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pregabalin (pregabalin, YuHan / YHD 1119 / YHD1119)

✓ Approved

YuHan · CACNA2D1 · Small Molecule

What is pregabalin?

pregabalin is a small molecule developed by YuHan. It is approved for therapeutic indications via oral (po).

Drug Profile

Brand Namespregabalin, YuHan, YHD 1119, YHD1119
CompanyYuHan
Drug ClassSmall Molecule
Molecular TargetCACNA2D1
RouteOral (PO)
StatusApproved
Sources: ClinicalTrials.gov, YuHan

Mechanism of Action

Molecular Targets

pregabalin acts on 1 molecular target:

CACNA2D1calcium voltage-gated channel auxiliary subunit alpha2delta 1 (LINC01112, CACNA2)
Want deeper analysis?Noah AI can explain complex mechanisms and compare to similar drugs.

Therapeutic Indications

pregabalin is developed for 2 unique indications across 1 therapeutic area.

Therapeutic AreaConditionPhase
Nervous system disordersDiabetic neuropathy✓ Approved
Nervous system disordersPost herpetic neuralgia✓ Approved

Related Research Articles

PubMedBritish journal of clinical pharmacology2026-07-25

Gabapentinoids-duloxetine combination therapy for chronic pain: A mechanism oriented rational to bridge theoretical knowledge and real life setting.

Nobili Stefania S, Evangelista Maurizio M, Lucarini Elena E, Giugliano Elena G EG et al.

Chronic pain represents a complex debilitating condition that extends beyond the protective function of physiological pain, often persisting as an independent disease entity. Chronic primary and secondary pain syndromes reflect a multifaceted continuum involving nociceptive, neuropathic and nociplastic mechanisms. The maladaptive plasticity of the peripheral and central nervous system (encompassing the ascending and descending pain pathways) sustains hypersensitivity and correlates with comorbid alterations in mood, cognition, sleep and fatigue, underpinned by functional reorganization of brain networks. In this scenario, traditional analgesics frequently demonstrate limited efficacy, while current guidelines recommend antiepileptic agents and antidepressants, particularly gabapentinoids and duloxetine, as first line pharmacological options. This review explores the mechanistic rationale and clinical evidence supporting the combined use of gabapentinoids and duloxetine in chronic pain management. These agents act on distinct yet complementary targets: gabapentinoids reduce excitatory neurotransmission via modulation of calcium channel activity, whereas duloxetine restores descending noradrenergic inhibition and alleviates comorbid symptoms. Clinical trial and meta-analyses highlight their individual efficacy in diabetic peripheral neuropathy, postherpetic neuralgia and fibromyalgia. Among gabapentinoids, pregabalin exhibits a favourable pharmacokinetic profile that allows rapid titration and demonstrates effectiveness against anxiety-related sleep disorders. Importantly, emerging evidence suggests that their combination may offer additional benefit, particularly in patients with residual pain despite monotherapy, though evidence remains limited to small, short-term studies. This review provides proof of concept by bridging theoretical knowledge and real-life clinical settings aiming to develop treatment protocols based on predominant pain mechanisms that can effectively control hypersensitivity and improve quality of life.

PMID 42498694
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PubMedNature and science of sleep2026-07-22

Once-Nightly Pregabalin for Co-Occurring Nightmares, Poor Sleep, and Headaches: A Case Series.

Bates James H JH, Rosin Sophia Brooke SB, Tobin Joshua A JA

Nightmares, nonrestorative sleep, and headaches co-occur, are common, underdiagnosed, and contribute to substantial disability. Pregabalin modulates excitatory neurotransmission, increases slow-wave sleep, and suppresses REM sleep, suggesting a potential therapeutic role in nightmares and sleep disturbance. Pregabalin's effect on nightmares has not been systematically studied. Although sedation is a common side effect when prescribed 2-3 times daily according to the package insert, the efficacy and tolerability of once-nightly administration remain poorly characterized. Our retrospective case series included 23 outpatients seen in the neurology department of a tertiary care center from November 2022 to August 2025. They were prescribed once-nightly pregabalin for nightmares, nonrestorative sleep, and headaches. Clinical data were extracted from medical records, including nightmare frequency, fraction of 24-hour periods with restorative sleep, headache frequency, severity, and duration, and MIDAS scores. Within-subject pre-post comparisons were performed using paired t-tests or Wilcoxon signed-rank tests. All p-values were Holm-Bonferroni adjusted. Nightmare frequency decreased 81% (17.5 to 3.3/month, padj=0.006). Nightmares decreased numerically more for those who transitioned from gabapentin to pregabalin (91%) than for those not initially taking gabapentin (73%). Restorative sleep frequency increased 127% (1.8 to 4.0/week, padj=0.006). Headache frequency decreased 50% (17.0 to 8.5/month, padj=0.040). Migraine Disability Assessment Questionnaire scores decreased numerically by 34% (38.0 to 24.0) but did not reach statistical significance after correction (padj=0.084). Six patients reported side effects, and 19 continued pregabalin at three months. Once-nightly pregabalin was associated with robust reductions in nightmare frequency, nonrestorative sleep, and headache frequency. The improvement in nightmares validates two prior case reports through systematic cohort evaluation. Nightmares improved even among patients transitioning from gabapentin to pregabalin, suggesting that pregabalin may be superior to gabapentin. No prior studies have addressed these three co-occurring problems simultaneously. Larger controlled studies are needed to test the hypothesis that once-nightly pregabalin may be useful for this patient population.

PMID 42483729
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PubMedInflammopharmacology2026-07-22

The effect of pregabalin on pain and function in knee osteoarthritis: a systematic review and meta-analysis of randomized controlled trials.

Kow Chia Siang CS, Ramachandram Dinesh Sangarran DS, Thiruchelvam Kaeshaelya K

Knee osteoarthritis (OA) is a prevalent chronic condition characterized by joint pain and functional impairment. While non-steroidal anti-inflammatory drugs (NSAIDs) remain the cornerstone of pharmacologic management, a subset of patients may experience persistent symptoms due to central sensitization. Pregabalin, a neuromodulator used in neuropathic pain, has been proposed as an adjunctive treatment for OA, but its efficacy remains unclear. To evaluate the effectiveness and safety of pregabalin in reducing pain and improving function among patients with knee OA through a systematic review and meta-analysis of randomized controlled trials (RCTs). We searched PubMed, Embase, Scopus, and Cochrane CENTRAL from inception to June 2025 for RCTs comparing pregabalin (alone or in combination with NSAIDs) versus control (NSAIDs or placebo) in knee OA patients. Primary outcomes were pain (Visual Analog Scale, VAS) and function (Western Ontario and McMaster Universities Osteoarthritis Index, WOMAC). A random-effects model was used to calculate pooled weighted mean differences (WMDs) with 95% confidence intervals (CIs). Risk of bias was assessed using the Cochrane RoB 2.0 tool. Three RCTs comprising four treatment arms with 214 patients were included. Pregabalin, when combined with NSAIDs, resulted in significant functional improvement (WMD: - 10.55; 95% CI: - 19.47 to - 1.63) and a non-significant trend toward pain reduction (WMD: - 0.63; 95% CI: - 1.44 to 0.18). Pregabalin monotherapy was less effective than combination therapy. Moderate to high heterogeneity was observed. Adverse events, primarily dizziness and somnolence, were mild and did not lead to discontinuation. Pregabalin may enhance functional outcomes and contribute to pain relief when used as adjunctive therapy with NSAIDs in knee OA patients. Its benefit as monotherapy remains limited. While pregabalin was generally well-tolerated, larger, high-quality trials with longer follow-up are needed to confirm its role and long-term safety.

PMID 42481863
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PubMedPain and therapy2026-07-21

How the Reclassification of Gabapentinoids Reshaped Neuropathic Pain Treatment in Saudi Arabia: A Survey of Healthcare Professionals.

Kaki Abdullah A, Hamdy Yousef Y, Amir Ashraf A

This study aimed to assess knowledge gaps, perceptions, and prescribing approaches of healthcare professionals (HCPs) in Saudi Arabia regarding pain management, particularly neuropathic pain, in the context of recent reclassification of gabapentinoids. A three-lecture webinar was attended by 4922 HCPs across Saudi Arabia. Two structured surveys were embedded within the lectures: a 9-item knowledge questionnaire on pain management and a 10-item questionnaire on HCPs' opinions and attitudes on gabapentinoid use and prescribing challenges. Responses were recorded on the platform's interactive dashboard as percentage. The knowledge scores were normalized to percentage. Overall knowledge levels varied across specialties with internal medicine (68.7%) and pain specialists (68.3%) having the top scores; non-pain organ specialists scored the lowest (59.1%). The majority of HCPs (68.8%) agreed that prescribing gabapentinoids has become more challenging than prescribing tramadol post reclassification, with patients' concerns related to substance dependence (32.6%) and extended process in obtaining medication (27.9%) cited by the majority. Gabapentinoids remained the preferred treatment for diabetic peripheral neuropathy by most HCPs (36.8%). Most HCPs (47.4%) reported initiating gabapentinoids at the lowest possible dose and increasing as needed, while a smaller proportion preferred initiating an appropriate dose with minimal adjustments (18.5%). Among pain specialists, these approaches were nearly evenly divided (37.7% and 31.9%, respectively). The majority (45.7%) selected pregabalin 300 mg as their preferred daily dose for transitioning from gabapentin 900 mg. This nationwide survey highlights substantial variability and knowledge gaps related to general pain, neuropathic pain management, and excessive caution among HCPs regarding prescribing gabapentinoids and patient concerns of developing dependence. To maintain gabapentinoid access and timely care for patients with legitimate needs, there is a need to implement educational programs for HCPs across specialties and develop a unified treatment approach that fulfils the guidelines and addresses exaggerated patient worries along with patient-focused initiatives to reduce hesitancy post reclassification of gabapentinoids.

PMID 42479365
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PubMedCurrent pain and headache reports2026-07-21

Sublingual Cyclobenzaprine for Fibromyalgia: Pharmacokinetic Rationale, Clinical Evidence, and Place in Therapy.

Abd-Elsayed Alaa A, Knezic Anna A, Asfour Julia J, Dewan Pranav P et al.

Fibromyalgia (FM) is a chronic nociplastic pain syndrome characterized by widespread pain, nonrestorative sleep, fatigue, and cognitive dysfunction, affecting approximately 2-6% of U.S. adults. Although oral cyclobenzaprine has been used off label for decades, its clinical utility has been limited by a narrow benefit-to-harm ratio, with the number needed to treat for symptomatic improvement approximating the number needed to harm for at least one adverse event at conventional doses. This review examines the mechanistic, pharmacokinetic, and clinical evidence supporting the August 2025 FDA approval of sublingual cyclobenzaprine (TNX-102 SL; Tonmya), the first new pharmacologic treatment approved for FM in more than 15 years. Emerging evidence suggests that cyclobenzaprine's therapeutic effects in FM are primarily mediated through antagonism of 5-HT2A and α1-adrenergic receptors, influencing central pain processing and sleep architecture rather than peripheral muscle relaxation. The sublingual formulation produces a unique pharmacokinetic profile, with peak plasma concentrations occurring 4-5 h after bedtime administration, aligning drug exposure with the middle of the sleep period. In the pivotal phase 3 RELIEF and RESILIENT trials, TNX-102 SL demonstrated significant improvements in daily pain compared with placebo, along with benefits in sleep quality, fatigue, and Patient Global Impression of Change scores. Meta-analyses encompassing four clinical trials have reported modest efficacy comparable to established agents such as duloxetine and pregabalin. The approval of TNX-102 SL represents a significant advance in FM management by providing a therapy specifically designed to target sleep-related mechanisms implicated in nociplastic pain. By shifting adverse effects from systemic manifestations to predominantly local oral effects, the sublingual formulation may offer improved tolerability compared with oral cyclobenzaprine. TNX-102 SL appears particularly well suited for patients with sleep-predominant FM symptoms who have not responded adequately to or cannot tolerate existing first-line treatments.

PMID 42479282
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PubMedClinics (Sao Paulo, Brazil)2026-07-18

Pregabalin beyond pain: A neuroprotective alternative in peripheral nerve injury.

Alcántara Montero Antonio A

PMID 42468374
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