BACKGROUND Sugammadex is a modified [gamma] cyclodextrin compound, which encapsulates rocuronium to provide for a rapid reversal of residual neuromuscular blockade. We tested the hypothesis that sugammadex would provide for a more rapid reversal of a moderately profound residual rocuronium-induced blockade than the commonly used cholinesterase inhibitors, edrophonium and neostigmine. METHODS ...

The molecular mechanism of penicillin action is closely analogous to that of neostigmine. Both drugs react covalently with the active-site serine of their target enzymes. In both cases, the susceptible enzymes self-catalyze their inactivation by their respective drugs. Kinetic analysis of cholinesterase by Richard J. Kitz and Irwin B. Wilson helped to establish that concept. Neostigmine and pen...

This review provides recommendations for anesthesia providers who may not yet have quantitative monitoring and sugammadex available and thus are providing care within the limitations of a conventional peripheral nerve stimulator (PNS) and neostigmine. In order to achieve best results, the provider needs to understand the limitations of the PNS. The PNS should be applied properly and early. All ...

BACKGROUND At present, reversal of neuromuscular block induced by steroidal neuromuscular blocking agents (NMBAs) is achieved by administration of cholinesterase inhibitors. Chemical encapsulation of steroidal NMBAs, such as rocuronium, by a cyclodextrin is a new concept in neuromuscular block reversal. The present study evaluates the capacity of nine synthetic cyclodextrin derivatives (Org 252...

The effect of temperature on the potencies of neuromuscular blocking agents remains unclear. This study was undertaken to examine the effects of different neuromuscular blocking agents at 37 and 27 degrees C at a constant carbon dioxide content (alpha stat principle). The effect of neostigmine 1 mumol litre-1 induced antagonism of these agents was also investigated. Phrenic nerve-hemidiaphragm ...

The authors examined the influence of acetylcholinesterase inhibitor (neostigmine) on the in vitro reactivity of urinary bladder smooth muscle (UBSM) in guinea pigs. The aim of the present study was to determine the participation of pharmacokinetic properties of acetylcholine and carbachol in different UBSM reactivity to these mediators. In vitro method of organ baths was used and reactivity of...

Prolonged neuromuscular block occurs when suxamethonium is given after neostigmine or pyridostigmine; however, studies of edrophonium and suxamethonium have yielded conflicting results. We have studied, therefore, interactions between suxamethonium and all three anticholinesterases in rats anaesthetized with pentobarbitone. After recovery from an initial bolus of suxamethonium, saline, edrophon...

Determination of plasma concentration of pyridostigmine in 20 myasthenic patients on maintenance therapy revealed rather small intraindividual variations within a dose interval. The predose concentration varied considerably between different patients and up to seven fold in patients on the same daily dose. No pharmacokinetic interaction between pyridostigmine and neostigmine was found in five p...