The agents used for sedation and analgesia during endoscopy have complex pharmacokinetic and pharmacodynamic properties. Knowledge of these characteristics is necessary for determining the proper agent and dose for specific patient needs. Short-acting agents, such as fentanyl, midazolam, and propofol, provide rapid sedation with a short duration of action that allows patients to return to normal functioning rapidly. When designing a dosing regimen with these agents, age and organ (liver, kidney) function of patients and concomitant medications that may interfere with metabolic and elimination pathways must be considered.