Neurica Mechanism of Action

Pharmacology: Mechanism of Action: Although the exact mechanism of action of pregabalin has not been elucidated, binding to the α₂-δ subunit may be involved in pregabalin's analgesic and anticonvulsant effects. In vitro, pregabalin reduces the calcium-dependent release of several neurotransmitters, including glutamate, norepinephrine, calcitonin gene-related peptide, and substance P, possibly by modulation of calcium channel function.
Pharmacodynamics: Pregabalin binds with high affinity to the α₂-δ site (an auxiliary subunit of voltage gated calcium channels) in CNS tissues.
Pharmacokinetics: Absorption: Pregabalin is well absorbed following oral administration and exhibits linear pharmacokinetics. Peak plasma concentrations are attained within 1.5 hour. Steady-state concentrations are achieved within 24-48 hours following repeated administration of conventional pregabalin. In pediatric patients receiving conventional pregabalin, peak plasma concentrations of the drug are achieved within 0.5-2 hours in the fasted state. The oral bioavailability of pregabalin administered as the conventional preparation) is at least 90% and is independent of dose. Administration of conventional preparations of pregabalin with food has been shown to delay the time to peak concentration and decrease peak plasma concentrations of the drug by approximately 25-30%, but does not affect the extent of absorption.
Distribution: Protein binding: 0%.
Metabolism: Negligible.
Excretion: Following administration of a single radiolabeled dose of pregabalin, approximately 90% of the administered dose was recovered in urine as unchanged drug. Clearance of pregabalin is nearly proportional to creatinine clearance in both adults and pediatric patients. In pediatric patients, the weight-normalized clearance of pregabalin is approximately 40% higher in those weighing less than 30 kg. The mean elimination half-life of pregabalin is 6.3 hours in adults with normal renal function, 3-4 hours in children up to 6 years of age, and 4-6 hours in children 7 years of age or older.