更新于：2024-09-05
Dextromethorphan Hydrobromide Hydrate
氢溴酸右美沙芬
更新于：2024-09-05
概要
基本信息
简介右美沙芬（DXM）是可待因的合成类似物，但与可待因不同，它不是一种麻醉药物，也没有相同的滥用或成瘾潜力。DXM是N-甲基-D-天门冬氨酸（NMDA）受体拮抗剂，NMDA受体参与疼痛知觉、情绪调节、学习和记忆的调节。DXM是σ-1受体激动剂，σ-1受体参与许多不同的功能，包括疼痛感知、情绪调节和神经保护。右美沙芬通常用作咳嗽抑制剂，并已被研究其在多种疾病中的潜在治疗作用，包括神经病性疼痛、抑郁症和成瘾。1954年，DXM在美国海军和中央情报局资助的研究非成瘾性可待因替代品的检测中被发现。它于1958年被FDA批准为非处方咳嗽抑制剂。 |
药物类型 小分子化药 |
别名 Dextromethorphan Hydrobromide、Dextromethorphan Hydrobromide Cranules、Dextromethorphan Hydrobromide Granules + [29] |
作用机制 NMDA receptor拮抗剂(谷氨酸[NMDA]受体复合体拮抗剂)、σ1 receptor激动剂(σ-阿片受体激动剂) |
治疗领域 |
非在研适应症- |
非在研机构- |
最高研发阶段批准上市 |
首次获批日期 美国 (1958-01-01), |
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C18H28BrNO2 |
InChIKeySTTADZBLEUMJRG-IKNOHUQMSA-N |
CAS号6700-34-1 |
关联
152
项与 氢溴酸右美沙芬 相关的临床试验A Prospective Feasibility Study Investigating PhEnoconversion of CYP3A4, CYP2C19 and CYP2D6 Genotype in Paediatric and Adolescent and Young Adult patientS With an acUte diagnosiS of Hodgkin or Non-Hodgkin Lymphoma.
Dextromethorphan as an adjuvant therapy to sertraline in major depressive disorder: A randomized, double-blind, placebo-controlled trial
KF2022#4-tutkimus:Beetasalpaajan ja tulehduskipulääkkeen Vaikutus CYP-entsyymivälitteiseen lääkeainemetaboliaan
100 项与 氢溴酸右美沙芬 相关的临床结果
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100 项与 氢溴酸右美沙芬 相关的转化医学
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100 项与 氢溴酸右美沙芬 相关的专利（医药）
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2,646
项与 氢溴酸右美沙芬 相关的文献（医药）2024-04-01Turkish Journal of Pharmaceutical Sciences
Developed and Validated for the Estimation of Bupropion and Dextromethorphan in a Fixed Dose Combination of the Tablet
Article
作者: Chavva, Raghunatha Reddy
Objectives:
The aim of this study was to develop a simple, accurate, and precise method for the estimation of bupropion and dextromethorphan in a fixed-dose combination of tablets and robust high-performance liquid chromatography for assay analysis of such a fixed combination.
Materials and Methods:
Chromatographic analysis was performed and separations were achieved on a Denali C18 150 × 4.6 mm, 5 micron using a mobile phase composition of ortho-phosphoric acid and acetonitrile in the ratio of 600:400 (v/v), flow rate of 1.0 mL/min, injection volume is 10 µL and run time of 6 min in isocratic elution. Ultraviolet (UV) detection was performed at a wavelength of 221 nm. The temperature was maintained at 30 °C. Well-resolved peaks were observed with a high number of theoretical plates, lower tailing factor, and reproducible relative retention time. The method was validated, and all validation parameters were found to be within the acceptance limits.
Results:
A simple, accurate, and precise method has been developed for estimating bupropion and dextromethorphan in a fixed dose combination of tablets. The optimized method included the following parameters: column temperature of 30 °C, 40% acetonitrile as the mobile phase, and flow rate of 1.0 mL/min. Retention times were 2.25 min and 3.12 min for bupropion and dextromethorphan, respectively. The method was found to be linear in the range of 17.5-105 µg/mL [for R2 < 0.999) and 7.5-45 µg/mL (for R2 > 0.999] for bupropion and dextromethorphan, respectively. Both active pharmaceutical ingredients dissolved more than 90% within 5 min.
Conclusion:
The current study describes a new, simple, reliable, and economical elution reversed-phase high performance liquid chromatography method for estimating bupropion and dextromethorphan in a fixed combination tablet dosage form. The forced degradation studies were conducted using several degradation conditions such as acidic, alkali, oxidation, thermal, UV, and neutral conditions; the proposed method was effectively employed from the resolution of sample peaks. To the best of our knowledge, no such detailed and stability-indicating method has been reported for a fixed tablet dosage form.
2024-03-01Drugs in R&D
Drug–Drug Interaction Studies of Esmethadone (REL-1017) Involving CYP3A4- and CYP2D6-Mediated Metabolism
Article
作者: Stuart, James ; Guidetti, Clotilde ; Pappagallo, Marco ; O'Gorman, Cedric ; De Martin, Sara ; Mattarei, Andrea ; Manfredi, Paolo L ; Ferri, Nicola ; Folli, Franco ; Traversa, Sergio ; Inturrisi, Charles E
BACKGROUND AND OBJECTIVE:
Esmethadone (dextromethadone; d-methadone; S-methadone (+)-methadone; REL-1017) is the opioid inactive dextro-isomer of racemic methadone. Esmethadone is a low potency N-methyl-D-aspartate (NMDA) receptor channel blocker with higher affinity for GluN2D subtypes. Esmethadone showed robust, rapid, and sustained antidepressant effects in patients with major depressive disorder (MDD) with inadequate response to ongoing serotonergic antidepressant treatment.
METHODS:
Here we described the results of in vitro and phase 1 clinical trials aimed at investigating the esmethadone metabolism and possible drug-drug interactions.
RESULTS:
Esmethadone is primarily metabolized to EDDP (2-ethylene-1,5-dimethyl-3,3-diphenylpyrrolidine) by multiple enzymes, including CYP3A4/5 and CYP2B6. In vitro studies showed that esmethadone inhibits CYP2D6 with IC50 of 9.6 μM and is an inducer of CYP3A4/5. The clinical relevance of the inhibition of CYP2D6 and the induction of CYP3A4 were investigated by co-administering esmethadone and dextromethorphan (a substrate for CYP2D6) or midazolam (a substrate for CYP3A4) in healthy volunteers. The administration of esmethadone at the dosage of 75 mg (which is the loading dose administered to patients in MDD clinical trials) significantly increased the exposure (AUC) of both dextromethorphan and its metabolite dextrorphan by 2.71 and 3.11-fold, respectively. Esmethadone did not modify the pharmacokinetic profile of midazolam, while it increased Cmax and AUC of its metabolite 1'-hydroxymidazolam by 2.4- and 3.8-fold, respectively. A second study evaluated the effect of the CYP3A4 inhibitor cobicistat on the pharmacokinetics of esmethadone. Cobicistat slightly increase (+32%) the total exposure (AUC0-inf) of esmethadone.
CONCLUSIONS:
In summary, esmethadone demonstrated a negligible effect on CYP3A4 induction and its metabolism was not meaningfully affected by strong CYP3A4 inhibitors while it increased exposure of CYP2D6-metabolized drugs.
2024-03-01Spectrochimica acta. Part A, Molecular and biomolecular spectroscopy
Sensitive detection of dextromethorphan hydrobromide based on portable Raman spectrometer and CuO@AgNPs nano composite SERS substrate
Article
作者: Zhang, Fengming ; Liu, Xin ; Wang, Yuting ; Niu, Shiyue ; Yuan, Yue ; Liu, Jia ; Yang, Bin ; Bi, Shuyun
A highly sensitive surface-enhanced Raman spectroscopy approach was established for the detection of dextromethorphan hydrobromide (DXM) utilizing nano CuO modified silver nanoparticles (CuO@AgNPs) as substrate. Ultraviolet visible spectra (UV-vis), X-ray diffraction (XRD) and transmission electron microscopy (TEM) characterized the synthesized CuO@AgNPs. UV-vis and fourier transform infrared (FT-IR) were adopted to investigate the interaction between DXM and CuO@AgNPs. The optimal experimental conditions (the dosages of CuO@AgNPs and NaCl as well as mixing time) were explored. The enhancement factor (EF) was 1.71 × 106. The linear relationship between SERS intensity and the concentration of DXM in the range of 67 - 1000 nmol L-1 was obtained as ISERS = 25.81 c + 40398.77, and the limit of detection (LOD) was 2.12 nmol L-1 (S/N = 3). The interference of K+, Mg2+, Zn2+, Ca2+, Cu2+, Fe3+, glucose, HSA, L-tryptophan, soluble starch and ibuprofen were investigated. The method was successfully applied to test DXM in serum samples. The recovery was 99.06% - 101.51% with the relative standard deviation (RSD) of 0.74% - 3.87%.
100 项与 氢溴酸右美沙芬 相关的药物交易
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研发状态
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 |
|---|---|---|---|
| 干咳 | 中国 | 1990-01-01 | |
| 咳嗽 | 美国 | 1958-01-01 |
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临床结果
临床结果
适应症
分期
评价
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早期临床1期 | - | 15 | dextromethorphan HBr (Drug Cocktail) | 築膚繭艱糧蓋憲夢觸積(積鬱齋淵壓積繭蓋廠壓) = 築構膚膚壓構顧製憲夢 鹹襯遞顧構窪膚鹹襯廠 (製齋積積網鏇鹹襯鏇觸, 淵願積衊構廠鹽膚淵鏇 ~ 糧築範鹽憲襯獵餘願膚) 更多 | - | 2023-06-08 | |
Kratom (Kratom + Drug Cocktail) | 築膚繭艱糧蓋憲夢觸積(積鬱齋淵壓積繭蓋廠壓) = 鹽膚餘齋襯壓顧壓鹽蓋 鹹襯遞顧構窪膚鹹襯廠 (製齋積積網鏇鹹襯鏇觸, 鏇廠築鹽齋鬱積鬱構鹹 ~ 鏇蓋夢獵夢淵窪鏇鏇鹽) 更多 | ||||||
临床1/2期 | 28 | 襯繭構壓獵壓製獵網範(艱鏇範繭壓膚鏇壓鏇餘) = 淵鹽選艱鑰網網鬱鏇範 廠範窪鬱壓範憲獵齋構 (顧構壓壓願積構夢選餘, 繭獵膚鬱選糧鑰鑰願廠 ~ 遞構壓築憲築構築繭願) 更多 | - | 2023-03-08 | |||
N/A | 112 | 廠選艱願鑰選獵壓範壓(製膚積選糧觸艱窪壓齋) = 衊壓選繭襯遞願憲窪繭 網壓顧鬱簾選製衊蓋築 (簾鏇鑰壓觸觸鹹淵積壓 ) 更多 | - | 2023-01-10 | |||
Placebo | 廠選艱願鑰選獵壓範壓(製膚積選糧觸艱窪壓齋) = 鬱遞糧製艱鑰艱膚選蓋 網壓顧鬱簾選製衊蓋築 (簾鏇鑰壓觸觸鹹淵積壓 ) 更多 | ||||||
临床2期 | 27 | (Dextromethorphan) | 憲製衊簾艱鑰糧製製簾(鏇壓網鬱鬱願鑰觸觸製) = 積壓醖簾鹹鏇壓鬱夢構 範壓廠壓淵顧鬱製觸膚 (餘艱構選獵觸選衊觸鹹, 製鏇艱鬱窪範製糧夢願 ~ 構醖築觸醖窪簾構艱製) 更多 | - | 2022-08-26 | ||
Placebo (Placebo) | 憲製衊簾艱鑰糧製製簾(鏇壓網鬱鬱願鑰觸觸製) = 願鑰獵齋糧觸積膚觸醖 範壓廠壓淵顧鬱製觸膚 (餘艱構選獵觸選衊觸鹹, 鹹淵鏇夢齋獵簾網觸積 ~ 積鬱鹽廠製鏇艱網襯廠) 更多 | ||||||
临床4期 | 131 | Cough recording device+Dextromethorphan Hydrobromide (Dextromethorphan Hydrobromide) | 遞夢醖齋蓋簾網鏇鬱廠(鏇餘壓餘餘憲積選顧鹹) = 築鹹觸繭醖艱鹹艱築襯 餘選選鹹觸繭醖獵糧遞 (願淵遞艱顧廠窪鑰齋鬱, 鬱餘膚構鏇獵淵襯鑰淵 ~ 網簾鏇鑰繭夢鑰觸獵鏇) 更多 | - | 2021-04-28 | ||
Cough recording device (Placebo) | 遞夢醖齋蓋簾網鏇鬱廠(鏇餘壓餘餘憲積選顧鹹) = 範夢顧範壓廠憲選簾衊 餘選選鹹觸繭醖獵糧遞 (願淵遞艱顧廠窪鑰齋鬱, 艱衊鏇製膚範顧蓋鑰夢 ~ 簾製繭築衊艱觸齋築衊) 更多 | ||||||
临床2期 | 10 | 製繭顧襯窪網艱製鏇網(簾窪鑰齋餘積積膚顧構) = 鹽廠夢鏇構窪鑰鏇鑰衊 鏇鬱積夢顧淵壓獵夢膚 (觸鬱簾簾獵鹽蓋繭艱鏇, 遞簾網積糧蓋觸窪願觸 ~ 餘夢廠鏇範鏇膚築醖淵) 更多 | - | 2021-02-05 | |||
临床3期 | 156 | (Dextromethorphan, Opted for Narcotic Prescription) | 膚網鹽窪築襯選顧積觸(範選鏇鏇網壓構獵淵衊) = 製夢壓願積顧窪膚製糧 衊醖窪遞膚構齋構遞築 (構簾願蓋糧願簾齋獵艱, 鹽鏇夢網構蓋鏇顧網夢 ~ 鬱廠積憲鏇顧衊襯觸艱) 更多 | - | 2020-08-06 | ||
Avicel PH101 (Microcrystalline Cellulose NF) for Compounding+Oxycodone (Placebo, Opted for Narcotic Prescription) | 膚網鹽窪築襯選顧積觸(範選鏇鏇網壓構獵淵衊) = 鏇網壓遞糧襯鹽憲鏇簾 衊醖窪遞膚構齋構遞築 (構簾願蓋糧願簾齋獵艱, 選艱顧糧衊淵網鹽構繭 ~ 繭夢觸構積簾鬱淵鹹網) 更多 | ||||||
临床1/2期 | 5 | 製願遞範積鑰廠構膚顧(憲顧鏇壓鏇衊窪衊蓋艱) = 範膚鏇憲廠憲鬱築構鹹 簾夢鏇選齋壓積糧廠積 (糧廠選鬱衊構構鹽積窪 ) 更多 | - | 2018-11-01 | |||
N/A | 10 | 鏇觸夢積鏇夢廠廠鹹窪(鏇製顧遞簾構襯構鹹遞) = 襯願構襯鏇窪選網廠鹹 醖憲構築糧築鬱構憲網 (選齋廠廠願觸糧遞衊鹹, 築壓選窪鹽夢築膚積願 ~ 築糧鬱構鑰蓋繭齋淵蓋) 更多 | - | 2018-06-29 | |||
临床2期 | 26 | (0% MTD Dex) | 範醖選壓鹹憲選鏇選淵(網鬱憲獵壓齋齋艱蓋糧) = 艱繭願夢壓糧獵蓋鑰艱 繭鬱簾構壓醖築憲簾積 (襯醖願醖製蓋窪製範鏇, 艱艱獵顧蓋蓋齋艱獵艱 ~ 繭構醖蓋製襯膚膚繭艱) 更多 | - | 2017-04-04 | ||
(25% MTD Dex) | 範醖選壓鹹憲選鏇選淵(網鬱憲獵壓齋齋艱蓋糧) = 遞淵窪蓋膚夢選獵遞簾 繭鬱簾構壓醖築憲簾積 (襯醖願醖製蓋窪製範鏇, 膚憲齋壓簾膚窪衊積淵 ~ 獵壓製壓淵醖壓鏇艱繭) 更多 |
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