Roberts E S, Van Lare K A, Marable B R, Salminen W F
Novartis Animal Health US, Inc., Greensboro, NC 27408, USA.
J Vet Pharmacol Ther. 2009 Aug;32(4):329-37. doi: 10.1111/j.1365-2885.2008.01043.x.
Although non-steroidal anti-inflammatory drugs (NSAIDs) are effective in reducing pain and inflammation, these agents have adverse effects. Selective inhibitors of COX-2 are an alternative to traditional NSAIDs. Deramaxx [Novartis Animal Health US, Inc. (NAH), Greensboro, NC, USA] contains the selective COX-2 inhibitor, deracoxib, and is approved for the relief of pain and inflammation associated with orthopedic surgery and osteoarthritis in dogs. The safety of Deramaxx was evaluated in two target animal safety studies: 40 dogs (four dogs/sex/group) received 0, 4, 6, 8, or 10 mg/kg/day deracoxib once daily for 21 days; and 60 dogs (five dogs/sex/group) received 0, 2, 4, 6, 8, or 10 mg/kg/day deracoxib once daily for 6 months. There was a dose-dependent trend towards increased blood urea nitrogen (BUN) in treated dogs, however mean BUN values remained within the reference range at the labeled doses. In both trials, histopathology revealed focal renal tubular degeneration/regeneration in some dogs receiving >or=6 mg/kg/day deracoxib. Focal renal papillary necrosis was seen in one dog treated with 8 mg/kg/day and in three dogs receiving 10 mg/kg/day deracoxib on the 6-month study. No other parameters of renal function were adversely affected for either study. Results show that Deramaxx is safe and well-tolerated in dogs when administered as directed.
尽管非甾体抗炎药（NSAIDs）在减轻疼痛和炎症方面有效，但这些药物有不良反应。COX-2选择性抑制剂是传统NSAIDs的替代品。Deramaxx[美国诺华动物保健公司（NAH），美国北卡罗来纳州格林斯博罗]含有选择性COX-2抑制剂德拉考昔，被批准用于缓解犬类骨科手术和骨关节炎相关的疼痛和炎症。在两项目标动物安全性研究中评估了Deramaxx的安全性：40只犬（每组4只/性别）每天接受0、4、6、8或10mg/kg/天的德拉考昔，持续21天；60只犬（每组5只/性别）每天接受0、2、4、6、8或10mg/kg/天的德拉考昔，持续6个月。治疗的犬中血尿素氮（BUN）有剂量依赖性升高趋势，然而在标记剂量下平均BUN值仍在参考范围内。在两项试验中，组织病理学显示，一些接受≥6mg/kg/天德拉考昔的犬出现局灶性肾小管变性/再生。在6个月的研究中，1只接受8mg/kg/天治疗的犬和3只接受10mg/kg/天德拉考昔治疗的犬出现局灶性肾乳头坏死。两项研究中肾功能的其他参数均未受到不利影响。结果表明，按指导给药时，Deramaxx在犬中是安全且耐受性良好的。
