预约演示
更新于：2025-02-05
Trazodone Hydrochloride
盐酸曲唑酮
更新于：2025-02-05
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 |
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
109
项与 盐酸曲唑酮 相关的临床试验IRCT20241121063793N1
A comparative study of the effect of trazodone, melatonin and trazodone/melatonine in the treatment of sleep disorders following traumatic brain injury
NCT06740188
Impact of Trazodone on Non-rapid Eye Movement Sleep Stage Ⅲ in Depressed Insomniac Co-morbid Patients: A Randomized Controlled Trial
CTR20244640
盐酸曲唑酮缓释片在健康受试者中空腹与餐后条件下开放、随机、单次给药、两制剂、两序列、两周期交叉设计生物等效性试验
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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3,990
项与 盐酸曲唑酮 相关的文献（医药）2025-03-01SLEEP MEDICINE
Trends in anti-insomnia medication utilization among pediatric patients in nine cities in China: A real-world study (2016–2023)
Article
作者: Li, Ziheng ; Xing, Lipeng ; Liu, Maochang ; Jiang, Hailun
OBJECTIVE:
To investigate prescription patterns of insomnia medications among Chinese children, assess the current status of drug treatment, and offer data to support the guidance of clinical prescribing practices.
METHODS:
This study analyzed pediatric prescriptions for insomnia medications from the China Hospital Prescription Analysis Cooperation Project database across nine cities between 2016 and 2023. The analysis focused on demographic characteristics, prescription trends, and frequency of medication use among pediatric insomnia patients. Patterns of combination therapy were also examined.
RESULTS:
The number of children receiving insomnia medications increased substantially from 228 in 2016 to 1166 in 2023, representing an approximate 409 % increase. A growing proportion of patients were aged 12-14 years, with female patients outnumbering males by a ratio of 1.50: 1. There was an increased representation of patients from psychiatry and neurology departments. Regarding medication choices, benzodiazepines (BZDs) remained the most commonly prescribed class, though their use showed a declining trend. Similarly, non-benzodiazepine receptor agonists (nBZRAs) demonstrated a downward trend (P > 0.05), while antidepressant prescriptions significantly increased (P < 0.05). The most commonly prescribed medications within each class were alprazolam, zolpidem, trazodone, sertraline, and quetiapine. A significant proportion of patients (37.25 %) received combination therapy, with benzodiazepine receptor agonists (BZRAs) plus antidepressants being the most common combination.
CONCLUSIONS:
The utilization of pharmacological interventions for pediatric insomnia in China has risen markedly in recent years. Despite growing concerns about adverse effects, BZDs continue to be the primary therapeutic choice. The increasing prevalence of combination therapy suggests a trend toward more individualized treatment approaches. These findings underscore the importance of careful monitoring and rational prescribing practices in pediatric insomnia management.
2025-02-01INTERNATIONAL IMMUNOPHARMACOLOGY
Innovative role of the antidepressant imipramine in esophageal squamous cell carcinoma treatment: Promoting apoptosis and protective autophagy
Article
作者: Bao, Shihao ; Zhang, Yifan ; Zhang, Hao ; Cheng, Yuan ; Li, Xianjie ; Song, Zuoqing ; Xu, Xiaohong ; Xu, Song ; Zu, Lingling ; Zhang, Bo ; Xia, Wei ; Wang, Hanqing ; Zeng, Jingtong
BACKGROUND:
Esophageal squamous cell carcinoma (ESCC) is among the most prevalent malignant tumors; it is associated with dismal prognosis, and effective therapeutic agents are lacking. Depression is prevalent concern among cancer patients and is linked to diminished quality of life, poor adherence to treatment, heightened risk of suicide, and poorer prognosis. Imipramine (IM) is a tricyclic antidepressant with anti-inflammatory activity. Recent reports have indicated antitumor effects of IM in various cancers, although its role in ESCC remains unclear.
METHODS:
The depression status of patients with ESCC was graded with the Patient Health Questionnaire-9, and the effects of antidepressants (moclobemide, milnacipran, venlafaxine, escitalopram, amitriptyline, trazodone, fluvoxamine, and IM) on cell viability were evaluated through CCK-8 assays. The effects of IM on cell proliferation were evaluated through clone formation assays, whereas Transwell assays were used to assess effects on ESCC cell migration and invasion. IM-induced apoptosis was confirmed with annexin V-FITC/Caspase-3 assays, and immunofluorescence staining was used to investigate the formation of IM-induced autophagosomes. Furthermore, western blotting analysis was conducted to determine the expression levels of apoptosis- and autophagy-related proteins. RNA sequencing (RNA-seq) was used to examine signaling pathway changes. Finally, we investigated the influence of IM on tumor progression in vivo in a xenograft model.
RESULTS:
The PHQ-9 scores of patients with ESCC were higher than those of healthy controls and positively correlated with the TNM stage of ESCC. Among the antidepressants examined in our study, IM demonstrated the most potent inhibitory effect on ESCC cell viability, and effectively suppressed the proliferation, migration, and invasion of ESCC cells. Additionally, IM treatment induced apoptosis and autophagy in ESCC cells. Furthermore, blocking autophagy with chloroquine (CQ) intensified IM-induced apoptosis, thereby suggesting a protective role of cellular autophagy against apoptosis. RNA-seq results indicated that the Hippo pathway was associated with IM treatment. Upregulation of YAP reversed the apoptosis and autophagy triggered by IM, and targeting YAP intensified this effect. Finally, in animal experiments, IM hindered the growth of ESCC cells and promoted apoptosis and autophagy in tumors while causing minimal toxicity.
CONCLUSION:
Our findings provide the first reported evidence that IM triggers apoptosis and protective autophagy in ESCC cells via the Hippo signaling pathway, thus suggesting that IM may offer a promising therapeutic approach for patients with ESCC and depression.
2025-02-01Clinical Pharmacology in Drug Development
Pharmacokinetics and Bioequivalence Evaluation of Trazodone Hydrochloride Sustained‐Release Tablets in Healthy Chinese Volunteers
Article
作者: Xu, Yuan ; Wang, Jingyan ; Zhao, Zhicheng ; Zou, Yang ; Lan, Yi ; Meng, Tian
Abstract:
The aim of this study was to investigate the pharmacokinetics, bioequivalence, and safety of generic trazodone hydrochloride sustained‐release tablet and its reference listed product in healthy Chinese subjects. An open, randomized, single‐dose, and 2‐period crossover study was involved under fasting and fed conditions, with a 7‐day washout period. A single oral dose of 150 mg of 2 trazodone hydrochloride sustained‐release tablets was administered to 84 healthy volunteers, with 36 in the fasting group and 48 consuming a high‐fat diet, respectively. The plasma concentrations of trazodone were analyzed using a liquid chromatography‐tandem mass spectrometry method, and pharmacokinetic parameters were obtained from concentration‐time profiles. The geometric mean ratio with 90% confidence intervals of the maximum trazodone concentration, area under the plasma concentration‐time curve (AUC) from time 0 to the last measurable concentration, and AUC from time 0 to infinity were within the bioequivalence acceptance criteria (80%‐125%) under fasting and fed conditions, which indicated that the test and reference formulations were bioequivalent. Compared with the fasting study, the concomitant administration of trazodone with a high‐fat diet had a negligible influence on the drug pharmacokinetic behavior. Adverse events were recorded, and no serious adverse events were observed during either fasting or fed conditions. Trazodone has proven to have an acceptable safety profile in the Chinese population, with bioequivalence successfully established under both fasting and fed conditions.
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
N/A | - | 123 | Trazodone users | 艱襯憲蓋齋糧構構獵網(膚顧簾鹹齋膚夢淵積襯) = 構壓鬱築餘鹹願繭構顧 選簾簾構遞鏇壓選鑰衊 (觸繭鏇壓構繭齋膚願積 ) 更多 | 不佳 | 2024-05-01 | |
Non-Trazodone users | 艱襯憲蓋齋糧構構獵網(膚顧簾鹹齋膚夢淵積襯) = 糧獵夢選淵選構願築繭 選簾簾構遞鏇壓選鑰衊 (觸繭鏇壓構繭齋膚願積 ) 更多 | ||||||
N/A | - | Selective Serotonin/Serotonin & Norepinephrine Reuptake Inhibitors (SSRI/SNRI) | 簾齋糧鬱淵鏇衊齋鹹醖(鹹襯壓獵繭廠鬱襯餘糧): RR = 1.33 (95% CI, 1.22 ~ 1.45) | 不佳 | 2024-02-01 | ||
Serotonergic Antidepressants (No AD) | |||||||
N/A | - | SSRI/SNRI | 網鹹範顧鹽膚鑰憲鏇網(鑰繭願醖鑰築願鑰鏇積): RR = 1.29 (95% CI, 1.11 ~ 1.5) | - | 2024-02-01 | ||
Dual Antiplatelet Therapy (DAPT) | |||||||
N/A | 716 | 廠窪製憲壓鏇膚餘繭窪(遞繭鏇餘鹽鬱遞餘繭齋) = 選憲鏇遞範鬱艱鬱淵膚 鹽鬱艱鏇觸衊廠餘積醖 (鹽窪鹽蓋鑰壓鹹簾壓願 ) | 积极 | 2023-10-23 | |||
廠窪製憲壓鏇膚餘繭窪(遞繭鏇餘鹽鬱遞餘繭齋) = 膚蓋願選簾觸鹽廠構網 鹽鬱艱鏇觸衊廠餘積醖 (鹽窪鹽蓋鑰壓鹹簾壓願 ) | |||||||
N/A | - | 構網構獵製膚鬱窪觸淵(餘餘範獵遞齋餘範製襯) = 襯糧鏇夢衊憲鬱構顧襯 觸蓋鹹範壓廠獵構顧簾 (構築簾願糧鹽範艱構構 ) | - | 2023-10-23 | |||
N/A | - | - | 鬱製夢淵顧獵顧選糧構(簾獵鏇壓鹹鏇網憲憲鹽) = Common presentations were QTc interval prolongation, bradycardia, and hyponatremia with seizures. Three case reports reported death as the final outcome. In another case, death was attributed to the ingestion of multiple drugs in combination. There were however no cases that reported hypotension. 製網醖壓範鑰蓋遞遞鑰 (衊築艱憲衊願膚選鏇鹹 ) | - | 2023-05-21 | ||
临床4期 | 22 | 鹹餘獵憲廠願餘簾鹹窪(繭遞廠廠鑰鑰網遞鹹鹹) = 憲齋糧淵鑰艱餘遞觸鏇 鹽構餘築顧糧鹽鬱膚構 (製鹽願糧蓋齋觸憲憲製 ) 更多 | - | 2021-02-24 | |||
Placebo | 鹹餘獵憲廠願餘簾鹹窪(繭遞廠廠鑰鑰網遞鹹鹹) = 糧蓋廠鏇積鬱膚觸艱簾 鹽構餘築顧糧鹽鬱膚構 (製鹽願糧蓋齋觸憲憲製 ) 更多 | ||||||
N/A | 15 | 衊簾衊遞積願築窪積廠(淵鏇顧醖襯糧壓壓築夢) = 鬱蓋鹹鹽製獵網願網淵 鬱製觸廠構遞齋範製簾 (膚製鹽窪餘鹽繭願獵憲 ) 更多 | - | 2020-12-15 | |||
Cognitive-Behavioral Therapy for Insomnia (CBT-I) | 衊簾衊遞積願築窪積廠(淵鏇顧醖襯糧壓壓築夢) = 觸夢繭襯鏇鬱膚憲廠膚 鬱製觸廠構遞齋範製簾 (膚製鹽窪餘鹽繭願獵憲 ) 更多 | ||||||
临床2期 | 142 | TRZ30 | 顧製醖夢積構壓糧選夢(簾積齋憲淵網壓網願鹹) = No serious adverse event occurred during the trial and the most frequent treatment-emergent adverse events involved nervous system, QT prolongation, and gastrointestinal disorders 遞願膚製餘襯網糧窪構 (遞醖夢簾範醖遞鹽廠鬱 ) | - | 2020-11-01 | ||
TRZ60 | |||||||
临床1期 | - | 20 | 鹽觸繭獵製淵餘鏇觸簾(獵鹹繭築獵構簾範廠餘) = 簾鬱構憲襯鹹繭衊鏇構 獵鹹鬱鹹鹽範鑰網構築 (顧鬱鹹築繭觸鑰範顧顧 ) | - | 2020-06-02 | ||
鹽觸繭獵製淵餘鏇觸簾(獵鹹繭築獵構簾範廠餘) = 獵製壓襯窪遞願願鹹顧 獵鹹鬱鹹鹽範鑰網構築 (顧鬱鹹築繭觸鑰範顧顧 ) |
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