Pregabalin: a new anxiolytic

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Abstract
Pregabalin (S-[+]-3-isobutylgaba) was designed as a lipophilic GABA (γ-aminobutyric acid) analogue substituted at the 3′-position in order to facilitate diffusion across the blood–brain barrier. It was originally developed as an anticonvulsant agent, however it has been shown to be effective in the treatment of several disorders including hyperalgesia and behavioural disorders. Although its exact mode of action remains unclear, pregabalin interacts with the same binding site and has a similar pharmacological profile as its predecessor, gabapentin (1-[aminomethyl] cyclohexane acetic acid). Its main site of action appears to be on the α2δ subunit of voltage-dependent calcium channels, widely distributed throughout the peripheral and central nervous system. Pregabalin appears to produce an inhibitory modulation of neuronal excitability. In healthy volunteers, it is rapidly absorbed with peak blood concentrations within 1 h and it has a bioavailability of ∼ 90%. In preclinical trials of anticonvulsant activit...

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