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Randomized placebo-controlled crossover studies were carried out in dogs to evaluate how two non-steroidal anti-inflammatory drugs (NSAID) might modulate an acute post-traumatic inflammatory reaction. Two "identical" surgical interventions were performed on the forelimbs of each animal with an interval of 28 days, to enable a paired comparison of the inflammatory signs and the wound/bone healing processes. At one operation 8 dogs received 300 mg phenylbutazone twice daily for 8 days starting on the day before surgery, and at the other operation matching placebo tablets were given. In a similar placebo-controlled trial another group of 8 dogs received 5 mg indomethacin twice daily. With phenylbutazone the post-operative swelling was not significantly reduced compared to placebo, but there was less pain and limping. With indomethacin the swelling was somewhat reduced, but there was no consistent difference to placebo in the pain and limping assessments. None of the drugs appeared to distinctly effect the wound or fracture healing, as evaluated by clinical inspection, comparison of radiographs and comparison of bone sections from the sites of surgery. It proved difficult to select an appropriate dosage of indomethacin due to its high potential to induce GI ulceration and bleeding in dogs. In this experimental surgical model with an acute inflammation, neither phenylbutazone nor indomethacin showed impressive anti-inflammatory or analgesic properties. In the same model paracetamol has proved to significantly and more efficiently, reduce both swelling and pain without any noticeable adverse effects, and appears to be a better alternative than the two presently tested NSAID. 相似文献
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Nonsteroidal anti-inflammatory drugs (NSAIDs) are powerful in anti-inflammatory, analgesic and antirheumatic effects, and widely used in treating the corresponding diseases. Over the years, many new dosage forms and structures of NSAIDs appear since aspirin was developed 112 years ago. However, the universal use of NSAIDs produces unavoidable mucosal lesions in gastrointestinal tract. As yet, proton pump inhibitor (PPI) has been used in the treatment of gastropathy induced by NSAIDs. This article will focus on the advances in prevention of NSAIDs-induced gastropathy by proton pump inhibitor. 相似文献
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为了探索千里光提取物冻干粉(SsE)的药物代谢动力学特征,首次采用耳肿胀度抑制率药理效应法测定SsE药动学参数。结果发现,在一定剂量范围内给小鼠腹腔注射SsE,能较迅速地产生药理效应,使耳肿胀度抑制率显著提高;SsE最低有效量为57.40 mg/kg,在小鼠体内代谢符合一级反应一室模型,模型表达式为:C=1 436.227 e^(-0.133 4 t)-1436.227 e^(-0.237 t),表观药动学参数为:一级消除速率常数Ke=0.133 4 h-1,消除半衰期t1/2Ke=5.194 9 h,一级吸收速率常数Ka=0.237 h-1,吸收半衰期t1/2Ka=2.924 1 h,血药峰浓度Cmax=1 436.227 mg/kg,达峰时间tmax=5.547 4 h,清除率Cl=0.055 3mg/kg.h,药-时曲线下面积AUC=16 826.35 mg/kg.h,表观分布容积V=0.414 2 mg/kg,滞后期t0=0.010 4 h。表明SsE具有良好的抗炎作用,在小鼠体内起效快,消除慢,生物利用度高,在机体内分布有限,较集中于血浆,组织摄入少。 相似文献
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建立了7种兽药中非法添加对乙酰氨基酚、安乃近、地塞米松和地塞米松磷酸钠药物的HPLC-PDA法。采用十八烷基键合硅胶为填充剂,磷酸二氢钠缓冲液(磷酸二氢钠3.0 g加水至1000 mL,加三乙胺1 mL,用氢氧化钠调pH值至7.0±0.2)-甲醇(80∶20)为流动相,梯度洗脱,二极管阵列检测器进行全扫描和240 nm波长测定,并采用峰纯度检查和光谱相似度检查辅助对照品比对方法,对四种目标分析物进行确证。结果显示,4种解热镇痛抗炎药物与其他物质峰分离良好,在测定范围内线性关系良好,平均回收率为73.5%~119.2%,RSD为0.1%~5.8%。本方法准确、可靠、重现性好,可用于兽药制剂中非法添加四种解热镇痛抗炎药物的定性和定量检测。 相似文献
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Cyclooxygenase (COX) inhibitors and the intestine 总被引:1,自引:0,他引:1
Little D Jones SL Blikslager AT 《Journal of veterinary internal medicine / American College of Veterinary Internal Medicine》2007,21(3):367-377
Nonsteroidal anti-inflammatory drugs (NSAIDs) have long been used for the treatment of pain and inflammation because of their inhibitory effects on cyclooxygenase (COX). For almost as long as NSAIDs have been in use, multiple adverse effects have been noted. Assessment of many of these adverse effects have been complicated because of the discovery of multiple splice variants of the cox gene, and a greater array of COX inhibitors, especially the COX-2 selective inhibitors have become available. Some of these adverse effects cannot be readily explained by the effect of these drugs on COX. This has sparked a new field of investigation into the COX-independent effects of the COX inhibitors. The major noncyclooxygenase targets of the COX inhibitors of particular relevance to inflammation and the gastrointestinal tract are phosphatidylinositol 3'-kinase Akt signaling, uncoupling of oxidative phosphorylation, PPARgamma, nuclear factor KB, mitogen activated protein kinases, and heat shock proteins. 相似文献
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