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American journal of veterinary research

Pharmacokinetics of phenylbutazone in camels.


PMID 9185972

Abstract

To document disposition variables of phenylbutazone and its metabolite, oxyphenbutazone, in camels (Camelus dromedarius) after single i.v. bolus administration of phenylbutazone, with a view to making recommendation on avoiding violative residues in racing camels. 6 healthy camels (4 males, 2 females), 5 to 7 years old, and weighing from 350 to 450 kg. Blood samples were collected to 0, 5, 10, 15, 45, and 60 minutes and at 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 24, 26, 28, 30, 40, 48, 50, 53, and 60 hours after i.v. administration of 4.5 mg of phenylbutazone per kg of body weight. Urine was obtained in fractions during the entire blood sample collection period. Serum and urine phenylbutazone concentrations were measured by high-performance liquid chromatography; assay sensitivity was 100 ng/ml. Serum oxyphenbutazone concentration was measured by gas chromatography/mass spectrometry; assay sensitivity was 10 ng/ml. Disposition of phenylbutazone was best described by a two-compartment open model. Mean +/- SEM elimination half-life was 13.44 +/- 0.44 hours. Total body clearance was 12.63 +/- 1.64 mg/kg/h. Renal clearance was between 0.3 and 0.4% of total body clearance. The elimination half-life of oxyphenbutazone was 23.9 +/- 2.09 hours. The elimination half-life and total body clearance of phenylbutazone in camels are intermediate between reported values in horses and cattle. Extrapolation of a dosage regimen from either species to camels is, therefore, not appropriate. Elimination of phenylbutazone in camels is mainly via metabolism. Owing to the long half-life of phenylbutazone and of oxyphenbutazone, and to the zero drug concentration regulation adopted by the racing commissioner in the United Arab Emirates, practicing veterinarians would be advised not to use phenylbutazone in camels for at least 7 days prior to racing.

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SML0540 Oxyphenbutazone, ≥98% (HPLC)
C19H20N2O3