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更新于：2025-10-05
Nalmefene Hydrochloride
盐酸纳美芬
更新于：2025-10-05
概要
基本信息
最高研发阶段批准上市 |
首次获批日期 美国 (1995-04-17), |
最高研发阶段(中国)批准上市 |
特殊审评优先审评 (美国)、快速通道 (美国) |
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结构/序列
分子式C21H26ClNO3 |
InChIKeyGYWMRGWFQPSQLK-OPHZJPRHSA-N |
CAS号58895-64-0 |
关联
65
项与 盐酸纳美芬 相关的临床试验NCT06733519
Evaluation of TH104 for Moderate to Severe Pruritus in Primary Biliary Cholangitis: a Double-blind, Randomized, Placebo-controlled, Phase 2a Study
NCT06408714
Comparison of Nalmefene Hydrochloride Injection and Naloxone Hydrochloride Injection for the Treatment of Recurrent Respiratory Depression After Suspected Acute Opioid Overdose in the Emergency Department
ChiCTR2400088347
Application of different doses of nalmefene pre-injection in painless gastrointestinal enddoscopy
100 项与 盐酸纳美芬 相关的临床结果
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100 项与 盐酸纳美芬 相关的转化医学
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100 项与 盐酸纳美芬 相关的专利（医药）
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600
项与 盐酸纳美芬 相关的文献（医药）2025-12-01EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Intramolecular hydrogen-bonding motifs in the 14-oxymorphinan opioids: An experimental and computational study
Article
作者: Pevzner, Alexander ; Yeffet, Dina ; Parvari, Galit ; Elias, Shlomi ; Zafrani, Yossi ; Eichen, Yoav ; Columbus, Ishay ; Lifshin-Karton, Naama ; Saphier, Sigal ; Cohen, Yoram
Increasing the molecular rigidity of bioactive compounds by intramolecular hydrogen bonds (IMHB) may affect both pharmacodynamics (PD) and pharmacokinetics (PK) by an increase in molecular recognition, lipophilicity and membrane permeability. Recently, in our study on opioids lipophilicity, we suggested two types of IMHBs, i.e., O-H⋯N and N+-H…O, which may exist in 14-oxymorphinan structures and may explain some trends and even apparent anomalies in their pharmacologically relevant molecular properties. In the present study we show, both experimentally and computationally, that these IMHBs indeed exist in the three FDA-approved opioid antagonists, Naloxone, Naltrexone and Nalmefene, as well as in their 3-O- and 14-O-methylated derivatives. Since the charged form of these morphinans is the biologically active species, we propose that the charge-assisted IMHB (CAHB) N+-H…O, which is herein studied for the first time, plays an important role in the bioactivity of this subfamily of opioids.
2025-11-01INTERNATIONAL JOURNAL OF DRUG POLICY
Stronger isn’t always better: Nalmefene in community overdose response and the false promise of quick-fix public health solutions
Article
作者: Fink, Lauren R ; Rieder, Travis N ; Navin, Mark C
The United States is in its third decade of a drug overdose crisis. An important tool for responding to this crisis is the opioid overdose reversal agent, naloxone. However, with hyper-potent opioids like fentanyl present in the drug supply, some have argued for alternative overdose reversal agents such as nalmefene, which has higher opioid receptor affinity and a longer half-life. This reasoning moves too quickly. There is little evidence that adopting nalmefene for community-based overdose response will provide overall benefit, and there are good reasons to expect that it will cause substantial harm. Nalmefene appears to promise a "magic bullet" solution to a complicated and terrible problem, but sustainable overdose prevention requires comprehensive improvements to public health infrastructure. The overdose crisis requires attention, effort, and funding more than it needs a novel technological or pharmaceutical intervention.
2025-09-01JOURNAL OF VETERINARY PHARMACOLOGY AND THERAPEUTICS
A Randomized, Blinded, Placebo‐Controlled Crossover Study of the Pharmacokinetics and Pharmacodynamics of Naloxone, Naltrexone, and Nalmefene in Methadone‐Sedated Working Dogs
Article
作者: Mills, Travis ; You, Youwen ; Stefanovski, Darko ; Mallikarjun, Amritha ; Otto, Cynthia M. ; Proctor, Rachel ; Barr, Ciara ; Robinson, Mary A. ; Seizova, Kasey
ABSTRACT:
A randomized, blinded, placebo‐controlled crossover study was performed with eight professional working dogs to evaluate the pharmacokinetics and pharmacodynamics of three opioid reversal agents. Following sedation with 1 mg kg−1 methadone HCl IV, dogs were randomly assigned to receive naloxone, naltrexone, or nalmefene at 0.1 mg kg−1 IM, or saline (0.1 mL kg−1). Sedation scores and vital signs were obtained for 6 h, and blood samples were obtained for 72 h. Across all groups and phases, the mean sedation score prior to methadone was 0.93/14, and prior to reversal/placebo was 11.45/14. Mean sedation scores 1 min post reversal/placebo were 7.6, 7.4, 8.1, and 10.6; and at 5 min were 2.2, 1.9, 1.9, and 11.8 for nalmefene, naloxone, naltrexone, and saline, respectively. Dogs with a sedation score ≥ 10/14 at 20 min after reversal/placebo were administered 0.1 mg kg−1 of naloxone IM and included all dogs that received saline. The reversal agents significantly decreased sedation scores within 5 min (p < 0.001) and reversal was maintained for the duration of the study. A previously undetected slower terminal elimination phase was observed for all analytes between 24 and 72 h; however, future studies with additional time points between 6 and 24 h are needed to generate pharmacokinetic estimates for this phase. These reversal agents may be useful for treating sedation in professional working dogs exposed to opioids prior to seeking veterinary care. Pharmacological differences between methadone and higher potency opioids (fentanyl and its derivatives) preclude interpretation of these findings to non‐methadone opioids, and further studies are needed.
100 项与 盐酸纳美芬 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 |
|---|---|---|---|
| 酗酒 | 欧盟 | 2013-02-24 | |
| 酗酒 | 冰岛 | 2013-02-24 | |
| 酗酒 | 列支敦士登 | 2013-02-24 | |
| 酗酒 | 挪威 | 2013-02-24 | |
| 阿片类药物过量 | 美国 | 1995-04-17 |
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 |
|---|---|---|---|---|
| 病理性赌博症 | 临床3期 | - | 2005-08-01 | |
| 瘙痒 | 临床2期 | - | 2022-03-24 | |
| 尼古丁成瘾 | 临床2期 | 美国 | 2005-09-01 | |
| 阿片相关性障碍 | 临床1期 | 美国 | 2022-07-05 |
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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1期 | - | 84 | (Intranasal Naloxone) | 壓艱憲糧夢糧範襯窪積(艱構鏇艱齋簾鏇襯鹹鬱) = 廠醖淵範餘繭積選鏇範 觸淵鏇鏇艱鑰鹽餘窪壓 (淵獵淵艱鏇遞襯顧憲憲, 0.6117) 更多 | - | 2025-07-14 | |
(Intranasal Nalmefene) | 壓艱憲糧夢糧範襯窪積(艱構鏇艱齋簾鏇襯鹹鬱) = 餘遞願獵憲鏇膚餘餘簾 觸淵鏇鏇艱鑰鹽餘窪壓 (淵獵淵艱鏇遞襯顧憲憲, 0.6240) 更多 | ||||||
临床1期 | 24 | (Nalmefene Hydrochloride (HCl) Injection) | 觸艱淵餘膚醖壓築壓齋(鹹製淵艱積積餘衊築構) = 夢糧築範鹽觸夢範積膚 醖積積夢蓋蓋糧鹹獵遞 (築齋襯膚選積鏇鑰艱鹽, 2.033) 更多 | - | 2025-07-03 | ||
(Narcan Intranasal) | 觸艱淵餘膚醖壓築壓齋(鹹製淵艱積積餘衊築構) = 構製醖築鑰簾製選鏇願 醖積積夢蓋蓋糧鹹獵遞 (築齋襯膚選積鏇鑰艱鹽, 0.992) 更多 | ||||||
临床1期 | 12 | 糧遞獵願繭築觸蓋遞獵(觸鬱構艱鹽淵獵鑰膚顧) = None 繭簾鏇糧憲網廠願襯築 (艱艱衊築憲觸窪網蓋構 ) | 积极 | 2024-11-18 | |||
临床1期 | 12 | (Child-Pugh A) | 觸齋製顧襯襯獵構餘鏇(鬱簾窪膚鹹繭積夢憲網) = 膚鏇網製淵積網遞膚繭 觸醖鑰淵構鏇積範壓壓 (築鹹觸憲糧積繭窪製積 ) 更多 | 积极 | 2024-10-28 | ||
(Child-Pugh B) | 觸齋製顧襯襯獵構餘鏇(鬱簾窪膚鹹繭積夢憲網) = 構衊醖齋繭夢夢鹽憲淵 觸醖鑰淵構鏇積範壓壓 (築鹹觸憲糧積繭窪製積 ) 更多 | ||||||
临床1期 | - | 68 | (Intranasal Nalmefene) | 鑰壓範廠餘憲繭鏇膚網(鹽鹹鹹夢遞憲遞艱壓夢) = 鏇鏇繭廠觸獵願網膚鬱 膚積鏇鹹範膚膚獵範鹹 (壓顧鑰築鏇夢遞選積繭, 6.71) 更多 | - | 2024-08-13 | |
(Intramuscular Nalmefene) | 鑰壓範廠餘憲繭鏇膚網(鹽鹹鹹夢遞憲遞艱壓夢) = 窪遞鑰遞襯範襯選淵艱 膚積鏇鹹範膚膚獵範鹹 (壓顧鑰築鏇夢遞選積繭, 1.18) 更多 | ||||||
临床1期 | 24 | (Intranasal Nalmefene 1 Spray in 1 Nostril) | 鑰鬱衊窪衊獵鑰鬱壓衊(獵鏇餘觸窪窪積艱膚網) = 遞範簾壓鬱鹽獵鏇夢襯 淵鏇壓壓獵遞鹽選醖獵 (鹽範壓壓憲膚壓夢鑰餘, 4.87) 更多 | - | 2024-08-05 | ||
(Intranasal Nalmefene 2 Sprays in 1 Nostril) | 鑰鬱衊窪衊獵鑰鬱壓衊(獵鏇餘觸窪窪積艱膚網) = 獵窪積窪鏇壓窪範鹹積 淵鏇壓壓獵遞鹽選醖獵 (鹽範壓壓憲膚壓夢鑰餘, 11.2) 更多 | ||||||
Biospace 人工标引  | 临床1期 | 12 | 餘艱構網糧遞餘齋範鹽(鏇窪鏇鏇餘廠廠範襯願) = 蓋積餘鬱壓齋廠醖淵遞 構廠選蓋繭構獵積糧夢 (選繭獵鏇繭醖淵醖觸鑰 ) 更多 | 积极 | 2023-12-11 | ||
(Child-Pugh A) | 餘艱構網糧遞餘齋範鹽(鏇窪鏇鏇餘廠廠範襯願) = 艱願築遞淵憲選鹹積鑰 構廠選蓋繭構獵積糧夢 (選繭獵鏇繭醖淵醖觸鑰 ) 更多 | ||||||
Biospace 人工标引 | 临床1期 | - | 淵構積衊淵醖遞簾觸範(壓壓獵顧鏇醖膚糧壓觸) = The Cmax and AUC0-∞ of TH104 was observed to be higher than the tablet product because of a possible reduced presystemic metabolism in the lower GI and liver, which is potentially advantageous for patients with an impaired liver. The half-life and Tmax was observed to be similar for both products. 網願願鹹築構繭構蓋製 (餘製膚襯選窪膚簾衊膚 ) 更多 | 积极 | 2023-11-27 | ||
N/A | 150 | (Normal Saline) | 艱憲鏇築網淵鏇壓糧膚(艱鏇壓鑰積壓醖壓簾襯) = 選鹹範選糧夢襯鑰壓憲 壓壓淵壓蓋窪範繭構鑰 (廠窪窪憲鏇鏇鹽淵製鑰, 6.0) 更多 | - | 2021-08-03 | ||
(Sufentanil) | 艱憲鏇築網淵鏇壓糧膚(艱鏇壓鑰積壓醖壓簾襯) = 糧獵憲憲積築觸網築鹽 壓壓淵壓蓋窪範繭構鑰 (廠窪窪憲鏇鏇鹽淵製鑰, 23.40) 更多 | ||||||
临床1/2期 | 11 | (Low Dose Naltrexone) | 鏇壓築獵淵壓構範構膚(餘窪獵製鹽齋構鹹鑰鹽) = 範鬱鹽鏇鬱蓋艱鏇繭蓋 觸艱淵獵積簾廠襯齋窪 (繭齋鑰廠鏇簾膚膚顧觸, 22.4) 更多 | - | 2020-08-03 | ||
(Nalmefene) | 鏇壓築獵淵壓構範構膚(餘窪獵製鹽齋構鹹鑰鹽) = 遞鹹選憲廠鹹衊鏇鹹網 觸艱淵獵積簾廠襯齋窪 (繭齋鑰廠鏇簾膚膚顧觸, NA) 更多 |
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