ropinirole (Requip CR / ropinirole 24hr / Requip LP)

✓ Approved

SkyePharma PLC · DRD2 · 小分子

什么是 ropinirole？

ropinirole 是一种小分子，由SkyePharma PLC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	Requip CR, ropinirole 24hr, Requip LP
公司	SkyePharma PLC
药物类别	小分子
分子靶点	DRD2, DRD3
给药途径	Oral (PO)
状态	Approved

来源： ClinicalTrials.gov, SkyePharma PLC

作用机制

分子靶点

ropinirole 作用于 2 个分子靶点：

DRD2	dopamine receptor D2 (D2DR, D2R)
DRD3	dopamine receptor D3 (D3DR, FET1)

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

ropinirole 针对 2 个适应症，涉及 1 个治疗领域。

治疗领域	疾病/病症	分期
Nervous system disorders	Parkinson's disease	✓ Approved
Nervous system disorders	Restless legs syndrome	Phase II

相关研究文献

PubMedBiological & pharmaceutical bulletin2026-10-25

Interleukin-31 Induces Itch-Related Responses with Precursor Behaviors in Mice and Its Suppression by the Dopamine D2/D3 Receptor Agonist Ropinirole.

Andoh Tsugunobu T, Suzuki Mami M

Recent research has revealed that human itch manifests in a variety of distinct phenotypes, such as muzumuzu (creepy-crawly itch, a bit like tickling). We have also demonstrated that scratching behaviors induced by pruritogens in mice are sometimes preceded by specific precursor behaviors, such as shivering or forelimb grooming, whereas in other cases, these precursors are absent. These findings suggest that mice, like humans, exhibit characteristic itch-related behaviors. In the present study, we focused on interleukin-31 (IL-31), which has been implicated in atopic dermatitis-associated itch, and investigated whether precursor behaviors were observed during IL-31-induced itch-related behaviors in mice. Male ICR mice were used in this study. Following intradermal injection of IL-31, subsequent behaviors were recorded with a digital video camera, and scratch behaviors were counted based on the presence or absence of precursor behaviors. Intradermal IL-31-induced scratching with precursor behaviors was significantly higher than that without them. Dopamine D2 receptor agonists are reported to be effective against restless sensations. Ropinirole, a dopamine D2/D3 receptor agonist, significantly suppressed IL-31-induced scratching with precursor behaviors. Interestingly, ropinirole also attenuated IL-31-induced scratching without precursor behaviors. Histamine induces scratching that is unaccompanied by precursor behaviors compared to those accompanied by them. Ropinirole also inhibited histamine-induced scratching, both with and without precursor behaviors. In conclusion, these findings provide the first evidence that IL-31-induced itch-related responses are primarily characterized by precursor behaviors. Moreover, the fact that ropinirole significantly suppressed both IL-31- and histamine-induced scratching suggests that ropinirole holds therapeutic promise for managing diverse itch signaling pathways.

PMID 42927937

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PubMedSleep science (Sao Paulo, Brazil)2026-10-22

A First Case of Compulsive Amnestic Sleep-Related Shopping Induced by Pramipexole Therapy of Restless Legs Syndrome.

Todd Michael M, Schenck Carlos H CH, Golden Erin E, Varghese Ranji R

Dopamine receptor agonists (DAs) such as pramipexole/ropinirole are recognized treatments for restless legs syndrome (RLS) and Parkinson's disease (PD). It is well established that these medications can cause impulse control disorders (ICDs) during wakefulness, side effects with serious and potentially life-altering consequences. Impulse control disorders are recurrent difficult-to-resist behaviors that can be harmful to the patient or others around them. Common examples include pathologic gambling and compulsive sexual behaviors, eating, and shopping. We present the case of a patient with RLS who developed pathologic nocturnal sleep-related shopping, without recalling the events, which resolved after discontinuing pramipexole. This case illustrates the devastating consequences that unrecognized medically-induced ICDs can have on patients' lives and the importance of counseling patients about ICDs during wake and sleep prior to starting DA therapy.

PMID 42904291

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PubMedEuropean journal of case reports in internal medicine2026-10-15

Adult-Onset Levodopa-Unresponsive Parkinsonism as the Presenting Feature of Aromatic L-Amino Acid Decarboxylase Deficiency.

Spiteri Matthew M, Tilney Russel R, Said Edith E, Vella Malcolm M

Aromatic L-amino acid decarboxylase is a critical enzyme required for the final step in the synthesis of dopamine and serotonin, two important neurotransmitters. Aromatic L-amino acid decarboxylase (AADC) deficiency is a rare autosomal recessive disorder of neurotransmitter biosynthesis caused by pathogenic variants in the dopa decarboxylase (DDC) gene. An absence or decrease of dopamine and serotonin levels may lead to severe motor and neurodevelopmental impairments. It classically presents within the first 6 months of life with a triad of hypotonia, oculogyric crises and developmental delay. Adult-onset presentations are extremely rare and underreported. We report the case of a 53-year-old man who presented with progressive left-sided bradykinesia, stiffness, rigidity and resting tremor over a year and a half. Examination demonstrated asymmetrical parkinsonism including facial hypomimia, cogwheel rigidity and a reduced arm swing on the left. A trial of levodopa of up to 1000 mg levodopa equivalent daily dose did not improve his condition. Magnetic resonance imaging of the brain was reported as normal without radiological signs of atypical parkinsonian neurodegenerative disorders. An autoimmune and onconeural antibody panel was negative. The patient's symptoms progressively deteriorated and he noted dysphagia requiring a tailored feeding plan Dopamine transporter single-photon emission computed tomography was performed demonstrating a marked reduction of nigrostriatal synaptic integrity at the right putamen and modest reduction at the left putamen. Targeted genetic testing identified a homozygous missense variant [NM_000790.3: c.710T>C p. (Phe237Ser)] in the DDC gene, establishing the diagnosis of AADC deficiency. Levodopa was substituted with a direct dopamine agonist (ropinirole) which resulted in a modest clinical improvement; however, dose escalation was limited by nausea. The patient subsequently developed neuropsychiatric symptoms which were managed with mirtazapine and sodium valproate. This case expands the recognised phenotypic spectrum of AADC deficiency and highlights the importance of considering neurotransmitter biosynthesis defects in levodopa-unresponsive adult parkinsonism. Aromatic L-amino acid decarboxylase (AADC) deficiency, classically an infantile-onset neurometabolic disorder, can present in adulthood as a levodopa-unresponsive parkinsonian syndrome and should be considered in adults with otherwise unexplained atypical parkinsonism.In cases of lack of response to adequate doses of levodopa in an apparent Parkinson's disease phenotype, consideration of a neuroreceptor biosynthesis defect should be made and direct dopamine agonists such as ropinirole can be trailed, as they bypass this metabolic block, and may produce clinical improvement.Unremarkable magnetic resonance imaging does not exclude a neurodegenerative or genetic parkinsonism. Dopamine transporter single-photon emission computed tomography can demonstrate reduced uptake representing nigrostriatal denervation in AADC deficiency. Biallelic dopa decarboxylase molecular genetic testing is first line for diagnosis, guiding drug selection and genetic counselling of the patient and relatives.

PMID 42877280

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PubMedInternational journal of pharmaceutics2026-09-18

Modulating microneedles' array design and application force for personalizing skin permeation using design of experiments.

Antonara Lefkothea L, Bampatsikou Charitini Georgia CG, Monou Paraskevi Kyriaki PK, Baltatzis George E GE et al.

Polymeric microneedle arrays are medical devices composed of micro-scale needles that enhance skin permeation by breaching stratum corneum's integrity and creating microchannels. Morphology as well as dimensional characteristics of these structures, namely height, base width, density of arrays and tip diameter can significantly affect the permeation profile of the active ingredient. Additionally, the force applied during application is also considered a key factor of drug delivery. Therefore, within the concept of personalizing the rate and amount of drug permeated through skin, a screening of the aforementioned factors was performed. Specifically, microneedles of various geometries and dimensions were prepared and evaluated with regards to their dimensional accuracy, insertion depth and drug permeation. For this purpose, Ropinirole Hydrochloride (RopHCl) was utilized as model drug due to its hydrophilic nature. In more detail, ten microneedle morphologies were evaluated in relation to their effect in the drug delivered, while a Definitive Screening Design (DSD) was implemented to screen the effect of the microneedle dimensional characteristics in the arrays' performance. Overall, significant differentiations between the microneedles shapes were observed across the permeation profiles while height, interspacing distance and insertion force were the main factors revealed as significant by the experimental design applied. Regarding base width, although it does not directly influence drug permeation, it affects the mechanical rigidity. It can be thus concluded that drug permeation through skin can be effectively personalized by tuning the microneedle array properties, while keeping a constant microneedle composition.

PMID 42759675

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PubMedCureus2026-09-11

Tramadol for Refractory Restless Legs Syndrome Following Methadone Intolerance: A Case Report.

Pham Binh B, Thai Vivian V

Restless legs syndrome (RLS) refractory to guideline-directed therapy may require treatment with low-dose opioids. Methadone is an established option for refractory RLS but may be limited by medication intolerance. We present a 52-year-old woman with refractory RLS who failed multiple pharmacologic therapies, including ropinirole, carbidopa/levodopa, gabapentin, and pregabalin. Methadone produced excellent symptom control but was discontinued because of dysphoria, emotional lability, cognitive slowing, and persistent daytime grogginess. Transition to tramadol 50 mg nightly resulted in sustained symptom control without recurrence of these adverse effects, allowing discontinuation of gabapentin and improved daytime functioning. This case highlights the importance of individualized opioid selection in refractory RLS and suggests that tramadol may be an effective alternative for carefully selected patients with methadone intolerance.

PMID 42723915

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PubMedEuropean child & adolescent psychiatry2026-08-25

Ropinirole adjunct to methylphenidate versus placebo adjunct to methylphenidate for attention-deficit/hyperactivity disorder: a randomized, double-blind, placebo-controlled trial.

Farahvash Aidin A, Naseh Ehsan E, Morovvati Mahdis M, Shamabadi Ahmad A et al.

Current therapeutics for attention-deficit/hyperactivity disorder (ADHD) have significant limitations, necessitating innovative therapies. This study aimed to investigate the efficacy and safety of ropinirole, a dopamine agonist with anti-inflammatory and neuroprotective properties, as an add-on to methylphenidate for children with ADHD. In this eight-week, randomized, double-blind trial, 66 outpatients aged 6-17 with a diagnosis of ADHD were randomized to receive methylphenidate plus either ropinirole 0.25 mg or a matching placebo twice daily. ADHD-related symptoms were assessed using the ADHD Rating Scale-IV (ADHD-RS-IV) reported by teachers and parents at baseline and weeks 4 and 8. Inattention and hyperactivity-impulsivity subscale scores were also recorded. Additionally, adverse effects were monitored throughout the study. Data from 65 participants were used for analyses. Baseline demographic and clinical characteristics were comparable between the arms. Significant time-by-treatment interaction was observed for the ADHD-RS-IV total scores as rated by teachers ([Formula: see text]= 0.051) and parents ([Formula: see text]= 0.153). The ropinirole group demonstrated significantly greater reductions in ADHD-RS-IV total scores from baseline to the endpoint as reported by teachers (Cohen's d = 0.530) and parents (Cohen's d = 0.504). Also, the ropinirole group achieved higher rates of response to treatment (69.7% versus 34.4%) and robust improvement (60.6% versus 25.0%). The incidence of adverse effects was comparable. In conclusion, methylphenidate + ropinirole was safe and beneficial compared to methylphenidate + placebo for reducing inattentive, hyperactive-impulsive, and total symptoms in children with ADHD. Further studies are required.

PMID 42640474

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ropinirole (Requip CR / ropinirole 24hr / Requip LP)

什么是 ropinirole？

药物档案

作用机制

分子靶点

治疗适应症

相关研究文献

Interleukin-31 Induces Itch-Related Responses with Precursor Behaviors in Mice and Its Suppression by the Dopamine D2/D3 Receptor Agonist Ropinirole.

A First Case of Compulsive Amnestic Sleep-Related Shopping Induced by Pramipexole Therapy of Restless Legs Syndrome.

Adult-Onset Levodopa-Unresponsive Parkinsonism as the Presenting Feature of Aromatic L-Amino Acid Decarboxylase Deficiency.

Modulating microneedles' array design and application force for personalizing skin permeation using design of experiments.

Tramadol for Refractory Restless Legs Syndrome Following Methadone Intolerance: A Case Report.

Ropinirole adjunct to methylphenidate versus placebo adjunct to methylphenidate for attention-deficit/hyperactivity disorder: a randomized, double-blind, placebo-controlled trial.

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