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恒河猴(猕猴)单次皮下注射头孢维星的药代动力学研究。

Single subcutaneous dosing of cefovecin in rhesus monkeys (Macaca mulatta): a pharmacokinetic study.

作者信息

Bakker J, Thuesen L R, Braskamp G, Skaanild M T, Ouwerling B, Langermans J A M, Bertelsen M F

机构信息

Animal Science Department, Biomedical Primate Research Centre, Rijswijk, The Netherlands.

出版信息

J Vet Pharmacol Ther. 2011 Oct;34(5):464-8. doi: 10.1111/j.1365-2885.2010.01265.x. Epub 2011 Feb 17.

DOI:10.1111/j.1365-2885.2010.01265.x
PMID:21323930
Abstract

Cefovecin is a third-generation cephalosporin approved for antibacterial treatment with a 14-day dosing interval in dogs and cats. This antibiotic may also be useful for zoo and wildlife veterinary medicine, because of its broad spectrum and long duration of activity. The aim of the study was to determine whether cefovecin is a suitable antibiotic to prevent skin wound infection in rhesus monkeys. Therefore, the pharmacokinetics (PK) of cefovecin after a single subcutaneous injection at 8 mg/kg bodyweight in four rhesus monkeys (Macaca mulatta) and sensitivity of bacterial isolates from fresh skin wounds were determined. After administration, blood, urine, and feces were collected, and concentrations of cefovecin were determined. Further, the minimum inhibitory concentrations (MIC) for bacteria isolated from fresh skin wounds of monkeys during a health control program were determined. The mean maximum plasma concentration (C(max) ) of cefovecin was 78 μg/mL and was achieved after 57 min. The mean apparent long elimination half-life (t½) was 6.6 h and excretion occurred mainly via urine. The MIC for the majority of the bacteria examined was >100 μg/mL. The PK of cefovecin in rhesus monkeys is substantially different than for dogs and cats. Cefovecin rapidly reached C(max) which however was lower than most of the MIC levels and with a very short t½. Therefore, cefovecin is not recommended for treating skin wounds in rhesus monkeys.

摘要

头孢维星是一种第三代头孢菌素,被批准用于犬猫的抗菌治疗,给药间隔为14天。由于其广谱抗菌活性和较长的作用持续时间,这种抗生素可能对动物园和野生动物兽医医学也有用。本研究的目的是确定头孢维星是否是预防恒河猴皮肤伤口感染的合适抗生素。因此,测定了4只恒河猴(猕猴)单次皮下注射8mg/kg体重头孢维星后的药代动力学(PK)以及新鲜皮肤伤口细菌分离株的敏感性。给药后,收集血液、尿液和粪便,并测定头孢维星的浓度。此外,还测定了健康对照项目期间从猴子新鲜皮肤伤口分离出的细菌的最低抑菌浓度(MIC)。头孢维星的平均最大血浆浓度(C(max))为78μg/mL,在57分钟后达到。平均表观长消除半衰期(t½)为6.6小时,排泄主要通过尿液。大多数检测细菌的MIC>100μg/mL。头孢维星在恒河猴体内的药代动力学与犬猫有很大不同。头孢维星迅速达到C(max),但低于大多数MIC水平,且t½很短。因此,不建议用头孢维星治疗恒河猴的皮肤伤口。

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