Antinociceptive efficacy and plasma concentrations of transdermal buprenorphine in dogs.
To assess the antinociceptive efficacy of transdermal (TD) buprenorphine (B) in dogs, a prospective, positive-controlled experimental study was performed in 10 healthy Beagles. In an open label crossover design, the dogs initially received intravenous B (IVB, 0.02 mg kg(-1)) as a positive control, followed by TDB (52.5 μg h(-1)) 4 months later. Blood was collected at regular intervals for determination of the plasma concentrations of B ([B]) and its metabolite norbuprenorphine. The antinociceptive efficacy was assessed using thermal and mechanical models of nociception. The peak concentration [B] was 1.54 ng mL(-1) (±1.98) 60 h after TDB application, although three dogs had no measurable [B] after TDB. Maximum thermal threshold (TT) was 52.6 °C (±0.48) at 1h after IVB administration and 51.63 °C (±1.01) 72 h after TDB application. The significant increase in TT indicated that effective antinociception was achieved beyond 36 h after the application of TDB, lasting until patch removal. There was hysteresis between [B] and the antinociceptive effect.
Pieper
Korbinian
K
Department of Small Animal Surgery, Faculty of Veterinary Medicine, Ludwig-Maximilians-Universität München, Munich, Germany. Korbinian.Pieper@lmu.de
Schuster
Tibor
T
Levionnois
Olivier
O
Matis
Ulrike
U
Bergadano
Alessandra
A
D000279:Administration, Cutaneous; D000701:Analgesics, Opioid / Q000493:pharmacokinetics* / Q000494:pharmacology; D000818:Animals; D002047:Buprenorphine / Q000493:pharmacokinetics* / Q000494:pharmacology; D018592:Cross-Over Studies; D004285:Dogs / Q000378:metabolism*; D005260:Female; D008297:Male; D010146:Pain / Q000517:prevention & control / Q000662:veterinary*; D011446:Prospective Studies; D011897:Random Allocation; D016896:Treatment Outcome
D000701:Analgesics, Opioid; D002047:Buprenorphine