Department of Life, Health and Environmental Sciences, University of L'Aquila, L'Aquila, Italy. francomarinangeli@gmail.
Eur Rev Med Pharmacol Sci. 2019 Nov;23(4 Suppl):5-13. doi: 10.26355/eurrev_201911_19378.
Musculoskeletal pain, encompassing back and osteoarthritis (OA) pain, represents the most frequent source of chronic pain in western countries, and it is particularly frequent in older adults. Remarkably, back and OA pain present, in most cases, both a nociceptive and a neuropathic component of pain. Treatment selection should, therefore, properly consider the ability of a drug to act on both components, reducing the possibility of plastic changes in the central nervous system, and consequently promoting physical rehabilitation. The pharmacological profile of tapentadol, combining synergistically µ-opioid receptor (MOR) agonist and norepinephrine reuptake inhibition (NRI) in one single molecule with a concomitant reduction in the burden of adverse events, is unique, to date, and makes this drug particularly suitable for the treatment of back pain and OA-associated pain, especially when a neuropathic component is present. Tapentadol is an innovative dual-acting analgesic molecule, which combines two mechanisms of action, namely MOR agonism and NRI. This narrative review will briefly discuss the pharmacological action of tapentadol and its rationale for use in back pain and OA.
肌肉骨骼疼痛，包括背部和骨关节炎（OA）疼痛，是西方国家最常见的慢性疼痛来源，在老年人中尤为常见。值得注意的是，背部和 OA 疼痛在大多数情况下都具有疼痛的伤害感受性和神经病理性成分。因此，治疗选择应适当考虑药物对这两个成分的作用能力，降低中枢神经系统发生可塑性变化的可能性，并促进身体康复。曲马多的药理学特征，将 μ 阿片受体（MOR）激动剂和去甲肾上腺素再摄取抑制（NRI）这两种协同作用于一个单一分子中，并同时降低不良反应的负担，是独一无二的，这使得该药物特别适合治疗背部疼痛和 OA 相关疼痛，特别是当存在神经病理性成分时。曲马多是一种创新的双作用镇痛分子，结合了两种作用机制，即 MOR 激动作用和 NRI。本综述将简要讨论曲马多的药理学作用及其在背部疼痛和 OA 中的应用原理。
