Chen Patty H, Boyd Kelli L, Fickle Erin K, Locuson Charles W
Division of Animal Care, Department of Pathology, Microbiology, and Immunology, Vanderbilt University Medical Center, Nashville, TN, USA.
Division of Animal Care, Vanderbilt University Medical Center, Nashville, TN, USA.
J Vet Pharmacol Ther. 2016 Aug;39(4):356-62. doi: 10.1111/jvp.12297. Epub 2016 Feb 20.
Meloxicam is a cyclooxygenase (COX) inhibitor with a higher selectivity for cyclooxygenase-2 (COX-2) than for cyclooxygenase-1 (COX-1). In the laboratory setting, this nonsteroidal anti-inflammatory drug (NSAID) is commonly selected for analgesia in mice and administered every 24 h. This study characterizes the plasma concentration achieved from a dose of 1.6 mg/kg of meloxicam administered once every 24 h subcutaneously for 72 h in male and female C57BL/6 mice. These values were compared, over time, to reference COX-2 inhibition constants for meloxicam. No significant differences in trough plasma concentrations were noted between genders. The plasma concentrations were below the COX-2 IC50 after 12 h. To maintain a plasma concentration at or above the COX-2 whole blood IC50, the study results suggest an administration frequency of every 12 h when using a dose of 1.6 mg/kg in C57BL/6 mice.
美洛昔康是一种环氧化酶(COX)抑制剂,对环氧化酶-2(COX-2)的选择性高于环氧化酶-1(COX-1)。在实验室环境中,这种非甾体抗炎药(NSAID)通常用于小鼠镇痛,每24小时给药一次。本研究描述了在雄性和雌性C57BL/6小鼠中,每24小时皮下注射一次1.6mg/kg美洛昔康,连续72小时后所达到的血浆浓度。随着时间的推移,将这些值与美洛昔康的参考COX-2抑制常数进行比较。两性之间的谷血浆浓度没有显著差异。12小时后血浆浓度低于COX-2 IC50。为了使血浆浓度维持在或高于COX-2全血IC50,研究结果表明,在C57BL/6小鼠中使用1.6mg/kg剂量时,给药频率应为每12小时一次。