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Clinical Drug Investigation

Published in:

01-03-2009 | Review Article

Pregabalin in the Treatment of Chronic Pain

An Overview

Authors: S. Chiechio, M. Zammataro, F. Caraci, L. Rampello, A. Copani, A. F. Sabato, Dr Ferdinando Nicoletti

Published in: Clinical Drug Investigation | Issue 3/2009

Abstract

Chronic ‘pathological’ pain is sustained by mechanisms of peripheral and central sensitization, which are being increasingly investigated at the molecular and cellular levels. The molecular determinants of nociceptive sensitization are natural targets for potential analgesic drugs used in the treatment of different forms of pain. Most of these determinants are common to all forms of chronic pain, and it is therefore not surprising that drugs specifically targeted for the treatment of neuropathic pain are effective in relieving nociceptive inflammatory pain and vice versa. The molecular mechanisms of sensitization that occur in peripheral nociceptors and the dorsal horns of the spinal cord are putative targets for context-dependent drugs, i.e. drugs that are able to discriminate between ‘normal’ and ‘pathological’ pain transmission. Among these, pregabalin and gabapentin bind to the α₂δ subunit of voltage-sensitive Ca²⁺ channels, which sustain the enhanced release of pain transmitters at the synapses between primary afferent fibres and second-order sensory neurons under conditions of chronic pain. Pregabalin in particular represents a remarkable example of a context-dependent analgesic drug that acts at a critical step of nociceptive sensitization. Preclinical and clinical data suggest that pregabalin is more than a structural and functional analogue of gabapentin and may be effective in the treatment of nociceptive inflammatory pain that is resistant to gabapentin.

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Title: Pregabalin in the Treatment of Chronic Pain
An Overview
Authors: S. Chiechio
M. Zammataro
F. Caraci
L. Rampello
A. Copani
A. F. Sabato
Dr Ferdinando Nicoletti
Publication date: 01-03-2009
Publisher: Springer International Publishing
Published in: Clinical Drug Investigation / Issue 3/2009
Print ISSN: 1173-2563
Electronic ISSN: 1179-1918
DOI: https://doi.org/10.2165/00044011-200929030-00006

Keynote webinar | Spotlight on medication adherence

Springer Medicine

Pregabalin in the Treatment of Chronic Pain

An Overview

Abstract

Keynote webinar | Spotlight on medication adherence

Springer Medicine

Abstract

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