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ATC code: N03AX16.
Pharmacology: Pharmacodynamics: Pregabalin is an antiepileptic, a gamma-aminobutyric acid analogue ((s)-3-(aminomethyl)-5-methylhaxanoic acid).
Mechanism of action: Pregabalin binds to an auxiliary subunit (α2-ẟ protein) of voltage-gated calcium channels in the central nervous system.
Pharmacokinetics: Absorption: Pregabalin is rapidly absorbed after oral doses and peak plasma concentrations occur within 1.5 hours. Oral bioavailability is about 90%. The rate but not the extent absorption is reduced if given with food but this is not clinically significant. Steady state is achieved after 1 to 2 days.
Distribution: In humans, the apparent volume of distribution of pregabalin following oral administration is approximately 0.5 L/kg. Pregabalin is not bound to plasma proteins.
Metabolism: Pregabalin undergoes negligible metabolism in humans.
Excretion: Pregabalin is eliminated by renal excretion 90% as unchanged drug. The mean elimination half-life is 6.3 hours. Pregabalin is removed by hemodialysis.
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