Menéndez Maria I, Phelps Mitch A, Hothem Elijah A, Bertone Alicia L
Comparative Orthopaedic Research Laboratory, Department of Clinical Sciences, College of Veterinary Medicine, The Ohio State University, Columbus, OH 43210, USA.
Am J Vet Res. 2012 Sep;73(9):1453-61. doi: 10.2460/ajvr.73.9.1453.
To determine the pharmacokinetics of methylprednisolone (MP) and the relationship between MP and hydrocortisone (HYD) concentrations in plasma and urine after intra-articular (IA) administration of 100 or 200 mg of MP acetate (MPA) to horses.
Five 3-year-old Thoroughbred mares.
Horses exercised on a treadmill 3 times/wk during the study. Horses received 100 mg of MPA IA, then 8 weeks later received 200 mg of MPA IA. Plasma and urine samples were obtained at various times for 8 weeks after horses received each dose of MPA; concentrations of MP and HYD were determined. Pharmacokinetic-pharmacodynamic estimates for noncompartmental and compartmental parameters were determined.
Maximum concentration of MP in plasma was similar for each MPA dose; concentrations remained greater than the lower limit of quantitation for 18 and 7 days after IA administration of 200 and 100 mg of MPA, respectively. Maximum concentration and area under the observed concentration-time curve for MP in urine were significantly higher (approximately 10-and 17-fold, respectively) after administration of 200 versus 100 mg of MPA. Hydrocortisone concentration was below quantifiable limits for ≥ 48 hours in plasma and urine of all horses after administration of each MPA dose.
Pharmacokinetics of MP may differ among IA MPA dosing protocols, and MP may be detected in plasma and urine for a longer time than previously reported. This information may aid veterinarians treating sport horses. Further research is warranted to determine whether plasma HYD concentration can aid identification of horses that received exogenous glucocorticoids.
确定向马关节腔内注射100或200mg醋酸甲泼尼龙(MPA)后甲泼尼龙(MP)的药代动力学以及血浆和尿液中MP与氢化可的松(HYD)浓度之间的关系。
5匹3岁的纯种母马。
在研究期间,马每周在跑步机上锻炼3次。马先接受100mg MPA关节腔内注射,然后在8周后接受200mg MPA关节腔内注射。在马接受每剂MPA后的8周内,于不同时间采集血浆和尿液样本;测定MP和HYD的浓度。确定非房室和房室参数的药代动力学-药效学估计值。
各MPA剂量下血浆中MP的最大浓度相似;在关节腔内注射200mg和100mg MPA后,MP浓度分别在18天和7天内保持高于定量下限。与注射100mg MPA相比,注射200mg MPA后尿液中MP的最大浓度和观察到的浓度-时间曲线下面积显著更高(分别约为10倍和17倍)。在每剂MPA给药后,所有马的血浆和尿液中氢化可的松浓度在≥48小时内低于可定量限。
MP的药代动力学可能因关节腔内MPA给药方案不同而有所差异,且MP在血浆和尿液中的检测时间可能比先前报道的更长。这些信息可能有助于兽医治疗运动马。有必要进一步研究以确定血浆HYD浓度是否有助于识别接受外源性糖皮质激素的马。