Pregabalin is a gabapentinoid that binds to the alpha-2-delta subunit of voltage-gated calcium channels in the central nervous system, reducing release of excitatory neurotransmitters involved in pain signaling and seizure propagation. It is used for neuropathic pain conditions such as diabetic peripheral neuropathy and postherpetic neuralgia, for fibromyalgia, and as adjunctive therapy for partial-onset seizures. Despite structural similarity to GABA, it does not act on GABA receptors. Clinical benefits stem from dampening hyperexcitable neural networks, with evidence across multiple pain syndromes and epilepsy settings supporting its role in comprehensive management plans that may include rehabilitation and psychosocial strategies.