Middleton S M, Kubier A, Dirikolu L, Papich M G, Mitchell M A, Rubin S I
Department of Veterinary Clinical Medicine, College of Veterinary Medicine, University of Illinois, Urbana, IL, USA.
Veterinary Specialty Center, Melbourne, FL, USA.
J Vet Pharmacol Ther. 2016 Feb;39(1):27-31. doi: 10.1111/jvp.12231. Epub 2015 Apr 13.
The current available formulations of itraconazole are not ideal for dosing in cats. The capsular preparation often does not allow for accurate dosing, the oral solution is difficult to administer and poorly tolerated, and the bioavailability of compounded formulations has been shown to be poor in other species. The aim of this study was to evaluate every other day dosing of 100 mg itraconazole capsule in healthy adult cats. Ten healthy adult cats received a 100 mg capsule of itraconazole orally every 48 h for 8 weeks. Peak and trough serum concentrations of itraconazole were measured weekly using high-performance liquid chromatography (HPLC). Physical examination, complete blood count (CBC), and chemistry profiles were performed weekly. The dosage regimen achieved average therapeutic trough concentrations (>0.5 μg/mL) within 3 weeks. The protocol yielded no adverse effects in 8 of the 10 study cats, with affected cats recovering fully with discontinuation of the drug and supportive care. At 8 weeks, an average peak concentration of 1.79 ± 0.952 μg/mL (95% CI: 0.996-2.588) and an average trough concentration of 0.761 ± 0.540 μg/mL (95% CI: 0.314-1.216) were achieved. Overall, a 100 mg every other day oral dosage regimen for itraconazole in cats yielded serum concentrations with minimal fluctuation and with careful monitoring may be considered for treatment of cats with systemic fungal disease.
伊曲康唑目前可用的制剂对于猫的给药并不理想。胶囊制剂常常无法实现精确给药,口服溶液难以给药且耐受性差,并且已证明复方制剂在其他物种中的生物利用度不佳。本研究的目的是评估在健康成年猫中每隔一天给予100mg伊曲康唑胶囊的情况。十只健康成年猫每48小时口服一粒100mg伊曲康唑胶囊,持续8周。每周使用高效液相色谱法(HPLC)测量伊曲康唑的血清峰浓度和谷浓度。每周进行体格检查、全血细胞计数(CBC)和血液生化分析。给药方案在3周内达到了平均治疗谷浓度(>0.5μg/mL)。该方案在10只研究猫中有8只未产生不良反应,受影响的猫在停药和给予支持治疗后完全康复。在8周时,平均峰浓度为1.79±0.952μg/mL(95%CI:0.996 - 2.588),平均谷浓度为0.761±0.540μg/mL(95%CI:0.314 - 1.216)。总体而言,猫每隔一天口服100mg伊曲康唑的给药方案产生的血清浓度波动最小,经过仔细监测,可考虑用于治疗患有全身性真菌病的猫。