Pregabalin is a structural derivative of the inhibitory neurotransmitter gamma-amino butyric acid (GABA). It does not bind directly to GABAA, GABAB, or benzodiazepine receptor. Pregabalin binds with high affinity to the alpha-2-delta site (an auxiliary subunit of voltage-gated calcium channels) in central nervous system tissues. Oral bioavailability of Pregabalin is ?90% and is independent of dose. It is eliminated from the systemic circulation primarily by renal excretion as unchanged drug with a mean elimination half-life of 6.3 hours in subjects with normal renal function.