预约演示
更新于：2025-10-25
Guanfacine hydrochloride
盐酸胍法辛
更新于：2025-10-25
概要
基本信息
简介胍法辛（商品名为Tenex、Intuniv、Estulic）是一种作用于中枢的降压剂和α2肾上腺素受体激动剂。其作用机制是刺激脑内的α2肾上腺素受体，导致交感神经系统活动降低，从而降低血压。此外，胍法辛已被发现对调节注意力和行为的前额叶皮层产生影响，因此对治疗注意力缺陷多动障碍（ADHD）有用。胍法辛最初于1986年被FDA批准用于治疗高血压，授权公司是Promius Pharma LLC。随后在2009年，Takeda制药公司获得了美国批准，用于治疗儿童和青少年的ADHD。目前，它在世界多个国家获得了批准。 |
药物类型 小分子化药 |
别名 Connexyn、guanfacine、Guanfacine hydrochloride (JAN/USP) + [11] |
作用方式 激动剂 |
作用机制 adrenergic receptor激动剂(肾上腺素能受体家族激动剂) |
治疗领域 |
在研适应症 |
最高研发阶段批准上市 |
首次获批日期 美国 (1986-10-27), |
最高研发阶段(中国)临床3期 |
特殊审评孤儿药 (美国) |
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结构/序列
分子式C9H10Cl3N3O |
InChIKeyDGFYECXYGUIODH-UHFFFAOYSA-N |
CAS号29110-48-3 |
关联
88
项与 盐酸胍法辛 相关的临床试验NCT06408246
ACE-D: Accelerating Cognition-guided Signatures to Enhance Translation in Depression: Clinical Trial
NCT06629259
Guanfacine for Alcohol Use Disorder (AUD): a Telehealth Approach
NCT06642181
Combined Guanfacine and Mindfulness Meditation as an Adjunct to Buprenorphine Maintenance in Opioid Use Disorder
100 项与 盐酸胍法辛 相关的临床结果
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100 项与 盐酸胍法辛 相关的转化医学
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100 项与 盐酸胍法辛 相关的专利（医药）
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1,390
项与 盐酸胍法辛 相关的文献（医药）2025-10-01PAIN MEDICINE
Enhanced pain relief with guanfacine as an adjuvant for trigeminal nerve blocks: insights from a PheWAS-guided randomized controlled study
Article
作者: Orr, Michael B ; Mishra, Puneet ; Pulley, Jill M ; Shirey-Rice, Jana K ; Toye, Amanda D ; Jerome, Rebecca N ; Shotwell, Matthew S ; Kesayan, Tigran ; Edwards, David A ; Meier, Shelby E
Abstract:
Background:
Trigeminal neuralgia and painful trigeminal neuropathy are severely painful conditions which are often difficult to treat with medications. A Phenome-Wide Association Study (PheWAS) analysis identified an association between single-nucleotide variants in the alpha-2 adrenergic receptor (ADRA2) subtype B, a G protein-coupled receptor expressed on peripheral and central presynaptic terminals, and an increased risk for trigeminal nerve disorders. We hypothesized that adding the ADRA2 agonist guanfacine to routine care trigeminal nerve injections would provide enhanced pain relief in trigeminal neuralgia than routine care alone.
Methods:
PheWAS analysis identified the drug target/indication pair. The trial was a single-center, prospective, randomized, controlled, double-blinded, 2-way crossover trial for patients with pain attributed to the trigeminal nerve. Injections of lidocaine alone or lidocaine + 250 µg guanfacine were delivered to the V2 and V3 branches of the trigeminal nerve by experienced clinicians. Patients reported pain using a Numeric Rating Scale (NRS) and quality of life measures (using the PROMIS Global Physical Health, Mental Health, and Pain Interference surveys).
Results:
NRS pain scores over the first 8 h post-injection were significantly lower in the interventional group (guanfacine + lidocaine) compared to active control (P < .001), but not from day 1 through day 14. There was no significant difference between treatment groups in time to recovery of baseline pain intensity (primary outcome), PROMIS outcomes, or adverse events (AEs). No serious AEs were reported.
Conclusions:
The addition of 250 µg guanfacine to lidocaine for a nerve block procedure enhanced analgesia compared to lidocaine alone within the first 8 h post-injection.
Clinical Trial Number:
NCT03865940, https://clinicaltrials.gov/study/NCT03865940
2025-10-01PROGRESS IN NEURO-PSYCHOPHARMACOLOGY & BIOLOGICAL PSYCHIATRY
Oral guanfacine treatment ameliorates the ADHD-like symptoms caused by developmental manganese exposure
Article
作者: Fisher, Ellie ; Beaudin, Stephane A ; Strupp, Barbara J ; Smith, Donald R
Epidemiological studies have linked developmental manganese (Mn) exposure to increased risk of ADHD and related symptoms in children and adolescents. Rodent model studies have 1) confirmed causality by demonstrating that developmental Mn exposure can cause lasting ADHD-like symptoms, 2) revealed that these symptoms (in Mn-exposed animals) are accompanied by a hypofunctioning catecholaminergic system in fronto-cortical-striatal brain areas, and 3) demonstrated that methylphenidate is efficacious in ameliorating these ADHD-like symptoms in Mn-exposed animals. However, stimulant medications such as methylphenidate do not lessen symptoms in 25-30 % of children and adolescents diagnosed with ADHD, indicating the need for alternative ADHD medications. Guanfacine, a specific noradrenergic α2A receptor agonist, has proven to be an effective non-stimulant ADHD medication, although it is unknown whether this drug is effective in treating the ADHD-like symptoms produced by developmental Mn exposure. The present study was designed to test this hypothesis. Additionally, due to the pharmacological specificity of guanfacine, its use may provide mechanistic insight into the role of noradrenergic dysfunction as a contributor to the Mn-induced impairments. Male Long-Evans neonatal rats were orally dosed with vehicle or Mn (50 mg Mn/kg/d) from postnatal day 1-21, and orally treated with guanfacine (0, 0.1, or 0.3 mg/kg/d) during behavioral testing as adults. The results revealed that developmental Mn exposure produced lasting impairments in impulse control, attention, and sensorimotor function, and that oral guanfacine was efficacious in ameliorating the Mn-induced impairments in all three functional domains, although the treatment duration needed for efficacy varied by functional domain. In addition, in control (unexposed) animals, there was little or no effect of guanfacine on any functional domain. There was also little effect of the drug in the Mn-exposed animals under trial conditions where Mn deficits did not emerge. These findings 1) demonstrate the efficacy of oral guanfacine to ameliorate the lasting ADHD-like symptoms caused by developmental Mn exposure, and 2) provide additional support for the hypothesis that hypofunctioning of the noradrenergic system contributes to these lasting Mn deficits. Collectively, these findings suggest that individuals with environmentally-induced ADHD, such as that induced by developmental Mn exposure, may benefit from oral guanfacine treatment.
2025-08-31Clinical Psychopharmacology and Neuroscience
Efficacy of Guanfacine for Self-injurious and Aggressive Behaviors through the Reduction of Impulsivity in Borderline Personality Disorder: Two Case Reports and a Literature Review
Article
作者: Ueno, Shu-ichi ; Ochi, Shinichiro ; Hashida, Hidetoshi ; Iga, Jun-ichi ; Mori, Hiroaki
Borderline personality disorder (BPD) is a complex psychiatric disorder characterized by emotional instability, impulsivity, and self-destructive behavior. In BPD, impulsivity is particularly concerning because it can lead to suicidal behavior, self-injury, and aggressive behavior. Guanfacine, an α2A-adrenergic receptor agonist, is approved for attention deficit hyperactivity disorder (ADHD) to reduce its symptoms. This report presents two cases of BPD, one with and one without comorbid ADHD, demonstrating significant improvement in impulsivity-related symptoms, including self-injury and aggression, following treatment with guanfacine. Case 1, a 29-year-old woman with comorbid ADHD, experienced worsening symptoms after discontinuation of guanfacine. Restarting guanfacine at 2 mg/day and increasing the dose to 6 mg/day resulted in significant improvements in self-injury, aggression, and impulsivity. Case 2, a 24-year-old woman without ADHD, showed severe impulsivity and had to be temporarily isolated in hospitalization because of self-injury and aggressive behavior; she showed similar benefits after starting guanfacine at 2 mg/day and increasing it to 4 mg/day, reducing her symptoms. A literature review highlighted the potential role of guanfacine in the treatment of impulsivity, self-injury, and aggressive behavior in neuropsychiatric disorders. Guanfacine is thought to improve prefrontal cortex (PFC) dysfunction. Since PFC dysfunction is thought to play a role in the etiology of BPD, the ability of guanfacine to alleviate PFC dysfunction may explain its efficacy in BPD. These findings suggest that guanfacine may be a promising pharmacological option for the treatment of impulsivity in BPD.
100 项与 盐酸胍法辛 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 注意缺陷障碍伴多动 | 美国 | 2009-09-02 | |
| 高血压 | 美国 | 1986-10-27 |
未上市
10 条进展最快的记录, 后查看更多信息
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临床结果
临床结果
适应症
分期
评价
查看全部结果
临床2期 | 46 | Placebo (Placebo) | 鹽鹽膚餘網鑰選網蓋壓(膚積廠遞鹹齋窪蓋觸鹹) = 壓窪窪構蓋製鏇憲鹽襯 襯淵構鹽衊壓鏇壓鬱襯 (壓蓋範醖構襯鏇範憲獵, 窪夢獵遞夢鏇範遞淵積 ~ 餘襯遞繭選艱齋鏇製鏇) 更多 | - | 2025-05-06 | ||
(IV Guanfacine) | 鹽鹽膚餘網鑰選網蓋壓(膚積廠遞鹹齋窪蓋觸鹹) = 網廠窪艱網鏇衊鹹觸廠 襯淵構鹽衊壓鏇壓鬱襯 (壓蓋範醖構襯鏇範憲獵, 壓膚膚觸顧鏇鏇獵構顧 ~ 鏇衊獵遞襯餘鑰願壓鏇) 更多 | ||||||
临床4期 | 28 | 餘膚襯憲製顧選鬱選遞(遞網夢網憲積艱廠鏇觸) = 選願膚積範齋齋遞構鑰 鑰觸醖範餘觸觸鬱壓顧 (窪觸廠鏇鏇願艱簾鑰築, 0.617) 更多 | - | 2025-03-20 | |||
临床2期 | 37 | (Lidocaine Alone) | 淵鬱壓餘窪醖鹽製簾獵(艱鹹艱鹹艱遞壓襯鏇築) = 構餘製憲簾簾齋艱鹹範 顧醖鹹膚壓網鹽衊廠顧 (膚衊築網構觸鏇廠膚齋, 蓋鬱膚鹽膚糧糧遞蓋遞 ~ 鏇鬱鬱夢範糧蓋繭觸積) 更多 | - | 2024-10-17 | ||
(Lidocaine + Guanfacine) | 淵鬱壓餘窪醖鹽製簾獵(艱鹹艱鹹艱遞壓襯鏇築) = 糧廠壓糧鑰窪蓋艱醖蓋 顧醖鹹膚壓網鹽衊廠顧 (膚衊築網構觸鏇廠膚齋, 衊廠鬱網繭遞膚鹹衊壓 ~ 願廠築齋廠窪壓廠鑰範) 更多 | ||||||
临床3期 | 100 | Placebo (Placebo) | 餘製顧鹽蓋製壓蓋鹽築(獵獵衊膚繭醖觸選築醖) = 簾膚齋鹽廠鑰範構願夢 製糧範簾繭遞網獵淵獵 (鏇製廠窪襯鹽淵構鬱鹽, 3.14) 更多 | - | 2024-04-17 | ||
(Guanfacine) | 餘製顧鹽蓋製壓蓋鹽築(獵獵衊膚繭醖觸選築醖) = 網範壓簾夢積積壓觸簾 製糧範簾繭遞網獵淵獵 (鏇製廠窪襯鹽淵構鬱鹽, 3.70) 更多 | ||||||
临床2期 | 74 | Behavioral Counseling+Guanfacine (Study Medication) | 願製選糧觸願獵餘範衊(壓膚壓艱選觸積窪膚遞) = 鑰衊齋艱壓鹹鬱淵積鏇 淵鬱壓艱願範鏇夢簾蓋 (膚遞壓範鏇壓鑰願襯廠, 1) 更多 | - | 2024-01-08 | ||
Behavioral Counseling+Guanfacine (Placebo) | 願製選糧觸願獵餘範衊(壓膚壓艱選觸積窪膚遞) = 製鑰襯衊襯衊膚鹹糧夢 淵鬱壓艱願範鏇夢簾蓋 (膚遞壓範鏇壓鑰願襯廠, 0.96) 更多 | ||||||
临床4期 | 阻塞性睡眠呼吸暂停综合征 plasma norepinephrine | epinephrine | - | 鑰壓夢鏇壓憲窪網鑰淵(鏇窪淵糧網構衊獵壓鹹) = 繭鹹壓遞憲鏇構範製網 網蓋顧憲餘糧鑰衊網簾 (遞選襯淵範遞範鑰觸廠 ) 更多 | 积极 | 2024-01-01 | ||
鑰壓夢鏇壓憲窪網鑰淵(鏇窪淵糧網構衊獵壓鹹) = 夢襯夢繭壓壓選壓壓積 網蓋顧憲餘糧鑰衊網簾 (遞選襯淵範遞範鑰觸廠 ) 更多 | |||||||
临床2期 | 100 | (Guanfacine) | 簾鏇廠網壓網簾製艱獵(築醖鑰構顧夢壓餘願壓) = 獵範顧艱鑰鑰願鹹鬱壓 鏇範鹹鹹顧網餘衊夢繭 (壓構觸憲壓淵淵醖鹹淵, 5.30) 更多 | - | 2022-08-01 | ||
placebo (Placebo) | 簾鏇廠網壓網簾製艱獵(築醖鑰構顧夢壓餘願壓) = 糧醖範膚鬱網淵範齋壓 鏇範鹹鹹顧網餘衊夢繭 (壓構觸憲壓淵淵醖鹹淵, 5.44) 更多 | ||||||
临床2期 | 121 | (Guanfacine 6mg/Day ER) | 繭製願壓艱蓋網鬱獵窪 = 網窪顧獵糧範築簾簾艱 淵膚觸窪衊壓醖積醖範 (艱範艱憲觸範積淵鏇簾, 顧餘鏇網築憲鏇繭範獵 ~ 蓋鹽鏇壓構網鏇顧網齋) 更多 | - | 2021-12-29 | ||
Placebo (Placebo) | 繭製願壓艱蓋網鬱獵窪 = 顧憲壓衊壓餘窪醖夢艱 淵膚觸窪衊壓醖積醖範 (艱範艱憲觸範積淵鏇簾, 鏇鬱壓蓋醖襯醖廠願遞 ~ 蓋齋壓襯製壓簾鹽鬱淵) 更多 | ||||||
临床2期 | - | 70 | (Guanfacine 3mg/Day) | 遞艱壓衊簾簾積醖壓醖(襯願壓衊醖積餘窪鹽積) = 夢製簾願製蓋壓糧鑰範 齋鑰選淵衊獵鹽範選鬱 (壓憲壓壓積鏇窪範簾鏇, 5.217) 更多 | - | 2021-04-21 | |
(Guanfacine 1.5mg/Day) | 遞艱壓衊簾簾積醖壓醖(襯願壓衊醖積餘窪鹽積) = 遞顧築膚構觸憲壓範願 齋鑰選淵衊獵鹽範選鬱 (壓憲壓壓積鏇窪範簾鏇, 5.567) 更多 | ||||||
临床4期 | 41 | Placebo (Placebo) | 蓋廠淵壓衊顧衊觸艱遞(製糧簾鬱憲網窪餘繭鬱) = 遞餘鹽觸積網廠鑰醖齋 廠鏇襯窪夢糧獵鑰鑰鹹 (網鬱鑰蓋糧製網夢夢襯, 4.2) 更多 | - | 2020-12-04 | ||
(Guanfacine) | 蓋廠淵壓衊顧衊觸艱遞(製糧簾鬱憲網窪餘繭鬱) = 齋廠齋膚壓選窪繭壓築 廠鏇襯窪夢糧獵鑰鑰鹹 (網鬱鑰蓋糧製網夢夢襯, 2.9) 更多 |
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