Sekis Ivana, Ramstead Kerry, Rishniw Mark, Schwark Wayne S, McDonough Sean P, Goldstein Richard E, Papich Mark, Simpson Kenneth W
Department of Clinical Sciences, College of Veterinary Medicine, Cornell University, Tower Road, Ithaca, NY 14853, United States.
J Feline Med Surg. 2009 Feb;11(2):60-8. doi: 10.1016/j.jfms.2008.06.011. Epub 2009 Jan 19.
Single-dose pharmacokinetics and genotoxicity of metronidazole in cats were evaluated. Cats received either 5mg/kg metronidazole intravenously, or 20mg/kg metronidazole benzoate (12.4mg/kg metronidazole base) orally in a single dose. Serial plasma samples were collected and assayed for metronidazole using high pressure liquid chromatography (HPLC). Genotoxicity was assessed in vitro in feline peripheral blood mononuclear cells (PBMC) and a feline T-cell lymphoma line incubated with metronidazole, and in vivo in PBMC collected before, during and 7 days after oral metronidazole, by use of the COMET assay. Systemic absorption of metronidazole was variable (mean=65+/-28%) with a peak of 8.84+/-5.4microg/ml at 3.6+/-2.9h. The terminal half-life was 5.34h from the intravenous dose and 5.16h from the oral dose. Systemic clearance was low (mean=91.57ml/h/kg [1.53ml/kg/min]), and the apparent volume of distribution (steady state) was 0.650+/-0.254l/kg. Genotoxicity was detected at all concentrations of metronidazole in feline PBMC and the T-cell lymphoma line in vitro. Genotoxicity was also observed in PBMC collected from cats after 7 days of oral metronidazole but resolved within 6 days of discontinuing metronidazole.
评估了甲硝唑在猫体内的单剂量药代动力学和遗传毒性。猫单次静脉注射5mg/kg甲硝唑,或口服20mg/kg甲硝唑苯甲酸酯(相当于12.4mg/kg甲硝唑碱)。采集系列血浆样本,采用高压液相色谱法(HPLC)测定甲硝唑含量。通过彗星试验,在体外对与甲硝唑共同孵育的猫外周血单核细胞(PBMC)和猫T细胞淋巴瘤细胞系进行遗传毒性评估,在体内对口服甲硝唑前、服药期间及停药7天后采集的PBMC进行遗传毒性评估。甲硝唑的全身吸收率可变(平均值=65±28%),在3.6±2.9小时达到峰值8.84±5.4μg/ml。静脉给药的末端半衰期为5.34小时,口服给药的末端半衰期为5.16小时。全身清除率较低(平均值=91.57ml/h/kg [1.53ml/kg/min]),稳态表观分布容积为0.650±0.254l/kg。在体外,在所有浓度的甲硝唑作用下,猫PBMC和T细胞淋巴瘤细胞系均检测到遗传毒性。口服甲硝唑7天后采集的猫PBMC中也观察到遗传毒性,但在停用甲硝唑6天内消退。