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Pharmacology: Pharmacodynamics: Pregabalin binds to alpha2-delta subunit of voltage-gated calcium channels within the CNS and modulates calcium influx at the nerve terminals, thereby inhibiting excitatory neurotransmitter release including glutamate, norepinephrine (noradrenaline), serotonin, dopamine, substance P, and calcitonin gene-related peptide. Although structurally related to GABA, it does not bind to GABA or benzodiazepine receptors.
Pharmacokinetics: Onset of action: Pain management: Effect may be noted as early as the first week of therapy.
Distribution: Vd: 0.5 L/kg.
Protein binding: 0%.
Metabolism: Negligible.
Bioavailability: >90%.
Half-life elimination: 6.3 hours.
Time to peak: plasma: 1.5 hours (3 hours with food).
Excretion: Urine (90% as unchanged drug; minor metabolites).
