Body fluid and endometrial concentrations of ketoconazole in mares after intravenous injection or repeated gavage.
After single oral administration of ketoconazole (30 mg/kg bodyweight [bwt]) in 50 ml of corn syrup to a healthy mare, the drug was not detected in serum. Ketoconazole in 0.2 N HC1 was administered intragastrically to six healthy adult horses in five consecutive doses of 30 mg/kg bwt at 12 h intervals. Ketoconazole concentrations were measured in serum, synovial fluid, peritoneal fluid, cerebrospinal fluid (CSF), urine and endometrium. Mean peak serum ketoconazole concentration was 3.76 micrograms/ml at 1.5 to 2 h after intragastric administration. Mean peak synovial concentration was 0.87 micrograms/ml 3 h after the fifth dose. Similarly, mean peritoneal concentration peaked 3 h after the fifth dose at 1.62 micrograms/ml. Mean endometrial concentrations peaked at 2.73 micrograms/ml 2 h after the fifth dose. Ketoconazole was detected in the CSF of only one of the six mares at a concentration of 0.28 micrograms/ml 3 h after the fifth dose. The highest measured concentration of ketoconazole in urine was 6.15 micrograms/ml 2 h after the fifth dose. A single intravenous injection of ketoconazole (10 mg/kg bwt) was given to one of the six mares; the overall elimination rate constant was estimated at 0.22/h and bioavailability after oral administration was 23 per cent.
Prades
M
M
Department of Surgical Sciences, College of Veterinary Medicine, University of Florida, Gainesville 32610-0136.
Brown
M P
MP
Gronwall
R
R
Houston
A E
AE
D000284:Administration, Oral / Q000662:veterinary; D000818:Animals; D001682:Biological Availability; D001826:Body Fluids / Q000378:metabolism*; D004717:Endometrium / Q000378:metabolism*; D005260:Female; D006736:Horses / Q000378:metabolism*; D007275:Injections, Intravenous / Q000662:veterinary; D007654:Ketoconazole / Q000008:administration & dosage / Q000097:blood / Q000134:cerebrospinal fluid / Q000493:pharmacokinetics* / Q000652:urine; D010529:Peritoneal Cavity / Q000378:metabolism; D013582:Synovial Fluid / Q000378:metabolism
D007654:Ketoconazole