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Pregabalin: new therapeutic contributions of calcium channel α<sub>2</sub>δ protein ligands on epilepsy and neuropathic pain

J.F. Horga de la Parte, A. Horga [REV NEUROL 2006;42:223-237] PMID: 16521062 DOI: https://doi.org/10.33588/rn.4204.2006038

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Volumen 42 | Number 04 | Nº of views of the article 13.074 | Nº of PDF downloads 1.541 | Article publication date 16/02/2006

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ABSTRACT

AIM To review and update the contributions of a new class of drugs, named calcium channel α₂δ protein ligands, on the treatment of epilepsy and neuropathic pain. DEVELOPMENT. A novel class of anticonvulsants are ligands for the auxiliary-associated protein α₂δ subunit of voltage-gated calcium channels in the central nervous system. Gabapentin and pregabalin are members of this group. Pregabalin is a higher-potency and higher-effective analogue of gabapentin that act as a potent ligand for this site. The anticonvulsant action of pregabalin is probably due to its ability to reduce neurotransmitter release from activated epileptogenic neurons, without demonstrated effects on GABAergic receptors or mechanisms. In well-done clinical trials, pregabalin 150-600 mg/day has been shown to be highly effective and well tolerated as adjunctive therapy in patients with partial seizures. In several randomized, double-blind, clinical trials, oral pregabalin 150-600 mg/day was superior to placebo in relieving neuropathic pain associated with diabetic neuropathy and postherpetic neuralgia. Pregabalin demonstrates in humans an extensive and rapid absorption and a highly predictable and linear pharmacokinetics, a profile that makes it easy to use in clinical practice. The pharmacological activity of pregabalin is similar but not identical to that of gabapentin, and pregabalin shows possible advantages.

CONCLUSIONS Pregabalin and calcium channel α₂δ protein ligands showed relevant advances on epilepsy and neuropathic pain treatment. In peripheral neuropathic pain conditions, if the criteria for efficacy are based on both pain relief and quality of life measures, pregabalin/gabapentin are suggested as choice treatment. KeywordsCalcium channel α₂δ protein ligands Epilepsy Gabapentin Neuropathic pain Pregabalin CategoriesDolor Epilepsias y síndromes epilépticos

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Pregabalin: new therapeutic contributions of calcium channel &alpha;<sub>2</sub>&delta; protein ligands on epilepsy and neuropathic pain

Pregabalin: new therapeutic contributions of calcium channel α<sub>2</sub>δ protein ligands on epilepsy and neuropathic pain