Gabapentinoids, including gabapentin and pregabalin, bind to the α2δ1 subunit of calcium channel (α2δ1) to relieve neuropathic pain. Although gabapentinoids are among the most effective medications to treat chronic neuropathic pain, their use in managing postoperative acute pain has been controversial. A recent meta-analysis of 281 randomized controlled trials by Verret et al. shows that gabapentinoids do not provide clinically significant analgesic effect for postoperative acute pain. It would be of great interest to discuss the potential mechanism behind why gabapentinoids have limited effect in postoperative acute pain.

α2δ1 is constitutively expressed in dorsal root ganglion. Its expression is greatly induced after nerve injury, and the upregulated α2δ1 is transported from dorsal root ganglion sensory neurons to spinal cord. Because α2δ1 is a subunit of the voltage-activated Ca2+ channel complex, it...

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