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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. Exerts antinociceptive and anticonvulsant activity. Pregabalin may also affect descending noradrenergic and serotonergic pain transmission pathways from the brainstem to the spinal cord.
Pharmacokinetics: Onset of action: Pain management: Effects 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: Immediate-release: Median: 0.7 hours fasting (range: 0.7 to 1.5 hours), 3 hours with food.
Excretion: Urine (90% as unchanged drug; minor metabolites).
