Waxman Samanta, Prados Ana Paula, de Lucas Julio, San Andres Manuel Ignacio, Sassaroli Juan Carlos, Orozco Marcela, Argibay Hernán, Rodriguez Casilda
Pharmacology Department, FCV, University of Buenos Aires, Chorroarin 280, 1427, Argentina.
Pharmacology Department, Universidad Complutense de Madrid, Av. Puerta de Hierro s/n, 28040, Spain.
J Avian Med Surg. 2013 Sep;27(3):180-6. doi: 10.1647/2012-022.
To determine the dosage of enrofloxacin in southern crested caracaras (Caracara plancus), plasma concentrations of enrofloxacin were measured by high-performance liquid chromatography after intravenous (IV) (5 mg/kg) and intramuscular (IM) (10 mg/kg) administration. This compound presented a relatively high volume of distribution (2.09 L/kg), a total body clearance of 0.24 L/kg x h, and a long permanence as shown by an elimination half-life of 7.81 hours after IV administration and a terminal half-life of 6.58 hours after IM administration. The areas under the concentration-time curves (AUC) were 21.92 and 34.38 microg x h/mL for IM and IV administration, respectively. Enrofloxacin was rapidly absorbed after IM administration with a time to reach maximum concentration of 0.72 hours and bioavailability of 78.76%. After IM administration, the peak drug concentration (C(max)) was 3.92 microg/mL. Values of minimum inhibitory concentration (MIC), C(max), and AUC have been used to predict the clinical efficacy of a drug in treating bacterial infections, with a C(max)/MIC value of 10 and an AUC/MIC ratio of 125-250 associated with optimal bactericidal effects. By using the study data and a MIC breakpoint of 0.25 microg/mL, values of C(max)/MIC were 13.74 and 15.94 and for AUC/MIC were 90.73 and 139.63, for the IV and IM routes respectively. For the treatment of infectious diseases caused by microorganisms with MIC < or = 0.25 microg/mL, the calculated optimal dosages were 7.5 and 9.5 mg/kg q24h by the IV and IM routes, respectively. For less susceptible bacteria, a dose increase should be evaluated. To treat caracara by the IV route against microorganisms with MIC < or = 0.25 microg/mL, the dose should be higher than the 5 mg/kg used in our study, but possible side effects derived from an increase in the IV dose and efficacy in sick birds should be assessed.
为确定恩诺沙星在南方凤头卡拉鹰(Caracara plancus)体内的给药剂量,在静脉注射(IV)(5毫克/千克)和肌肉注射(IM)(10毫克/千克)后,通过高效液相色谱法测定了恩诺沙星的血浆浓度。该化合物呈现出相对较高的分布容积(2.09升/千克)、全身清除率为0.24升/千克·小时,并且具有较长的滞留时间,静脉注射后消除半衰期为7.81小时,肌肉注射后末端半衰期为6.58小时。肌肉注射和静脉注射后浓度-时间曲线下面积(AUC)分别为21.92和34.38微克·小时/毫升。肌肉注射后恩诺沙星迅速吸收,达峰时间为0.72小时,生物利用度为78.76%。肌肉注射后,药物峰浓度(C(max))为3.92微克/毫升。最低抑菌浓度(MIC)、C(max)和AUC值已被用于预测药物治疗细菌感染的临床疗效,C(max)/MIC值为10以及AUC/MIC比值为125 - 250与最佳杀菌效果相关。利用研究数据以及0.25微克/毫升的MIC折点,静脉注射和肌肉注射途径下C(max)/MIC值分别为13.74和15.94,AUC/MIC值分别为90.73和139.63。对于由MIC≤0.25微克/毫升的微生物引起的传染病治疗,通过静脉注射和肌肉注射途径计算出的最佳剂量分别为7.5和9.5毫克/千克,每24小时一次。对于敏感性较低的细菌,应评估增加剂量的情况。为通过静脉注射途径治疗凤头卡拉鹰对抗MIC≤0.25微克/毫升的微生物,剂量应高于我们研究中使用的5毫克/千克,但应评估静脉注射剂量增加可能产生的副作用以及对患病鸟类的疗效。