Norton T M, Kollias G V, Clark C H, Gaskin J, Wilson R C, Coniglario J
Department of Small Animal Clinical Sciences, College of Veterinary Medicine, University of Florida, Gainesville 32610.
J Vet Pharmacol Ther. 1992 Sep;15(3):252-8. doi: 10.1111/j.1365-2885.1992.tb01014.x.
The pharmacokinetics of intravenous (i.v.) and intramuscular (i.m.) single-dose administration of acyclovir were determined in Quaker parakeets. After i.v. injection at a dose of 20 mg/kg of acyclovir, elimination half-life was estimated at 0.65 h, volume of distribution at steady state was 627.65 ml/kg, and clearance was 11.22 ml/kg/min. The estimated pharmacokinetic values after i.m. injection at a dose of 40 mg/kg of acyclovir were an elimination half-life of 0.71 h and a bioavailability of 90.1%. The peak plasma acyclovir concentration occurred at 15 min when the drug was administered i.m. Plasma concentrations of acyclovir were undetectable 4-6 h after i.v. administration and 6-8 h after i.m. administration. Oral (capsules) and intravenous (sodium salt) formulations of acyclovir were given by gavage at 80 mg/kg. Peak concentrations with the sodium salt formulation were lower and developed more slowly than with the capsules. In studies designed to detect excessive drug accumulation or adverse side effects, acyclovir was administered i.m. at 40 mg/kg every 8 h for 7 days. Plasma concentrations were determined 15 min after (peak) and just prior to drug administration (trough). In another study acyclovir was gavaged at a dose of 80 mg/kg every 8 h for 4 days. Acyclovir plasma concentrations were determined just prior to and 2 h after drug administration. In both experiments, the birds maintained normal appetite and weight and did not exhibit excessive drug accumulation. Acyclovir plasma concentrations ranging from 2.07 +/- 1.09 micrograms/ml to 3.93 +/- 1.13 micrograms/ml were maintained for 4 days when acyclovir was administered in the feed and water (sole source of food and water).(ABSTRACT TRUNCATED AT 250 WORDS)
在和尚鹦鹉中测定了阿昔洛韦静脉注射(i.v.)和肌肉注射(i.m.)单剂量给药的药代动力学。以20mg/kg的剂量静脉注射阿昔洛韦后,消除半衰期估计为0.65小时,稳态分布容积为627.65ml/kg,清除率为11.22ml/kg/分钟。以40mg/kg的剂量肌肉注射阿昔洛韦后,估计的药代动力学值为消除半衰期0.71小时,生物利用度90.1%。肌肉注射给药时,阿昔洛韦血浆峰浓度出现在15分钟。静脉注射后4 - 6小时和肌肉注射后6 - 8小时,阿昔洛韦血浆浓度检测不到。以80mg/kg的剂量通过灌胃给予阿昔洛韦的口服(胶囊)和静脉(钠盐)制剂。钠盐制剂的峰浓度低于胶囊制剂,且出现得更慢。在旨在检测药物过度蓄积或不良反应的研究中,每8小时以40mg/kg的剂量肌肉注射阿昔洛韦,持续7天。在给药后15分钟(峰浓度)和给药前(谷浓度)测定血浆浓度。在另一项研究中,每8小时以80mg/kg的剂量灌胃给予阿昔洛韦,持续4天。在给药前和给药后2小时测定阿昔洛韦血浆浓度。在这两个实验中,鸟类保持正常食欲和体重,未表现出药物过度蓄积。当在饲料和水中(食物和水的唯一来源)给予阿昔洛韦时,阿昔洛韦血浆浓度在2.07±1.09微克/毫升至3.93±1.13微克/毫升范围内维持了4天。(摘要截断于250字)