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用于治疗骨关节炎疼痛的缓释曲马多

Tramadol Extended-Release for the Management of Pain due to Osteoarthritis.

作者信息

Angeletti Chiara, Guetti Cristiana, Paladini Antonella, Varrassi Giustino

机构信息

Anesthesiology and Pain Medicine, University of L'Aquila, Viale San Salvatore, Edificio 6, Coppito, 67100 L'Aquila, Italy.

出版信息

ISRN Pain. 2013 Sep 4;2013:245346. doi: 10.1155/2013/245346. eCollection 2013.

DOI:10.1155/2013/245346
PMID:27335872
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4893407/
Abstract

Current knowledge on pathogenesis of osteoarticular pain, as well as the consequent several, especially on the gastrointestinal, renal, and cardiovascular systems, side effects of NSAIDs, makes it difficult to perform an optimal management of this mixed typology of pain. This is especially observable in elderly patients, the most frequently affected by osteoarthritis (OA). Tramadol is an analgesic drug, the action of which has a twofold action. It has a weak affinity to mu opioid receptors and, at the same time, can result in inhibition of the reuptake of noradrenaline and serotonin in nociceptorial descending inhibitory control system. These two mechanisms, "opioidergic" and "nonopioidergic," are the grounds for contrasting certain types of pain that are generally less responsive to opioids, such as neuropathic pain or mixed OA pain. The extended-release formulation of tramadol has good efficacy and tolerability and acts through a dosing schedule that allows a high level of patients compliance to therapies with a good recovery outcome for the patients' functional status.

摘要

目前关于骨关节炎疼痛发病机制的知识,以及非甾体抗炎药随之而来的多种副作用,尤其是对胃肠道、肾脏和心血管系统的副作用,使得对这种混合型疼痛进行最佳管理变得困难。这在老年患者中尤为明显,他们是骨关节炎(OA)最常见的受影响人群。曲马多是一种镇痛药,其作用具有双重性。它对μ阿片受体的亲和力较弱,同时可抑制伤害性下行抑制控制系统中去甲肾上腺素和5-羟色胺的再摄取。这两种机制,即“阿片样物质能的”和“非阿片样物质能的”,是对抗某些通常对阿片类药物反应较差的疼痛类型(如神经性疼痛或混合型骨关节炎疼痛)的依据。曲马多缓释制剂具有良好的疗效和耐受性,其作用通过给药方案实现,该方案能使患者高度依从治疗,对患者功能状态的恢复有良好效果。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/00ff/4893407/46a460e04e73/ISRN.PAIN2013-245346.003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/00ff/4893407/66c4a8434511/ISRN.PAIN2013-245346.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/00ff/4893407/05a65e0e8ea8/ISRN.PAIN2013-245346.002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/00ff/4893407/46a460e04e73/ISRN.PAIN2013-245346.003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/00ff/4893407/66c4a8434511/ISRN.PAIN2013-245346.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/00ff/4893407/05a65e0e8ea8/ISRN.PAIN2013-245346.002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/00ff/4893407/46a460e04e73/ISRN.PAIN2013-245346.003.jpg

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Genetically polymorphic OCT1: another piece in the puzzle of the variable pharmacokinetics and pharmacodynamics of the opioidergic drug tramadol.遗传多态性 OCT1:阿片类药物曲马多可变药代动力学和药效学的难题又一块。
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CYP2D6 in the metabolism of opioids for mild to moderate pain.CYP2D6 在治疗轻中度疼痛的阿片类药物代谢中的作用。
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