Pharmacokinetics of intravenous and intramuscular buprenorphine in the horse. 2012

J L Davis, and K M Messenger, and D H LaFevers, and B M Barlow, and L P Posner
Department of Clinical Sciences, North Carolina State University, College of Veterinary Medicine, Raleigh, NC 27606, USA. jennifer_davis@ncsu.edu

The purpose of this study was to determine the pharmacokinetics of buprenorphine following intravenous (i.v.) and intramuscular (i.m.) administration in horses. Six horses received i.v. or i.m. buprenorphine (0.005 mg/kg) in a randomized, crossover design. Plasma samples were collected at predetermined times and horses were monitored for adverse reactions. Buprenorphine concentrations were measured using ultra-performance liquid chromatography with electrospray ionization mass spectrometry. Following i.v. administration, clearance was 7.97±5.16 mL/kg/min, and half-life (T(1/2)) was 3.58 h (harmonic mean). Volume of distribution was 3.01±1.69 L/kg. Following i.m. administration, maximum concentration (C(max)) was 1.74±0.09 ng/mL, which was significantly lower than the highest measured concentration (4.34±1.22 ng/mL) after i.v. administration (P<0.001). Time to C(max) was 0.9±0.69 h and T(1/2) was 4.24 h. Bioavailability was variable (51-88%). Several horses showed signs of excitement. Gut sounds were decreased 10±2.19 and 8.67±1.63 h in the i.v. and i.m. group, respectively. Buprenorphine has a moderate T(1/2) in the horse and was detected at concentrations expected to be therapeutic in other species after i.v. and i.m. administration of 0.005 mg/kg. Signs of excitement and gastrointestinal stasis may be noted.

UI MeSH Term Description Entries
D007273 Injections, Intramuscular Forceful administration into a muscle of liquid medication, nutrient, or other fluid through a hollow needle piercing the muscle and any tissue covering it. Intramuscular Injections,Injection, Intramuscular,Intramuscular Injection
D007275 Injections, Intravenous Injections made into a vein for therapeutic or experimental purposes. Intravenous Injections,Injection, Intravenous,Intravenous Injection
D008297 Male Males
D002047 Buprenorphine A derivative of the opioid alkaloid THEBAINE that is a more potent and longer lasting analgesic than MORPHINE. It appears to act as a partial agonist at mu and kappa opioid receptors and as an antagonist at delta receptors. The lack of delta-agonist activity has been suggested to account for the observation that buprenorphine tolerance may not develop with chronic use. 6029-M,Buprenex,Buprenorphine Hydrochloride,Buprex,Prefin,RX-6029-M,Subutex,Temgesic,Temgésic,6029 M,6029M,Hydrochloride, Buprenorphine,RX 6029 M,RX6029M
D005260 Female Females
D006207 Half-Life The time it takes for a substance (drug, radioactive nuclide, or other) to lose half of its pharmacologic, physiologic, or radiologic activity. Halflife,Half Life,Half-Lifes,Halflifes
D006736 Horses Large, hoofed mammals of the family EQUIDAE. Horses are active day and night with most of the day spent seeking and consuming food. Feeding peaks occur in the early morning and late afternoon, and there are several daily periods of rest. Equus caballus,Equus przewalskii,Horse, Domestic,Domestic Horse,Domestic Horses,Horse,Horses, Domestic
D000701 Analgesics, Opioid Compounds with activity like OPIATE ALKALOIDS, acting at OPIOID RECEPTORS. Properties include induction of ANALGESIA or NARCOSIS. Opioid,Opioid Analgesic,Opioid Analgesics,Opioids,Full Opioid Agonists,Opioid Full Agonists,Opioid Mixed Agonist-Antagonists,Opioid Partial Agonists,Partial Opioid Agonists,Agonist-Antagonists, Opioid Mixed,Agonists, Full Opioid,Agonists, Opioid Full,Agonists, Opioid Partial,Agonists, Partial Opioid,Analgesic, Opioid,Full Agonists, Opioid,Mixed Agonist-Antagonists, Opioid,Opioid Agonists, Full,Opioid Agonists, Partial,Opioid Mixed Agonist Antagonists,Partial Agonists, Opioid
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D018592 Cross-Over Studies Studies comparing two or more treatments or interventions in which the subjects or patients, upon completion of the course of one treatment, are switched to another. In the case of two treatments, A and B, half the subjects are randomly allocated to receive these in the order A, B and half to receive them in the order B, A. A criticism of this design is that effects of the first treatment may carry over into the period when the second is given. (Last, A Dictionary of Epidemiology, 2d ed) Cross-Over Design,Cross-Over Trials,Crossover Design,Crossover Studies,Crossover Trials,Cross Over Design,Cross Over Studies,Cross Over Trials,Cross-Over Designs,Cross-Over Study,Crossover Designs,Crossover Study,Design, Cross-Over,Design, Crossover,Designs, Cross-Over,Designs, Crossover,Studies, Cross-Over,Studies, Crossover,Study, Cross-Over,Study, Crossover,Trial, Cross-Over,Trial, Crossover,Trials, Cross-Over,Trials, Crossover

Related Publications

J L Davis, and K M Messenger, and D H LaFevers, and B M Barlow, and L P Posner
May 1984, American journal of veterinary research,
J L Davis, and K M Messenger, and D H LaFevers, and B M Barlow, and L P Posner
June 1985, Journal of veterinary pharmacology and therapeutics,
J L Davis, and K M Messenger, and D H LaFevers, and B M Barlow, and L P Posner
July 2002, Veterinary journal (London, England : 1997),
J L Davis, and K M Messenger, and D H LaFevers, and B M Barlow, and L P Posner
October 2014, Journal of veterinary pharmacology and therapeutics,
J L Davis, and K M Messenger, and D H LaFevers, and B M Barlow, and L P Posner
August 2014, American journal of veterinary research,
J L Davis, and K M Messenger, and D H LaFevers, and B M Barlow, and L P Posner
August 1989, British journal of clinical pharmacology,
J L Davis, and K M Messenger, and D H LaFevers, and B M Barlow, and L P Posner
August 2013, Drug and alcohol dependence,
J L Davis, and K M Messenger, and D H LaFevers, and B M Barlow, and L P Posner
October 1988, Masui. The Japanese journal of anesthesiology,
J L Davis, and K M Messenger, and D H LaFevers, and B M Barlow, and L P Posner
October 1995, Pharmaceutical research,
J L Davis, and K M Messenger, and D H LaFevers, and B M Barlow, and L P Posner
January 1984, International journal of clinical pharmacology research,
Copied contents to your clipboard!