex might make succinylcholine obsolete for intubation.
Antisuccinylcholine in action
Selectively binds to rocuronium
Used along with rocuronium for rapid induction Anesthesia
Discovered to reverse the effects of atracurium
Local and Regional Anesthesia