The spectrum of sedative and analgesic agents available to those who provide pediatric sedation and analgesia in the emergency department has broadened considerably over the past 2 decades. Pharmacologic agents that can be used alone or in combination in this context include nitrous oxide, midazolam, chloral hydrate, pentobarbital, etomidate, dexmedetomidine, propofol, and ketamine. The pharmacology, common clinical uses, advantages, and disadvantages of each of these agents are reviewed. Pharmacokinetics of the agents is addressed in tabular form, whereas pharmacodynamic aspects of each agent are discussed in more detail. Clinical uses addressed include noninvasive as well as invasive procedures. Relevant studies involving comparison of various sedative regimens for common emergency department procedures are reviewed.