ReviewPharmacology research & perspectives2016
Mechanisms of the gabapentinoids and α 2 δ-1 calcium channel subunit in neuropathic pain.
Review in Pharmacology research & perspectives, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 133 papers, 10 of them syntheses that pooled it.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
133 citing papers in PubMed, 10 syntheses or guidelines pooled it, 257 citations in OpenAlex.
- The effect of pregabalin on pain and function in knee osteoarthritis: a systematic review and meta-analysis of randomized controlled trials.Inflammopharmacology · 2026Pooled it
- Pooled it
- Efficacy of gabapentin and pregabalin for treatment of post refractive surgery pain: a systematic review and meta-analysis.International ophthalmology · 2024Pooled it
- Persistent sodium currents in neurons: potential mechanisms and pharmacological blockers.Pflugers Archiv : European journal of physiology · 2024Pooled it
- Analgesic Efficacy of Gabapentin and Pregabalin in Patients Undergoing Laparoscopic Bariatric Surgeries: a Systematic Review and Meta-analysis.Obesity surgery · 2022Pooled it
- Pharmacological Probes to Validate Biomarkers for Analgesic Drug Development.International journal of molecular sciences · 2022Pooled it
- Pregabalin withdrawal in patients without psychiatric disorders taking a regular dose of pregabalin: A case series and literature review.Neuropsychopharmacology reports · 2021Pooled it
- Pregabalin for neuropathic pain in adults.The Cochrane database of systematic reviews · 2019Pooled it
- Position Paper for the Treatment of Nightmare Disorder in Adults: An American Academy of Sleep Medicine Position Paper.Journal of clinical sleep medicine : JCSM : official publication of the American Academy of Sleep Medicine · 2018Guideline
- Benefits and safety of gabapentinoids in chronic low back pain: A systematic review and meta-analysis of randomized controlled trials.PLoS medicine · 2017Pooled it
- Exploratory study of heart rate variability among participants with opioid use disorder inducted on gabapentin versus placebo during outpatient buprenorphine-assisted transition to injection naltrexone.Experimental and clinical psychopharmacology · 2025Trial
- Safety, Tolerability and Pharmacokinetics of Single and Multiple Doses of Mirogabalin in Healthy Chinese Participants: A Randomized, Double-Blind, Placebo-Controlled Study.Advances in therapy · 2023Trial
- Trial
- Effectiveness of preanesthetic administration of gabapentin on sedative action during intravenous sedation with propofol.Journal of anesthesia · 2018Trial
- Association Between the Use of Gabapentinoids and Exacerbations of Chronic Obstructive Pulmonary Disease: A Systematic Review and Meta-analysis.Current therapeutic research, clinical and experimental · 2026Review
- Effects of Kalanchoe pinnata, exercise, and stimulation on neuroinflammation, redox homeostasis, and neuropathic pain in a Wistar-rat model.World journal of experimental medicine · 2026Article
- Therapeutic potential of CMPP, a novel maleimide derivative, in a reserpine-induced mouse model of pain-depression dyad.Biochemistry and biophysics reports · 2026Article
- Pharmacological Relevance of β-, γ-, and LINGO Auxiliary Subunits in BK Channel Modulation.ChemMedChem · 2026Review
- Molecular Mechanisms of Acute Drug Toxicity in Polypharmacy: Analgesic-Psychotropic Interactions.International journal of molecular sciences · 2026Review
- Perioperative pregabalin does not alter behavioural or diffuse noxious inhibitory control responses in 2 rat models of chronic pain.Pain reports · 2026Article
73 more citing papers are in PubMed but not listed here.
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
2 authors at 1 institution in 1 country.
Funding
Abstract
The gabapentinoid drugs gabapentin and pregabalin are key front-line therapies for various neuropathies of peripheral and central origin. Originally designed as analogs of GABA, the gabapentinoids bind to the α 2 δ-1 and α 2 δ-2 auxiliary subunits of calcium channels, though only the former has been implicated in the development of neuropathy in animal models. Transgenic approaches also identify α 2 δ-1 as key in mediating the analgesic effects of gabapentinoids, however the precise molecular mechanisms remain unclear. Here we review the current understanding of the pathophysiological role of the α 2 δ-1 subunit, the mechanisms of analgesic action of gabapentinoid drugs and implications for efficacy in the clinic. Despite widespread use, the number needed to treat for gabapentin and pregabalin averages from 3 to 8 across neuropathies. The failure to treat large numbers of patients adequately necessitates a novel approach to treatment selection. Stratifying patients by sensory profiles may imply common underlying mechanisms, and a greater understanding of these mechanisms could lead to more direct targeting of gabapentinoids.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.