更新于：2024-11-04
Dolasetron Mesylate
甲磺酸多拉司琼
更新于：2024-11-04
概要
基本信息
药物类型 小分子化药 |
别名 Anemet、Anzemet、Dolasetron + [7] |
作用机制 5-HT3 receptor拮抗剂(5-羟色胺受体3拮抗剂) |
治疗领域 |
非在研适应症 |
原研机构 |
最高研发阶段批准上市 |
首次获批日期 美国 (1997-09-11), |
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C20H26N2O7S |
InChIKeyQTFFGPOXNNGTGZ-BHSFMSKKSA-N |
CAS号878143-33-0 |
关联
7
项与 甲磺酸多拉司琼 相关的临床试验Effects of the Ten-Degree Reverse- Trendelenburg position and dolasetron on postoperative nausea and vomiting in patients undergoing thyroid surgery
Real-time Decision Support for Postoperative Nausea and Vomiting (PONV) Prophylaxis
An Open-Label, Three-Part, Two Period, Single Sequence Study to Assess the Pharmacokinetic Interaction Between Repeat Doses of Oral Casopitant and Repeat Oral Doses of Dolasetron, Granisetron or Rosiglitazone When Co-Administered in Healthy Adult Subjects
100 项与 甲磺酸多拉司琼 相关的临床结果
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100 项与 甲磺酸多拉司琼 相关的转化医学
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100 项与 甲磺酸多拉司琼 相关的专利（医药）
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266
项与 甲磺酸多拉司琼 相关的文献（医药）2024-07-01CLINICAL PHARMACOLOGY & THERAPEUTICS
Results from a Joined Prospective Study to Evaluate the Sensitivity of the In Vivo Dog QT Assay in Line with the ICH E14 /S7B Q&A Best Practices
Article
作者: Drieu la Rochelle, Christophe ; Loiseau, Mathilde ; Possémé, Celine ; Weinelt, Ferdinand ; Martel, Eric ; Delpy, Eric ; Delaunois, Annie ; Bétat, Anne‐Marie ; Valentin, Jean‐Pierre ; Poizat, Gwendoline ; Maurin, Anne
The ICH E14/S7B Q&As highlighted the need for best practices concerning the design, execution, analysis, interpretation, and reporting of the in vivo non‐rodent QT assay as a component of the integrated risk assessment to potentially support a TQT waiver or substitute. We conducted a dog telemetry study to assess the effects on QTc of six reference compounds (five positive and one negative) previously evaluated by Darpo et al. (2015) in humans. The sensitivity of the assay to detect QTc increases was determined, and exposure–response analysis was performed, as done in clinical practice. By‐timepoint analysis showed QTc prolongation induced by moxifloxacin, dofetilide, dolasetron, ondansetron, and quinine within human relevant plasma exposures ranges. Moreover, a hysteresis was observed for quinine. As expected, levocetirizine showed no statistically significant effect on QTc across a range of exposure, well exceeding the therapeutic Cmax. Power analyses confirmed the study ability to detect statistically significant QTc changes of less than 10 milliseconds with 80% probability, even with a sample size as low as n = 4 animals. Finally, concentration‐QTc modeling enabled to predict the minimal plasma concentration needed to detect a 10 milliseconds QTc prolongation, including for quinine. The comparison with clinical available data supported the relevance of dogs under these experimental conditions as a robust translational predictor of drug‐induced QTc prolongation in humans as a key pillar of the integrated risk assessment.
2023-06-01Minerva anestesiologica
The efficacy of 5HT3-receptor antagonists in postoperative nausea and vomiting: the role of pharmacogenetics
Review
作者: Staikou, Chryssoula ; Theodosopoulou, Polyxeni ; Rekatsina, Martina
INTRODUCTION:
Genetic variants may affect drug efficacy on postoperative nausea and vomiting (PONV). The understanding of these mechanisms will help to identify the surgical patients who might benefit from specific prophylactic and therapeutic antiemetic treatment. The aim of the present review was to investigate gene polymorphisms that influence 5-hydroxytryptamine (serotonin) type 3 receptor antagonists (5HT3RA) efficacy in PONV.
EVIDENCE AQUISITION:
We included articles published from 2005 to 2022, utilizing the electronic databases PUBMED, EMBASE, COHRANE Library and ScienceDirect. To explore the relationship between genetic variations and 5HT3 receptor antagonist efficacy in PONV we focused on three different gene polymorphisms: the cytochrome P450 mono-oxygenase system gene (CYP2D6), the adenosine triphosphate (ATP)-binding cassette subfamily B gene (ABCB1) as well as the 5HT3 receptor gene (5HT3R). We also explored the relationship between the above genetic variations and their impact on 5HT3RA efficacy in the context of chemotherapy induced nausea and vomiting.
EVIDENCE SYNTHESIS:
Our search retrieved a total of 70 articles; 29 of them were included in the present review. Regarding polymorphisms of the CYP2D6 gene and the efficacy of serotonin antagonists in PONV, the ultra-rapid metabolizer genotype was associated with reduced efficacy of ondansetron, dolasetron and tropisetron, with the latter presenting more pronounced failure in these patients, while granisetron's efficacy remained unaffected. Regarding variations in the ABCB1 gene, three polymorphisms ("2677G>T/A" in exon 21; "3435C>T" in exon 27; "C1236T" in exon 12) were associated with a better response to ondansetron and ramosetron, while they did not affect palonosetron's efficacy. Additionally, polymporphisms of the 5-HT3B receptor gene were associated with ondancetron's postoperative efficacy; the "100_-102AAG" deletion variant was associated with reduced efficacy, while the Y129S variant did not show any effect on the drug's antiemetic effect.
CONCLUSIONS:
This review highlights that inefficacy of a specific drug in managing PONV could be attributed to specific genetic profiles and patients would possibly benefit from a drug switch.
2022-06-01The Journal of international medical research
Incidence and risk factors of postoperative nausea and vomiting in lung cancer patients following lobectomy and application of analgesic pumps
Article
作者: Ma, Fen ; Liao, Yixia ; Wu, Suwen ; Hong, Yutong ; Duan, Hao ; Huang, Xiaoling ; Gan, Chune ; Jiang, Dongping ; Lin, Peng ; Xu, Ye
Objective:
To investigate the occurrence rate and risk factors of postoperative nausea and vomiting (PONV) in lung cancer patients following lobectomy and application of analgesic pumps.
Methods:
This retrospective study reviewed clinical data from patients that had undergone lobectomy for lung cancer under general anaesthesia. The risk factors of PONV were analysed using binary logistic regression models.
Results:
A total of 203 patients (97 females) were enrolled. The rate of PONV was 29.6% (60 of 203 patients) for all patients, 42.3% (41 of 97 patients) for female patients and 17.9% (19 of 106 patients) for male patients. Female patients undergoing thoracotomy (odds ratio [OR] 7.770, 95% confidence interval [CI] 1.747, 34.568) or having surgery durations ≥120 min (OR 4.493, 95% CI 1.502, 12.851) were significantly more susceptible to PONV. The risk of PONV in female patients that received postoperative dolasetron (100 mg, once a day) was significantly lower (OR 0.075, 95% CI 0.007, 0.834). For male patients, the risk of PONV was significantly lower in those with a body mass index ≥24 kg/m2 (OR 0.166; 95% CI 0.035, 0.782).
Conclusion:
Female and male patients have different risk factors for PONV following lobectomy for lung cancer and application of analgesic pumps.
100 项与 甲磺酸多拉司琼 相关的药物交易
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研发状态
批准上市
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 恶心 | 中国 | 2011-07-18 | |
| 呕吐 | 中国 | 2011-07-18 | |
| 恶心和呕吐 | 加拿大 | 1997-09-25 | |
| 化疗引起的恶心和呕吐 | 美国 | 1997-09-11 | |
| 术后恶心呕吐 | 美国 | 1997-09-11 |
未上市
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 精神障碍 | 临床3期 | 欧盟 | - |
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