预约演示
更新于：2025-05-11
Trazodone Hydrochloride
盐酸曲唑酮
更新于：2025-05-11
概要
基本信息
简介曲唑酮是一种小分子药物，靶向血清素转运蛋白并作为血清素再摄取抑制剂。虽然被批准用于治疗多种疾病，包括重度抑郁症、糖尿病神经病、睡眠开始和维持障碍以及早泄，但该药物的作用机制仍然难以捉摸。Angelini Pharma于1981年12月率先批准使用该药物。通过增加大脑中的血清素水平，盐酸曲唑酮可减轻抑郁症状并改善情绪。此外，该药物具有镇静特性，可有效治疗睡眠障碍。然而，曲唑酮可能会产生不必要的副作用，如头晕、嗜睡和口干，并与其他药物相互作用，导致不良后果。 |
药物类型 小分子化药 |
别名 Oleptro、Trazodone、Trazodone HCl + [17] |
作用方式 拮抗剂 |
作用机制 5-HT2 receptor拮抗剂(5-羟色胺2受体拮抗剂)、5-羟色胺重摄取抑制剂 |
非在研适应症 |
权益机构- |
最高研发阶段批准上市 |
首次获批日期 美国 (1981-12-24), |
最高研发阶段(中国)批准上市 |
特殊审评孤儿药 (美国) |
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结构/序列
分子式C19H23Cl2N5O |
InChIKeyOHHDIOKRWWOXMT-UHFFFAOYSA-N |
CAS号25332-39-2 |
关联
125
项与 盐酸曲唑酮 相关的临床试验NCT05299398
Prevention of Postpartum Depression: A Pilot Placebo-controlled Trial of Trazodone
CTR20250832
盐酸曲唑酮缓释片在健康受试者中的随机、开放、两制剂、两周期、双交叉空腹及餐后生物等效性试验
CTR20250261
盐酸曲唑酮片（50mg）在中国健康受试者中空腹和餐后给药条件下随机、开放、单剂量、两序列、两周期、双交叉生物等效性试验
100 项与 盐酸曲唑酮 相关的临床结果
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100 项与 盐酸曲唑酮 相关的转化医学
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100 项与 盐酸曲唑酮 相关的专利（医药）
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4,060
项与 盐酸曲唑酮 相关的文献（医药）2025-09-01JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
Evaluating the carcinogenic potential of trazodone hydrochloride via duplex DNA targeting: Molecular interaction, binding mechanism and affinity assessment via structural calculations
Article
作者: Ali, Mohd Sajid ; Singh, Shweta ; Rani, Majji Sai Sudha ; Gopi, Priyanka ; Singh, Pratik ; Pandya, Prateek ; Sharma, Palak
Trazodone Hydrochloride (TRZ) is a selective serotonin antagonist reuptake inhibitor (SARI) antidepressant that is widely prescribed to treat depression. In this study, we have observed that TRZ disturbs the duplex DNA structure around the binding site causing base flip in the major groove and disrupting sequence readout. TRZ binds in the minor groove, yet it disturbs the DNA structure significantly, causing problems in sequence readout. Therefore, it would be interesting to investigate the interaction between duplex DNA. DNA binding study was conducted using multi-spectroscopic methods coupled with molecular simulations. Fluorescence investigations revealed a static quenching mechanism between TRZ and CT-DNA with a moderate binding strength (2.7 ×104 LM-1 at 288 K, 1.1 ×104 LM-1 at 298 K, 5.2 ×103 LM-1 at 308 K). The thermodynamic parameters suggested that the complexation was spontaneous, enthalpy-driven (-69.006 kJ/mol), with an entropy of -0.168 kJ/mol and Gibbs free energy ranging between -18.93 to -16.03 kJ/mol. Complexation was primarily facilitated by the formation of hydrogen bonds and Van der Waals forces which corroborated by the MM/PBSA findings. Detailed assessment of the binding mode and interaction mechanism through Molecular Docking and Molecular Dynamics Simulations (150 ns) indicated TRZ's affinity for the minor groove of CT-DNA which was further validated experimentally through displacement study with the known minor groove binder, DAPI. CD spectroscopy of CT-DNA in the absence and presence of TRZ revealed minor variations in the negative and positive bands indicative of groove binding. The structural variations of TRZ observed during binding indicated minor conformational adjustments and repositioning, especially at piperazine and chlorophenyl ring, providing stable interactions in the form of stacking forces leading to better fit within the binding site, particularly within the AT region of the CT-DNA's minor groove. The findings from this study will enhance our understanding of the interaction between TRZ and CT-DNA, adding depth to existing knowledge in the field.
2025-05-04Expert Opinion On Drug Safety
Compartment syndrome associations with drugs: a pharmacovigilance study of the FDA adverse event reporting system (FAERS)
Article
作者: Yang, Xueting ; Shu, Yunfeng ; Tang, Juan ; Wan, Jie ; Kong, Wenqiang
BACKGROUND:
Compartment syndrome is an uncommon but life-threatening condition. No study has comprehensively compared compartment syndrome (CS) association with available drugs. The objective of this study was to estimate the association between CS and drugs using the FDA Adverse Event Report System (FAERS).
RESEARCH DESIGN AND METHODS:
FAERS reports from the first quarter of 2004 to the third quarter of 2023 were analyzed. The Medical Dictionary for Regulatory Activities (MedDRA) was used to identify CS cases. Reporting odds ratio (ROR), corresponding to 95% confidence intervals (95% CI) were calculated to detect a positive signal.
RESULTS:
A total of 2197 reports were considered in the study after the inclusion criteria were applied. Totally 100 drugs were found to be associated with CS. The median time for drug-associated CS was 45 days.
CONCLUSIONS:
By analyzing the FAERS database, the study revealed that certain drugs are significantly associated with compartment syndrome. Further studies are needed to verify whether these drugs are associated with such a risk.
2025-05-01WATER RESEARCH
Fate and transformation of psychotropic drugs in urban wastewater systems and receiving rivers via the integration of targeted and suspect screening analysis
Article
作者: Hu, Li-Xin ; Xu, Mei-Ying ; Yu, Zhi-Qiang ; Liang, Yin-Xiu ; Liu, You-Sheng ; Ying, Guang-Guo ; Zhang, Jin-Na ; Wang, An-Guo
Psychotropic drugs rank among the most prescribed pharmaceuticals in the world. The ubiquitous occurrence of psychotropic drugs in the environment evoked rising concerns due to their various toxic effect on non-target organisms at low concentrations. However, the removal, transformation, and discharging of these drugs throughout wastewater treatment plants (WWTPs) have rarely been reported. Based on the targeted analysis and suspected screening, this study investigated the distribution of psychotropic drugs and their transformation products (TPs) within the entire treatment processes in WWTPs and their receiving rivers. The results indicated that 13 out of 47 psychotropic drugs are widely observed across wastewater, sludge, receiving river water, and sediment, respectively. The aqueous removal efficiencies of most psychotropic drugs exhibited their significant recalcitrance in wastewater treatment processes. For instance, venlafaxine (VEL) was slightly removed by 2.64 % and 10.8 % in these two WWTPs. The concentrations of oxazepam (OZP) and lamotrigine (LMT) dramatically increased after the overall treatment processes due to their metabolic conversion and regeneration processes, respectively. Given the recalcitrance of psychotropic drugs, the identified TPs generated within WWTPs were not abundant, but a wider variety of TPs were identified from human metabolites. A total of 25 TPs were identified via the suspect screening analysis, of which nine were newly identified. In receiving rivers, the risk quotient (RQ) presented OZP, sertraline (SER), and VEL posed high potential risks; the integration of the toxicological priority index (ToxPi) and the toxicity-weighted concentration (TWC) suggested TP-CIT-322 and TP-OCX-195 as the high-priority contaminants. Given the recalcitrance and environmental risks of psychotropic drugs and their TPs in WWTPs and environments, it is crucial for the further exploration of their effective treatment technologies and emission control strategies .
100 项与 盐酸曲唑酮 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 |
|---|---|---|---|
| 抑郁症 | 日本 | 1991-06-28 | |
| 抑郁症 | 日本 | 1991-06-28 | |
| 重度抑郁症 | 美国 | 1981-12-24 |
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 |
|---|---|---|---|---|
| 糖尿病性神经病变 | 临床2期 | 捷克 | 2017-05-16 | |
| 糖尿病性神经病变 | 临床2期 | 匈牙利 | 2017-05-16 | |
| 糖尿病性神经病变 | 临床2期 | 波兰 | 2017-05-16 | |
| 糖尿病周围神经病变 | 临床2期 | 中国 | 2017-05-09 | |
| 入睡和睡眠障碍 | 临床2期 | 中国 | 2015-10-19 | |
| 早泄 | 临床1期 | 中国 | 2015-06-17 | |
| 焦虑症 | 临床1期 | 中国 | 2011-11-10 | |
| 焦虑症 | 临床1期 | 中国 | 2011-11-10 |
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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4期 | 155 | 繭憲範鏇積積網壓淵願(糧艱簾醖襯鹹膚齋範築) = 齋選衊觸憲鑰餘築鹹遞 鏇鏇窪鹽鹹鹹願醖構鑰 (艱壓衊淵築網鏇襯蓋艱, 鹹築製願醖鑰齋衊窪築 ~ 繭糧壓醖構夢艱膚窪構) 更多 | - | 2025-02-24 | |||
Internet Cognitive Behavioral Therapy for Insomnia (CBT-I) (Internet Cognitive Behavioral Therapy for Insomnia (CBT-I)) | 繭憲範鏇積積網壓淵願(糧艱簾醖襯鹹膚齋範築) = 範鏇醖鏇積淵餘廠夢範 鏇鏇窪鹽鹹鹹願醖構鑰 (艱壓衊淵築網鏇襯蓋艱, 鹽簾淵顧鑰壓鏇範夢構 ~ 遞壓憲夢製艱壓蓋簾廠) 更多 | ||||||
N/A | 123 | Trazodone users | 鬱鹽鹹網觸蓋構築鏇願(夢選廠鑰膚願遞艱艱鑰) = 願築艱構構遞衊網遞網 網糧製衊廠糧廠鏇選簾 (網製鏇膚觸鑰網窪願鑰 ) 更多 | 不佳 | 2024-05-01 | ||
Non-Trazodone users | 鬱鹽鹹網觸蓋構築鏇願(夢選廠鑰膚願遞艱艱鑰) = 夢願構鏇遞鹹齋壓範願 網糧製衊廠糧廠鏇選簾 (網製鏇膚觸鑰網窪願鑰 ) 更多 | ||||||
临床3期 | 126 | Cognitive Behavioral Therapy for Insomnia (CBT-I) | 鏇製範遞獵顧獵遞繭膚(廠選鑰選築鬱網獵構壓) = 餘鹹鹹淵艱齋窪製糧餘 繭顧鑰淵範範簾構築蓋 (夢鬱鑰衊積鹽積繭顧鬱, 衊築構醖齋築簾糧衊簾 ~ 簾齋窪顧繭選獵窪鑰窪) 更多 | - | 2024-02-05 | ||
(Medication- Trazodone) | 鏇製範遞獵顧獵遞繭膚(廠選鑰選築鬱網獵構壓) = 構廠鑰鏇衊襯製鬱壓蓋 繭顧鑰淵範範簾構築蓋 (夢鬱鑰衊積鹽積繭顧鬱, 夢製製鏇觸遞觸窪膚遞 ~ 衊選網鑰積選製網築範) 更多 | ||||||
N/A | - | SSRI/SNRI | 鏇構製鹹襯構構觸餘壓(淵醖齋繭窪願網顧繭壓): RR = 1.29 (95% CI, 1.11 ~ 1.5) | - | 2024-02-01 | ||
Dual Antiplatelet Therapy (DAPT) | |||||||
N/A | - | Selective Serotonin/Serotonin & Norepinephrine Reuptake Inhibitors (SSRI/SNRI) | 簾構膚鬱糧餘顧壓淵製(鹹獵構淵製鹹顧醖顧蓋): RR = 1.33 (95% CI, 1.22 ~ 1.45) | 不佳 | 2024-02-01 | ||
Serotonergic Antidepressants (No AD) | |||||||
N/A | - | 鹹鑰餘鑰鹽夢簾簾積獵(衊觸構淵鹽醖齋襯夢齋) = 憲淵製廠襯範鹹鏇獵鬱 鹽範獵糧遞餘衊顧觸壓 (餘鬱糧齋鹽醖繭廠鹹艱 ) | - | 2023-10-23 | |||
N/A | 716 | 窪鑰艱簾構衊襯鏇艱構(獵顧獵夢夢憲願鹹願醖) = 築選膚鬱觸蓋鏇餘餘簾 獵淵選獵選醖網鬱積選 (鏇鹹鑰醖憲夢膚齋艱遞 ) | 积极 | 2023-10-23 | |||
窪鑰艱簾構衊襯鏇艱構(獵顧獵夢夢憲願鹹願醖) = 繭齋製壓遞鹹糧網憲鬱 獵淵選獵選醖網鬱積選 (鏇鹹鑰醖憲夢膚齋艱遞 ) | |||||||
临床4期 | 22 | 夢餘遞鏇製壓鹹繭鹽醖(願糧選醖艱獵願窪選壓) = 選鑰壓憲鹹鬱衊觸製淵 醖遞簾鹽襯鏇夢夢簾鏇 (醖獵觸糧觸襯觸糧蓋獵 ) 更多 | - | 2021-02-24 | |||
Placebo | 夢餘遞鏇製壓鹹繭鹽醖(願糧選醖艱獵願窪選壓) = 淵願鹽顧壓鏇蓋願糧鑰 醖遞簾鹽襯鏇夢夢簾鏇 (醖獵觸糧觸襯觸糧蓋獵 ) 更多 | ||||||
N/A | 15 | 願願簾糧餘糧遞範憲鏇(遞築遞鬱遞範鬱選衊蓋) = 齋窪夢衊鹹顧糧壓蓋顧 選範願積糧鏇築遞簾遞 (獵築遞醖衊廠製衊獵網 ) 更多 | - | 2020-12-15 | |||
Cognitive-Behavioral Therapy for Insomnia (CBT-I) | 願願簾糧餘糧遞範憲鏇(遞築遞鬱遞範鬱選衊蓋) = 醖積膚觸壓憲糧積餘夢 選範願積糧鏇築遞簾遞 (獵築遞醖衊廠製衊獵網 ) 更多 | ||||||
临床2期 | 142 | TRZ30 | 襯簾顧鏇鏇窪選鹹艱窪(範顧鏇獵艱夢夢鑰繭齋) = No serious adverse event occurred during the trial and the most frequent treatment-emergent adverse events involved nervous system, QT prolongation, and gastrointestinal disorders 憲願廠製願夢齋淵顧廠 (鑰簾選獵糧餘醖鏇鹹醖 ) | - | 2020-11-01 | ||
TRZ60 |
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