Neuromuscular blockade, induced by neuromuscular blocking agents, has allowed prescribed immobility, improved surgical exposure, optimal airway management conditions, and facilitated mechanical ventilation. However, termination of the effects of neuromuscular blocking agents has, until now, remained limited. A novel cyclodextrin encapsulation process offers improved termination of the paralytic effects of aminosteroidal non-depolarizing neuromuscular blocking agents. Sugammadex sodium is the fi rst in a new class of drug called selective relaxant binding agents. Currently, in clinical trials, sugammadex, a modifi ed gamma cyclodextrin, has shown consistent and rapid termination of neuromuscular blockade with few side effects. The pharmacology of cyclodextrins in general and sugammadex in particular, together with the results of current clinical research are reviewed. The ability of sugammadex to terminate the action of neuromuscular blocking agents by direct encapsulation is compared to the indirect competitive antagonism of their effects by cholinesterase inhibitors. Also discussed are the clinical implications that extend beyond fast, effective reversal, including numerous potential peri-operative benefi ts.
Propofol has become the most widely used sedation and anesthetic drug worldwide. Previously it was thought to lack abuse and dependence potential. Increased awareness of actual propofol abuse cases, however, is providing greater understanding of the associated (or perceived) motivations and rewards of propofol abuse. We report the details of two new propofol abuse cases including the motivations for choosing this drug, abuse practices, subjective experiences, and outcomes. An exploration of reported objective and subjective patterns in propofol abuse case reports was conducted using a modified process of thematic (pattern) analysis. These patterns include: healthcare providers are the most frequent propofol abusers, 23 hospital drug diversion is a primary access, abuse regimens consist of frequent injections, there often exists underlying psychological unrest, typically there is a history of prior drug and alcohol abuse, abusers are seeking relief from anxiety and stress along with restful sleep, abusers report a craving desire, death is frequently an outcome, and rehabilitation programs can be effective treatments. We conclude restrictive regulation of propofol is necessary to better monitor and control its abuse.
Cyclodextrins encapsulate and electrostatically bind to lipophilic molecules. The exterior of cyclodextrins are water-soluble and maintain aqueous solubility despite encapsulation of non-aqueous soluble molecules. This unique ability to encapsulate lipophilic molecules and maintain water solubility confers numerous pharmacologic advantages for both drug delivery and removal. Cyclodextrins, a component part of supramolecular chemistry, may be in its infancy of anesthetic application but recent advances have been described as novel and revolutionary. A review of current research coupled with an understanding of cyclodextrin properties is necessary to fully appreciate the current uses and future potentials of these unique molecules.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.