Nervica Mechanism of Action

PHARMACOLOGY: PHARMACODYNAMICS: Pregabalin is a gamma-aminobutyric acid (GABA) analog that strongly binds to the alpha₂-delta site (α₂-δ; a subunit of voltage-gated calcium channels) in CNS tissues. The exact mechanism of action is not fully understood.
Binding to the alpha₂-delta subunit may be involved in pregabalin's effects on neuropathic pain and seizure control. Pregabalin reduces the calcium-dependent release of pro-nociceptive neurotransmitters, possibly by modulation of calcium channel function. Pregabalin may also interact with descending noradrenergic and serotonergic pathways in the brainstem that modulate pain transmission in the spinal cord.
PHARMACOKINETICS: Absorption: Tmax, adults: 0.7 to 1.5 hours.
Tmax, pediatrics: 0.5 to 2 hours (fasted state).
Bioavailability: 90% or greater.
Effect of food: No clinically relevant effect on total absorption, increase Tmax to 3 hours.
Onset of action: Pain management: Effects may be noted as early as the first week of therapy.
Distribution: Protein binding: 0%.
Volume of distribution (Vd): 0.5 L/kg.
Metabolism: Hepatic: Negligible.
Metabolite, N-methylated derivative (major): Activity not reported.
Excretion: Renal clearance: 67 to 80.9 mL/min.
Renal: 90% unchanged in the urine.
Dialyzable: approximately 50% removed after a 4-hour dialysis treatment.
Elimination Half Life: Adults: 6.3 hours.
Pediatrics: 3 to 4 hours (up to 6 years); 4 to 6 hours (7 years or older).