Drug Database
PR

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

PubMedJournal of pain research2026-05-22

Efficacy and Safety of Pregabalin-Tizanidine vs Pregabalin in Patients with Fibromyalgia: Study Protocol for a Multicenter, Prospective, Randomized, Controlled, Open-Label, Blinded Endpoint Trial.

Liu Qiang Q, Wen Chuanbing C, Dai Yuee Y, Ma Teng T et al.

The global prevalence of fibromyalgia (FM) in the general population is estimated to range from 2% to 4%. Pregabalin, a gamma-aminobutyric acid (GABA) analogue, is one of the most widely prescribed medications for FM. However, at therapeutic doses, its limited efficacy and/or unacceptable side effects mean that many patients derive only partial benefit, often leading to treatment discontinuation. Cyclobenzaprine is a centrally acting muscle relaxant. In August 2025, the United States Food and Drug Administration approved a sublingual formulation of cyclobenzaprine hydrochloride for treating FM in adults. However, its availability is largely confined to North America. Tizanidine, like cyclobenzaprine, is also a muscle relaxant with a central mechanism; however, there is no codified posology for FM treatment with tizanidine. This study aims to recruit 164 adult patients diagnosed with FM. Participants will be randomly assigned in a 1:1 ratio to either the intervention group (pregabalin plus tizanidine) or the control group (pregabalin monotherapy). The primary outcome is the change from baseline to week 12 in average pain intensity (during the last 7 days) assessed using the first item of the symptom domain of the Revised Fibromyalgia Impact Questionnaire (FIQR). Secondary outcomes, assessed at weeks 4, 8, 12, 16, 20, and 24, will include: widespread pain, symptom severity, functional performance, balance, muscle strength and power, psychological functioning, sleep quality, self-efficacy, treatment durability, and health-related quality of life. This study was approved by the Institutional Review Board of Beijing Tiantan Hospital (KY2025-217-03-08) and was registered with ClinicalTrials.gov (NCT07382921). All study procedures will be conducted in accordance with the Declaration of Helsinki (1964) and its subsequent amendments (7th revision, Fortaleza, Brazil, 2013). This trial will provide evidence for the efficacy and safety of pregabalin combined with tizanidine in the treatment of FM.

PMID 42170616
Read full article →
PubMedJournal of pain research2026-05-22

Efficacy and Safety of Adjunctive Therapy Using Single High-Dose S-Ketamine Infusion for Fibromyalgia: A Multicenter, Prospective, Randomized, Controlled, Open-Label, Blinded-Endpoint Study Protocol.

Shrestha Niti N, Liu Minying M, Niu Shaoning S, Cheng Hao H et al.

Fibromyalgia (FM) is a chronic pain syndrome with limited response and delayed onset to current treatments. Esketamine (ESK) shows potential as a rapid-acting analgesic in FM patients, but previous low-dose studies have had limited efficacy and are constrained by single-center designs, monotherapy approaches, and small sample sizes. The efficacy of higher-dose ESK administered as an adjunct to guideline-recommended pharmacotherapy in FM remains unclear. Multicenter, prospective, randomized, controlled, open-label, blinded-endpoint trial. A total of 92 adult FM patients will be randomized in a 1:1 ratio to either the treatment group (single intravenous infusion of ESK plus oral pregabalin and venlafaxine) or the control group (oral pregabalin and venlafaxine alone). In the treatment group, ESK will be administered as a single intravenous infusion at a dose of 1 mg/kg on the day of enrollment. Both groups will follow identical dose titration regimens for pregabalin and venlafaxine, with dose escalation individualized according to patient tolerability and clinical response. Plasma concentrations of ESK and its metabolites will be measured at the end of infusion to enable a limited characterization of systemic exposure and to support exploratory exposure-response analyses. Participants will be followed for 12 weeks. The primary outcome is the change from baseline in the mean pain intensity during the first week after treatment. The secondary outcomes include average pain intensity, worst pain intensity, and proportion of patients achieving ≥50% and ≥30% pain reduction, median pain relief time, maximal tolerated doses of pregabalin and venlafaxine, patient-reported outcomes (Revised FM Impact Questionnaire, Hospital Anxiety and Depression Scale, Short Form 36 Health survey, Multidimensional Fatigue Inventory, and Medical Outcomes Study Sleep Scale), plasma concentrations of ESK and its metabolites at the end of infusion, and adverse events throughout the study period. ClinicalTrails.gov identifier: NCT07230171. Registered on November 13, 2025 (https://www.clinicaltrials.gov/search?term=NCT07230171).

PMID 42170615
Read full article →
PubMedDrug design, development and therapy2026-05-22

Therapeutic Targets, Pharmacological Mechanisms, and Delivery Strategies for Diabetic Peripheral Neuropathy.

Wang Fanjing F, Shen Chuqiao C, Guo Weizhen W, Wang Junyu J et al.

With the global diabetes population projected to reach 783 million by 2045, diabetic peripheral neuropathy (DPN) remains a common and debilitating complication characterized by metabolic stress, inflammation, and microvascular dysfunction. This review summarizes current interventions for DPN from the perspective of therapeutic targets, pharmacological mechanisms, and emerging delivery strategies. Conventional pharmacotherapy mainly provides symptomatic relief; first-line analgesics such as duloxetine and pregabalin offer only moderate benefit, with a number needed to treat of approximately 4-5. Natural products, including resveratrol, ginkgo biloba, and tanshinone IIA, show antioxidant and anti-inflammatory potential, although supporting evidence remains largely preclinical. Emerging targeted therapies and nanocarrier-based delivery systems may improve disease modification and drug bioavailability. Overall, DPN treatment remains limited by the lack of disease-modifying therapies, insufficient high-quality clinical evidence, and major translational barriers. Future priorities include mechanism-based stratification, combination strategies, and rigorous trials incorporating objective and patient-reported outcomes.

PMID 42170520
Read full article →
PubMedThe Journal of pharmacy and pharmacology2026-05-21

Rutin enhances the analgesic efficacy of low-dose pregabalin without sedative side effects in a rat model of chronic constriction injury.

Helvacı Gülsüm G, Arslan Rana R, Bektaş Nurcan N

The aim of this study was to evaluate the antiallodynic and antihyperalgesic effects of rutin alone and in combination with pregabalin in a chronic constriction injury-induced neuropathic pain model. The potential antiallodynic and antihyperalgesic effects of combining rutin at doses of 25, 50, and 100 mg/kg with 3 mg/kg of pregabalin were evaluated in a rat neuropathic pain model induced by chronic constriction injury. Assessments were conducted over a 180-minute period using an electronic von Frey device and the plantar test. Spontaneous locomotor activity was evaluated using a Plexiglas activity cage. All combination groups exhibited statistically significant antiallodynic and antihyperalgesic effects at specific time intervals compared to the groups where rutin or 3 mg/kg pregabalin were administered alone. Furthermore, the efficacy of the combinations was found to be comparable to that of the group treated with 30 mg/kg pregabalin. The 25 mg/kg rutin combination was most effective and independent of locomotor activity. Given rutin's low side-effect profile and the dose-dependent risks of pregabalin, their combination at low-dose pregabalin may represent a safe and effective alternative for neuropathic pain treatment.

PMID 42166536
Read full article →
PubMedJournal of clinical anesthesia2026-05-21

Association of perioperative gabapentinoids with persistent opioid requirements following below knee amputation - A nationwide claims-based retrospective cohort study.

Hussain Nasir N, Brull Richard R, Gilron Ian I, Bhatia Anuj A et al.

Gabapentin and pregabalin (gabapentinoids) are commonly used in enhanced recovery protocols to reduce postoperative pain and opioid requirements. Below knee amputation (BKA) patients experience intense nociceptive and neuropathic pain post-BKA, increasing their risk of chronic pain and long-term opioid dependence, while multimodal analgesia including gabapentinoids is considered protective against these outcomes. We evaluated the role of gabapentinoids in reducing long-term opioid requirements post-BKA. A nationwide claims database was searched for opioid-naïve patients who had BKA between January-2010 and April-2022. We evaluated the association between newly prescribed perioperative gabapentinoid claims and continued opioid claims at three and six months post-BKA using multivariable regression modelling. We also explored this association using sensitivity analysis based on gabapentinoid type (gabapentin vs. pregabalin), claim timing (preoperative vs. postoperative), and post-BKA analgesics claims as acute pain control indicators. The matched cohort included 27,264 opioid-naïve BKA patients; 3338 had gabapentinoids claims in the 30 days pre- and/or post-BKA, while 23,926 did not. After multivariable adjustment, patients with gabapentinoid claims had higher odds of continued opioid claims at three and six months, with ratios (OR)[95% confidence interval] of 3.07[2.76, 3.42](p < 0.0001) and 2.44[2.17, 2.75](p < 0.0001), respectively. Three-month sensitivity analysis based on gabapentinoid type maintained a strong association; gabapentin and pregabalin OR = 3.08[2.45, 3.87](p < 0.0001) and 3.47[3.07, 3.94](p < 0.0001), respectively. Similarly, both pre-BKA and post-BKA gabapentinoids maintained an association; OR = 3.26[2.92, 3.63](p < 0.0001) and 5.32[3.72, 7.59](p < 0.0001), respectively. Finally, postoperative pain severity, estimated by analgesics claims, only marginally explained this association, OR = 1.34[1.23, 1.47](p < 0.0001). Perioperative gabapentinoid appears to be associated with a higher odds of persistent opioid claims in opioid-naïve BKA patients. While novel and requiring randomized trial confirmation, these findings may undermine gabapentinoids protective and opioid-sparing effects, and merit reexamining their use in multimodal perioperative pathways and pain regimens.

PMID 42160880
Read full article →
PubMedBrain and nerve = Shinkei kenkyu no shinpo2026-05-20

[Hansen's Disease].

Shiozaki Yu Y, Kimura Mai M, Ishii Norihisa N

Hansen's disease is a chronic infection of the skin and peripheral nerves caused by Mycobacterium leprae and Mycobacterium lepromatosis. Recently, only a few new cases have been reported in Japan. Diagnosis is based on the demonstration of the bacillus through skin smears, histopathology, or polymerase chain reaction, as well as other clinical and laboratory findings. Nerve conduction studies can detect subclinical neuropathy. Clinical classification is determined by variations in the host's cell-mediated immunity. The World Health Organization divides leprosy into paucibacillary (PB) and multibacillary (MB) forms. Ridley and Jopling classified the disease along a continuous spectrum from tuberculoid to lepromatous. Leprosy reactions, both type 1 and type 2, can lead to rapid nerve deterioration, necessitating immediate anti-inflammatory treatment and the continuation of multidrug therapy. The standard multidrug therapy regimen includes dapsone, rifampicin, and clofazimine, with typical durations of 6 months for PB and 12 months for MB. Peripheral nerve damage is irreversible once it occurs, making prevention the most effective strategy. Neuropathic pain is treated with agents such as pregabalin and amitriptyline. Rehabilitation is provided for muscle atrophy, and orthoses and prostheses are used to address deformities of the fingers and toes as well as limb deficiencies. Collaboration between dermatologists and physiatrists is essential.

PMID 42156030
Read full article →

+5195 more articles available with a free account

Sign up free to view all articles →

Ask about pregabalin