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昔康类药物及其与咖啡因组合的外周镇痛活性研究

Investigation of the Peripheral Analgesic Activity of Oxicams and Their Combinations with Caffeine.

作者信息

Syrova Anna, Lukyanova Larisa, Kozub Svetlana, Zavada Oksana, Levashova Olga, Shaposhnik Viktor

机构信息

Kharkiv National Medical University, Department of Medical and Bioorganic Chemistry, Kharkiv, Ukraine.

Kharkiv National Medical University, Kharkiv, Ukraine.

出版信息

Turk J Pharm Sci. 2020 Aug;17(4):408-411. doi: 10.4274/tjps.galenos.2019.92063. Epub 2020 Aug 28.

Abstract

OBJECTIVES

Therapy of pain syndromes involves exposure to its source, receptors, and peripheral fibers. Treatment of acute pain and inflammation involves the use of nonsteroidal anti-inflammatory drugs and nonnarcotic analgesics. An alternative to obsolete analgesics is combined compositions. Experimental results clearly indicates that caffeine effectively enhances the peripheral analgesic activity when combined in an analgesic. The aim of the present study was to evaluate the peripheral analgesic activity of meloxicam, piroxicam, and their pharmacological combinations with caffeine.

MATERIALS AND METHODS

The peripheral analgesic activity of piroxicam, meloxicam, and their combinations with caffeine was studied using the abdominal writhing test. This method was used to induce pain of peripheral origin by intraperitoneal injection of 0.6% acetic acid solution. The investigated drugs, their combinations, and 3% starch mucilage were administrated 1 h before the introduction of the algogen. The cumulative number of writhing responses induced by acetic acid was determined over the subsequent 20 min.

RESULTS

All investigated drugs supplied a decrease in writhing in rats. Meloxicam and caffeine showed peripheral analgesic activity of 63.6% and 64.5%, respectively (p<0.05). The pharmaceutical combination of meloxicam and caffeine showed analgesic potential of 76.4%. Thus, caffeine potentiates the analgesic activity of meloxicam. The results exceeded the corresponding value of diclofenac sodium (67.3%).

CONCLUSION

Experimental results clearly indicates that caffeine effectively enhances the peripheral analgesic action of meloxicam when combined in a pharmaceutical composition. These results can serve as a basis for the development of new domestic combined drugs.

摘要

目的

疼痛综合征的治疗涉及作用于其源头、受体和外周神经纤维。急性疼痛和炎症的治疗涉及使用非甾体抗炎药和非麻醉性镇痛药。替代过时镇痛药的是复方制剂。实验结果清楚地表明,咖啡因与镇痛药联合使用时能有效增强外周镇痛活性。本研究的目的是评估美洛昔康、吡罗昔康及其与咖啡因的药理组合的外周镇痛活性。

材料与方法

采用腹部扭体试验研究吡罗昔康、美洛昔康及其与咖啡因组合的外周镇痛活性。该方法通过腹腔注射0.6%醋酸溶液诱导外周源性疼痛。在引入致痛剂前1小时给予受试药物、其组合以及3%淀粉黏液。在随后的20分钟内测定醋酸诱导的扭体反应的累积次数。

结果

所有受试药物均使大鼠扭体次数减少。美洛昔康和咖啡因的外周镇痛活性分别为63.6%和64.5%(p<0.05)。美洛昔康与咖啡因的药物组合显示出76.4%的镇痛潜力。因此,咖啡因增强了美洛昔康的镇痛活性。结果超过了双氯芬酸钠的相应值(67.3%)。

结论

实验结果清楚地表明,咖啡因与药物组合物联合使用时能有效增强美洛昔康的外周镇痛作用。这些结果可为开发新型国产复方药物提供依据。

相似文献

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1
Caffeine and pain.咖啡因与疼痛。
Pain. 2011 Apr;152(4):726-729. doi: 10.1016/j.pain.2010.10.011. Epub 2010 Oct 30.
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Renal effects of nonselective NSAIDs and coxibs.
Cleve Clin J Med. 2002;69 Suppl 1:SI53-8. doi: 10.3949/ccjm.69.suppl_1.si53.

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