Burhenne Jürgen, Haefeli Walter E, Hess Michael, Scope Alexandra
Clinical Pharmacology and Pharmacoepidemiology, Department of Internal Medicine VI, University of Heidelberg, Im Neuenheimer Feld 410, D-69120 Heidelberg, Germany.
J Avian Med Surg. 2008 Sep;22(3):199-207. doi: 10.1647/2007-003.1.
Voriconazole, a highly potent triazole antifungal agent with high in vitro activity against a wide variety of fungal pathogens, appears to be an option for the treatment of aspergillosis in birds. To gain initial information on pharmacokinetics, bioavailability, and tissue distribution of voriconazole in birds, we evaluated voriconazole in chickens in a 4-part study that analyzed dose linearity, bioavailability, pharmacokinetics, and tissue distribution. Chickens received voriconazole orally and/or intravenously. Blood samples were drawn and analyzed by validated high-pressure liquid chromatography and high-pressure liquid chromatography coupled with mass spectrometry methods. Voriconazole was detectable at low concentrations in plasma up to 6 hours after oral administration, which resulted in a low absolute bioavailability. Concentrations in tissues 12 hours after administration could be quantified up to 7.37 microg/g (liver). No accumulation in tissues could be detected after 30 days of oral treatment with 10 mg/kg voriconazole. Clinical application of voriconazole for the treatment of aspergillosis in birds appears to be promising, because this drug has a high effectiveness and wide tissue distribution, and long-term treatment did not cause clinical signs of adverse effects or organ damage in chickens.
伏立康唑是一种高效的三唑类抗真菌药物，对多种真菌病原体具有高体外活性，似乎是治疗鸟类曲霉病的一种选择。为了获得关于伏立康唑在鸟类体内的药代动力学、生物利用度和组织分布的初步信息，我们在一项分为四个部分的研究中对鸡进行了伏立康唑评估，该研究分析了剂量线性、生物利用度、药代动力学和组织分布。鸡通过口服和/或静脉注射接受伏立康唑。采集血样并通过经过验证的高压液相色谱法和高压液相色谱-质谱联用法进行分析。口服给药后长达6小时，血浆中可检测到低浓度的伏立康唑，这导致绝对生物利用度较低。给药12小时后组织中的浓度最高可定量至7.37微克/克（肝脏）。用10毫克/千克伏立康唑口服治疗30天后，未检测到组织中有蓄积。伏立康唑在鸟类曲霉病治疗中的临床应用似乎很有前景，因为这种药物具有高效性和广泛的组织分布，并且长期治疗未在鸡身上引起不良反应的临床症状或器官损伤。
