An enigmatic role of tonic inhibition in gabapentin therapy

Reddy, Doodipala Samba

doi:10.1016/j.ebiom.2019.03.047

Cited by 4 publications

(2 citation statements)

References 9 publications

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“…In 2011, a case report described the effectiveness of gabapentin in reducing the dementia-associated nocturnal agitation [181]. Gabapentin is an FDA-approved drug for the treatment of epilepsy [182]. Gabapentin blocks the α2δ subunit-containing voltage-dependent calcium channels (Fig.…”

Section: α2δ Subunit-containing Voltage-dependent Calcium Channel Blomentioning

confidence: 99%

Management of Dementia-Related Psychosis, Agitation and Aggression: A Review of the Pharmacology and Clinical Effects of Potential Drug Candidates

et al. 2020

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Along with cognitive decline, 90% of patients with dementia experience behavioral and psychological symptoms of dementia, such as psychosis, aggression, agitation, and depression. Atypical antipsychotics are commonly prescribed off-label to manage certain symptoms, despite warnings from the regulatory agencies regarding the increased risk of mortality associated with their use in elderly patients. Moreover, these compounds display a limited clinical efficacy, mostly owing to the fact that they were developed to treat schizophrenia, a disease characterized by neurobiological deficits. Thus, to improve clinical efficacy, it has been suggested that patients with dementia should be treated with exclusively designed and developed drugs that interact with pharmacologically relevant targets. Within this context, numerous studies have suggested druggable targets that might achieve therapeutically acceptable pharmacological profiles. Based on this, several different drug candidates have been proposed that are being investigated in clinical trials for behavioral and psychological symptoms of dementia. We highlight the recent advances toward the development of therapeutic agents for dementia-related psychosis and agitation/ aggression and discuss the relationship between the relevant biological targets and their etiology. In addition, we review the compounds that are in the early stage of development (discovery or preclinical phase) and those that are currently being investigated in clinical trials for dementia-related psychosis and agitation/aggression. We also discuss the mechanism of action of these compounds and their pharmacological utility in patients with dementia.

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Section: α2δ Subunit-containing Voltage-dependent Calcium Channel Blomentioning

confidence: 99%

Management of Dementia-Related Psychosis, Agitation and Aggression: A Review of the Pharmacology and Clinical Effects of Potential Drug Candidates

et al. 2020

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“…Gabapentin, originally developed for the treatment of epilepsy [ 41 ], is also currently used in the treatment of neuropathic pain. As a lipophilic analog of GABA, it interacts with the α2δ subunit of voltage-gated calcium channels [ 42 ]. Subsequent pharmacological research has resulted in the development of pregabalin [ 38 ], which has become the gold standard for the treatment of chronic pain associated with diabetic neuropathy.…”

Section: Clinical and Preclinical Studies On Ion Channel Signaling Mo...mentioning

confidence: 99%

Mechanisms of Transmission and Processing of Pain: A Narrative Review

Maio

Villano

Ilardi

et al. 2023

IJERPH

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Knowledge about the mechanisms of transmission and the processing of nociceptive information, both in healthy and pathological states, has greatly expanded in recent years. This rapid progress is due to a multidisciplinary approach involving the simultaneous use of different branches of study, such as systems neurobiology, behavioral analysis, genetics, and cell and molecular techniques. This narrative review aims to clarify the mechanisms of transmission and the processing of pain while also taking into account the characteristics and properties of nociceptors and how the immune system influences pain perception. Moreover, several important aspects of this crucial theme of human life will be discussed. Nociceptor neurons and the immune system play a key role in pain and inflammation. The interactions between the immune system and nociceptors occur within peripheral sites of injury and the central nervous system. The modulation of nociceptor activity or chemical mediators may provide promising novel approaches to the treatment of pain and chronic inflammatory disease. The sensory nervous system is fundamental in the modulation of the host’s protective response, and understanding its interactions is pivotal in the process of revealing new strategies for the treatment of pain.

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