Pharmacokinetic and pharmacodynamic characteristics of medications used for moderate sedation

Abstract

The ability to deliver safe and effective moderate sedation is crucial to the ability to perform invasive procedures. Sedative drugs should have a quick onset of action, provide rapid and clear-headed recovery, and be easy to administer and monitor. A number of drugs have been demonstrated to provide effective sedation for outpatient procedures but since each agent has its own limitations, a thorough knowledge of the available drugs is required to choose the appropriate drug, dose and/or combination regimen for individual patients. Midazolam, propofol, ketamine and sevoflurane are the most frequently used agents, and all have a quick onset of action and rapid recovery. The primary drawback of midazolam is the potential for accumulation of the drug, which can result in prolonged sedation and a hangover effect. The anaesthetics propofol and sevoflurane have recently been used for sedation in procedures of short duration. Although effective, these agents require monitored anaesthesia care. Ketamine is an effective agent, particularly in children, but there is concern regarding emergence reactions. AQUAVAN injection (fospropofol disodium), a phosphorylated prodrug of propofol, is an investigational agent possessing a unique and distinct pharmacokinetic and pharmacodynamic profile. Compared with propofol emulsion, AQUAVAN is associated with a slightly longer time to peak effect and a more prolonged pharmacodynamic effect. Advances in the delivery of sedation, including the development of new sedative agents, have the potential to further improve the provision of moderate sedation for a variety of invasive procedures.