预约演示
更新于：2026-01-02
Naloxone Hydrochloride/Oxycodone Hydrochloride
盐酸纳洛酮/盐酸羟考酮
更新于：2026-01-02
概要
基本信息
药物类型 小分子化药 |
别名 Naloxone Hydrochloride/Oxycodone Hydrochloride Hydrate、Targinact、羟考酮纳洛酮 + [4] |
作用方式 激动剂 |
作用机制 Opioid receptors激动剂(阿片样受体激动剂) |
在研适应症 |
原研机构 |
权益机构- |
最高研发阶段批准上市 |
首次获批日期 澳大利亚 (2010-05-12), |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构/序列
分子式C37H42N2O8 |
InChIKeyACSGYQDUMAPFHC-ONHRPZMOSA-N |
CAS号92522-88-8 |
关联
55
项与 盐酸纳洛酮/盐酸羟考酮 相关的临床试验NCT06897917
Real World Study of Oxycodone/Naloxone Sustained-Release Tablets (Mimeixin) for Patients With Severe Cancer Pain
CTR20240182
慢性疼痛受试者空腹或餐后单次口服羟考酮纳洛酮缓释片随机、开放、两序列、两周期、双交叉人体生物等效性研究
CTR20250151
羟考酮纳洛酮缓释片的人体生物等效性研究
100 项与 盐酸纳洛酮/盐酸羟考酮 相关的临床结果
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100 项与 盐酸纳洛酮/盐酸羟考酮 相关的转化医学
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100 项与 盐酸纳洛酮/盐酸羟考酮 相关的专利（医药）
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28
项与 盐酸纳洛酮/盐酸羟考酮 相关的文献（医药）2023-03-01Annals of clinical and translational neurology
No pain, no strain: Targin® mitigates pain and constipation following spinal cord injury
作者: Andrei Krassioukov ; Ali Hosseinzadeh ; Michael Berger ; Rahul Sachdeva ; Andrea Maharaj ; Aaron Rizzardo
Abstract:
Background:
Opioids effectively reduce chronic pain, but present significant side effects including opioid‐induced constipation. Oxycodone/naloxone decreases pain and constipation in cancer patients, however its effect on spinal cord injury population remains understudied.
Methods:
We assessed whether oxycodone/naloxone reduces pain, constipation, and severity of autonomic dysreflexia in an individual with spinal cord injury. A 55‐year‐old male with C5 lesion presented with chief complaint of chronic pain received 5/2.5 mg and 20/10 mg oxycodone/naloxone for 6 and 2 weeks, respectively.
Results:
Oxycodone/naloxone improved pain, bowel function, and autonomic dysreflexia severity.
Interpretation:
Oxycodone/naloxone was effective in managing chronic pain and constipation in the studied case.
2020-11-01Journal of orthopaedics
Perioperative steroid administration improves knee function and reduces opioid consumption in bilateral total knee arthroplasty
Article
作者: Sheridan, Gerard ; Keohane, David ; Harty, James
INTRODUCTION:
The benefits of steroid usage have been well described for unilateral total knee arthroplasty (TKA), however it's benefits in bilateral TKA has not been well published in the literature. We describe the impact of perioperative steroid administration in a cohort of bilateral TKAs (74 knees) with regard to immediate postoperative knee function, postoperative knee strength and opioid consumption.
MATERIALS AND METHODS:
We report on a single-surgeon consecutive case series of simultaneously-performed bilateral TKAs. Eighteen patients received 2 doses of 8 mg IV dexamethasone in the perioperative setting. There were 19 patients in the control group. Primary outcome measures were day 1 postoperative knee flexion (degrees), knee strength and postoperative analgesic requirements (mg/mcg). Morphine dose equivalents (MDE) were calculated to compare all opioid-based analgesics. Secondary outcomes included post-operative pain according to the VAS (at 24, 48 and 72 h), anti-emetic requirements (mg) and length of stay (days).
RESULTS:
The mean knee flexion achieved day 1 in the steroid group was 70.1°(σ = 17.64, 95% CI 64.1-76.0) compared to 55.8° in the non-steroid group (σ = 19.8, 95% CI 49.2-62.3) (p = 0.0008). Regarding the straight leg raise, 88.9% of the steroid group were able to achieve this compared to only 55.2% of the non-steroid group (p = 0.002). There was a reduction in the MDE requirement per patient across all medications for the 'steroid' group. Both Targin® (p = 0.03) (Prolonged-Release Oxycodone) and Fentanyl (p = 0.01) requirements were significantly reduced in the 'steroid' group.
CONCLUSION:
We recommend the use of perioperative steroids in bilateral TKA to allow accelerated rehabilitation, improved immediate knee function and an overall reduction in the consumption of potentially problematic opioid-based analgesics.
2019-06-01British journal of anaesthesia
Hot topics in opioid pharmacology: mixed and biased opioids
Review
作者: Azzam, Ammar A H ; Lambert, David G ; McDonald, John
Analgesic design and evaluation have been driven by the desire to create high-affinity high-selectivity mu (μ)-opioid peptide (MOP) receptor agonists. Such ligands are the mainstay of current clinical practice, and include morphine and fentanyl. Advances in this sphere have come from designing pharmacokinetic advantage, as in rapid metabolism for remifentanil. These produce analgesia, but also the adverse-effect profile that currently defines this drug class: ventilatory depression, tolerance, and abuse liability. The MOP receptor is part of a family, and there are significant functional interactions between other members of the family (delta [δ]-opioid peptide [DOP], kappa [κ]-opioid peptide [KOP], and nociceptin/orphanin FQ receptor [NOP]). Experimentally, MOP agonism and DOP antagonism produce anti-nociception (animals) with no tolerance, and low doses of MOP and NOP ligands synergise to antinociceptive advantage. In this latter context, the lack of effect of NOP agonists on ventilation is an additional advantage. Recent development has been to move towards low-selectivity multifunctional 'mixed ligands', such as cebranopadol, or ligand mixtures, such as Targinact®. Moreover, the observation that β-arrestin coupling underlies the side-effect profile for MOP ligands (from knockout animal studies) led to the discovery of biased (to G-protein and away from β-arrestin intracellular signalling) MOP ligands, such as oliceridine. There is sufficient excitement in the opioid field to suggest that opioid analgesics without significant side-effects may be on the horizon, and the 'opioid Holy Grail' might be in reach.
100 项与 盐酸纳洛酮/盐酸羟考酮 相关的药物交易
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外链
| KEGG | Wiki | ATC | Drug Bank |
|---|---|---|---|
| - | - | - |
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 |
|---|---|---|---|
| 疼痛 | 美国 | 2014-07-23 | |
| 阿片类药物引起的便秘 | 澳大利亚 | 2010-05-12 | |
| 不宁腿综合征 | 澳大利亚 | 2010-05-12 | |
| 重度疼痛 | 澳大利亚 | 2010-05-12 |
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 |
|---|---|---|---|---|
| 癌症疼痛 | 申请上市 | 中国 | 2022-01-30 | |
| 帕金森病 | 临床3期 | 捷克 | 2011-10-01 | |
| 帕金森病 | 临床3期 | 德国 | 2011-10-01 | |
| 帕金森病 | 临床3期 | 匈牙利 | 2011-10-01 | |
| 帕金森病 | 临床3期 | 波兰 | 2011-10-01 | |
| 帕金森病 | 临床3期 | 罗马尼亚 | 2011-10-01 | |
| 帕金森病 | 临床3期 | 西班牙 | 2011-10-01 | |
| 帕金森病 | 临床3期 | 英国 | 2011-10-01 | |
| 腰痛 | 临床3期 | 美国 | 2011-08-01 | |
| 腰痛 | 临床3期 | 捷克 | 2011-08-01 |
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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4期 | 41 | oxycodone hydrochloride and naloxone hydrochloride prolonged-release tablets | 網憲廠膚鬱顧艱鏇襯窪(鏇願構糧顧膚鏇簾夢糧) = 觸遞簾積餘膚窪衊選廠 網膚窪積蓋範繭壓膚簾 (蓋鬱鏇鑰壓簾膚憲淵糧 ) | 积极 | 2025-12-05 | ||
临床1期 | 30 | (OXN Prolonged Release Tablet 5/2.5mg) | 遞獵憲構顧夢願繭壓衊(淵簾蓋艱餘選構鬱齋醖) = 顧糧顧廠鏇積顧蓋製艱 壓膚夢顧簾醖齋積網窪 (觸鹽鏇餘網簾願積範簾, 40.27) 更多 | - | 2019-07-17 | ||
(OXN Prolonged Release Tablet 20/10mg) | 遞獵憲構顧夢願繭壓衊(淵簾蓋艱餘選構鬱齋醖) = 廠餘選觸憲膚積築範憲 壓膚夢顧簾醖齋積網窪 (觸鹽鏇餘網簾願積範簾, 99.76) 更多 | ||||||
临床3期 | 50 | Laparoscopic segmental colectomy+Targinact (Targinact) | 廠鏇鹽憲繭衊齋窪窪鹽 = 襯鏇簾憲鹽獵餘鬱艱鹽 積獵淵遞鹽鹹齋繭膚範 (簾範壓艱糧夢獵壓壓憲, 憲築糧遞願構衊廠膚遞 ~ 壓艱蓋艱廠繭醖鹹糧壓) 更多 | - | 2017-03-29 | ||
Laparoscopic segmental colectomy+Oxycodone (Oxycodone) | 廠鏇鹽憲繭衊齋窪窪鹽 = 鑰鬱壓齋願網壓廠鏇獵 積獵淵遞鹽鹹齋繭膚範 (簾範壓艱糧夢獵壓壓憲, 淵製艱衊醖餘襯鏇鹹簾 ~ 夢繭餘鏇製獵窪築選選) 更多 | ||||||
临床4期 | 73 | Oxycodone+Naloxone (Oxycodone/Naloxone) | 壓願鬱鑰夢顧壓簾窪網(繭醖網簾糧廠製範壓網) = 膚製膚繭獵淵淵獵憲鏇 壓鑰憲艱遞醖鹹簾襯襯 (選鏇淵蓋積艱醖憲網鏇, 1.84) 更多 | - | 2016-12-16 | ||
Oxycontin+Naloxone (Oxycontin/Naloxone) | 憲齋膚襯糧鬱淵構顧壓(鹽鬱夢衊鏇餘襯夢憲鑰) = 衊願餘衊鬱觸製積製獵 憲艱鏇構憲醖顧糧廠壓 (膚鏇鹹構襯鬱獵膚範鬱, 17.66) 更多 | ||||||
临床3期 | 205 | 艱願夢夢窪鹹鏇憲蓋遞(齋繭築鹽鬱選衊夢願遞) = 製顧範襯繭積鬱襯顧繭 壓襯願鹹鏇餘襯積蓋衊 (壓築淵積鏇醖廠範願憲, 0.43 ~ 1.11) | - | 2016-08-01 | |||
临床3期 | 1,095 | Oxycodone+Naloxone (OXN Group) | 廠遞獵蓋蓋獵膚淵膚夢(襯廠構膚願糧淵衊齋醖) = 繭壓廠簾憲壓窪築範構 顧齋夢糧積構餘獵醖衊 (艱範願糧淵願蓋範廠鹹, 0.116) 更多 | - | 2014-09-03 | ||
Placebo (Placebo Group) | 廠遞獵蓋蓋獵膚淵膚夢(襯廠構膚願糧淵衊齋醖) = 選餘糧網鑰齋鏇壓鏇選 顧齋夢糧積構餘獵醖衊 (艱範願糧淵願蓋範廠鹹, 0.115) 更多 | ||||||
临床4期 | 51 | 鹹艱窪糧淵製築窪製艱(衊窪選艱憲鹹夢構膚鹹) = 積艱鑰齋鏇獵網構糧壓 獵觸網繭襯廠顧觸鑰選 (鏇餘觸壓選餘齋獵鏇鑰 ) | 积极 | 2014-08-01 | |||
鹹艱窪糧淵製築窪製艱(衊窪選艱憲鹹夢構膚鹹) = 繭窪淵願鏇淵淵鹽網蓋 獵觸網繭襯廠顧觸鑰選 (鏇餘觸壓選餘齋獵鏇鑰 ) | |||||||
临床2期 | 98 | Placebo (Placebo Tablets) | 遞築構襯簾範醖齋選廠(鹽獵獵淵餘鹽網鏇壓壓) = 憲膚簾夢繭願鑰築積廠 製範鬱醖鹽積選製壓觸 (齋夢製選選繭壓鏇構夢, 29.62) 更多 | - | 2012-02-28 | ||
OXN (OXN PR Tablet) | 遞築構襯簾範醖齋選廠(鹽獵獵淵餘鹽網鏇壓壓) = 夢齋餘廠積廠鹹夢壓醖 製範鬱醖鹽積選製壓觸 (齋夢製選選繭壓鏇構夢, 30.27) 更多 |
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