OBJECTIVE To determine the pharmacokinetics and sedative effects of 2 doses of a concentrated buprenorphine formulation after SC administration to red-tailed hawks (Buteo jamaicensis). ANIMALS 6 adult red-tailed hawks. PROCEDURES Concentrated buprenorphine (0.3 mg/kg, SC) was administered to all birds. Blood samples were collected at 10 time points over 24 hours after drug administration to determine plasma buprenorphine concentrations. After a 4-week washout period, the same birds received the same formulation at a higher dose (1.8 mg/kg, SC), and blood samples were collected at 13 time points over 96 hours. Hawks were monitored for adverse effects and assigned agitation-sedation scores at each sample collection time. Plasma buprenorphine concentrations were quantified by liquid chromatography-tandem mass spectrometry. RESULTS Mean time to maximum plasma buprenorphine concentration was 7.2 minutes and 26.1 minutes after administration of the 0.3-mg/kg and 1.8-mg/kg doses, respectively. Plasma buprenorphine concentrations were > 1 ng/mL for mean durations of 24 and 48 hours after low- and high-dose administration, respectively. Mean elimination half-life was 6.23 hours for the low dose and 7.84 hours for the high dose. Mean agitation-sedation scores were higher (indicating some degree of sedation) than the baseline values for 24 hours at both doses. No clinically important adverse effects were observed. CONCLUSIONS AND CLINICAL RELEVANCE Concentrated buprenorphine was rapidly absorbed, and plasma drug concentrations considered to have analgesic effects in other raptor species were maintained for extended periods. Most birds had mild to moderate sedation. Additional studies are needed to evaluate the pharmacodynamics of these doses of concentrated buprenorphine in red-tailed hawks.
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http://dx.doi.org/10.2460/ajvr.79.1.13 | DOI Listing |
Pharmaceutics
December 2024
Pharmathen SA, 31 Spartis Str., 14452 Metamorfosi Attica, Greece.
Regulatory authorities typically require bioequivalence to be demonstrated by comparing pharmacokinetic parameters like area under the plasma concentration-time curve (AUC) and maximum plasma concentration (C). Because in certain cases, AUC and C alone may not be adequate to identify formulation differences in early and/or late segments of the dosing interval, partial AUCs (pAUCs) have been proposed as additional metrics to evaluate bioequivalence. Even though cut-off points for pAUCs are usually decided based on clinical relevance, the identification of the correct cut-off range remains elusive in many other cases and tends to contribute to increased pAUC estimate variabilities.
View Article and Find Full Text PDFVet Anaesth Analg
January 2025
Department of Surgical and Radiological Sciences, School of Veterinary Medicine, University of California, Davis, CA, USA.
Objective: To characterize the effect of buprenorphine on the minimum alveolar concentration of isoflurane (MACiso) in cats.
Study Design: Randomized, crossover, experimental study.
Animals: A group of six healthy male neutered cats, aged 2-8 years with body mass 5.
Eur J Pharmacol
January 2025
Department of Pharmacology, University of Texas Health Science Center at San Antonio, San Antonio, TX, USA, United States. Electronic address:
Buprenorphine is an FDA approved drug for the treatment of opioid use disorder and is a long-lasting, low efficacy (partial) agonist of the μ opioid receptor. As a partial agonist, buprenorphine can act as either an agonist or an antagonist depending on the efficiency of the cellular signaling system. Here we investigated the antagonist properties of buprenorphine using a genetically-encoded biosensor to monitor cAMP levels in real time in HEK293 cells expressing a relatively low density of the human μ receptor.
View Article and Find Full Text PDFJ Addict Med
December 2024
From Camurus AB, Lund, Sweden (SP, FT); New York State Psychiatric Institute, Columbia University Irving Medical Center, New York, NY (EVN); and Center on Drug and Alcohol Research, University of Kentucky College of Medicine, Lexington, KY (MRL, SLW).
J Addict Med
December 2024
From the Department of Pharmacological and Pharmaceutical Sciences, College of Pharmacy, University of Houston, Houston, TX (ZZ, JC, SS, VTŠ, TY, RS, MH); School of Dentistry, University of Texas Health Science Center at Houston, TX (BW).
Objectives: The US Food and Drug Administration (FDA) issued a warning about buprenorphine-induced dental caries of unknown mechanism in 2022. To investigate the potential mechanism, the association between local buprenorphine exposure and dental biofilm formation will be explored in this study.
Methods: Female F344 rats were dosed with sublingual buprenorphine film or intravenous injection to explore the oral cavity exposure of the buprenorphine.
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