Effective clinical management of pain requires an understanding of the underlying mechanisms responsible for its generation. A skillful approach—based upon better knowledge concerning the anatomical structures, pathways, and events that result in pain—is more likely to lead to effective clinical management of pain. The ability to explain the complex process of pain transmission in a less complex manner can better enable the patient and caregivers to play a greater role in the treatment of painful disorders. The discussion will also include an overview of medication classes typically considered for pain and the pathways they affect.