The pharmacokinetics and analgesic effects of extended‐release buprenorphine administered subcutaneously in healthy dogs

• Published in: Journal of veterinary pharmacology and therapeutics Vol. 41; no. 4; pp. 502 - 512
• Main Authors: Barletta, M., Ostenkamp, S. M., Taylor, A. C., Quandt, J., Lascelles, B. D. X., Messenger, K. M.
• Format: Journal Article
• Language: English
• Published: England 01.08.2018
• Subjects: buprenorphine; dog; extended‐release; pharmacodynamics; pharmacokinetics; pharmacokinetics; buprenorphine; dog; pharmacodynamics; extended-release
• ISSN: 0140-7783; 1365-2885
• DOI: 10.1111/jvp.12497

Buprenorphine is a partial μ agonist opioid used for analgesia in dogs. An extended‐release formulation (ER‐buprenorphine) has been shown to provide effective analgesia for 72 hr in rats and mice. Six healthy mongrel dogs were enrolled in a randomized, blinded crossover design to describe and compare the pharmacokinetics and pharmacodynamics of ER‐buprenorphine administered subcutaneous at 0.2 mg/kg (ER‐B) and commercially available buprenorphine for injection intravenously at 0.02 mg/kg (IV‐B). After drug administration, serial blood samples were collected to measure plasma buprenorphine concentrations using liquid chromatography/mass spectrometry detection. Heart rate, respiratory rate, body temperature, sedation score, and thermal threshold latency were recorded throughout the study. Median (range) terminal half‐life, time to maximum concentration, and maximum plasma concentration of ER‐buprenorphine were 12.74 hr (10.43–18.84 hr), 8 hr (4–36 hr), and 5.00 ng/ml (4.29–10.98 ng/ml), respectively. Mild bradycardia, hypothermia, and inappetence were noted in both groups. Thermal threshold latency was significantly prolonged compared to baseline up to 12 hr and up to 72 hr in IV‐B and ER‐B, respectively. These results showed that ER‐buprenorphine administered at a dose of 0.2 mg/kg resulted in prolonged and sustained plasma concentrations and antinociceptive effects up to 72 hr after drug administration.