Wood T, Tai C L, Taylor D G, Woods W E, Wang C J, Houtz P K, Tai H H, Weckman T J, Yang J M, Sturma L
Maxwell H. Gluck Equine Research Center, Department of Veterinary Science, University of Kentucky, Lexington 40546-0099.
Res Commun Chem Pathol Pharmacol. 1989 Feb;63(2):263-79.
Detomidine is a potent non-narcotic sedative agent which is currently in the process of being approved for veterinary clinical use in the United States. Since no effective screening method in horses is available for detomidine, we have developed an 125I radioimmunoassay for detomidine in equine blood and urine as part of a panel of tests for illegal drugs in performance horses. Our 125I radioimmunoassay has an I-50 for detomidine of approximately 2 ng/ml. Our assay shows limited cross-reactivity with the pharmacodynamically similar xylazine, but does not cross-react with acepromazine, epinephrine, haloperidol or promazine. The plasma kinetic data from clinical (greater than or equal to 5 mg/horse) as well as sub-clinical doses indicate first-order elimination in a dose-dependent manner. Within the first 30 minutes after intravenous (IV) administration of 30 mg/horse, plasma levels peak at approximately 20 ng/ml and then decline with an apparent plasma half-life of 25 minutes. Diuresis can occur with administration of clinical doses of detomidine and this effect was accounted for in the analysis of urine samples. Using this method, administration of 30 mg/horse can be readily detected in equine urine for up to 8 hours after IV injection. Additionally, doses as low as 0.5 mg/horse can be detected for short periods of time in blood and urine with use of this assay. Utilization of this assay by research scientists and forensic analysts will allow for the establishment of proper guidelines and controls regarding detomidine administration to performance horses and assurance of compliance with these guidelines.
地托咪定是一种强效非麻醉性镇静剂,目前正在美国进行兽医临床使用的审批。由于马体内没有有效的地托咪定筛查方法,我们开发了一种用于检测马血和尿中地托咪定的125I放射免疫分析法,作为赛马违禁药物检测组合的一部分。我们的125I放射免疫分析法测定地托咪定的I-50约为2 ng/ml。我们的检测方法显示,与药效学上类似的赛拉嗪有有限的交叉反应,但与乙酰丙嗪、肾上腺素、氟哌啶醇或丙嗪无交叉反应。临床剂量(大于或等于5 mg/马)及亚临床剂量的血浆动力学数据表明,其消除呈一级动力学,与剂量有关。静脉注射30 mg/马后30分钟内,血浆水平在约20 ng/ml时达到峰值,然后下降,表观血浆半衰期为25分钟。临床剂量的地托咪定给药后可出现利尿,在分析尿样时已考虑到这种影响。使用这种方法,静脉注射后8小时内可在马尿中轻松检测到30 mg/马的给药量。此外,使用该检测方法,在血液和尿液中短时间内可检测到低至0.5 mg/马的剂量。研究科学家和法医分析师使用该检测方法将有助于制定关于向赛马给药地托咪定的适当指导方针和控制措施,并确保遵守这些指导方针。