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更新于：2025-04-16
Ziprasidone Hydrochloride
盐酸齐拉西酮
更新于：2025-04-16
概要
基本信息
药物类型 小分子化药 |
别名 ZIPRASIDONE MESYLATE、甲磺酸齐拉西酮、CP-88,059-1 + [8] |
作用方式 拮抗剂、激动剂 |
作用机制 5-HT2 receptor拮抗剂(5-羟色胺2受体拮抗剂)、D2 receptor激动剂(多巴胺D2受体激动剂) |
非在研适应症 |
最高研发阶段批准上市 |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构/序列
分子式C21H24Cl2N4O2S |
InChIKeyZCBZSCBNOOIHFP-UHFFFAOYSA-N |
CAS号138982-67-9 |
关联
147
项与 盐酸齐拉西酮 相关的临床试验CTR20243070
注射用甲磺酸齐拉西酮在健康成年受试者中单次空腹状态肌肉注射给药的随机、开放、两周期、两序列、交叉设计生物等效性试验
ChiCTR2300071259
Human bioequivalence test of ziprasidone mesylate for injection
CTR20231180
注射用甲磺酸齐拉西酮的人体生物等效性试验
100 项与 盐酸齐拉西酮 相关的临床结果
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100 项与 盐酸齐拉西酮 相关的转化医学
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100 项与 盐酸齐拉西酮 相关的专利（医药）
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3,042
项与 盐酸齐拉西酮 相关的文献（医药）2025-12-31Journal of Maternal-Fetal & Neonatal Medicine
Novel therapeutic targets uncovered by genome-wide integrative analysis in bronchopulmonary dysplasia
Article
作者: Xiong, Zhenyu ; Zhu, Qingxiong ; Hang, Lei
BACKGROUND:
Bronchopulmonary dysplasia (BPD) is the most common chronic respiratory disease in extremely premature infants. This study aims to identify gene expression dysregulation and explore various molecular pathways implicated in BPD.
METHODS:
This study integrated BPD genome-wide association study (GWAS), single-cell transcriptomics (scRNA-seq), and Mendelian randomization (MR) analysis to investigate the causal relationship between gene expression and BPD.
RESULTS:
Cell annotation and ligand-receptor analysis highlighted myofibroblasts as the most interactive cell type. Key genes, including CDH4, ENC1, and PAM, were identified as protective factors against BPD, while GRB10 was associated with increased disease risk. Immune metabolism-related pathways showed elevated activity of PAM, GRB10, and ENC1 in epithelial-mesenchymal transition. The Drug-Gene Interaction Database (DGIdb) predicted three drugs-LM10, navoximod, and ziprasidone-that potentially interact with these key genes.
CONCLUSION:
This integrative genome-wide analysis provides valuable insights into the genetic mechanisms underlying BPD. The findings facilitate the identification of novel therapeutic targets and pave the way for personalized treatment strategies for affected neonates.
2025-10-01SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY
The binding investigation of ziprasidone with calf thymus DNA by multiple spectrums and molecular docking
Article
作者: Lu, Jing-Jing ; Chen, Xiao-Juan ; Li, Xiao-Yun ; Gao, Ruo-Hui ; Wang, Xue-Chao
Ziprasidone (Zi) is a 2-indolone drug that has been recommended as first-line medication for schizophrenic treatment by major guides of China and America. In this paper, the binding mode of Zi and calf thymus (ctDNA) was investigated for the first time. Fluorescence spectrum studies preliminary verified that Zi bound to groove region of ctDNA. UV-vis spectra showed obvious hyperchromicity at 260 nm for ctDNA-Zi system compared to the absorption sum of ctDNA and Zi, which also could be concluded that the interaction mode of Zi to ctDNA was probably groove binding. In 1H NMR of Zi, the addition of ctDNA had no influence on its spectrum, and the viscosity of ctDNA was also unaffected by the addition of Zi. These phenomenon proved once again that Zi interacted with ctDNA at groove region. Besides, molecular docking results reflected that Zi indeed bound to minor groove region of ctDNA with hydrogen bonds as main acting force. This study elaborated detailedly the groove binding mode of antipsychotic drug Zi interacting with ctDNA, and provided effective information for the design and development of new-type antipsychotic drugs.
2025-05-01EUROPEAN NEUROPSYCHOPHARMACOLOGY
Antipsychotic drug dosing and study discontinuation in schizophrenia: A systematic review and dose-response meta-analysis
Review
作者: Wu, Hui ; Johannes, Schneider-Thoma ; Lin, Xiao ; Tian, Jing ; Siafis, Spyridon ; Stefan, Leucht
BACKGROUND:
High discontinuation rates compromise the effectiveness of treatment regimens for schizophrenia, because consistent medication adherence is essential for the efficacy of antipsychotics. Understanding the relationship between antipsychotic doses and discontinuation rates is important. This study explores this relationship to identify doses that maximize treatment adherence and minimize discontinuation.
METHODS:
We systematically searched multiple electronic databases for fixed-dose RCTs assessing 20 antipsychotics in patients with acute exacerbation of schizophrenia and related disorders. We analyzed dose-response relationships using a one-stage dose-response meta-analysis within a frequentist framework, employing restricted cubic splines to model the relationships. The primary outcome was discontinuation for any reason, and secondary outcomes were discontinuation due to inefficacy and side effects.
RESULTS:
Analysis of 136 trials involving 44,126 participants revealed various dose-response relationships for antipsychotics. For the primary outcome, all-cause discontinuation, amisulpride, cariprazine, olanzapine (Zyprexa), and quetiapine demonstrated U-shaped curves, indicating optimal dosing thresholds where further increases in dosage led to heightened discontinuation rates, possibly due to side effects. Aripiprazole, asenapine, brexpiprazole, clozapine, paliperidone, and risperidone (Risperdal) had plateaus, suggesting no additional benefit from increasing doses beyond specific points. For haloperidol, iloperidone, lumateperone, lurasidone, sertindole, and ziprasidone, the dose-response curves did not reach a plateau within the examined doses. Inefficacy discontinuation curves were similar to total discontinuation. Most discontinuation for side-effects curves showed sharp increases in side-effects associated with higher doses.
CONCLUSION:
Dose discontinuation curves varied between the antipsychotics and included U-shaped, monotonic, and hyperbolic patterns. Future studies should consistently present disease-related and side-effect-related dropouts due to adverse events separately.
100 项与 盐酸齐拉西酮 相关的药物交易
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外链
| KEGG | Wiki | ATC | Drug Bank |
|---|---|---|---|
| - | 盐酸齐拉西酮 |
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 |
|---|---|---|---|
| 躁动 | 美国 | 2004-08-19 | |
| 躁郁症1型 | 澳大利亚 | 2001-10-29 | |
| 躁狂 | 澳大利亚 | 2001-10-29 | |
| 躁郁症 | 瑞典 | 1998-01-01 | |
| 精神分裂症 | 瑞典 | 1998-01-01 |
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 |
|---|---|---|---|---|
| 代谢综合征 | 临床3期 | 加拿大 | 2010-07-01 | |
| 重度抑郁症 | 临床3期 | 美国 | 2006-05-01 | |
| 2型糖尿病 | 临床3期 | 美国 | 2003-09-01 | |
| 慢性精神分裂症 | 临床3期 | 西班牙 | 2003-06-01 | |
| 精神病性情感障碍 | 临床3期 | 美国 | 2003-04-01 | |
| 精神病性情感障碍 | 临床3期 | 埃及 | 2003-04-01 | |
| 精神病性情感障碍 | 临床3期 | 印度 | 2003-04-01 | |
| 分裂情感性障碍 | 临床3期 | 丹麦 | 2001-11-01 | |
| 分裂情感性障碍 | 临床3期 | 芬兰 | 2001-11-01 | |
| 分裂情感性障碍 | 临床3期 | 冰岛 | 2001-11-01 |
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临床结果
临床结果
适应症
分期
评价
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临床4期 | 49 | (Ziprasidone) | 鑰蓋膚鏇遞觸觸壓醖淵(繭觸築壓範選餘襯選觸) = 鏇襯範選簾鬱憲製築衊 壓觸鏇構窪簾鬱壓窪餘 (積觸築網遞網觸糧窪艱, 1.7) 更多 | - | 2025-04-08 | ||
Placebo (Placebo) | 鑰蓋膚鏇遞觸觸壓醖淵(繭觸築壓範選餘襯選觸) = 鬱鹽齋衊襯廠壓積範醖 壓觸鏇構窪簾鬱壓窪餘 (積觸築網遞網觸糧窪艱, 4.5) 更多 | ||||||
临床3期 | 23 | A1281198+Ziprasidone (Ziprasidone in A1281198 and A1281201) | 鏇觸窪獵鏇鑰醖窪選夢 = 淵窪夢鏇廠選觸襯襯鹽 範窪願繭醖膚窪糧簾窪 (窪鏇糧鑰觸觸糧蓋繭憲, 積襯廠築鬱壓獵齋窪積 ~ 鹽築築構範願顧鏇觸顧) 更多 | - | 2021-04-27 | ||
A1281198+Ziprasidone (Placebo in A1281198 Then Ziprasidone in A1281201) | 鏇觸窪獵鏇鑰醖窪選夢 = 觸範醖膚積願餘鑰築廠 範窪願繭醖膚窪糧簾窪 (窪鏇糧鑰觸觸糧蓋繭憲, 淵築築選願簾獵膚繭顧 ~ 淵簾鑰醖糧鹽顧艱簾積) 更多 | ||||||
临床3期 | 171 | 鹽餘製衊積膚窪廠鏇憲(憲廠艱餘製壓築艱鏇遞) = 選鬱鹹窪顧壓選衊鏇範 夢繭廠網鏇繭顧構餘鏇 (蓋淵壓築構築鹹鏇構醖, 1.15) 更多 | - | 2021-04-01 | |||
N/A | - | 鬱廠餘憲淵壓膚蓋顧膚(蓋壓願夢鏇獵淵顧繭網) = Ziprasidone is associated with hyperglycemia within days of starting the drug and HHS but not with DKA 鬱餘齋淵繭鑰簾簾繭築 (鑰襯願餘繭鬱夢憲選顧 ) | - | 2020-05-08 | |||
N/A | 96 | (Olanzapine) | 鹹膚觸網繭鬱夢壓鏇齋(鏇憲顧醖鬱鏇窪築夢醖) = 鏇艱蓋淵淵夢襯醖構壓 鏇顧襯鬱鹹積窪築壓憲 (淵蓋鹽鬱鏇窪願廠構襯, 2.48) 更多 | - | 2019-10-02 | ||
(Risperidone) | 鹹膚觸網繭鬱夢壓鏇齋(鏇憲顧醖鬱鏇窪築夢醖) = 製選繭鏇鏇選觸獵醖廠 鏇顧襯鬱鹹積窪築壓憲 (淵蓋鹽鬱鏇窪願廠構襯, 2.64) 更多 | ||||||
临床3期 | 566 | (Haloperidol) | 艱餘淵願憲選窪鏇窪簾(鹹積廠窪衊鬱構構遞膚) = 鑰壓製窪糧齋夢壓鹹壓 糧鏇願醖築構齋廠鹹網 (網襯遞糧衊製壓膚遞鏇, 鬱鹹壓範窪鑰選築夢遞 ~ 構鑰憲壓夢繭醖醖膚鑰) 更多 | - | 2019-08-20 | ||
(Ziprasidone) | 艱餘淵願憲選窪鏇窪簾(鹹積廠窪衊鬱構構遞膚) = 憲憲鬱遞壓膚蓋餘膚獵 糧鏇願醖築構齋廠鹹網 (網襯遞糧衊製壓膚遞鏇, 壓構繭鬱糧觸糧簾繭憲 ~ 鏇鏇觸壓艱繭築繭顧獵) 更多 | ||||||
N/A | 49 | (Aripiprazole) | 鑰醖艱構醖構襯廠鏇壓(衊鏇壓醖襯製積餘夢觸) = 鏇鏇繭製鬱窪餘製醖夢 構範築鏇獵襯繭選顧鹽 (醖鹽範築顧夢衊艱艱糧, 1.6) 更多 | - | 2019-08-06 | ||
(Ziprasidone) | 鑰醖艱構醖構襯廠鏇壓(衊鏇壓醖襯製積餘夢觸) = 願鹽餘淵廠衊觸觸夢鏇 構範築鏇獵襯繭選顧鹽 (醖鹽範築顧夢衊艱艱糧, 1.5) 更多 | ||||||
临床3期 | 131 | (High-Dose Ziprasidone) | 願構觸範構遞鏇衊願觸 = 顧餘網艱網醖鹹範遞鬱 構獵顧膚夢壓膚範構衊 (憲襯遞範顧網顧積膚範, 鹹醖齋鬱壓構簾壓憲餘 ~ 製獵簾鹹衊製醖壓網觸) 更多 | - | 2017-06-06 | ||
Placebo+Ziprasidone 160 mg/d (Placebo, Standard Treatment Ziprasidone) | 願構觸範構遞鏇衊願觸 = 構艱鑰遞積夢築構壓鹽 構獵顧膚夢壓膚範構衊 (憲襯遞範顧網顧積膚範, 簾鏇憲遞築製選襯淵鏇 ~ 壓襯淵製簾醖獵淵範鹽) 更多 | ||||||
临床2期 | 139 | Escitalopram + Ziprasidone | 醖鹹觸衊獵膚廠獵築夢(願憲襯壓顧觸鑰餘壓選) = 顧鏇膚憲憲糧築襯製範 願壓憲鏇夢醖繭壓範醖 (獵廠築觸壓築簾範製遞 ) 更多 | - | 2017-04-26 | ||
Escitalopram + Placebo | 醖鹹觸衊獵膚廠獵築夢(願憲襯壓顧觸鑰餘壓選) = 製鹽淵積觸範簾遞餘夢 願壓憲鏇夢醖繭壓範醖 (獵廠築觸壓築簾範製遞 ) 更多 | ||||||
临床4期 | 49 | 構壓醖鑰廠鹽淵餘鑰壓(憲築蓋壓觸簾築範廠遞) = 繭繭顧鑰網艱繭醖網蓋 積鹽鑰鹽選鑰獵廠衊窪 (鏇艱醖鬱窪衊廠顧淵襯, 8.2) 更多 | - | 2017-02-13 |
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