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Terbinafine pharmacokinetics after single dose oral administration in the dog.

机译:狗单次口服后特比萘芬的药代动力学。

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Terbinafine is an allylamine antifungal prescribed for the treatment of mycoses in humans. It is increasingly being used in veterinary patients. The purpose of this study was to evaluate the pharmacokinetic properties of terbinafine in dogs after a single oral dose. Ten healthy adult dogs were included in the study. A single dose of terbinafine (30-35 mg/kg) was administered orally, and blood samples were periodically collected over a 24 h period during which dogs were monitored for adverse effects. Two of 10 dogs developed transient ocular changes. A high-performance liquid chromatography assay was developed and used to determine plasma terbinafine concentrations. Pharmacokinetic analysis was performed using PK SolutionsReg. computer software. Area under the curve (AUC) from time 0 to 24 h was 15.4 micro g.h/mL (range 5-27), maximal plasma concentration (Cmax) was 3.5 micro g/mL (range 3-4.9 micro g/mL) and time to Cmax (Tmax) was 3.6 h (range 2-6 h). The time above minimal inhibitory concentration (T > MIC) as well as AUC/MIC was calculated for important invasive fungal pathogens and dermatophytes. The T > MIC was 17-18 h for Blastomyces dermatitidis, Histoplasma capsulatum and dermatophytes (Microsporum spp. and Trichophyton mentagrophytes), while the MIC for Sporothrix schenckii and Coccidioides immitis was exceeded for 9.5-11 h. The AUC/MIC values ranged from 9 to 13 micro g h/mL for these fungi. Our results provide evidence supporting the use of terbinafine as an oral therapeutic agent for treating systemic and subcutaneous mycoses in dogs.
机译:特比萘芬是一种用于治疗人类真菌病的烯丙胺抗真菌药。它越来越多地用于兽医患者。这项研究的目的是评估单次口服剂量后特比萘芬在犬中的药代动力学特性。研究中包括十只健康的成年狗。口服特比萘芬单剂量(30-35 mg / kg),并在24小时内定期收集血样,在此期间监测狗的不良反应。 10只狗中有2只出现短暂的眼球变化。开发了一种高效液相色谱法,用于测定血浆特比萘芬的浓度。使用PK SolutionsReg进行药代动力学分析。电脑软件。从0到24小时的曲线下面积(AUC)为15.4 micro gh / mL(范围5-27),最大血浆浓度( C max )为3.5 micro g / mL(范围3-4.9 micro g / mL)和达到 C max ( T max )的时间是3.6小时(范围2-6小时)。对于重要的侵入性真菌病原体和皮肤真菌,计算了超过最小抑制浓度( T spp。and 毛癣菌),而申氏孢子虫和球孢子虫免疫的MIC超过9.5-11 h。这些真菌的AUC / MIC值范围从9到13微克h / mL。我们的结果提供了支持使用特比萘芬作为口服治疗剂治疗犬全身和皮下真菌病的证据。

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