Objective: To investigate the influence of preemptive analgesia with flurbiprofen axetil on postoperative pain and agitation during the emergence from general anesthesia of the patients undergoing radical masterctomy. Methods: One hundred and twenty patients who were scheduled to undergo radical masterctomy under general anesthesia (ASA I-II) were included. The patients were randomly designated to group A (a dose of 50 mg of flurbiprofen axetil was given immediately after the induction of general anesthesia and another dose of 50 mg was given on completion of incision closure), group B (flurbiprofen axetil 100 mg was given immediately after the induction of general anesthesia), group C (flurbiprofen axetil 100 mg was given on completion of incision closure) and group D (served as the control group, and the same volume of saline was given on completion of incision closure), with 30 patients in each group. Among the groups, the visual analogue scale (VAS) scores at 1, 3, 6, 12 and 24 h after surgery, cardiovascular responses at the end of surgery and after extubation, and incidences of emergence agitation were compared. Results: The VAS scores of the three observation groups were all significantly lower than those of the control group at each time point within 12 h after surgery (all P<0.05), in which, the VAS scores of group A were lower than those of the group C (all P<0.05) at each time points within 12 h and lower than those of group B at 1 and 3 h time points (both P<0.05), while the VAS scores of group B were significantly lower than those of the group C at 1 and 3 h time points (both P<0.05). However, the VAS scores had no significant differences among the four groups at 24 h after surgery (all P>0.05). The alterations of mean arterial pressures (MAP) and heart rates (HR) had no significant differences among the four group at the end of surgery (all P>0.05), but at the time of extubation, the alterations of both parameters of the three observation groups were all less evident than those of the control group (all P<0.05), in which group A showed the minimum changes and followed by group B and group C (all P<0.05). The incidences of emergence agitation were 13.3% in group A, 23.3% in group B, 33.3% in group C and 43.3% in group D, respectively, and all the differences among them had statistical significances (all P<0.05). Conclusion: Preemptive analgesia by flurbiprofen axetil for patients undergoing radical masterctomy can effectively reduce the early postoperative pain and cardiovascular responses as well as the incidence of emergence agitation.