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氟虫腈和双甲脒在犬局部应用后血浆和毛发中的药代动力学。

Pharmacokinetics of metaflumizone and amitraz in the plasma and hair of dogs following topical application.

作者信息

DeLay R L, Lacoste E, Mezzasalma T, Blond-Riou F

机构信息

Fort Dodge Animal Health, P.O. Box 5366, Princeton, NJ 08543, USA.

出版信息

Vet Parasitol. 2007 Dec 15;150(3):251-7. doi: 10.1016/j.vetpar.2007.08.045. Epub 2007 Oct 17.

Abstract

Controlled laboratory studies have shown that a metaflumizone plus amitraz combination (ProMeris/ProMeris Duo for Dogs, Fort Dodge Animal Health, Overland Park, KS) applied topically is effective for the treatment and control of fleas and ticks on dogs. Two studies were conducted to determine the distribution of both metaflumizone and amitraz in the plasma and hair of dogs following treatment at the minimum recommended dose of approximately 20mg/kg of each active ingredient. Six purpose-bred, adult Beagle dogs were used in each study. Plasma or hair samples were collected from each dog just prior to dosing and periodically through 56 days after treatment. Samples were analyzed by HPLC methods validated for the simultaneous determination of metaflumizone and amitraz. Amitraz was detectable (>3.2ng/ml) but not quantifiable (<50ng/ml) in only two plasma samples, collected 1 and 2 days post-treatment from different dogs. Metaflumizone concentrations in plasma were generally detectable (>1.0ng/ml) but not quantifiable (<50ng/ml). Measurable levels were found in one dog 7 days post-treatment, increasing to a maximum of four dogs at 42 days after dosing, with a metaflumizone range of 59-138ng/ml. Analysis of hair samples indicated that both metaflumizone and amitraz were widely distributed at basically similar levels in the hair within 1-day after administration, reaching maximum concentrations between 2 and 7 days post-treatment. Low but quantifiable levels of both compounds were still present on hair at the end of the 56-day study. These studies indicate that the ectoparasitic activity is due to exposure of the parasites to metaflumizone and amitraz on the surface of the host (hair and/or skin), not to exposure via the circulatory system of the host.

摘要

对照实验室研究表明,氟虫腈与双甲脒的组合制剂(犬用ProMeris/ProMeris Duo,美国堪萨斯州欧弗兰帕克市道奇动物保健公司)局部应用对治疗和控制犬身上的跳蚤和蜱虫有效。进行了两项研究,以确定在以每种活性成分约20mg/kg的最低推荐剂量治疗后,氟虫腈和双甲脒在犬血浆和毛发中的分布情况。每项研究使用了6只专门培育的成年比格犬。在给药前及给药后至56天期间定期从每只犬采集血浆或毛发样本。通过经验证可同时测定氟虫腈和双甲脒的高效液相色谱法对样本进行分析。仅在治疗后第1天和第2天从不同犬采集的两份血浆样本中检测到双甲脒(>3.2ng/ml),但无法定量(<50ng/ml)。血浆中的氟虫腈浓度一般可检测到(>1.0ng/ml),但无法定量(<50ng/ml)。在一只犬治疗后7天发现有可测量水平,给药后42天增至最多四只犬,氟虫腈浓度范围为59 - 138ng/ml。毛发样本分析表明,给药后1天内,氟虫腈和双甲脒在毛发中的分布基本相似,且分布广泛,在治疗后2至7天达到最大浓度。在为期56天的研究结束时,毛发上仍存在低水平但可定量的两种化合物。这些研究表明,体外寄生虫活性是由于寄生虫接触宿主表面(毛发和/或皮肤)的氟虫腈和双甲脒,而非通过宿主循环系统接触所致。

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