OBJECTIVE To assess effects of buprenorphine hydrochloride (BH), sustained-release buprenorphine (SRB), and high-concentration buprenorphine (HCB) formulations in healthy rats. ANIMALS 8 Sprague-Dawley rats. PROCEDURES In a crossover-design study, rats received BH (0.05 mg/kg), SRB (1.2 mg/kg), HCB (0.30 mg/kg), or 5% dextrose solution (0.2 mL/kg), SC, once. Self-injurious behavior and thermal sensitivity (hind limb withdrawal latencies) were assessed prior to injection (time 0) and 1, 4, 8, 12, and 24 hours after injection. Food intake, kaolin intake, and fecal output were measured over 12-hour light and dark periods before and after each treatment. Values were compared among treatments and time points. RESULTS Self-injurious behavior was detected with all buprenorphine treatments; scores were greater at all time points during the 12 hours after HCB and 24 hours after SRB administration than at time 0. Percentage change in hind limb withdrawal latencies from time 0 was higher with BH and HCB 1 hour after injection than at other time points. Postinjection light-period food intake was higher (BH and HCB) and dark-period food intake was lower (BH, HCB, and SRB), compared with preinjection values for the same treatments. For SRB, postinjection light-period kaolin intake was greater than the preinjection value, and postinjection light- and dark-period kaolin intake was greater than that for other treatments. CONCLUSIONS AND CLINICAL RELEVANCE Hypoalgesic effects were briefly observed after administration of BH or HCB in healthy rats; adverse effects were detected in some rats with all buprenorphine formulations. Studies comparing effects of BH, SRB, and HCB in rats undergoing surgery or other noxious stimuli are indicated to determine clinical benefits in this species.

OBJECTIVE To evaluate effects of high-concentration buprenorphine (HCB) on self-injurious behavior, food intake, fecal output, and thermal withdrawal latencies in healthy rats. ANIMALS 8 Sprague-Dawley rats. PROCEDURES Rats received 4 SC treatments (HCB at 0.075, 0.15, or 0.30 mg/kg [HCB0.075, HCB0.15, and HCB0.30, respectively] or 5% dextrose solution [0.20 mL/kg]) in a randomized, crossover-design study. Self-injurious behavior was assessed for 8 hours after injection. Food intake and fecal output were assessed for predetermined periods before and after treatment and separated into 12-hour light and dark periods for further analysis. Withdrawal latencies were assessed before (time 0) and at predetermined times after injection. Data were compared among treatments and time points. RESULTS Self-injurious behavior was observed up to 8 hours after injection for all HCB, but not dextrose, treatments. Preinjection food intake and fecal output amounts were similar among groups and higher during the dark period than during the light period. Food intake after all HCB treatments was higher during the light period and lower during the dark period, compared with preinjection results for the same treatments and with postinjection results for dextrose administration. Light-period fecal output was lower after HCB0.15 and HCB0.30 administration, compared with preinjection values for the same treatments and postinjection values for dextrose administration. Percentage change in withdrawal latency was significantly higher than that at time 0 (ie, 0%) for only 1 treatment (HCB0.30) at 1 time point (1 hour after injection). CONCLUSIONS AND CLINICAL RELEVANCE Although HCB0.30 produced a degree of thermal hypoalgesia in healthy rats, self-injurious behavior and alterations in food intake and fecal output were detected, potentially affecting clinical utility of the treatment.