Pharmacokinetic and pharmacodynamic profile of pregabalin and its role in the treatment of epilepsy

Introduction: Pregabalin, the S-enantiomer of 3-aminomethyl-5-methylhaxanoic acid, is a second-generation antiepileptic drug (AED) developed after gabapentin with improved pharmacokinetic and pharmacodynamics properties. Pregabalin has a linear uptake without transporter saturation at therapeutic dosages, high bioavailability with rapid absorption independent of food intake. There is no binding to plasma proteins, and more than 90% of the drug is renally excreted, mostly without prior metabolization. Binding to the α2δ subunit of P/Q-type voltage-gated calcium channels, pregabalin is thought to exert its antiepileptic potency by modulating calcium channel traffic and physiology thus reducing the presynaptic calcium influx and subsequent neurotransmitter release.