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topiramate (USL255 / Qudexy XR)

✓ Approved

Upsher-Smith Laboratories, LLC. · GRIA1 · 小分子

什么是 topiramate？

topiramate 是一种小分子，由Upsher-Smith Laboratories, LLC.研发。该药已获批，用于治疗相关适应症，给药途径：Oral (PO)。

药物档案

商品名USL255, Qudexy XR
公司Upsher-Smith Laboratories, LLC.
药物类别小分子
分子靶点GRIA1, SCN5A
给药途径Oral (PO)
状态Approved
来源： ClinicalTrials.gov, Upsher-Smith Laboratories, LLC.

作用机制

分子靶点

topiramate 作用于 2 个分子靶点：

GRIA1glutamate ionotropic receptor AMPA type subunit 1 (GLUR1, HBGR1)
SCN5Asodium voltage-gated channel alpha subunit 5 (CMD1E, SSS1)
需要更深入的分析？Noah AI 可解释复杂机制并与同类药物比较。

治疗适应症

topiramate 针对 2 个适应症，涉及 2 个治疗领域。

治疗领域疾病/病症分期
Nervous system disordersPartial seizures✓ Approved
Surgical and medical proceduresMigraine prophylaxis✓ Approved

相关研究文献

PubMedEuropean archives of psychiatry and clinical neuroscience2026-08-04

Efficacy and safety of add-on topiramate vs. metformin on cardiometabolic profile in patients of schizophrenia on atypical antipsychotics with metabolic syndrome: an active-controlled, rater-blinded, parallel-design randomized controlled trial.

Chakraborty Radhika R, Mohapatra Debadatta D, Biswas Tathagata T, Ramasubbu Mathan Kumar MK et al.

Metabolic syndrome is common among patients with schizophrenia, but current treatment options are limited, with metformin being the most studied. While placebo-controlled studies suggest potential benefits of topiramate, comparative efficacy and safety data are lacking. This study aimed to compare the efficacy and safety of topiramate versus metformin for treating metabolic syndrome and reducing cardiovascular risks among patients with schizophrenia. A randomised, open-label, parallel-group clinical trial was conducted on 60 patients of schizophrenia with metabolic syndrome, randomised equally to receive either topiramate (50 mg/day) or metformin (1000 mg/day) for eight weeks. Primary outcome was cardiovascular risk score (QRISK3), and secondary outcomes were LDL∶HDL ratio, insulin resistance (HOMA-IR), positive and negative syndrome scale (PANSS), Montreal Cognitive Assessment (MoCA) and clinical global impression-Schizophrenia scale (CGI-SCH) scores. Over the study period, QRISK3 scores improved significantly in both groups [topiramate: MD = 0.61 (0.02 to 1.21), p = 0.04; metformin: MD = 0.45 (0.07 to 0.83), p = 0.02], with no significant between-group difference in unadjusted analysis (p = 0.648). However, ANCOVA adjusting for baseline QRISK3 revealed a significantly greater improvement in the topiramate group (β = -0.324, p = 0.043). Metformin showed significant within-group improvements in LDL: HDL ratio and HOMA-IR; however, ANCOVA adjusting for baseline HOMA-IR showed the between-group difference remained non-significant (β = -1.209, p = 0.078). Both groups showed significant improvements in PANSS and CGI-SCH scores, with no significant between-group differences in MoCA scores. A moderate correlation between the QRISK3 change, the PANSS change, and the CGI-SCH-I scores was observed in the topiramate group and the total population. Regression analysis identified PANSS change as a predictor of QRISK3 improvement. Topiramate demonstrated comparable, and on adjusted analysis superior, cardiovascular risk reduction compared to metformin, supporting its use as a viable alternative in the management of metabolic syndrome in patients with schizophrenia on atypical antipsychotics, particularly where metformin is contraindicated.

PMID 42550195
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PubMedThe journal of headache and pain2026-07-31

Twelve-months prospective real-world assessment of effectiveness and safety of eptinezumab in migraine patients difficult-to-treat and naïve to CGRP monoclonal antibodies: results of the French FHU INOVPAIN registry.

Ferrao-Malheiro S S, Fabre R R, Jiacomini T T, Lanteri-Minet M M

Randomized clinical trials have demonstrated the efficacy and safety of eptinezumab. The aim of this study was to evaluate the effectiveness and safety of eptinezumab in a real-world setting among patients with difficult-to-treat migraine in France. This is a one year-prospective real-word study including all consecutive adult patients from the Federation Hospitalo-Universitaire InovPain registry who received intravenous eptinezumab 100 mg. Three hundred and two patients (83.8% female / mean age of 48.0 ± 13.9 years) were included. Patients had at least 8 monthly migraine days, had failed at least 3 previous prophylactic treatments across amitryptiline, betablockers, botulinum toxin, candesartan, and topiramate and were Calcitonin Gene Related Peptide monoclonal antibodies naïve. Among them, 184 patients (60.9%) had chronic migraine and 118 (39.1%) had episodic migraine, whereas 229 patients (75.8%) presented a medication overuse. Regarding the primary endpoint, 50% responder rate at month 3, month 6, and month 12 was 35.4% (107/302), 39.0% (96/246), and 45.7% (63/138), respectively. ≥30% responder rate at month 3, month 6, and month 12 was 48.7% (147/302), 56.1% (138/246), and 63.0% (87/138), respectively. ≥75% responder rates at M3, M6, and M12 was 10.9% (33/302), 15.4% (38/246), and 23.2% (32/138), respectively. The effectiveness of eptinezumab was confirmed by significant changes in the values of all patient reported outcome measures at all assessment time points compared with baseline, demonstrating improvement in functional impact (Headache Impact Test-6), emotional impact (Hospital Anxiety Depression Scale), interictal burden (Migraine Interictal Burden Scale-4), and quality of life (Euro Qol-5 Dimensions descriptive system and visual analogue scale). According to Patient Global Impression of Change, the proportions of patients reporting being "much improved" or "very much improved" were 41.9% at month 3, 54.8% at month 6 and 74.4% at month 12. Overall, effectiveness appeared similar in episodic migraine and chronic migraine except at month12, where rates of 50% and 75% response were significantly higher in the chronic migraine (50% response: 53.8% vs. 34.5%, p = 0.025; 75% response: 30% vs. 13.8%, p = 0.026). Adverse events were uncommon and mostly mild, transient, and self-limited with few expected hypersensitivity reactions. This French real-word study confirms the effectiveness and safety of eptinezumab in difficult-to-treat patients with migraine who and have failed non-specific preventive migraine treatments and are naïve to Calcitonin Gene Related Peptide monoclonal antibodies. Not applicable.

PMID 42533319
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PubMedEinstein (Sao Paulo, Brazil)2026-07-29

Acute-onset bilateral myopia induced by hydrochlorothiazide.

Zimmermann Luiza Moschetta LM, Resende José Marcos de Araújo JMA, Castro Heloiza de H, Barcellos Ronaldo Boaventura RB

Sulfonamides are widely prescribed in clinical practice. Although rare, these have been shown to trigger an idiosyncratic reaction characterized by an acute myopic shift, likely caused by ciliochoroidal effusion and anterior rotation of the ciliary body, resulting in forward displacement of the iris-lens diaphragm. We report the case of a patient who developed blurred vision and acute myopia on cycloplegic refraction after initiating hydrochlorothiazide. The symptoms resolved completely after discontinuation of the medication. Although most of the literature highlights this reaction in association with topiramate, it is important to note that any sulfonamide can potentially lead to a similar clinical presentation.

PMID 42524931
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PubMedCephalalgia : an international journal of headache2026-07-27

Treatment patterns and Reasons for Discontinuing Preventive Treatment in Cluster Headache: A prospective cohort study.

Petersen Anja Sofie AS, Laursen Sophie Bryde SB, Søborg Marie-Louise Kulas MK, Barløse Mads M et al.

BackgroundPharmacological prevention of cluster headache aims to reduce the frequency and intensity of attacks, but the long-term effect and tolerance of treatments remain uncertain. The aim of the study was twofold. First, to quantify the discontinuation rates of preventive treatment due to side effects; and second, to assess the proportion of verapamil responders who maintained preventive effectiveness at follow-up.MethodsIn total, 596 participants with cluster headache fulfilling the ICHD-criteria (the baseline cohort) completed a semi-structured interview between 2017 and 2023. Of these, 430 were re-interviewed after a median time of 4.6 years constituting the follow-up cohort.ResultsIn the baseline cohort, 457 participants (76.7%) had taken a preventive medicine for cluster headache. Among these, 123 (26.9%) had discontinued a treatment due to intolerable side effects. The discontinuation rate for the first-line treatment verapamil was 18%, whereas the second-line treatments with lithium or topiramate had been discontinued in nearly half. The odds of discontinuing due to intolerable side effects of lithium or topiramate therapy were four times higher than for verapamil (p < 0.0001).In the follow-up cohort, only 143 participants (33.3%) still received a preventive treatment at the time of the second interview. Of the initial 182 verapamil users, 77 (42.3%) continued, 54 (29.7%) had discontinued due to remission, and 51 (28%) discontinued due to intolerable side effects, lack of effect, or for other reasons. At follow-up including new users, a total of 91 participants were treated with verapamil and 50 of them (54.9%) were 50% responders.ConclusionEffective therapeutic prevention of cluster headache is hindered by intolerance and insufficient efficacy of the available preventives. Though verapamil remains effective over time for initial responders, there is a high rate of discontinuation due to side effects or lack of efficacy. Taken together with the low proportion of 50% responders, the findings underscore the need for new tolerable and effective preventive treatment for cluster headache.

PMID 42506063
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PubMedHeadache2026-07-27

Clinical characteristics, neurovascular compression, and treatment outcomes in SUNCT and SUNA: A contemporary Japanese consecutive case series.

Kikui Shoji S, Danno Daisuke D, Nawata Masahiro M, Iwai Yoshiyasu Y et al.

This study aimed to characterize the contemporary clinical phenotype of short-lasting unilateral neuralgiform headache attacks (SUNHA) in Japan, evaluate the prevalence and clinical relevance of neurovascular compression (NVC), and assess real-world medical and surgical treatment outcomes. SUNHA, comprising short-lasting unilateral neuralgiform headache attacks with conjunctival injection and tearing (SUNCT) and those with cranial autonomic symptoms (SUNA), is a rare trigeminal autonomic cephalalgia disorder. Although several large cohorts have been reported in Western countries, data from Asia, particularly Japan, remain limited. Moreover, the clinical significance of NVC and the role of microvascular decompression (MVD) in medically refractory cases have not been fully established, and no standardized operational definition of refractory SUNHA exists. We conducted a retrospective consecutive case series of 28 patients with SUNHA (14 SUNCT and 14 SUNA) who were evaluated at a tertiary headache center in Japan between 2011 and 2024. Diagnoses were made according to the International Classification of Headache Disorders, 3rd edition. Clinical features, trigger factors, cranial autonomic symptoms, comorbidities, and treatment responses were systematically reviewed and analyzed. High-resolution constructive interference in steady-state (CISS) magnetic resonance imaging was used to assess the NVC. Treatment response was defined as a subjective reduction of ≥50% in the attack burden. Refractory SUNHA was operationally defined as failure of or intolerance to at least two of the three principal preventive drug classes (lamotrigine, gabapentinoids, and topiramate). Surgical outcomes following MVD were evaluated in the refractory cases. SUNHA accounted for 0.2% of all patients with headache evaluated in this study. The mean age at onset was 53.1 ± 20.9 years, with 17 male and 11 female patients. Right-sided pain (20/28, 71%) and ophthalmic (V1) trigeminal distribution (20/28, 71%) predominated. No statistically significant differences were detected between SUNCT and SUNA with respect to attack duration, frequency, triggers, or treatment responsiveness. NVC was identified in 17 of 27 evaluable patients (17/27, 63%; 95% confidence interval [CI]: 44.3%-78.5%) and was strongly associated with a history of TN-like pain (12/17 vs. 0/10, p < 0.001). Seven of 28 patients (7/28, 25%; 95% CI: 12.7%-43.4%) met criteria for refractory SUNHA, and all refractory cases (7/7, 100%; 95% CI: 64.6%-100%) demonstrated NVC. Five of seven refractory patients (5/7, 71%) underwent MVD and achieved complete and sustained remission. In this contemporary Japanese SUNHA cohort, no statistically significant clinical differences were detected between SUNCT and SUNA. NVC was relatively common and appeared to be associated with medical refractoriness. In carefully selected patients with refractory SUNHA and convincing NVC, MVD may provide durable clinical benefit.

PMID 42503640
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PubMedBMJ case reports2026-07-25

Fenfluramine in refractory SCN1A-related 'genetic epilepsy with febrile seizures plus'.

Takahashi Tatsuya T, Abe Yuichi Y, Hayakawa Itaru I

A child with SCN1A-related 'genetic epilepsy with febrile seizures plus' (GEFS+) presented in infancy with recurrent febrile and afebrile seizures, frequently progressing to generalised tonic-clonic status epilepticus. Despite a severe seizure burden and typical Dravet-like triggers, neurodevelopment remained entirely normal and a familial SCN1A variant supported a diagnosis of GEFS+. The variant (c.5666T>A, p.Met1889Lys) was classified as a variant of uncertain significance fulfilling PM2, PP1 and PP3 criteria and absent from The Genome Aggregation Database (gnomAD) and ClinVar. Identification of the same variant in a neurodevelopmentally normal parent supported inherited GEFS+ rather than Dravet syndrome. After treatment failure with sodium valproate, clobazam and topiramate, low-dose fenfluramine (2.2 mg/day, 0.15 mg/kg/day) achieved seizure freedom maintained for more than 1 year with no adverse effects. This dose is substantially lower than the 0.2-0.7 mg/kg/day used in Dravet syndrome trials, suggesting GEFS+ may require lower therapeutic thresholds.

PMID 42498321
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