Pharmacokinetic and pharmacodynamic studies on phenylbutazone and oxyphenbutazone in goats. 1997

Z Cheng, and E Welsh, and A Nolan, and Q A McKellar
Department of Veterinary Pharmacology, University of Glasgow Veterinary School.

Phenylbutazone was administered intravenously and orally to six goats as a single dose of 4.4 mg/kg and its disposition and bioavailability and the disposition of its active metabolite, oxyphenbutazone, in plasma were investigated. The effect of the administration of the drug of oxyphenbutazone on ex vivo serum thromboxane (TX)B2 generation in platelets was also studied. Phenylbutazone was eliminated slowly with mean (se) elimination half-lives (t1/2 beta) of 15.3 (1.15) hours and 22.0 (3.32) hours after intravenous and oral administration, respectively. The bioavailability of phenylbutazone paste administered orally was 61 (7) per cent (corrected by the t1/2 beta) and relatively slow absorption was observed, as indicated by a time of maximum drug concentration (tmax) of 3.47 (0.39) hours and a mean absorption time (MAT) of 10.4 (8.61) hours. The concentration of oxyphenbutazone in plasma was low and the ratio of the areas under the curve (AUC) of oxyphenbutazone to phenylbutazone was approximately 0.02:1 after both intravenous and oral administration. Thromboxane B2 generation in the platelets was significantly inhibited (P < 0.05) from one to 12 hours after intravenous administration and from two to 12 hours after oral administration. The results suggest that phenylbutazone is a potentially useful non-steroidal anti-inflammatory drug for use in goats by either route of administration.

UI MeSH Term Description Entries
D007275 Injections, Intravenous Injections made into a vein for therapeutic or experimental purposes. Intravenous Injections,Injection, Intravenous,Intravenous Injection
D008297 Male Males
D010113 Oxyphenbutazone A non-steroidal anti-inflammatory drug. Oxyphenbutazone eyedrops have been used abroad in the management of postoperative ocular inflammation, superficial eye injuries, and episcleritis. (From AMA, Drug Evaluations Annual, 1994, p2000) It had been used by mouth in rheumatic disorders such as ankylosing spondylitis, osteoarthritis, and rheumatoid arthritis but such use is no longer considered justified owing to the risk of severe hematological adverse effects. (From Martindale, The Extra Pharmacopoeia, 30th ed, p27) Hydroxyphenylbutazone,Diflamil,Oxyphenylbutazone,Tanderil
D010653 Phenylbutazone A butyl-diphenyl-pyrazolidinedione that has anti-inflammatory, antipyretic, and analgesic activities. It has been used in ANKYLOSING SPONDYLITIS; RHEUMATOID ARTHRITIS; and REACTIVE ARTHRITIS. Diphenylbutazone,Fenilbutazon,Butacote,Butadion,Butadione,Butapirazol,Butapyrazole,Butazolidin
D005260 Female Females
D006041 Goats Any of numerous agile, hollow-horned RUMINANTS of the genus Capra, in the family Bovidae, closely related to the SHEEP. Capra,Capras,Goat
D000284 Administration, Oral The giving of drugs, chemicals, or other substances by mouth. Drug Administration, Oral,Administration, Oral Drug,Oral Administration,Oral Drug Administration,Administrations, Oral,Administrations, Oral Drug,Drug Administrations, Oral,Oral Administrations,Oral Drug Administrations
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
D000894 Anti-Inflammatory Agents, Non-Steroidal Anti-inflammatory agents that are non-steroidal in nature. In addition to anti-inflammatory actions, they have analgesic, antipyretic, and platelet-inhibitory actions. They act by blocking the synthesis of prostaglandins by inhibiting cyclooxygenase, which converts arachidonic acid to cyclic endoperoxides, precursors of prostaglandins. Inhibition of prostaglandin synthesis accounts for their analgesic, antipyretic, and platelet-inhibitory actions; other mechanisms may contribute to their anti-inflammatory effects. Analgesics, Anti-Inflammatory,Aspirin-Like Agent,Aspirin-Like Agents,NSAID,Non-Steroidal Anti-Inflammatory Agent,Non-Steroidal Anti-Inflammatory Agents,Nonsteroidal Anti-Inflammatory Agent,Anti Inflammatory Agents, Nonsteroidal,Antiinflammatory Agents, Non Steroidal,Antiinflammatory Agents, Nonsteroidal,NSAIDs,Nonsteroidal Anti-Inflammatory Agents,Agent, Aspirin-Like,Agent, Non-Steroidal Anti-Inflammatory,Agent, Nonsteroidal Anti-Inflammatory,Anti-Inflammatory Agent, Non-Steroidal,Anti-Inflammatory Agent, Nonsteroidal,Anti-Inflammatory Analgesics,Aspirin Like Agent,Aspirin Like Agents,Non Steroidal Anti Inflammatory Agent,Non Steroidal Anti Inflammatory Agents,Nonsteroidal Anti Inflammatory Agent,Nonsteroidal Anti Inflammatory Agents,Nonsteroidal Antiinflammatory Agents
D001682 Biological Availability The extent to which the active ingredient of a drug dosage form becomes available at the site of drug action or in a biological medium believed to reflect accessibility to a site of action. Availability Equivalency,Bioavailability,Physiologic Availability,Availability, Biologic,Availability, Biological,Availability, Physiologic,Biologic Availability,Availabilities, Biologic,Availabilities, Biological,Availabilities, Physiologic,Availability Equivalencies,Bioavailabilities,Biologic Availabilities,Biological Availabilities,Equivalencies, Availability,Equivalency, Availability,Physiologic Availabilities

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