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▴ Pregabalin, the pharmacologically active S-enantiomer of 3-aminomethyl-5-methylhexanoic acid, possesses anticonvulsant activity. Pregabalin binds with high affinity and specificity to voltage-gated calcium channel ζ2-δ proteins. The putative mechanism of action of the drug is reduced excitatory neurotransmitter release caused by binding to the α2-δ protein, resulting in allosteric modulation of P/ Q-type voltage-gated calcium channels.
▴ In three well designed trials, oral pregabalin as adjunctive therapy in patients with refractory partial seizures was significantly (p ≤ 0.0007) more effective than placebo in reducing seizure frequency when administered at dosages of 150–600 mg/day (as two or three divided doses).
▴ Adjunctive pregabalin produced an overall mean 41.3% improvement from baseline in 28-day seizure-free rate in four long-term (maximum exposure 1764 days), open-1abel studies in 1480 patients.
▴ CNS-related effects (e.g. dizziness and somnolence) were the most frequent dose-related treatment-emergent adverse events associated with adjunctive pregabalin therapy.
KeywordsPregabalin Alprazolam Partial Seizure Seizure Frequency Diabetic Peripheral Neuropathy
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