Pain, which is often inadequately treated, accompanies the more than 23 million surgical procedures performed each year and may persist long after tissue heals. Preemptive analgesia, an evolving clinical concept, involves the introduction of an analgesic regimen before the onset of noxious stimuli, with the goal of preventing sensitization of the nervous system to subsequent stimuli that could amplify pain. Surgery offers the most promising setting for preemptive analgesia because the timing of noxious stimuli is known. When adequate drug doses are administered to appropriately selected patients before surgery, intravenous opiates, local anesthetic infiltration, nerve block, subarachnoid block and epidural block offer benefits that can be observed as long as one year after surgery. The most effective preemptive analgesic regimens are those that are capable of limiting sensitization of the nervous system throughout the entire perioperative period.