▴ Pregabalin, the pharmacologically activeS-enantiomer of 3-aminomethyl-5-methylhexanoic acid, possesses anticonvulsant activity. Pregabalin binds with high affinity and specificity to voltage-gated calcium channel α2-δ proteins. The putative mechanism of action of the drug is reduced excitatory neurotransmitter release caused by binding to the α2-δ protein, resulting in allosteric modulation of P/Q-type voltage-gated calcium channels.▴ In three well designed trials, oral pregabalin as adjunctive therapy in patients with refractory partial seizures was significantly (p ≤ 0.0007) more effective than placebo in reducing seizure frequency when administered at dosages of 150–600 mg/day (as two or three divided doses).▴ Adjunctive pregabalin produced an overall mean 41.3% improvement from baseline in 28-day seizure-free rate in four long-term (maximum exposure 1764 days), open-label studies in 1480 patients.▴ CNS-related effects (e.g. dizziness and somnolence) were the most frequent dose-related treatment-emergent adverse events associated with adjunctive pregabalin therapy.Table. Features and properties of pregabalin (Lyrica®, CI-1008)