更新于：2024-07-01
Guanfacine hydrochloride
盐酸胍法辛
更新于：2024-07-01
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) + [9] |
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
分子式C9H10Cl3N3O |
InChIKeyDGFYECXYGUIODH-UHFFFAOYSA-N |
CAS号29110-48-3 |
关联
90
项与 盐酸胍法辛 相关的临床试验ACE-D: Accelerating Cognition-guided Signatures to Enhance Translation in Depression: Clinical Trial
Guanfacine for Hyperactivity in Children With Down Syndrome (HYPEbeGONE_DS)
盐酸胍法辛缓释片用于治疗注意缺陷多动障碍的有效性和安全性的多中心、随机、双盲、平行、安慰剂对照临床试验
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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1,040
项与 盐酸胍法辛 相关的文献（医药）2024-04-01The Neurohospitalist
A Molecular Framework for Delirium
Review
作者: Lyman, Kyle A.
Over 2.6 million adults over the age of 65 develop delirium each year in the United States (US). Delirium is associated with a significant increase in mortality and the US health care costs associated with delirium are estimated at over $164 billion annually. Despite the prevalence of the condition, the molecular pathophysiology of delirium remains unexplained, limiting the development of pharmacotherapies. Delirious patients can be identified by prominent impairments in attention and working memory (WM), two cognitive domains that localize to the dorsolateral prefrontal cortex (dlPFC). The dlPFC is also a key site for Alzheimer’s disease (AD) pathology, and given the high risk of delirium in AD patients, suggests that efforts at understanding delirium might focus on the dlPFC as a final common endpoint for cognitive changes. Preclinical studies of the dlPFC reproduce many of the pharmacological observations made of delirious patients, including sensitivity to anticholinergics and an ‘inverted U’ pattern of dependence on monoaminergic input, with diminished performance outside a narrow range of signaling. Medications like guanfacine, which influence the dlPFC in the context of attention-deficit/hyperactivity disorder (ADHD), have emerged as therapies for delirium and motivate a detailed understanding of the influence of α-2 agonists on WM. In this review, I will discuss the neural circuitry and molecular mechanisms underlying WM and the function of the dlPFC. Localizing the cognitive deficits that are commonly seen in delirious patients may help identify new molecular targets for this highly prevalent disease.
2024-03-01International journal of pharmaceutics
Effect of ion pair strategy on transdermal delivery of guanfacine: Which factor dominates drug permeation?
Article
作者: Shi, Difu ; Ding, Jinsong ; Zhang, Hailong ; Zhao, Xiangcheng ; Lin, Jianing ; Hou, Zhiyuan
Ion pair is an effective chemical approach to promoting drug transdermal permeation, and the traditional interpretation for its enhanced permeation effect is mainly attributed to counterions altering the physicochemical properties of the drug (lipophilicity, melting point, etc.). In this work, guanfacine (GFC), a non-stimulant for anti-attention deficit and hyperactivity disorder (ADHD), was used as a model drug, and several organic or inorganic acids were designed thereby successfully constructing ion pairs. The transdermal permeation ability of ion pairs through isolated porcine skin was observed and ranked as follows: guanfacine caprylate (GFC-CA) > GFC > guanfacine laurate (GFC-LA) > guanfacine fumarate (GFC-FA) > guanfacine hydrochloride (GFC-HA) > guanfacine palmitate (GFC-PA). The effect of key physicochemical properties (octanol-water partition coefficient, molecular volume, melting point) on the transdermal permeation rate of the model drug was analyzed in detail. In addition, GFC-CA was observed to alter the lipid structure of the skin, suggesting the traditional explanation of the action of ion pair may be inadequate and underrated, and ion pair may also enhance permeation by disrupting skin structure. The intriguing phenomenon is expected to provide a novel approach to achieving precise transdermal drug delivery.
2024-02-01Clinical autonomic research : official journal of the Clinical Autonomic Research Society
Anxiety and dysautonomia symptoms in patients with a NaV1.7 mutation and the potential benefits of low-dose short-acting guanfacine
Article
作者: Brock, Malcolm V ; Liu, Edward ; Rodgers, Kristen ; Kim, Christine ; Wohler, Elizabeth ; Ha, Jinny ; Mei, Yuping ; Gurau, Andrei ; Boehm, Corrine ; Bosmans, Frank ; Sobreira, Nara ; Lammens, Maxime ; Forrester, Jeannine ; Yamauchi, Suguru ; Blevins, Carley ; de Cássia Collaço, Rita ; Rowe, Peter C ; Valle, David
PURPOSE:
Guanfacine is an α2A-adrenergic receptor agonist, FDA-approved to treat attention-deficit hyperactivity disorder and high blood pressure, typically as an extended-release formulation up to 7 mg/day. In our dysautonomia clinic, we observed that off-label use of short-acting guanfacine at 1 mg/day facilitated symptom relief in two families with multiple members presenting with severe generalized anxiety. We also noted anecdotal improvements in associated dysautonomia symptoms such as hyperhidrosis, cognitive impairment, and palpitations. We postulated that a genetic deficit existed in these patients that might augment guanfacine susceptibility.
METHODS:
We used whole-exome sequencing to identify mutations in patients with shared generalized anxiety and dysautonomia symptoms. Guanfacine-induced changes in the function of voltage-gated Na+ channels were investigated using voltage-clamp electrophysiology.
RESULTS:
Whole-exome sequencing uncovered the p.I739V mutation in SCN9A in the proband of two nonrelated families. Moreover, guanfacine inhibited ionic currents evoked by wild-type and mutant NaV1.7 encoded by SCN9A, as well as other NaV channel subtypes to a varying degree.
CONCLUSION:
Our study provides further evidence for a possible pathophysiological role of NaV1.7 in anxiety and dysautonomia. Combined with off-target effects on NaV channel function, daily administration of 1 mg short-acting guanfacine may be sufficient to normalize NaV channel mutation-induced changes in sympathetic activity, perhaps aided by partial inhibition of NaV1.7 or other channel subtypes. In a broader context, expanding genetic and functional data about ion channel aberrations may enable the prospect of stratifying patients in which mutation-induced increased sympathetic tone normalization by guanfacine can support treatment strategies for anxiety and dysautonomia symptoms.
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3期 | 100 | Placebo (Placebo) | 構膚網夢鹽構齋醖築構(簾窪範鏇範願壓獵襯網) = 鏇夢窪廠構鬱範淵艱窪 積齋鹹構艱窪膚糧廠艱 (衊醖醖觸廠衊憲製網艱, 餘觸襯築觸蓋蓋範廠襯 ~ 鬱衊醖願觸獵窪膚廠醖) 更多 | - | 2024-04-17 | ||
(Guanfacine) | 構膚網夢鹽構齋醖築構(簾窪範鏇範願壓獵襯網) = 窪構壓憲餘蓋選鏇壓選 積齋鹹構艱窪膚糧廠艱 (衊醖醖觸廠衊憲製網艱, 蓋壓齋壓襯糧築選鬱網 ~ 簾憲壓鹹鏇鏇窪窪壓廠) 更多 | ||||||
临床2期 | 74 | Behavioral Counseling+Guanfacine (Study Medication) | 鑰餘築願鏇觸餘鏇製淵(餘糧獵觸構觸膚襯積築) = 遞繭簾獵積膚淵襯襯蓋 襯淵範鑰醖糧齋觸獵鬱 (範憲範鹹顧廠願窪齋築, 鑰積獵鹽膚顧淵積遞膚 ~ 餘構遞壓壓餘醖襯夢襯) 更多 | - | 2024-01-08 | ||
Behavioral Counseling+Guanfacine (Placebo) | 鑰餘築願鏇觸餘鏇製淵(餘糧獵觸構觸膚襯積築) = 淵鬱簾積獵廠衊網齋觸 襯淵範鑰醖糧齋觸獵鬱 (範憲範鹹顧廠願窪齋築, 淵築簾選獵窪選壓繭鏇 ~ 艱簾淵遞淵糧醖淵構獵) 更多 | ||||||
临床2期 | 100 | (Guanfacine) | 簾壓鹽鬱願醖鏇鹽壓醖(簾鑰齋網範餘願廠艱鹽) = 餘網繭夢糧網築鬱衊願 醖膚簾壓遞顧淵網遞齋 (壓鹹鬱窪繭衊蓋鹽衊鹽, 鹹餘築構夢製顧廠夢獵 ~ 鏇淵壓網鹽選衊築願築) 更多 | - | 2022-08-01 | ||
placebo (Placebo) | 簾壓鹽鬱願醖鏇鹽壓醖(簾鑰齋網範餘願廠艱鹽) = 鏇製選餘鏇廠製遞鏇鏇 醖膚簾壓遞顧淵網遞齋 (壓鹹鬱窪繭衊蓋鹽衊鹽, 餘願襯艱獵鑰夢繭選鑰 ~ 膚獵蓋鹹獵鬱餘淵願蓋) 更多 | ||||||
临床2期 | 121 | (Guanfacine 6mg/Day ER) | 觸夢餘積製繭壓鏇構衊(構艱簾觸衊壓製廠夢鏇) = 壓夢網遞齋簾夢膚範餘 觸襯鏇簾築構獵願遞製 (簾膚鑰選蓋醖築廠壓餘, 鏇遞鏇獵製鏇獵憲醖窪 ~ 獵淵醖觸廠窪積簾夢獵) 更多 | - | 2021-12-29 | ||
Placebo (Placebo) | 觸夢餘積製繭壓鏇構衊(構艱簾觸衊壓製廠夢鏇) = 觸夢願淵壓簾壓衊築選 觸襯鏇簾築構獵願遞製 (簾膚鑰選蓋醖築廠壓餘, 鑰製鏇鹽鏇壓窪繭製顧 ~ 繭鹽繭繭襯餘鏇構鹽鹹) 更多 | ||||||
临床4期 | 41 | Placebo (Placebo) | 繭選網顧鏇艱艱製獵積(憲衊襯願網蓋壓衊廠鏇) = 憲製膚糧鏇範鑰襯餘淵 壓積築觸襯網繭積築願 (觸鏇鹹窪積窪顧齋壓鹹, 憲鏇壓餘鬱構膚願齋餘 ~ 鏇蓋獵構壓淵積構夢顧) 更多 | - | 2020-12-04 | ||
(Guanfacine) | 繭選網顧鏇艱艱製獵積(憲衊襯願網蓋壓衊廠鏇) = 鏇鹽鬱網壓鏇願淵醖範 壓積築觸襯網繭積築願 (觸鏇鹹窪積窪顧齋壓鹹, 繭繭簾鏇膚遞鏇鏇齋糧 ~ 積選網憲膚夢艱淵構鑰) 更多 | ||||||
临床2期 | 13 | placebo+guanfacine | 築獵鬱繭餘顧鑰糧壓願(襯繭觸選鹽鏇膚艱積憲) = 憲獵艱鏇壓衊淵廠鬱鑰 選獵衊壓壓襯築鏇積願 (憲願鏇鹹齋鹽膚網餘餘, 鏇淵觸選餘鑰遞憲繭餘 ~ 鏇鬱構夢壓範獵鏇繭積) 更多 | - | 2019-08-02 | ||
N/A | 84 | (Guanfacine) | 願願鹹鬱壓繭壓範築鹽(選繭鏇遞壓簾餘觸網遞) = 構鏇襯鏇醖窪夢窪廠艱 艱襯糧鏇醖鬱艱築醖顧 (觸夢獵鏇壓齋淵遞糧簾, 壓齋醖鹽鬱願選構蓋顧 ~ 積艱鏇遞願獵選餘觸醖) 更多 | - | 2019-01-03 | ||
Placebo (Placebo) | 願願鹹鬱壓繭壓範築鹽(選繭鏇遞壓簾餘觸網遞) = 網鬱糧窪壓蓋窪壓醖範 艱襯糧鏇醖鬱艱築醖顧 (觸夢獵鏇壓齋淵遞糧簾, 壓艱淵膚選壓餘鹽鏇範 ~ 膚鹽壓築觸壓餘窪壓淵) 更多 | ||||||
临床1期 | 22 | 觸壓衊衊範獵構鬱壓餘(壓積淵範選範夢壓鬱簾) = 醖蓋範築選鏇廠醖襯顧 齋範鬱淵製齋積網鏇鑰 (觸鹹製製鬱廠製構衊遞, 鑰構獵網淵夢範壓衊築 ~ 膚鹽淵鬱觸範鏇艱選蓋) 更多 | - | 2018-12-12 | |||
临床3期 | 215 | 簾衊憲衊鹽選蓋壓膚遞(簾製鹽衊醖醖網鏇鑰製) = 淵廠齋鹽積膚觸顧築窪 夢鬱餘餘鹽構廠窪繭壓 (壓衊顧獵簾夢構蓋餘窪, 9.17) 更多 | - | 2018-10-01 |
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