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Synthesis, Enzyme Localization, and Regulation of Neurosteroids
Published in Sheryl S. Smith, Neurosteroid Effects in the Central Nervous System, 2003
2002), ethanol (Sundstrom-Poromaa et al., 2002), etomidate (Brown et al., 2002), the anesthetic isofluorane (Lees and Edwards, 1998), and protons (Krishek et al., 1995). Interestingly, there is recent evidence that GABA itself may interact differently with δ subunit-containing receptors. Adkins et al. (2001) found that the synthetic GABA analog THIβ showed greater efficacy at a4p38 receptors, raising the possibility that incorporation of the δ subunit may render GABA a partial agonist. Finally, just as there is evidence for a subtype dependence of aPy receptor functional properties, a recent study indicated that the a subtype can further specify the enhancement of peak currents and desensitization by neurosteroids (Figure
Trends in gabapentin and baclofen exposures reported to U.S. poison centers
Published in Clinical Toxicology, 2020
Kimberly Reynolds, Robert Kaufman, Amanda Korenoski, Laura Fennimore, Joshua Shulman, Michael Lynch
Gabapentin, a gamma-aminobutyric acid (GABA) analog, was developed as an anticonvulsant and is commonly prescribed as an analgesic, primarily for neuropathic pain as well as multiple off label uses including: migraines, mental illness, and fibromyalgia [9]. Many providers have embraced gabapentin as a safer alternative to opioids for pain management. Gabapentin prescribing increased 64% from 39 million prescriptions in 2012 to 64 million by 2016 when it was the 10th most commonly prescribed medication in the United States [10]. Significant misuse and diversion of gabapentin have been well-documented [11–17]. Individuals have reported euphoria, relaxation, improved sociability, a marijuana-like “high”, and a sense of calm following gabapentin use. Gabapentin overdose may be fatal, though far less commonly than opioids. Gabapentin is renally excreted so clearance will be prolonged in patients with impaired renal function [18]. There is no antidote for gabapentin and given the long half-life, overdose treatment may require prolonged, intensive management including hemodialysis [19,20].
Trending gabapentin exposures in Kentucky after legislation requiring use of the state prescription drug monitoring program for all opioid prescriptions#
Published in Clinical Toxicology, 2019
Kiran A. Faryar, Ashley N. Webb, Bikash Bhandari, Timothy G. Price, George M. Bosse
Gabapentin is a gamma-aminobutyric acid (GABA) analog structurally related to the GABA neurotransmitter although it does not interact with GABA receptors or inhibit GABA uptake or degradation [1]. Gabapentin also binds to the alpha-2-delta subunit of calcium channels, which inhibits calcium current and decreases neurotransmitter release. Binding at this receptor has been associated with anticonvulsant activity [2,3]. It is approved by the US Food and Drug Administration (FDA) for the treatment of partial seizures and post-herpetic neuralgia [4,5]. Clinically, it is frequently used off-label for a wide array of medical conditions including mood disorders, posttraumatic stress disorder, behavioral disorders [6], restless leg syndrome, cocaine withdrawal, insomnia, neuropathy[7], tremors, and chronic pain [8,9]. Gabapentin has a wide therapeutic window and few serious adverse side effects with therapeutic use [4]. Side effects are non-specific and include somnolence, dizziness, ataxia, fatigue, nystagmus, and movement disorder [6,10].
Pharmacotherapeutic options for the treatment of menopausal symptoms
Published in Expert Opinion on Pharmacotherapy, 2021
Andrea R. Genazzani, Patrizia Monteleone, Andrea Giannini, Tommaso Simoncini
Gabapentin is a gamma-aminobutyric acid (GABA) analogue but does not affect the neurotransmitter GABA binding, uptake, or degradation. Gabapentin has binding sites throughout the brain, through which it exerts analgesic and anticonvulsant activity. This drug was first experimented in 2000 as a non-hormonal option to relieve vasomotor symptoms [206]. The exact mechanism through which it alleviates vasomotor symptoms is unknown, but the hypothesis is that it reduces adrenergic hyperactivity, thus widening the thermoregulatory zone in the hypothalamus [206].