Since the advent of their use over a hundred years ago, local anesthetics have continued to shape the field of dentistry and its specialties by providing the means with which to accomplish a multitude of procedures in an office setting without the need for a general anesthetic. In oral and maxillofacial surgery, local anesthetics have the added benefit of providing hemostasis to the surgical field, resulting in increased visualization and attenuation of blood loss. In addition, long-acting local anesthetics have become increasingly popular for the control of postoperative pain, mitigating the need for the prescription of narcotic pain medication. A variety of agents, both for topical use and for injection, are available on the market in the United States. While the mechanism of action of these local anesthetic agents is similar, each drug offers its own unique characteristics, allowing the practitioner to tailor his or her selection of local anesthetic to the needs of the patient and the demands of the procedure. The aim of this chapter will be to introduce the basic pharmacology of local anesthetic agents and to familiarize the reader with the variety of drugs currently available on the market, their unique properties, and potential risks and complications associated with their use.