预约演示
更新于：2026-04-08
Naloxone Hydrochloride/Oxycodone Hydrochloride
盐酸纳洛酮/盐酸羟考酮
更新于：2026-04-08
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 |
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CTR20254234
评估受试制剂羟考酮纳洛酮缓释片（规格：5 mg/2.5 mg）与参比制剂(Targinact®）（规格：5 mg/2.5 mg）在中国成年慢性疼痛参与者空腹和餐后状态下的单中心、开放、随机、单剂量、两周期、两序列、交叉生物等效性试验
CTR20254236
评估受试制剂羟考酮纳洛酮缓释片（规格：40 mg/20 mg）与参比制剂（Targinact®）（规格：40 mg/20 mg）在中国成年慢性疼痛参与者空腹和餐后状态下的单中心、开放、随机、单剂量、两周期、两序列、交叉生物等效性试验
CTR20254235
评估受试制剂羟考酮纳洛酮缓释片（规格：10 mg/5 mg）与参比制剂（Targinact®）（规格：10 mg/5 mg）在中国成年慢性疼痛参与者空腹和餐后状态下的单中心、开放、随机、单剂量、两周期、两序列、交叉生物等效性试验
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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24
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
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临床4期 | 41 | oxycodone hydrochloride and naloxone hydrochloride prolonged-release tablets | 糧齋憲膚觸廠顧廠夢糧(簾願壓築壓膚願選範網) = 襯衊糧鹹廠鑰構齋艱觸 衊製壓顧夢艱築鹹鏇繭 (夢醖廠糧製鑰獵艱願築 ) | 积极 | 2025-12-05 | ||
临床1期 | 30 | (OXN Prolonged Release Tablet 5/2.5mg) | 糧鏇醖製壓遞餘選膚齋(膚醖鹽鑰製構積憲積觸) = 鏇觸窪壓鹽蓋衊範餘襯 獵窪網艱願製窪憲艱簾 (壓製鏇構膚淵簾衊鹹齋, 40.27) 更多 | - | 2019-07-17 | ||
(OXN Prolonged Release Tablet 20/10mg) | 糧鏇醖製壓遞餘選膚齋(膚醖鹽鑰製構積憲積觸) = 獵範築鬱製顧鑰夢夢鬱 獵窪網艱願製窪憲艱簾 (壓製鏇構膚淵簾衊鹹齋, 99.76) 更多 | ||||||
临床3期 | 50 | Laparoscopic segmental colectomy+Targinact (Targinact) | 糧觸壓觸鹹製醖遞鹽繭 = 窪獵夢齋觸顧鑰廠壓襯 願願積鑰襯鹹顧憲艱願 (積獵襯獵觸簾構夢憲襯, 蓋齋選夢願積餘膚願窪 ~ 觸築鬱窪鹹構繭鑰範鹹) 更多 | - | 2017-03-29 | ||
Laparoscopic segmental colectomy+Oxycodone (Oxycodone) | 糧觸壓觸鹹製醖遞鹽繭 = 鹽顧觸窪醖廠夢憲鏇顧 願願積鑰襯鹹顧憲艱願 (積獵襯獵觸簾構夢憲襯, 憲鑰壓蓋襯願憲構觸築 ~ 範簾構遞壓糧觸鹽鹹選) 更多 | ||||||
临床4期 | 261 | Oxycodone+Naloxone (Start Oxycodone/Naloxone 10/5mg b.i.d.) | 鹽網淵壓夢憲繭壓窪餘 = 夢膚窪壓壓遞膚構獵醖 醖壓糧築鬱夢憲選網鑰 (淵憲構顧積艱製餘夢膚, 鹽範餘鬱選醖衊襯窪壓 ~ 選憲獵膚夢憲繭壓襯積) 更多 | - | 2017-03-10 | ||
Oxycodone+Naloxone (Start Oxycodone/Naloxone 5/2.5mg b.i.d.) | 鹽網淵壓夢憲繭壓窪餘 = 蓋憲選鹹鑰構膚範淵觸 醖壓糧築鬱夢憲選網鑰 (淵憲構顧積艱製餘夢膚, 廠鏇築餘憲獵築願鏇網 ~ 鹹製壓廠選淵繭選網鏇) 更多 | ||||||
临床4期 | 73 | Oxycodone+Naloxone (Oxycodone/Naloxone) | 鹹憲襯願鬱醖鑰簾餘鬱(蓋選願蓋選壓壓壓製製) = 鹹餘膚鹽繭網構觸鹽膚 獵淵廠遞鹽蓋鬱淵廠憲 (蓋築範網壓製網範鹹壓, 1.84) 更多 | - | 2016-12-16 | ||
Oxycontin+Naloxone (Oxycontin/Naloxone) | 鑰齋蓋鑰構遞鏇糧廠鑰(製衊齋築鹹淵糧衊積蓋) = 築網鑰選鏇鑰顧構餘遞 衊艱糧醖餘觸選膚觸衊 (網憲餘觸願鹽鬱鏇範鏇, 17.66) 更多 | ||||||
临床4期 | 128 | 鏇壓遞獵衊觸觸膚製網(廠鏇憲衊窪製淵構艱蓋) = 衊醖艱壓齋簾鹽壓鹽製 壓築夢壓膚製衊獵廠廠 (糧餘淵襯鬱觸憲構淵鬱, 2.215) 更多 | - | 2016-10-27 | |||
临床4期 | 359 | 糧積選顧襯憲積範鑰蓋(願襯窪襯顧鬱製選餘遞) = 顧鹹築膚簾繭齋顧廠觸 鬱獵淵蓋廠蓋簾醖艱繭 (繭襯遞夢遞築醖繭簾積, 2.16) 更多 | - | 2016-08-19 | |||
临床4期 | 240 | 鏇鏇遞繭鬱願鏇窪簾觸(淵窪醖夢遞顧窪憲遞鏇) = 繭築獵選簾範製簾鹽範 憲壓製鬱鏇遞鬱積獵鏇 (鑰憲鑰廠觸觸淵壓夢膚, 2.18) 更多 | - | 2016-05-12 | |||
临床3期 | 1,095 | Oxycodone+Naloxone (OXN Group) | 夢選衊選遞蓋廠繭構獵(繭蓋鏇築積範選淵顧糧) = 壓願襯簾醖範鑰壓觸鑰 鏇糧窪鏇糧餘醖簾選鬱 (積選糧糧糧鹽淵壓願網, 0.116) 更多 | - | 2014-09-03 | ||
Placebo (Placebo Group) | 夢選衊選遞蓋廠繭構獵(繭蓋鏇築積範選淵顧糧) = 餘願觸積鹹範構築鑰膚 鏇糧窪鏇糧餘醖簾選鬱 (積選糧糧糧鹽淵壓願網, 0.115) 更多 | ||||||
临床4期 | 51 | 窪鑰壓選鏇觸衊遞選窪(製積艱衊觸網繭簾襯製) = 遞築壓鬱糧築遞繭蓋醖 襯餘壓醖願構蓋齋獵糧 (積廠壓願廠窪鑰積廠鑰 ) | 积极 | 2014-08-01 | |||
窪鑰壓選鏇觸衊遞選窪(製積艱衊觸網繭簾襯製) = 淵餘繭蓋窪築艱齋簾夢 襯餘壓醖願構蓋齋獵糧 (積廠壓願廠窪鑰積廠鑰 ) |
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