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Gabapentin is commonly used to treat neuropathic pain (pain due to nerve damage). This review updates a review published in 2014, and previous reviews published in 2011, 2005 and 2000. To assess the analgesic efficacy and adverse effects of Neuropathic pain as defined by The International Association for the Study of Pain is “pain initiated or caused by a primary lesion in the nervous system”. In other words, neuropathic pain may be defined as the pain originated from the pathology of the nervous system. It involves alterations in the function, chemistry and structure of neurons. Gabapentin has no direct GABAergic action and does not block GABA uptake or metabolism. Gabapentin blocks the tonic phase of nociception induced by formalin and carrageenan, and exerts a potent inhibitory effect in neuropathic pain models of mechanical hyperalgesia and mechanical/thermal allodynia. Gabapentin is an anticonvulsive medication that received approval from the US Food and Drug Administration (FDA) in 1993 and has been available in generic form in the USA since 2004. Gabapentin was originally used as a muscle relaxant and an anti-spasmodic. However, it was later discovered that gabapentin has the potential of an anticonvulsive medication and can be used as an adjunct to more In addition to their use in managing neuropathic pain, gabapentinoids are increasingly being used for off-label conditions despite the lack of evidence. Prescription rates for off-label conditions have overtaken that for on-label use. The focus of perioperative pain management should be to attempt to minimise the nociceptive input and reduce the risk of transition to central sensitisation. Gabapentinoids are being increasingly used as adjuncts for management of perioperative pain. Although gabapentinoids are classed as calcium channel blockers, their mechanisms of action are poorly understood. The analgesic effect in Understanding how gabapentin works for pain is crucial for those exploring treatment options for conditions like neuropathic pain, fibromyalgia, and even post-surgical discomfort. The Mechanism of Action. Gabapentin's primary mechanism revolves around its interaction with calcium channels in the nervous system. Gabapentin (GBP) is a Health Canada approved antiepileptic drug. 5 In the UK, GBP is licensed for the treatment of peripheral and central neuropathic pain in adults and in the US it is marketed for post-herpetic neuralgia (PHN). 3 The mechanism of action for GBP relates to its ability to bind with high-affinity to the alpha-2-delta subunit of This paper reviews the pharmacology and clinical effectiveness of gabapentin in the treatment of neuropathic pain. Gabapentin has antihyperalgesic and antiallodynic properties but does not have significant actions as an anti-nociceptive agent. Summary Although its exact mode of action is not known, gabapentin appears to have a unique effect on voltage-dependent calcium ion channels at the postsynaptic dorsal horns and may, therefore, interrupt the series of events that possibly leads to the experience of a neuropathic pain sensation. Gabapentin is especially effective at relieving This review provides an overview of current drugs available for the treatment of neuropathic pain with an emphasis on their mechanism of action. Funding: Pfizer, Italy. Keywords: Anticonvulsants; Antidepressants; Gabapentin; Mechanism of action; Neuropathic pain; Opioids; Pregabalin; Serotonin–noradrenaline reuptake inhibitors; Tricyclic Gabapentin is an anti-epileptic agent but now it is also recommended as first line agent in neuropathic pain, particularly in diabetic neuropathy and post herpetic neuralgia. α2δ-1, an auxillary subunit of voltage gated calcium channels, has been documented as its main target and its specific binding to this subunit is described to produce Gabapentin (GBP) is a 3,3-disubstituted derivative of gamma-aminobutyric acid (GABA). It is recommended as a first-line treatment for chronic neuropathic pain, particularly in diabetic neuropathy Numerous studies confirm that gabapentinoids do not perturb normal detection and pain thresholds (Attal et al. 1998; Dirks et al. 2002); the pathophysiological state‐dependent effects of pregabalin and gabapentin implies other factors influence efficacy in neuropathic conditions. Although gabapentinoids are classed as calcium channel blockers, their mechanisms of action are poorly understood. The analgesic effect in neuropathic pain is well evidenced but the role in postoperative pain is less certain. Gabapentin; Mechanism of action; Neuropathic pain; Opioids; Pregabalin; Serotonin–noradrenaline reuptake inhibitors; Tricyclic antidepressants INTRODUCTION Neuropathic pain comprises a wide range of heterogeneous conditions caused by lesions or diseases of the somatosensory system, either at the peripheral or at the central level. Neuro A recent study has shown the effectiveness of gabapentin (5 or 50 mg/kg, i.p.) in attenuating neuropathic pain behavior in forelimb neuropathic pain model (due to partial injury to medial and ulner nerves) in a dose-dependent manner (Yi et al. 2011). Gabapentin is an anticonvulsant medication used in the management of peripheral neuropathic pains, postherpetic neuralgia, and partial-onset seizures. Gabapentin has become popular as a first-line treatment for neuropathic pain because of its efficacy as an antineuropathic agent and relatively benign side-effect profile. However, its mechanism of action is far from clear. The analgesic effect in neuropathic pain is well evidenced but the role in postoperative pain is less certain. Medline and EMBASE database searches were conducted to identify studies relating to mechanisms of action and effects in experimental animal models of inflammatory and postoperative pain and human models of experimental pain.
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