Synthesized in 1990 as an anticonvulsant agent, pregabalin was designed as a lipophilic gamma-aminobutyric acid (GABA) analog substituted at the 3'-position in order to facilitate diffusion across the blood-brain barrier. It is an alpha2delta1 ligand that binds to, and modulates, voltage-gated calcium channels. This modulation is characterized by a reduction of the excessive neurotransmitter release that is observed in certain neurologic and psychotic disorders. Pregabalin has analgetic, anticonvulsant, and anxiolytic activity and has demonstrated efficacy in the management of neuropathic pain associated with diabetic peripheral neuropathy, postherpetic neuralgia, and as adjuvant therapy for adult patients with partial onset seizures. Pregabalin was significantly more effective than placebo for the treatment of generalized anxiety disorder as well as of fibromyalgia and was well tolerated by most of the patients.