Pregabalin is an alpha2-gamma ligand indicated for the treatment of peripheral and central neuropathic pain. In this article, we will review the pharmacodynamics, pharmacokinetics, randomized clinical trials supporting its efficacy for a wide array of neuropathic painful conditions, and the tolerability of this medication. We will comment the main differences with gabapentin, its parent compound, both from the pharmacological and clinical perspective. Our experience in the clinical practice setting with pregabalin, its use in patients with refractory neuropathic pain and its rational use in combination regimens will also be reviewed. With all this information in mind, the place of pregabalin in the pharmacotherapy of neuropathic pain is explored, mainly through the review of recent clinical guidelines which, in fact, place pregabalin among the first-line treatments for the management of most neuropathic painful conditions.
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