Most children are able to cooperate during conventional, in-office dental treatment using traditional, communicative behavior guidance techniques that are carefully selected and applied to the developmental needs of a particular child. Children who are unable to cooperate during conventional treatment due to a lack of psychological or emotional maturity and/or the existence of a mental, physical, or medical disability may require pharmacologic techniques such as procedural sedation or general anesthesia to complete rehabilitative dental treatment. Patient safety dictates that careful preparation and robust case selection processes guide clinical decision-making related to pharmacologic behavior guidance. Before using these techniques, the sedation provider must demonstrate an adequate understanding of these techniques, from definitions and best practices to case selection and patient safety. This article presents essential information-with an emphasis on best practices and patient safety-for dentists who are considering pharmacologic behavior guidance for the children they treat.