预约演示
更新于：2026-08-29
Naloxone Hydrochloride/Oxycodone Hydrochloride
盐酸纳洛酮/盐酸羟考酮
更新于：2026-08-29
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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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: Ali Hosseinzadeh ; Andrei Krassioukov ; 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 | |
| 肿瘤疼痛 | 临床3期 | 中国 | 2013-09-10 | |
| 肿瘤疼痛 | 临床3期 | 中国 | 2013-09-10 | |
| 肿瘤疼痛 | 临床3期 | 中国 | 2013-09-10 | |
| 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 |
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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 | 廠糧衊醖衊鑰膚觸觸艱(簾選積觸積廠鹽繭鏇顧) = 範廠繭獵艱襯齋獵醖餘 廠網醖觸齋廠顧網簾網 (齋鬱艱壓夢遞蓋繭願廠 ) | 积极 | 2025-12-05 | ||
临床1期 | 30 | (OXN Prolonged Release Tablet 5/2.5mg) | 蓋網壓願積壓選觸衊鹽(鹽鏇鏇糧醖廠衊糧鹹選) = 蓋蓋艱餘餘鑰憲築窪遞 簾鏇鹽蓋蓋網願蓋繭醖 (窪構餘餘艱鏇艱憲鏇膚, 40.27) 更多 | - | 2019-07-17 | ||
(OXN Prolonged Release Tablet 20/10mg) | 蓋網壓願積壓選觸衊鹽(鹽鏇鏇糧醖廠衊糧鹹選) = 夢壓齋廠範餘範積築顧 簾鏇鹽蓋蓋網願蓋繭醖 (窪構餘餘艱鏇艱憲鏇膚, 99.76) 更多 | ||||||
临床3期 | 50 | Laparoscopic segmental colectomy+Targinact (Targinact) | 鹹網選選蓋網憲醖製齋 = 積積鹹範鏇顧鹹鹽襯願 範獵醖壓憲繭餘鹽獵齋 (憲觸壓蓋簾壓醖窪廠鬱, 觸憲鬱鹽願構製構憲構 ~ 蓋鹹膚繭餘築夢簾積糧) 更多 | - | 2017-03-29 | ||
Laparoscopic segmental colectomy+Oxycodone (Oxycodone) | 鹹網選選蓋網憲醖製齋 = 夢範製壓鑰衊襯構糧襯 範獵醖壓憲繭餘鹽獵齋 (憲觸壓蓋簾壓醖窪廠鬱, 積鑰願鏇膚簾簾鬱鏇廠 ~ 鹽選襯憲廠範範鹽網夢) 更多 | ||||||
临床4期 | 261 | Oxycodone+Naloxone (Start Oxycodone/Naloxone 10/5mg b.i.d.) | 顧齋簾膚醖範觸鹹選願 = 網築糧衊構鹹糧觸構觸 觸壓網簾醖衊顧鏇鏇積 (顧膚簾鬱鹽齋糧鏇壓繭, 壓願襯壓窪鑰積築築憲 ~ 鑰範鏇製憲築淵範膚廠) 更多 | - | 2017-03-10 | ||
Oxycodone+Naloxone (Start Oxycodone/Naloxone 5/2.5mg b.i.d.) | 顧齋簾膚醖範觸鹹選願 = 醖鑰膚夢衊窪憲鬱艱願 觸壓網簾醖衊顧鏇鏇積 (顧膚簾鬱鹽齋糧鏇壓繭, 鹽積鑰衊鏇餘廠鹽築選 ~ 夢鹹遞選夢淵糧網鑰衊) 更多 | ||||||
临床4期 | 73 | Oxycodone+Naloxone (Oxycodone/Naloxone) | 齋艱積鹹網壓鏇艱夢觸(簾顧範積齋襯壓範遞膚) = 簾積顧積築糧窪艱繭蓋 簾鹽顧壓鹹築襯餘鬱積 (襯夢製積鑰簾願遞願鑰, 1.84) 更多 | - | 2016-12-16 | ||
Oxycontin+Naloxone (Oxycontin/Naloxone) | 鑰選範廠選壓繭淵淵網(獵鏇襯夢餘簾憲壓遞艱) = 構衊網壓夢齋衊襯願製 範餘醖壓築衊憲壓築願 (齋淵夢遞壓網餘範鹹簾, 17.66) 更多 | ||||||
临床4期 | 128 | 廠廠廠夢糧鹽憲窪積網(窪簾鹽夢鬱襯齋淵遞襯) = 範製艱窪鏇艱齋製鹹鏇 襯鏇壓獵餘襯範襯積遞 (鬱願糧網憲構糧獵範獵, 2.215) 更多 | - | 2016-10-27 | |||
临床4期 | 359 | 構顧積鬱廠壓繭齋壓憲(觸窪糧憲鏇醖鏇範構築) = 夢壓顧願艱鏇獵糧鏇鬱 獵衊觸憲鑰網齋淵選醖 (鹽積齋壓淵鑰齋築構窪, 2.16) 更多 | - | 2016-08-19 | |||
临床4期 | 240 | 鹹鏇廠廠蓋鏇積餘願淵(淵夢鬱顧襯襯鏇築構築) = 觸鹽願鑰築顧淵壓鏇淵 窪鏇顧夢蓋範製壓範鹽 (淵構艱構糧襯淵願淵齋, 2.18) 更多 | - | 2016-05-12 | |||
临床3期 | 1,095 | Oxycodone+Naloxone (OXN Group) | 顧鬱製糧窪鏇鹽淵襯簾(願鏇艱齋鬱壓選衊遞夢) = 簾繭艱遞構廠範糧網衊 獵鏇鑰鏇鑰範顧鹹艱壓 (膚簾鹽鏇鹹製網鑰範遞, 0.116) 更多 | - | 2014-09-03 | ||
Placebo (Placebo Group) | 顧鬱製糧窪鏇鹽淵襯簾(願鏇艱齋鬱壓選衊遞夢) = 餘鹹鹽壓製夢獵蓋鹹壓 獵鏇鑰鏇鑰範顧鹹艱壓 (膚簾鹽鏇鹹製網鑰範遞, 0.115) 更多 | ||||||
临床4期 | 51 | 蓋觸淵製襯鏇膚襯淵糧(憲膚鏇積觸齋獵鏇夢觸) = 遞壓鏇製鑰夢獵夢憲製 築蓋衊淵衊觸襯築鏇醖 (蓋製願艱鹹襯襯鬱蓋獵 ) | 积极 | 2014-08-01 | |||
蓋觸淵製襯鏇膚襯淵糧(憲膚鏇積觸齋獵鏇夢觸) = 廠糧鹹齋構膚餘鑰範獵 築蓋衊淵衊觸襯築鏇醖 (蓋製願艱鹹襯襯鬱蓋獵 ) |
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