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Background
Gabapentin (GBP), also known as 1-(aminomethyl)-cyclohexaneacetic acid, is synthesized synthetically and is structurally similar to γ-aminobutyric acid (GABA). The drug was initially used as an anti-seizure treatment and was later approved by the FDA as a first-line drug for postherpetic neuralgia (PHN) treatment. Gabapentin has been found to reduce seizure frequency in combination with traditional antiepileptic drugs and has unique advantages in the treatment of chronic pain, especially in neuropathic pain.
Figure 1. Structure of gamma-aminobutyric acid (GABA) and gabapentin (Source: Rissardo JP, et al. 2023)
Although gabapentin is structurally related to GABA, it does not interact with GABA receptors. It is neither metabolized to GABA or GABA agonists, nor is it an inhibitor of GABA uptake or degradation. It has been found that gabapentin has no affinity for many common receptor sites at concentrations up to 100 μm. Therefore, the pharmacological effects of gabapentin have not yet been clarified. The bioavailability of gabapentin is disproportionate to the dose and decreases when the dose is increased. It has a half-life of 5 to 7 hours and is eliminated from the circulatory system primarily in its original form via renal excretion and is not significantly metabolized in the body.
Gabapentin has significant antiepileptic effects and can be combined with other antiepileptic drugs for combination therapy, primarily for add-on therapy for drug-resistant epilepsy over the age of 12 and for limited seizures that are intolerable to other drugs. GBP also has unique advantages in the treatment of neuropathic pain, for example, general painkillers are ineffective or have limited therapeutic effects in PHN, whereas the continued use of gabapentin effectively relieves mood changes and significantly improves the quality of life of patients with PHN. In addition, the drug can be used for other neuropathic pain treatments such as trigeminal neuralgia and migraines. Gabapentin has been shown to be effective in perioperative pain management. Currently, perioperative analgesia is mainly provided with a combination of opioids and nonsteroidal anti-inflammatory drugs, which have significant side effects, whereas gabapentin has good antinociceptive abnormalities and antinociceptive hypersensitivity, as well as few side effects. Common adverse effects of oral gabapentin include dizziness, drowsiness, ataxia, and peripheral edema, diarrhea, constipation, dry mouth, nausea and vomiting. These side effects are common in the early stages of medication and can be tolerated by most people as long as they start with a small dose and increase the dose slowly.
Alternative Names
Anti-GBP Monoclonal antibody
References
1. Quintero GC. Review about gabapentin misuse, interactions, contraindications and side effects. J Exp Pharmacol. 2017 Feb 9;9:13-21.
2. Rissardo JP, et al. Gabapentin-Associated Movement Disorders: A Literature Review. Medicines (Basel). 2023 Sep 6;10(9):52.
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References
Anxiolytic-like effects of mirogabalin, a novel ligand for alpha(2)delta ligand of voltage-gated calcium channels, in rats repeatedly injected with acidic saline intramuscularly, as an experimental model of fibromyalgia
Background Mental disorders including anxiety and depression are common comorbidities in fibromyalgia patients, and exert a profound impact on their quality of life. Mirogabalin, a novel ligand for the alpha(2)delta-subunit of voltage-gated calcium channels, shows analgesic effects in fibromyalgia and neuropathic pain models. To provide additional information regarding its potential utility for treating chronic pain, we examined its anxiolytic-like effects in rats repeatedly injected with acidic saline intramuscularly (Sluka model), as an experimental fibromyalgia model. Methods Male Sprague-Dawley rats received two intramuscular injections of acidic saline (pH 4.0) into the gastrocnemius muscle. After the development of tactile allodynia demonstrated by decreased paw withdrawal threshold to von Frey filaments, anxiety-like behaviours were evaluated using the open field test and the elevated plus maze test. Results Sluka model rats exhibited anxiety-like behaviours in the open field test (significant decreases in distance travelled and time spent in the central area, and significant increases in time spent in the wall area) and the elevated plus maze test (significant decreases in time spent in the open arms and significant increases in time spent in the closed arms). A single oral dose of mirogabalin (3 or 10 mg/kg) significantly alleviated and normalised these anxiety-like behaviours. Conclusions Sluka model rats exhibited anxiety-like behaviours in the open field test and the elevated plus maze test, but mirogabalin alleviated these behaviours. Mirogabalin might thus have the potential to relieve anxiety in fibromyalgia patients.
Pregabalin alleviates clinical signs of syringomyelia-related central neuropathic pain in Cavalier King Charles Spaniel dogs: a randomized controlled trial
VETERINARY ANAESTHESIA AND ANALGESIA
Authors: Thoefner, Maria S.; Skovgaard, Lene T.; McEvoy, Fintan J.; Berendt, Mette; Bjerrum, Ole J.
Objective We aimed to assess the efficacy and benefit-risk profile of pregabalin (PGN) to reduce the clinical signs of central neuropathic pain (CNeP) as reflected by scratching episodes in dogs with symptomatic syringomyelia (SM). Study design Randomized, double-blind, placebo-controlled crossover study. Animals A total of 12 client-owned Cavalier King Charles Spaniels (age, 1.1-7.4 years, bodyweight, 8.2-10.8 kg) with magnetic resonance imaging-confirmed SM and clinical signs of CNeP. Methods Dogs were randomized to either PGN 150 mg or placebo for 25 days, followed by 48 hour washout period before crossover to the alternate phase of 25 days. The primary outcome was defined as number of scratching events during 10 minutes of video-recorded physical activity. Treatment effect was estimated using a generalized estimation equation model. Benefit-risk and quality of life assessments were obtained through owner interviews focusing on potential adverse events. Results The treatment effect estimate was an 84% (95% confidence interval = 75-89%) reduction in mean number of scratching events relative to baseline compared with placebo (p < 0.0001). Owner-assessed satisfactory quality of life was status quo and rated as 'good' or 'could not be better' in six/11 dogs and improved in four/11 dogs. The most prevalent adverse events were increased appetite in nine/12 dogs and transient ataxia in nine/12 dogs. There was one dog withdrawn by the owner 7 days after crossover to PGN owing to persistent ataxia. No dogs needed rescue analgesia during the trial. Conclusions and clinical relevance PGN is superior to placebo in the reduction of clinical signs of SM-related CNeP in dogs. At a dose range of 13-19 mg kg(-1) orally twice daily, the encountered adverse events were acceptable to all but one owner.
COA
Publication 
Figure 1. Structure of gamma-aminobutyric acid (GABA) and gabapentin
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