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罗替戈汀缓释微球单独或与塞来昔布联合使用对炎性疼痛的影响。

The Effect of Rotigotine Extended-Release Microspheres Alone or With Celecoxib on the Inflammatory Pain.

作者信息

Li Keke, Zhang Yijia, Tian Enming, Liu Zikai, Wang Tian, Fu Fenghua

机构信息

School of Pharmacy, Key Laboratory of Molecular Pharmacology and Drug Evaluation (Yantai University), Ministry of Education, Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shandong, Yantai University, Yantai, China.

School of Pharmacy, Binzhou Medical University, Yantai, China.

出版信息

Front Pharmacol. 2020 Oct 30;11:594387. doi: 10.3389/fphar.2020.594387. eCollection 2020.

DOI:10.3389/fphar.2020.594387
PMID:33192533
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7663167/
Abstract

Clinical trials of rotigotine extended-release microspheres (RTGT-MS), which provides a sustained release of rotigotine for near 2 weeks , have been conducted in the treatment of Parkinson's disease (PD). This study was to investigate the analgesic effect of RTGT-MS, and to know whether RTGT-MS have synergistic interaction with non-steroidal anti-inflammatory drug, celecoxib. The inflammatory pain model of rats was prepared by carrageenan-induced paw edema. The thermal and mechanical stimuli were applied and the hindpaw withdrawal latency (HWL) response was evaluated. Treatment with RTGT-MS increased the HWL in a dose-dependent manner. The ED50 of RTGT-MS was 24.68 ± 1.02 mg/kg. Isobolographic analysis shows that the combination of RTGT-MS and celecoxib resulted in a synergistic antinociceptive effect. Further results demonstrated that antinociceptive effect of RTGT-MS was accompanied with that PKA, cAMP, COX-2, and PGE2 levels were decreased. Chlorpromazine, a dopamine receptor blocker, not only weakened the analgesic effect of RTGT-MS, but also increased the levels of cAMP, PKA, COX-2, and PGE2. These findings provide a rationale for the combination of RTGT-MS and celecoxib in the treatment of PD, which may reduce the dose of celecoxib, thereby lowering the incidence of adverse effects and improving the pain management in PD patients.

摘要

罗替戈汀长效微球（RTGT-MS）可使罗替戈汀持续释放近2周，已开展其治疗帕金森病（PD）的临床试验。本研究旨在探讨RTGT-MS的镇痛作用，以及其与非甾体抗炎药塞来昔布是否存在协同相互作用。通过角叉菜胶诱导的足爪水肿制备大鼠炎性疼痛模型。施加热刺激和机械刺激并评估后爪缩足潜伏期（HWL）反应。RTGT-MS治疗以剂量依赖性方式增加HWL。RTGT-MS的半数有效剂量（ED50）为24.68±1.02mg/kg。等效线图分析表明，RTGT-MS与塞来昔布联合使用产生协同镇痛作用。进一步结果表明，RTGT-MS的镇痛作用伴随着蛋白激酶A（PKA）、环磷酸腺苷（cAMP）、环氧化酶-2（COX-2）和前列腺素E2（PGE2）水平降低。多巴胺受体阻滞剂氯丙嗪不仅削弱了RTGT-MS的镇痛作用，还增加了cAMP、PKA、COX-2和PGE2的水平。这些发现为RTGT-MS与塞来昔布联合治疗PD提供了理论依据，这可能会减少塞来昔布的剂量，从而降低不良反应的发生率并改善PD患者疼痛的管理。

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本文引用的文献

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Expert Opin Pharmacother. 2019 Oct;20(14):1689-1702. doi: 10.1080/14656566.2019.1645123. Epub 2019 Jul 24.
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Effects of rotigotine and rotigotine extended-release microsphere therapy on myocardial ischemic injury in mice.罗替高汀及罗替高汀控释微球治疗对小鼠心肌缺血性损伤的影响。
Eur J Pharm Sci. 2019 Jun 15;134:1-6. doi: 10.1016/j.ejps.2019.04.009. Epub 2019 Apr 5.
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