Novel pharmacological approaches for the antagonism of neuromuscular blockade.
Gamma cyclodextrin and purified plasma cholinesterase are 2 novel pharmacological agents being investigated as to their suitability for antagonism of neuromuscular blockade. Both of these agents are devoid of cholinergic stimulation and the accompanying side effects because their action is independent of acetylcholinesterase inhibition. Gamma cyclodextrin antagonizes the steroidal neuromuscular blocker rocuronium via the chemical encapsulation of the molecule forming a "host-guest" complex through van der Waals and hydrophobic interactions in the plasma. Encapsulation decreases plasma drug concentrations, shifting the neuromuscular blocking drug molecules from the neuromuscular junction back to the plasma compartment resulting in a rapid recovery of the neuromuscular function. Org 25969, a modified gamma cyclodextrin, will antagonize profound neuromuscular block induced by rocuronium in approximately 2 minutes. A commercial preparation of purified human plasma cholinesterase has been shown to be effective in reversing succinylcholine or mivacurium-induced block. Administration of exogenous plasma cholinesterase also has been shown to be effective in antagonizing mivacurium-induced neuromuscular block, cocaine toxicity, and organophosphate poisoning.
Pic
Lisa C
LC
University of Iowa College of Nursing, Anesthesia Nursing Program, Iowa City, Iowa, USA.
D000732:Androstanols / Q000037:antagonists & inhibitors; D002802:Cholinesterases / Q000494:pharmacology / Q000627:therapeutic use*; D006801:Humans; D007546:Isoquinolines / Q000037:antagonists & inhibitors; D000077590:Mivacurium; D019148:Neuromuscular Blockade; D003473:Neuromuscular Nondepolarizing Agents / Q000037:antagonists & inhibitors*; D000077123:Rocuronium; D000077122:Sugammadex; D047408:gamma-Cyclodextrins / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*
D000732:Androstanols; D007546:Isoquinolines; D003473:Neuromuscular Nondepolarizing Agents; D047408:gamma-Cyclodextrins; D000077122:Sugammadex; D000077590:Mivacurium; D002802:Cholinesterases; D000077123:Rocuronium