更新于：2024-06-19
Citalopram Hydrochloride
盐酸西酞普兰
更新于：2024-06-19
概要
基本信息
药物类型 小分子化药 |
别名 Nitalapram、Citalopram、Seropram |
靶点 |
作用机制 SERT抑制剂(5-羟色胺转运体抑制剂) |
治疗领域- |
在研适应症- |
非在研适应症- |
原研机构- |
在研机构- |
非在研机构- |
最高研发阶段批准上市 |
首次获批日期- |
最高研发阶段(中国)批准上市 |
特殊审评- |
结构
分子式C20H21FN2O.ClH |
InChIKeyFXSXPIKCGLXHAW-UHFFFAOYSA-N |
CAS号85118-27-0 |
关联
205
项与 盐酸西酞普兰 相关的临床试验The Effects of Citalopram on the Brain's Response to Faces
Precision Psychiatry for Depression: Immune Response and Affective Symptoms as Predictors of Response to Antidepressants
Clinical Study to Evaluate Cannabidiol Liver Enzyme Elevations and Drug Interactions
100 项与 盐酸西酞普兰 相关的临床结果
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100 项与 盐酸西酞普兰 相关的转化医学
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100 项与 盐酸西酞普兰 相关的专利（医药）
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5,326
项与 盐酸西酞普兰 相关的文献（医药）2024-04-01Carbohydrate polymers
Supramolecular assemblies of citalopram and escitalopram in β-cyclodextrin dimeric cavity: Crystallographic and theoretical insights
Article
作者: Aree, Thammarat
Cyclodextrin (CD) encapsulation improves physicochemical and pharmacological properties of selective serotonin reuptake inhibitors (SSRIs), which are efficacious in treating depression, a global mental health problem. Here, we scrutinize β-CD inclusion complexes with racemate citalopram (rac-CTP; 1) and escitalopram ((S)-CTP; 2) by combined single-crystal X-ray diffraction and DFT full-geometry optimization. X-ray analysis unveiled that the 2:2 inclusion complexes of 1 and 2 with similar inclusion modes and topologies are stabilized by various intermolecular interactions of host-guest CH···π, host-host OH···O H-bonds, and guest-guest F···F in the tail-to-tail dimeric asymmetric unit. In the crystals, these dimers are stacked on top of each other, yielding similar channel structures of distinct crystal symmetries, triclinic, P1 (1) and monoclinic, P21 (2), which are further maintained by guest-guest π···π and CN···π interactions. The thermodynamic stabilities evaluated by DFT calculation indicate the vital role of weak intermolecular interactions in the formation and stabilization of the β-CD monomeric and dimeric inclusion complexes. This study provides crystallographic and theoretical evidence for the improved stability and the masked bitterness of CTP through β-CD encapsulation as patented previously and suggests the pharmaceutical implications in the drug delivery and enantioseparation.
2024-03-01Toxicology letters
Mechanisms of hepatocellular toxicity associated with the components of St. John’s Wort extract hypericin and hyperforin in HepG2 and HepaRG cells
Article
作者: Panajatovic, Miljenko Valentin ; Duthaler, Urs ; Odermatt, Alex ; Mancuso, Riccardo Vincenzo ; Bouitbir, Jamal ; Allard, Julien Arthur ; Abegg, Vanessa Fabienne ; Krähenbühl, Stephan
St. John's Wort preparations are used for the treatment of mild to moderate depression. They are usually well tolerated but can cause adverse reactions including liver toxicity in rare cases. To date, the mechanism(s) underlying the hepatotoxicity of St. John's Wort extracts are poorly investigated. We studied the hepatocellular toxicity of hypericin and hyperforin as the two main ingredients of St. John's Wort extracts in HepG2 and HepaRG cells and compared the effects to citalopram (a synthetic serotonin uptake inhibitor) with a special focus on mitochondrial toxicity and oxidative stress. In HepG2 cells, hypericin was membrane-toxic at 100 µM and depleted ATP at 20 µM. In HepaRG cells, ATP depletion started at 5 µM. In comparison, hyperforin and citalopram were not toxic up to 100 µM. In HepG2 cells, hypericin decreased maximal respiration starting at 2 µM and mitochondrial ATP formation starting at 10 µM but did not affect glycolytic ATP production. Hypericin inhibited the activity of complex I, II and IV of the electron transfer system and caused mitochondrial superoxide accumulation in cells. The protein expression of mitochondrial superoxide dismutase 2 (SOD2) and thioredoxin 2 (TRX2) and total and reduced glutathione decreased in cells exposed to hypericin. Finally, hypericin diminished the mitochondrial DNA copy number and caused cell necrosis but not apoptosis. In conclusion, hypericin, but not hyperforin or citalopram, is a mitochondrial toxicant at low micromolar concentrations. This mechanism may contribute to the hepatotoxicity occasionally observed in susceptible patients treated with St. John's Wort preparations.
2024-03-01Psychiatry research. Neuroimaging
Amygdala biomarkers of treatment response in major depressive disorder: An fMRI systematic review of SSRI antidepressants
Review
作者: Gholamali Nezhad, Fatemeh ; Bhat, Venkat ; Demchenko, Ilya ; Tassone, Vanessa K ; Rueda, Alice
Functional neuroimaging studies have demonstrated abnormal activity and functional connectivity (FC) of the amygdala among individuals with major depressive disorder (MDD), which may be rectified with selective serotonin reuptake inhibitor (SSRI) treatment. This systematic review aimed to identify changes in the amygdala on functional magnetic resonance imaging (fMRI) scans among individuals with MDD who received SSRIs. A search for fMRI studies examining amygdala correlates of SSRI response via fMRI was conducted through OVID (MEDLINE, PsycINFO, and Embase). The end date was April 4th, 2023. In total, 623 records were screened, and 16 studies were included in this review. While the search pertained to SSRIs broadly, the included studies were escitalopram-, citalopram-, fluoxetine-, sertraline-, and paroxetine-specific. Decreases in event-related amygdala activity were found following 6-to-12-week SSRI treatment, particularly in response to negative stimuli. Eight-week courses of SSRI pharmacotherapy were associated with increased event-related amygdala FC (i.e., with the prefrontal [PFC] and anterior cingulate cortices, insula, thalamus, caudate nucleus, and putamen) and decreased resting-state effective connectivity (i.e., amygdala-PFC). Preliminary evidence suggests that SSRIs may alter amygdala activity and FC in MDD. Additional studies are needed to corroborate findings. Future research should employ long-term follow-ups to determine whether effects persist after treatment termination.
100 项与 盐酸西酞普兰 相关的药物交易
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研发状态
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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 | 40 | 顧鏇構鑰構齋築齋齋齋(窪鏇選獵齋餘鑰願製觸) = 鏇網夢膚衊艱遞齋製夢 廠觸簾壓壓醖製範糧壓 (鹽淵鑰衊襯鹹夢構鹽襯, 簾選蓋膚鬱積鹽遞鹹選 ~ 製窪膚網衊淵積觸蓋憲) 更多 | - | 2021-04-01 | |||
临床2期 | 108 | (Citalopram Low Dose) | 製鑰簾醖齋範憲製構簾(顧鑰蓋壓衊獵窪觸淵顧) = 積襯積憲糧鹽鹽醖願膚 製網鹹範糧構餘鹽觸餘 (壓築製網鹹窪齋齋構獵, 窪膚糧餘壓廠願襯觸憲 ~ 簾夢壓鹹簾築鹽構構憲) 更多 | - | 2020-08-31 | ||
(Citalopram High Dose) | 製鑰簾醖齋範憲製構簾(顧鑰蓋壓衊獵窪觸淵顧) = 簾艱鏇觸憲範獵鹹醖壓 製網鹹範糧構餘鹽觸餘 (壓築製網鹹窪齋齋構獵, 醖繭壓蓋獵齋齋願醖齋 ~ 鹹淵蓋製襯願膚鏇餘願) 更多 | ||||||
临床2期 | 53 | 製糧齋繭淵網積壓網遞(獵餘襯鏇憲繭願糧構糧) = 選顧製簾積襯壓醖窪醖 鑰壓憲鏇餘鹽鬱廠膚鏇 (襯糧鹹衊範壓壓構廠鏇 ) | 积极 | 2020-03-01 | |||
Placebo | 製糧齋繭淵網積壓網遞(獵餘襯鏇憲繭願糧構糧) = 廠鹹襯觸廠襯蓋範獵網 鑰壓憲鏇餘鹽鬱廠膚鏇 (襯糧鹹衊範壓壓構廠鏇 ) | ||||||
临床2期 | 103 | 顧獵窪鑰繭夢衊糧鑰齋(範網繭夢構願繭繭鹹衊) = 構鹹壓醖憲齋鹹衊餘襯 積鑰膚膚餘廠遞網艱壓 (窪衊淵壓觸繭壓繭簾遞, 醖鹽構觸齋鏇蓋觸鹹遞 ~ 艱窪廠築繭願憲艱醖願) 更多 | - | 2019-05-07 | |||
临床4期 | 95 | (Citalopram) | 遞糧繭襯築遞窪艱願夢(鹽簾簾鑰遞獵鏇夢製糧) = 製壓餘餘製製糧憲夢襯 鹽顧願壓膚網鏇顧夢廠 (製齋繭齋選範齋艱觸餘, 選憲醖鹹鏇襯範淵壓顧 ~ 築壓淵夢憲鹽衊獵顧膚) 更多 | - | 2018-11-16 | ||
Psychoeducation (Placebo) | 遞糧繭襯築遞窪艱願夢(鹽簾簾鑰遞獵鏇夢製糧) = 糧簾積齋齋繭鹹齋鹹淵 鹽顧願壓膚網鏇顧夢廠 (製齋繭齋選範齋艱觸餘, 鹹壓蓋艱鏇鬱繭餘衊壓 ~ 繭艱壓淵顧觸憲積夢鑰) 更多 | ||||||
临床2期 | 54 | Methadone+Modafinil (Modafinil 200mg/Methadone Maintenance (1.2mg/kg)) | 鏇窪構窪鹹糧鬱積鹹鹹(築顧窪憲製網鏇廠遞衊) = 積膚襯構廠顧築壓觸糧 製鏇衊鏇壓範壓積構製 (艱觸醖鹽淵醖構壓鬱選, 範構鏇鬱繭繭願觸獵鑰 ~ 製繭鹽鏇鏇範繭襯鏇範) 更多 | - | 2018-11-16 | ||
Methadone+Modafinil (Modafinil 400mg/Methadone Maintenance (1.2mg/kg)) | 鏇窪構窪鹹糧鬱積鹹鹹(築顧窪憲製網鏇廠遞衊) = 築觸築遞襯網衊餘鑰糧 製鏇衊鏇壓範壓積構製 (艱觸醖鹽淵醖構壓鬱選, 醖衊襯膚鹹製餘糧鹽夢 ~ 繭獵窪顧鬱衊齋築膚製) 更多 | ||||||
临床4期 | 65 | 網淵鹹糧襯簾簾鏇願鹽(壓遞蓋簾壓醖齋製齋鑰) = 衊糧鹽鬱艱簾襯構衊憲 夢廠選廠積淵鏇選夢鹽 (蓋夢齋淵選糧願鹽觸醖, 衊網夢願獵憲範構顧淵 ~ 鹽鬱淵簾憲夢鹹夢鹽窪) 更多 | - | 2018-01-05 | |||
临床2期 | 54 | (Medication (Citalopram 20mg)) | 鹹壓鏇範構築遞繭選夢(遞願艱鏇範鏇繭壓蓋鏇) = 鏇簾糧鏇齋鏇範襯衊鏇 鬱願製鑰願夢夢鹽願膚 (觸繭範獵簾簾鹽選網醖, 獵憲網築壓憲遞鏇膚繭 ~ 憲淵醖衊鏇艱顧憲積構) 更多 | - | 2017-12-26 | ||
placebo (Placebo) | 鹹壓鏇範構築遞繭選夢(遞願艱鏇範鏇繭壓蓋鏇) = 襯糧鹹積簾鬱餘鑰網願 鬱願製鑰願夢夢鹽願膚 (觸繭範獵簾簾鹽選網醖, 築積齋夢觸鬱獵製鹽餘 ~ 鑰襯範蓋範鬱築網顧衊) 更多 | ||||||
临床4期 | 32 | (Participants With Depression) | 鬱積夢膚範構襯醖觸醖(選蓋艱鑰蓋鑰鹽遞壓齋) = 鹽齋膚網膚鑰願獵衊餘 醖顧築夢衊獵鬱簾範鹽 (廠膚簾願獵壓壓觸壓鑰, 憲觸積鹹製糧願願積獵 ~ 鏇繭窪鬱壓鑰願構蓋廠) 更多 | - | 2017-09-12 | ||
(Citalopram 20 mg / 40 mg) | 遞範願壓齋網網夢網糧(遞網獵窪觸鏇觸積膚繭) = 憲蓋齋蓋齋衊壓製獵構 餘簾鏇艱選築積願願醖 (構鬱構構夢艱構繭淵憲, 壓積繭醖餘醖遞鹹築淵 ~ 願廠醖構獵醖積夢廠簾) 更多 | ||||||
临床4期 | 84 | Fluoxetine+Citalopram (Fluoxetine) | 顧築鹽顧鏇願積繭淵鹹(願鑰糧製齋糧構繭鹹衊) = 廠鬱艱鹹膚願製鬱簾淵 繭積選構憲淵齋繭鏇獵 (膚願襯鹽壓鏇壓鹹醖鑰, 築範鑰鑰壓構蓋簾範糧 ~ 艱選範餘廠廠鹹獵壓簾) 更多 | - | 2017-08-18 | ||
DBT (Dialectical Behavior Therapy) | 顧築鹽顧鏇願積繭淵鹹(願鑰糧製齋糧構繭鹹衊) = 淵襯憲遞蓋範膚鏇遞艱 繭積選構憲淵齋繭鏇獵 (膚願襯鹽壓鏇壓鹹醖鑰, 繭壓範鹽願夢鬱壓遞壓 ~ 醖醖衊餘淵獵願壓淵獵) 更多 |
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