Lybalin Mechanism of Action

PHARMACOLOGY: Pharmacodynamics: Pregabalin binds with high affinity to the alpha₂-delta site (an auxiliary subunit of voltage-gated calcium channels) in CNS tissues. The mechanism of action of pregabalin is unknown.
Pharmacokinetics: Absorption: Pregabalin is rapidly absorbed after oral doses and peak plasma concentrations are achieved within 1.5 hours. Pregabalin oral bioavailability is about 90% or more and is independent of dose. The rate but not the extent of absorption is reduced if given with food but this is not clinically significant. Therefore, pregabalin can be taken with or without food. Steady state is achieved after 1 to 2 days.
Distribution: Pregabalin is not bound to plasma proteins. The apparent volume of distribution of pregabalin following oral administration is approximately 0.5 L/kg.
Metabolism: Pregabalin undergoes negligible metabolism in humans. Following a dose of radiolabeled pregabalin, approximately 90% of the administered dose was recovered in the urine as unchanged pregabalin. The N-methylated derivative of pregabalin, the major metabolite of pregabalin found in urine, is accounted for 0.9% of the dose.
Elimination: About 98% of a dose is eliminated from the systemic circulation primarily by renal excretion as unchanged drug. The mean elimination half-life is 6.3 hours. Pregabalin is removed by hemodialysis.