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methylphenidate (Methydur)

✓ Approved

Durect · SLC6A2 · 小分子

什么是 methylphenidate？

methylphenidate 是一种小分子，由Durect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Methydur
公司Durect
药物类别小分子
分子靶点SLC6A2, SLC6A3
给药途径Oral (PO)
状态Approved
来源： ClinicalTrials.gov, Durect

作用机制

分子靶点

methylphenidate 作用于 2 个分子靶点：

SLC6A2solute carrier family 6 member 2 (NAT1, NET)
SLC6A3solute carrier family 6 member 3 (PKDYS, DAT1)
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

methylphenidate 针对 1 个适应症，涉及 1 个治疗领域。

治疗领域疾病/病症分期
Psychiatric disordersAttention deficit hyperactivity disorder✓ Approved

相关研究文献

PubMedCurrent opinion in neurology2026-10-26

Psychopharmacological advances in neurorehabilitation after traumatic brain injury.

Arcani Vincent V, Iruthayanathar Charles C, Rauen Katrin K

Pharmacotherapy is widely used to manage neuropsychiatric sequelae that may interfere with neurorehabilitation after traumatic brain injury (TBI), despite limited TBI-specific evidence. This review summarizes psychopharmacological evidence from the past 18 months and proposes a three-step approach: deprescribing potentially recovery-limiting medications, characterizing individual neuropsychiatric symptoms, and selecting symptom-targeted treatments to support cognitive, emotional, behavioral, and functional recovery after TBI. Methylphenidate shows the most consistent evidence for selected cognitive outcomes, particularly attention and processing speed. Pharmacological approaches to agitation, sleep-wake disorders, depression, fatigue, and posttraumatic headache have been studied, but TBI-specific evidence remains limited or heterogeneous. Sedative, anticholinergic, and cognitive adverse effects, cardiovascular risks, and dependence require consideration in TBI neurorehabilitation. No pharmacological treatment is established as disease-modifying after TBI. Given the limited evidence, psychopharmacotherapy should be individualized, symptom-targeted, and integrated into multidisciplinary TBI neurorehabilitation. Continuous medication review and deprescribing should accompany careful treatment selection and monitoring. Future trials should determine whether symptom improvement translates into better rehabilitation participation, functional independence, and long-term health-related quality of life.

PMID 42929311
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PubMedFrontiers in endocrinology2026-10-24

Isolated increased free-triiodothyronine in medication-naïve children and adolescents with ADHD: a retrospective observational study.

Caci Hervé H, Caron Philippe P

Thyroid hormones, free triiodothyronine (free-T3) in particular, are crucial for fetal development and child growth and may influence neurodevelopmental disorders including Attention-Deficit/Hyperactivity Disorder (ADHD) in children and adolescents. Yet data are scarce and inconsistent, often relying on adult rather than pediatric reference intervals or on incomplete thyroid panels, and the value of free-T3 as a biomarker across development remains unclear. In this retrospective observational study, we characterized thyroid function in medication-naïve patients aged 6 to 17 years with ADHD, using community laboratory results collected between March 2004 and December 2022 in a university pediatric department. Thyroid testing was prescribed prior to methylphenidate initiation. We determined the percentage of patients with free-T3, free-T4, and TSH levels below, within, or above age- and sex-adjusted reference intervals. In the largest immunoassay subgroup (ADVIA Centaur; n = 404), individual free-T3 values were converted to z-scores using published pediatric normative data. A longitudinal ancillary analysis assessed temporal stability in patients with repeat measurements. No non-ADHD comparison group was available. Among 715 medication-naïve patients with ADHD (570 boys, 145 girls) with normal TSH, approximately one-third presented with isolated increased free-T3 concentrations (2IfT3 profile) - 33.68% of boys, 27.59% of girls - the most frequent thyroid anomaly observed. In the ADVIA Centaur subgroup, free-T3 z-scores were higher than the pediatric norms across all age groups, with the largest deviation in boys aged 11-14 years. Among 57 patients with repeat testing (median interval 2.57 years), instability was marked: 53.57% of those initially showing 2IfT3 normalized, while 50% of those initially normal developed 2IfT3. Isolated increased free-T3 is frequent in medication-naïve pediatric ADHD and most pronounced in boys aged 11-14 years, but its marked temporal instability precludes its use as a stable biomarker. In the absence of a concurrent non-ADHD comparison group, these findings describe the frequency of this biochemical profile within an ADHD cohort rather than establishing an association with ADHD itself. The 2IfT3 profile may reflect a developmentally and state-dependent neuroendocrine pattern, and warrants prospective study incorporating direct pubertal staging, standardized assay methodology, and appropriate controls.

PMID 42920592
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PubMedProceedings of the National Academy of Sciences of the United States of America2026-10-23

Neuropharmacology of language: ERP evidence for catecholaminergic modulation of syntactic processing.

Tan Yingying Y, Lewis Ashley G AG, Schmits Iris C IC, Verkes Robert-Jan RJ et al.

A few studies have shown that brain catecholamines are implicated in language comprehension. However, the specific cognitive processes they modulate remain underexplored. We hypothesized that catecholamines enhance the unification of syntactic roles and word meanings into coherent multiword structures. This study combined electroencephalography and psychopharmacology to examine the effects of a catecholaminergic stimulant (methylphenidate) on processing sentences containing local syntactic ambiguities. Methylphenidate amplified the P600 event-related potential effect, which has been linked to the recruitment of cognitive resources for processing sentences with increased syntactic load. The drug's impact on semantic processing was subtler, showing a suggestive attenuation of the N400 effect to ambiguous sentences. Furthermore, the increase in the P600 effect under methylphenidate was most pronounced in participants with lower working memory capacity. This study provides evidence for linking catecholamine activity to syntactic unification in healthy individuals. Elevated catecholamine levels appear to increase the cognitive effort invested in syntactic unification, and to support the dynamic prioritization of syntactic information when contextual demands require it.

PMID 42911864
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PubMedMovement disorders clinical practice2026-10-22

When Tics and Autism Meet: Phenomenology, Severity, and Treatment Patterns.

Aldurayhim Fatimah F, Martino Davide D, Sarna Justyna R JR, Pringsheim Tamara T

Tic disorders frequently co-occur with neurodevelopmental conditions, including autism spectrum disorder (ASD). However, the impact of ASD on tic phenomenology, severity, and treatment patterns remains incompletely understood. To compare clinical characteristics, tic phenomenology, severity, and treatment patterns in individuals with tic disorders with and without comorbid ASD. We conducted a cross-sectional analysis of 535 participants from Calgary Child and Adult Tic Disorders Clinical Registries. Tic severity was assessed using the Yale Global Tic Severity Scale (YGTSS). Comorbidities, tic phenomenology, and pharmacological treatments were recorded. ASD and non-ASD groups were compared using t-tests and chi-square tests. Mean age at tic onset was 6.79 years; 73.3% were male, and 9.2% had ASD. ASD was associated with higher rates of complex motor (arm 20.4% vs 9.9%; hand 24.5% vs 13.9%) and vocal tics (phrases 12.2% vs 3.5%; palilalia 20.4% vs 8.3%; blocking/stuttering 16.3% vs 6.2%) compared with non-ASD participants (all P < 0.05), with similar overall severity. ASD was also associated with higher rates of ADHD (81.6% vs 44.7%) and greater use of guanfacine, aripiprazole, risperidone, methylphenidate, and dextroamphetamine compared with non-ASD participants (all P < 0.05). In multivariable analysis, ASD was independently associated with lower tic-related impairment (β = -4.49, 95% CI -8.46 to -0.51; P = 0.027). Comorbid ASD in tic disorders is associated with higher rates of complex motor and vocal tics, while severity is similar to non-ASD. Lower tic-related impairment may reflect communication differences. Comorbid symptoms influenced treatment supporting the need for individualized management.

PMID 42902960
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PubMedBMC gastroenterology2026-10-20

Parabacteroides distasonis ameliorates methylphenidate hydrochloride-induced colonic inflammatory responses and associated gastrointestinal distress.

Yao Jinwen J, Gao Xia X, Zhu Lin L, Wang Linlin L et al.

Attention-deficit/hyperactivity disorder (ADHD) is a common neurodevelopmental disorder in childhood, with methylphenidate hydrochloride (MPH) as its first-line pharmacotherapy. Though effective, MPH is associated with underrecognized gastrointestinal adverse events warranting further investigation. Recently, the gut microbiota has attracted attention for treating gastrointestinal distress, but research on its role in alleviating MPH-induced gastrointestinal reactions remains scarce. Herein, Wistar-Kyoto rats (WKY) served as controls alongside spontaneously hypertensive rats (SHR) to explore MPH-induced gastrointestinal adverse drug reactions. The gastrointestinal phenotypes, colonic histopathological characteristics, and inflammatory factor levels were evaluated, and the gut microbiota profiles were analyzed via 16S rRNA gene sequencing. The protective effect of Parabacteroides distasonis (P. distasonis) was further verified by supplementing the treated rats with this strain. We demonstrated MPH induced diarrhea and colonic inflammatory responses in rats. 16S rRNA gene amplicon sequencing revealed that MPH-treated rats had significantly decreased gut microbiota health index, increased dysbiosis index, and reduced P. distasonis abundance, suggesting MPH-induced gastrointestinal reactions may correlate closely with reduced P. distasonis. Further experiments confirmed that P. distasonis supplementation effectively alleviated diarrhea and colonic inflammatory responses in MPH-treated rats. Collectively, this is the first study verifying that P. distasonis supplementation mitigates MPH-induced gastrointestinal adverse reactions, providing a novel intervention strategy to improve tolerance of ADHD pharmacotherapy.

PMID 42897488
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PubMedBrain and behavior2026-10-19

Efficacy of Saffron as an Adjunct to Methylphenidate in Treating ADHD in Children Aged 6-12: A Randomized Clinical Trial.

Hosseinpourfardi Asieh A, Sahaf Seyyed Mohammad Saeid SMS, Afzaljavan Fahimeh F, Soltanifar Atefeh A et al.

Attention-deficit/hyperactivity disorder (ADHD) is a common childhood disorder often managed with stimulant medications such as methylphenidate. Around 30% of patients with ADHD do not respond to treatment or cannot tolerate its side effects, which necessitates the consideration of alternative options. This study evaluated the effectiveness of adding the saffron extract to methylphenidate on ADHD symptoms and working memory in children aged 6-12. In a randomized clinical trial, 58 children diagnosed with ADHD were randomized into two groups: a methylphenidate (0.5-1 mg/kg/day, divided into 2-3 doses)/saffron (20-30 mg/day based on weight: 20 mg for <30 kg, 30 mg for >30 kg) group and a control group receiving only methylphenidate (0.5-1 mg/kg/day, divided into 2-3 doses) for six weeks. The severity of ADHD was evaluated using subjective (Conners' Parent Rating Scale-revised) and objective (Corsi block-span task and continuous performance test) tests at the start and end (in the sixth week) of the study. 22 participants in the methylphenidate/saffron group and 21 in the control group completed the study. The changing trend of total ADHD scores (p = 0.002, Cohen's d = 0.85), hyperactivity score (p = 0.024, d = 0.62), impulsivity score (p = 0.031, d = 0.58), and attention score (p = 0.001, d = 0.92) was significantly different between groups based on subjective parent reports. However, no significant differences were found in impulsivity, inattention, or sustained attention on the CPT, though reaction time improved significantly (p = 0.023, d = 0.45). Scores on the Corsi Block Span Task indicated no significant changes in working memory between groups. The combination treatment was well-tolerated, with no reports of severe adverse effects. The findings suggest that the combination of saffron with methylphenidate may enhance subjective reports of ADHD symptoms, particularly hyperactivity and impulsivity; however, objective cognitive measures showed limited changes. Given the favorable safety profile of saffron and study limitations, this supports its potential role as a complementary option, pending confirmation in placebo-controlled trials with larger samples and long-term evaluations.

PMID 42895808
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