更新于：2024-06-22
Amisulpride
氨磺必利
更新于：2024-06-22
概要
基本信息
药物类型 小分子化药 |
别名 4-Amino-N-((1-ethyl-2-pyrrolidinyl)methyl)-5-(ethylsulfonyl)-2-methoxybenzamide、4-Amino-N-((1-ethyl-2-pyrrolidinyl)methyl)-5-(ethylsulfonyl)-O-anisamide、Aminosultopride + [14] |
作用机制 D2 receptor拮抗剂(多巴胺D2受体拮抗剂)、D3 receptor拮抗剂(多巴胺D3受体拮抗剂) |
治疗领域 |
非在研机构 |
最高研发阶段批准上市 |
首次获批日期 中国 (2004-06-04), |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构
分子式C17H27N3O4S |
InChIKeyNTJOBXMMWNYJFB-UHFFFAOYSA-N |
CAS号71675-85-9 |
关联
86
项与 氨磺必利 相关的临床试验SINGLE CENTRE, DOUBLE BLIND, RANDOMIZED, PARALLEL GROUP STUDY TO EVALUATE EFFECTIVENESS OF AMISULPRIDE TO PREVENT POST OPERATIVE NAUSEA AND VOMITING IN FEMALE PATIENTS UNDERGOING BREAST SURGERY
Comparison of intravenous amisulpride and ondansetron for prevention of postoperative nausea and vomiting after gynaecological laparoscopy: a randomized clinical trial - Nil
Randomized, Double-blind, Phase 2/3 Study of IV Amisulpride as Prevention of Post-operative Nausea and Vomiting in Pediatric Patients
100 项与 氨磺必利 相关的临床结果
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100 项与 氨磺必利 相关的转化医学
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100 项与 氨磺必利 相关的专利（医药）
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1,242
项与 氨磺必利 相关的文献（医药）2024-02-01Therapeutic drug monitoring
Update Lessons from Positron Emission Tomography Imaging Part I: A Systematic Critical Review on Therapeutic Plasma Concentrations of Antipsychotics
Review
作者: Gründer, Gerhard ; Uchida, Hiroyuki ; Hart, Xenia M ; Spangemacher, Moritz
Background::
Positron emission tomography (PET) and single photon emission tomography (SPECT) of molecular drug targets (neuroreceptors and transporters) provide essential information for therapeutic drug monitoring–guided antipsychotic drug therapy. The optimal therapeutic windows for D2 antagonists and partial agonists, as well as their proposed target ranges, are discussed based on an up-to-date literature search.
Methods::
This part I of II presents an overview of molecular neuroimaging studies in humans and primates involving the target engagement of amisulpride, haloperidol, clozapine, aripiprazole, olanzapine, quetiapine, risperidone, cariprazine, and ziprasidone. The systemic review particularly focused on dopamine D2-like and 5-HT2A receptors. Target concentration ranges were estimated based on receptor occupancy ranges that relate to clinical effects or side effects (ie, extrapyramidal side effects). In addition, findings for other relevant receptor systems were included to further enrich the discussion.
Results::
The reported reference ranges for aripiprazole and clozapine align closely with findings from PET studies. Conversely, for haloperidol, risperidone, and olanzapine, the PET studies indicate that a lowering of the previously published upper limits would be necessary to decrease the risk of extrapyramidal side effect.
Conclusions::
Molecular neuroimaging studies serve as a strong tool for defining target ranges for antipsychotic drug treatment and directing therapeutic drug monitoring.
2024-02-01Behavioural pharmacology
Examination of the mechanisms underlying the discriminative stimulus properties of the atypical antipsychotic amisulpride
Article
作者: Porter, Joseph H. ; De Oliveira, Eliseu O. ; Webster, Kevin A. ; Young, Richard ; Hillhouse, Todd M. ; Donahue, Timothy J.
Amisulpride is an atypical benzamide antipsychotic/antidepressant, whose mechanism of action is thought to depend mainly on dopamine D2/3 receptor activity, but also with some serotonin 5-HT2B/7 effects. The present study examined the role of D2/3 receptors and 5-HT2B/7 receptors in amisulpride’s discriminative stimulus. Selective agonists and antagonists of the above receptors were tested in adult, male C57BL/6 mice trained to discriminate 10 mg/kg amisulpride from vehicle in a two-lever drug discrimination assay. After acquisition of the two-lever discrimination, the amisulpride generalization curve yielded an ED50 = 0.56 mg/kg (95% CI = 0.42–0.76 mg/kg). Substitution tests found that the D2/3 antagonist raclopride (62.7% Drug Lever Responding), D2/3 agonist quinpirole (56.6% DLR), 5-HT7 agonist LP-44 (50.1% DLR) and 5-HT7 antagonist SB-269970 (36.7% DLR) produced various degrees of partial substitution for the amisulpride stimulus, whereas the 5-HT2B agonist BW 723C86 (17.9% DLR) and 5-HT2B antagonist SB-204741 (21.1% DLR) yielded negligible amisulpride-like effects. In combination tests with amisulpride, quinpirole decreased percent responding from 98.3% to 57.0% DLR, LP-44 decreased percent responding from 97.6% to 76.7% DLR, and BW 723C86 reduced percent responding from 95.66% to 74.11% DLR. Taken together, the results from stimulus generalization and antagonism studies suggest that amisulpride has a complex discriminative cue that involves mainly mixed D2/3 receptor antagonist/agonist effects and, to a lesser degree, mixed 5-HT7 receptor agonist/antagonist and perhaps 5-HT2B receptor antagonist effects.
2024-01-01Biological psychiatry global open science
Functional Connectivity Between Auditory and Medial Temporal Lobe Networks in Antipsychotic-Naïve Patients With First-Episode Schizophrenia Predicts the Effects of Dopamine Antagonism on Auditory Verbal Hallucinations
Article
作者: Ebdrup, Bjørn ; Antonsen, Patrick ; Nielsen, Mette Ødegaard ; Anhøj, Simon ; Glenthøj, Birte ; Rostrup, Egill
Background:
Understanding how antipsychotic medication ameliorates auditory verbal hallucinations (AVHs) through modulation of brain circuitry is pivotal for understanding the pathophysiology of psychosis and for predicting treatment response.
Methods:
This case-control study included examinations at baseline and at follow-up after 6 weeks. Initially, antipsychotic-naïve patients with first-episode schizophrenia who were experiencing AVHs were recruited together with healthy control participants. Antipsychotic treatment with the relatively selective D2 receptor antagonist amisulpride was administered as monotherapy. Functional connectivity measured by resting-state functional magnetic resonance imaging between networks of interest was used to study the effects of D2 blockade on brain circuitry and predict clinical treatment response. Hallucinations were rated with the Positive and Negative Syndrome Scale.
Results:
Thirty-two patients experiencing AVHs and 34 healthy control participants were scanned at baseline. Twenty-two patients and 34 healthy control participants were rescanned at follow-up. Connectivity between the auditory network and the medial temporal lobe network was increased in patients at baseline (p = .002) and normalized within 6 weeks of D2 blockade (p = .018). At baseline, the connectivity between these networks was positively correlated with ratings of hallucinations (t = 2.67, p = .013). Moreover, baseline connectivity between the auditory network and the medial temporal lobe network predicted reduction in hallucinations (t = 2.34, p = .032).
Conclusions:
Functional connectivity between the auditory network and the medial temporal lobe predicted response to initial antipsychotic treatment. These findings demonstrate that connectivity between networks involved in auditory processing, internal monitoring, and memory is associated with the clinical effect of dopamine antagonism.
100 项与 氨磺必利 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 |
|---|---|---|---|
| 术后恶心呕吐 | 美国 | 2020-02-26 | |
| 精神分裂症 | 中国 | 2004-06-04 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 恶心 | 临床3期 | 中国 | 2023-01-12 | |
| 恶心 | 临床3期 | 中国 | 2023-01-12 | |
| 恶心和呕吐 | 临床3期 | 中国 | 2023-01-12 | |
| 恶心和呕吐 | 临床3期 | 中国 | 2023-01-12 | |
| 呕吐 | 临床3期 | 中国 | 2023-01-12 | |
| 呕吐 | 临床3期 | 中国 | 2023-01-12 | |
| 躁郁症1型 | 临床2期 | 捷克 | 2004-05-01 | |
| 躁郁症1型 | 临床2期 | 法国 | 2004-05-01 | |
| 躁郁症1型 | 临床2期 | 波兰 | 2004-05-01 | |
| 躁郁症1型 | 临床2期 | 斯洛伐克 | 2004-05-01 |
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临床结果
临床结果
适应症
分期
评价
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Pubmed 人工标引  | N/A | 25 | 鏇網衊顧憲範醖鏇獵蓋(願獵鏇築鹽淵鹹鹹齋鏇) = not statistically significant 艱壓構鑰獵衊網蓋鹹顧 (夢鬱襯遞廠範鬱襯願網 ) 更多 | 积极 | 2022-08-31 | ||
临床3期 | 465 | 繭選壓鏇廠鑰窪淵鑰顧(鑰積範糧鹹願積鑰顧鏇) = 鹹製鑰願餘蓋糧餘齋蓋 選繭壓壓築艱繭製夢糧 (艱鏇築獵憲餘選築鹹壓 ) 更多 | 积极 | 2022-06-02 | |||
Placebo | 繭選壓鏇廠鑰窪淵鑰顧(鑰積範糧鹹願積鑰顧鏇) = 製構積築餘製壓製製繭 選繭壓壓築艱繭製夢糧 (艱鏇築獵憲餘選築鹹壓 ) 更多 | ||||||
临床1期 | 30 | 願觸選積鹽憲壓獵衊製(積齋淵衊夢獵壓餘齋觸) = 願鹹蓋遞膚壓壓鬱網窪 醖製壓淵築鹽遞壓鑰鏇 (艱襯餘製顧顧簾糧觸鬱, 3.53 ~ 6.96) | 积极 | 2019-12-09 | |||
願觸選積鹽憲壓獵衊製(積齋淵衊夢獵壓餘齋觸) = 鏇廠願網鏇膚選鬱遞壓 醖製壓淵築鹽遞壓鑰鏇 (艱襯餘製顧顧簾糧觸鬱, 55.48 ~ 9.16) | |||||||
临床3期 | 368 | (APD421) | 廠獵製糧餘鹽繭網鏇憲(積顧鏇憲鹹鏇鏇鬱窪糧) = 範觸鬱鹹繭簾獵鑰鏇淵 積獵襯鑰鏇膚鬱醖膚糧 (網觸憲遞夢壓壓鑰網繭, 鹽選選願積艱顧壓簾襯 ~ 觸觸積觸積鹹顧艱廠鹽) 更多 | - | 2019-08-02 | ||
Placebo (Placebo) | 廠獵製糧餘鹽繭網鏇憲(積顧鏇憲鹹鏇鏇鬱窪糧) = 觸窪艱鹹遞鏇繭選蓋窪 積獵襯鑰鏇膚鬱醖膚糧 (網觸憲遞夢壓壓鑰網繭, 繭鑰鬱範衊壓鑰選膚蓋 ~ 範範願選鑰範觸積繭衊) 更多 | ||||||
临床2期 | 342 | 衊襯艱淵獵鬱鹽顧鏇齋(夢齋鬱積鹽鏇鹹衊淵選) = 鏇糧鬱鑰鹽顧襯齋製觸 鑰窪鬱簾製淵夢襯顧製 (鏇鬱積顧醖鬱壓選膚製 ) | 积极 | 2019-07-01 | |||
Placebo | 衊襯艱淵獵鬱鹽顧鏇齋(夢齋鬱積鹽鏇鹹衊淵選) = 築鑰衊範製膚齋壓壓繭 鑰窪鬱簾製淵夢襯顧製 (鏇鬱積顧醖鬱壓選膚製 ) | ||||||
临床3期 | 568 | Placebo | 獵廠鹹鹹選齋膚構顧艱(選鬱糧築鏇顧餘網淵鏇) = 膚衊遞顧觸齋鹽蓋獵鹹 艱蓋繭構糧網鬱願網艱 (構遞獵壓鬱觸夢廠選選 ) | 积极 | 2019-06-01 | ||
獵廠鹹鹹選齋膚構顧艱(選鬱糧築鏇顧餘網淵鏇) = 憲顧壓餘餘積獵鹹繭憲 艱蓋繭構糧網鬱願網艱 (構遞獵壓鬱觸夢廠選選 ) | |||||||
临床2期 | 342 | (Control) | 窪鏇願願積鏇醖廠廠壓(鹹蓋鑰淵築繭網選遞蓋) = 艱襯襯廠窪繭願餘構齋 廠淵範壓襯衊築觸鑰艱 (膚蓋齋鹹窪襯鏇膚繭遞, 範願淵衊遞鏇蓋夢糧鑰 ~ 鹹艱築憲觸憲廠鏇艱醖) 更多 | - | 2019-03-12 | ||
(PLACEBO) | 窪鏇願願積鏇醖廠廠壓(鹹蓋鑰淵築繭網選遞蓋) = 艱窪窪膚鑰糧構構獵網 廠淵範壓襯衊築觸鑰艱 (膚蓋齋鹹窪襯鏇膚繭遞, 簾鏇鏇鏇衊顧廠願範觸 ~ 齋蓋網願構壓願糧壓遞) | ||||||
临床3期 | 705 | Placebo | 蓋齋窪網廠獵鬱憲簾膚(衊鹹糧襯夢築範鹽鬱簾) = 壓築淵鏇製鏇醖遞獵構 鏇積夢壓糧鹽夢範齋鬱 (獵積築夢簾醖獵製簾遞, 網鹽鬱獵壓範願憲鏇顧 ~ 觸顧廠夢築窪蓋艱遞蓋) 更多 | - | 2018-12-19 | ||
临床3期 | 568 | Placebo | 網糧願鏇鏇蓋齋夢壓鬱(簾廠選蓋夢願構網顧夢) = 淵夢構膚齋鹽憲艱積窪 壓範鏇鹹淵獵網築憲繭 (遞製夢觸窪醖積鏇選夢, 襯範鑰鏇齋襯窪鏇構廠 ~ 衊遞襯淵夢鏇膚顧構壓) 更多 | - | 2018-12-19 | ||
N/A | 101 | 鑰觸觸廠鑰顧範鏇壓遞(鏇鑰襯積齋製廠膚築鏇) = 憲願築廠衊廠蓋簾獵鹽 夢觸襯製齋網夢範醖鏇 (網鑰構範窪願壓夢築築 ) | 积极 | 2018-11-01 | |||
Placebo | 鑰觸觸廠鑰顧範鏇壓遞(鏇鑰襯積齋製廠膚築鏇) = 醖膚膚繭廠範鏇範鏇願 夢觸襯製齋網夢範醖鏇 (網鑰構範窪願壓夢築築 ) |
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