Juzwiak J S, Brown M P, Gronwall R, Houston A E
Peterson and Smith Equine Hospital, Ocala, FL 32674.
Am J Vet Res. 1989 Oct;50(10):1742-7.
Cephapirin (20 mg/kg of body weight, IV) was administered before and after 3 doses of probenecid (25, 50, or 75 mg/kg, intragastrically, at 12-hour intervals) to 2 mares. Clearance and apparent volume of distribution, based on area under the curve, were negatively correlated with probenecid dose. Clearance of cephapirin was decreased by approximately 50% by administration of 50 mg of probenecid/kg. Serum, synovial fluid, peritoneal fluid, CSF, urinary, and endometrial concentrations of cephapirin were determined after 5 doses of cephapirin (20 mg/kg, IM, at 12-hour intervals) without and with concurrently administered probenecid (50 mg/kg, intragastrically) to 6 mares, including the 2 mares given cephapirin, IV. Highest mean serum cephapirin concentrations were 16.1 +/- 2.16 micrograms/ml at 0.5 hour after the 5th cephapirin dose [postinjection (initial) hour (PIH) 48.5] in mares not given probenecid and 23.7 +/- 1.30 micrograms/ml at 1.5 hours after the 5th cephapirin dose (PIH 49.5) in mares given probenecid. Mean peak peritoneal fluid and synovial fluid cephapirin concentrations were 6.2 +/- 0.57 micrograms/ml and 6.6 +/- 0.58 micrograms/ml, respectively, without probenecid administration and 12.3 +/- 0.46 micrograms/ml and 10 +/- 0.78 micrograms/ml, respectively, with concurrent probenecid administration. Mean trough cephapirin concentrations for peritoneal and synovial fluids in mares given probenecid were 2 to 3 times higher than trough concentrations in mares not given probenecid. Overall mean cephapirin concentrations were significantly higher for serum, peritoneal fluid, synovial fluid, and endometrium when probenecid was administered concurrently with cephapirin (P less than 0.01).(ABSTRACT TRUNCATED AT 250 WORDS)
对2匹母马静脉注射头孢匹林（20毫克/千克体重），在3次给予丙磺舒（25、50或75毫克/千克，胃内给药，间隔12小时）之前和之后进行。基于曲线下面积的清除率和表观分布容积与丙磺舒剂量呈负相关。给予50毫克丙磺舒/千克可使头孢匹林的清除率降低约50%。对6匹母马（包括之前静脉注射头孢匹林的2匹母马），在不给予和同时给予丙磺舒（50毫克/千克，胃内给药）的情况下，每隔12小时肌肉注射5次头孢匹林（20毫克/千克）后，测定血清、滑液、腹腔液、脑脊液、尿液和子宫内膜中头孢匹林的浓度。在未给予丙磺舒的母马中，第5次注射头孢匹林后0.5小时（注射后初始小时48.5）血清头孢匹林最高平均浓度为16.1±2.16微克/毫升，在给予丙磺舒的母马中，第5次注射头孢匹林后1.5小时（注射后初始小时49.5）血清头孢匹林最高平均浓度为23.7±1.30微克/毫升。在未给予丙磺舒时，腹腔液和滑液中头孢匹林的平均峰值浓度分别为6.2±0.57微克/毫升和6.6±0.58微克/毫升，同时给予丙磺舒时分别为12.3±0.46微克/毫升和10±0.78微克/毫升。给予丙磺舒的母马腹腔液和滑液中头孢匹林的平均谷浓度比未给予丙磺舒的母马高2至3倍。当丙磺舒与头孢匹林同时给药时，血清、腹腔液、滑液和子宫内膜中头孢匹林的总体平均浓度显著更高（P<0.01）。（摘要截短至250字）
