Pharmacology and Therapeutics of Gabapentin in the Treatment of Psychiatric Disorders; Present and Future Perspectives

Megna, James L; Iqbal, Mian Muhammad Ahmad; Aneja, Ashish

doi:10.2174/1570159033477125

Cited by 4 publications

(2 citation statements)

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“…Although gabapentin appears to have diverse therapeutic utility in the treatment of pain disorders [1], psychiatric illnesses [2] and epilepsy [3], there is controversy regarding its molecular mechanisms of action. Whether the actions of gabapentin and pregabalin are mediated through GABAergic mechanisms or GABA receptors remains particularly contentious [4-6].…”

Section: Introductionmentioning

confidence: 99%

A study comparing the actions of gabapentin and pregabalin on the electrophysiological properties of cultured DRG neurones from neonatal rats

et al. 2004

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Background: Gabapentin and pregabalin have wide-ranging therapeutic actions, and are structurally related to the inhibitory neurotransmitter GABA. Gabapentin, pregablin and GABA can all modulate voltage-activated Ca 2+ channels. In this study we have used whole cell patch clamp recording and fura-2 Ca 2+ imaging to characterise the actions of pregabalin on the electrophysiological properties of cultured dorsal root ganglion (DRG) neurones from neonatal rats. The aims of this study were to determine whether pregabalin and gabapentin had additive inhibitory effects on high voltage-activated Ca 2+ channels, evaluate whether the actions of pregabalin were dependent on GABA receptors and characterise the actions of pregabalin on voltage-activated potassium currents.

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Section: Introductionmentioning

confidence: 99%

A study comparing the actions of gabapentin and pregabalin on the electrophysiological properties of cultured DRG neurones from neonatal rats

et al. 2004

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“…A 50-µL aliquot of each working standard solution was added to 950 µL blank equine plasma in a pre-labeled 1.5-mL microcentrifuge tube (Fisher Scientific) to prepare 10,20,40,80,200, 400, 800, 2000, and 2500 ng/mL calibrators. Quality control (QC) plasma samples, each at 40, 400, and 2000 ng/mL, were similarly prepared.…”

Section: Preparation Of Calibration Samples and Quality Control Samplesmentioning

confidence: 99%

Analysis of Gabapentin in Equine Plasma with Measurement Uncertainty Estimation by Liquid Chromatography-Tandem Mass Spectrometry

Liu

Uboh

Soma

et al. 2011

Journal of Analytical Toxicology

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Gabapentin (GPT) is an antiepileptic drug that was approved in 1993 for use in the management of neurotrophic pain and as an adjunctive therapy for refractory partial seizure in humans.It is also being tested in veterinary medicine as an adjunctive medication in the treatment of pain due to laminitis, neuropathic, or chronic pain. Gabapentin is readily available by prescription and even on the internet; therefore, it has the potential of being used in racehorses to mask pain. It is for this reason that a sensitive liquid chromatography-tandem mass spectrometry method has now been developed for the analysis of GPT in equine plasma and for studying the pharmacokinetic and pharmacodynamic profiles of GPT in the horse. Sample preparation was by rapid protein precipitation with acetonitrile. Analyte separation was achieved on a reversed-phase ACE C 18 column and analyzed by a hybrid triple-quadrupole linear ion trap mass spectrometer in positive electrospray ionization mode. Limits of detection, quantification, and confirmation of GPT were 1, 10, and 20 ng/mL, respectively. Calibration curve showed excellent linearity within the 10-2500 ng/mL range (r 2 > 0.999). Intra-and interday precision defined by coefficient of variation was <10%. Intra-and interday accuracy (bias %) was within 90-110%. Measurement uncertainty estimation was 8.6%. The method has been successfully used in the analysis of GPT in equine plasma following its administration to research horses for pharmacokinetic studies and in routine forensic analysis for doping control in racehorses in the State of Pennsylvania.

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Mechanisms of the Antinociceptive Action of Gabapentin

2006

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Abstract. Gabapentin, a γ-aminobutyric acid (GABA) analogue anticonvulsant, is also an effective analgesic agent in neuropathic and inflammatory, but not acute, pain systemically and intrathecally. Other clinical indications such as anxiety, bipolar disorder, and hot flashes have also been proposed. Since gabapentin was developed, several hypotheses had been proposed for its action mechanisms. They include selectively activating the heterodimeric GABA B receptors consisting of GABA B1a and GABA B2 subunits, selectively enhancing the NMDA current at GABAergic interneurons, or blocking AMPA-receptor-mediated transmission in the spinal cord, binding to the L-α-amino acid transporter, activating ATP-sensitive K + channels, activating hyperpolarization-activated cation channels, and modulating Ca 2+ current by selectively binding to the specific binding site of [3 H]gabapentin, the α 2 δ subunit of voltage-dependent Ca 2+ channels. Different mechanisms might be involved in different therapeutic actions of gabapentin. In this review, we summarized the recent progress in the findings proposed for the antinociceptive action mechanisms of gabapentin and suggest that the α 2 δ subunit of spinal N-type Ca 2+ channels is very likely the analgesic action target of gabapentin.

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Pharmacology and Therapeutics of Gabapentin in the Treatment of Psychiatric Disorders; Present and Future Perspectives

Cited by 4 publications

References 0 publications

A study comparing the actions of gabapentin and pregabalin on the electrophysiological properties of cultured DRG neurones from neonatal rats

A study comparing the actions of gabapentin and pregabalin on the electrophysiological properties of cultured DRG neurones from neonatal rats

Analysis of Gabapentin in Equine Plasma with Measurement Uncertainty Estimation by Liquid Chromatography-Tandem Mass Spectrometry

Mechanisms of the Antinociceptive Action of Gabapentin

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