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Pharmacology: Pharmacodynamics: Mechanism of action: Pregabalin binds to alpha2 – delta subunit of voltage-gated calcium channels within the CNS and modulated calcium influx at the nerve terminals, thereby inhibiting excitatory neurotransmitter release including glutamate, norepinephrine (noradrenaline), serotonin, dopamine, substance P and calcitonin gene-related peptide. 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 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.
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