Department of Physical Therapy, School of Health and Human Sciences, Indiana University, Indianapolis, IN, 46202, USA.
Indiana Center for Musculoskeletal Health, Indiana University, Indianapolis, IN, 46202, USA.
Curr Osteoporos Rep. 2022 Dec;20(6):365-378. doi: 10.1007/s11914-022-00750-x. Epub 2022 Sep 23.
In this review, we discuss the mechanism of action of gabapentinoids and the potential consequences of long-term treatment with these drugs on the musculoskeletal system.
Gabapentinoids, such as gabapentin (GBP) and pregabalin (PGB) were designed as antiepileptic reagents and are now commonly used as first-line treatment for neuropathic pain and increasingly prescribed off-label for other pain disorders such as migraines and back pain. GBP and PGB exert their analgesic actions by selectively binding the αδ auxiliary subunit of voltage-sensitive calcium channels, thereby inhibiting channel function. Numerous tissues express the αδ subunit where GBP and PGB can alter calcium-mediated signaling events. In tissues such as bone, muscle, and cartilage, αδ has important roles in skeletal formation, mechanosensation, and normal tissue function/repair that may be affected by chronic use of gabapentinoids. Long-term use of gabapentinoids is associated with detrimental musculoskeletal outcomes, including increased fracture risk. Therefore, understanding potential complications is essential for clinicians to guide appropriate treatments.
在这篇综述中，我们讨论了加巴喷丁类药物的作用机制，以及长期使用这些药物对肌肉骨骼系统可能产生的潜在影响。
加巴喷丁类药物，如加巴喷丁（GBP）和普瑞巴林（PGB），最初被设计为抗癫痫药物，现在常用于治疗神经病理性疼痛，并且越来越多地被开处方用于治疗其他疼痛疾病，如偏头痛和背痛。GBP 和 PGB 通过选择性结合电压门控钙通道的辅助亚基 αδ，从而抑制通道功能，发挥其镇痛作用。许多组织表达 GBP 和 PGB 可以改变钙介导的信号事件的 αδ 亚基。在骨骼、肌肉和软骨等组织中，αδ 在骨骼形成、机械感觉和正常组织功能/修复中发挥重要作用，而这些功能可能会受到加巴喷丁类药物的慢性使用的影响。长期使用加巴喷丁类药物与有害的肌肉骨骼结果有关，包括骨折风险增加。因此，了解潜在的并发症对于临床医生指导适当的治疗至关重要。
