Pregabalin: A Multifunctional Modulator in Neuropathic Pain and Beyond.

INTRODUCTION: Pregabalin is a structural analogue of γ-aminobutyric acid (GABA) that functions as a potent modulator of excitatory neurotransmission through high-affinity binding to the α2δ subunit of voltage-gated calcium channels. This review provides a comprehensive overview of its pharmacological properties, clinical efficacy, and therapeutic scope across neuropathic and non-neuropathic conditions. METHOD: This review is a narrative, descriptive, and integrative type of review conducted using current evidence regarding pharmacology, therapeutic applications, comparative efficacy, and pregabalin safety profile. RESULTS: Pregabalin exhibits rapid absorption, high bioavailability, linear pharmacokinetics, renal elimination, and minimal hepatic metabolism, supporting predictable dosing. Clinically, it demonstrates proven efficacy in neuropathic pain syndromes, including diabetic neuropathy, postherpetic neuralgia, fibromyalgia, and spinal cord injury-related pain, where it acts as a first-line or adjunctive agent. Beyond analgesia, pregabalin serves as an adjunct in partial seizures, a recognized treatment for generalized anxiety disorder, and an emerging option for sleep disturbances and comorbid psychiatric conditions. Comparative analyses indicate similar or superior efficacy to gabapentin and other first-line agents, with added benefit in improving sleep and global function. Adverse effects such as dizziness, somnolence, and peripheral edema are generally mild and dose-related. DISCUSSION: Future studies should clarify its role in treatment-resistant pain, psychiatric comorbidities, and sleep-related disorders to optimize its clinical use. CONCLUSION: Owing to its favorable safety profile, limited drug-drug interactions, and broad therapeutic potential, pregabalin remains an essential component of neuropathic pain.