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The efficacies of bupivacaine and lidocaine together with a preoperatively administered single-dose oral combination of normal- and sustained-release preparations of diclofenac in preventing postoperative pain after third molar removal were compared in a double-blind crossover study. Bilaterally impacted lower third molars were removed in two sessions. Each patient was given one type of local anesthetic on one session and the other in the second. Pain was recorded using a visual analog scale. When the diclofenac combination (150 mg) was given before the operation, postoperative analgesia was better with bupivacaine plus diclofenac than with lidocaine plus diclofenac. Twenty-five out of 40 patients preferred bupivacaine to lidocaine for local anesthesia. It is possible to achieve effective postoperative pain prevention by combining bupivacaine and preoperative normal- and sustained-release preparations of diclofenac.