pregabalin in epilepsy

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Pregabalin is an antiepileptic medication that works by binding to alpha 2 delta subunit of the voltage-dependent calcium channels present in presynaptic neurons

  • its pharmacokinetic advantages include rapid and almost complete absorption, lack of protein binding, linear kinetics, absence of enzyme induction, and absence of interactions with other drugs
    • like gabapentin it works by binding to alpha 2 delta subunit of the P/Q-type voltage-sensitive Ca2+ channels (VSCC) which are present in presynaptic neurons
    • pregabalin is structurally related to both the neurotransmitter gamma- aminobutyric acid (GABA), and the older antiepileptic drug, gabapentin
    • the primary mechanism underlying the pharmacological action of pregabalin does not appear to involve the GABA system
      • in particular, pregabalin does not bind to GABA-A, GABA-B, or benzodiazepine receptors
        • pregabalin is neither metabolically converted to GABA or to a GABA agonist, nor does it have any effect on the uptake or degradation of GABA.
    • does not block calcium channels rather it modulates calcium channels
    • is rapidly and completely absorbed after oral dosing in the fasting state (bioavailability is >90%) (1)
      • absorption is not dose-dependent
      • is not protein-bound
      • maximal plasma concentrations are reached in 1 hour after single or multiple doses, and steady state is achieved within 24 to 48 hours after repeated administration
        • therefore, pregabalin can be taken with or without food

  • is approved in multiple countries worldwide as an add-on therapy for focal onset seizures in adult and paediatric populations (2)

  • a systematic review found pregabalin significantly more effective than placebo at producing a 50% or greater seizure reduction and seizure freedom with increasing effectiveness at 600 mg doses, although with tolerability issues (2)


Last edited 04/2022 and last reviewed 04/2022