Pharmacokinetics and metabolism of amitraz in ponies and sheep.
Amitraz and its active metabolite BTS27271 were given intravenously to ponies and sheep at equimolar doses of 1 mg/kg and 0.68 mg/kg, respectively, and the plasma concentrations of amitraz and BTS27271 estimated at various times thereafter. Amitraz was hydrolysed to BTS27271 in both species. Amitraz was undetectable in sheep plasma after approximately 5 min but persisted in the plasma of ponies for at least 90 min. The persistence of unmetabolized amitraz in ponies may have implications for the toxicity of amitraz in that species. The primary and secondary disposition half-lives of amitraz in ponies were 2 and 39 min, respectively. BTS27271 was distributed rapidly outside the plasma in both species with a primary disposition half-life of 4.4 min in sheep and 5.9 min in ponies. The secondary disposition half-lives were 51 and 55 min, respectively. The secondary phase of the disposition of BTS27271 was similar whether BTS27271 was given directly or derived by hydrolysis from amitraz. However, significant differences were evident in the primary phase of the disposition of BTS27271. Sheep demonstrated a larger apparent volume of distribution of BTS27271 than ponies and more rapid body clearance.
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Department of Physiology and Pharmacology, University of Queensland, St. Lucia, Australia.
Mogg
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D000042:Absorption; D000578:Amidines / Q000493:pharmacokinetics; D000818:Animals; D005260:Female; D006207:Half-Life; D006736:Horses / Q000378:metabolism*; D006868:Hydrolysis; D007275:Injections, Intravenous / Q000662:veterinary; D007306:Insecticides / Q000493:pharmacokinetics*; D008297:Male; D012756:Sheep / Q000378:metabolism*; D014052:Toluidines / Q000493:pharmacokinetics*
D000578:Amidines; D007306:Insecticides; D014052:Toluidines; C025699:U 40481; C014983:amitraz