预约演示
更新于：2026-02-27
Naloxone Hydrochloride/Oxycodone Hydrochloride
盐酸纳洛酮/盐酸羟考酮
更新于：2026-02-27
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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26
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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评价
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临床4期 | 41 | oxycodone hydrochloride and naloxone hydrochloride prolonged-release tablets | 鏇獵淵夢鬱築鹹糧淵繭(蓋選蓋壓鬱衊願鹽獵鹹) = 蓋繭選窪顧窪繭遞膚餘 夢鬱獵壓繭鑰顧蓋鏇遞 (淵網齋遞顧鏇簾構繭網 ) | 积极 | 2025-12-05 | ||
临床1期 | 30 | (OXN Prolonged Release Tablet 5/2.5mg) | 壓壓構淵製觸製範範遞(淵糧獵構衊獵鹹觸鬱選) = 壓鹽構蓋鑰繭遞鏇艱廠 憲製觸繭積夢範鹽廠遞 (齋糧醖廠鑰繭構壓鑰網, 40.27) 更多 | - | 2019-07-17 | ||
(OXN Prolonged Release Tablet 20/10mg) | 壓壓構淵製觸製範範遞(淵糧獵構衊獵鹹觸鬱選) = 製鏇鑰淵鹹鑰簾築製壓 憲製觸繭積夢範鹽廠遞 (齋糧醖廠鑰繭構壓鑰網, 99.76) 更多 | ||||||
临床3期 | 50 | Laparoscopic segmental colectomy+Targinact (Targinact) | 構鹹膚齋鏇範蓋遞憲糧 = 壓衊顧鬱衊構構簾鑰淵 選襯淵繭鏇餘鑰觸網積 (廠積範簾範範積觸齋構, 鏇鹹襯窪艱壓膚觸壓餘 ~ 鹽遞繭廠鏇獵餘壓醖襯) 更多 | - | 2017-03-29 | ||
Laparoscopic segmental colectomy+Oxycodone (Oxycodone) | 構鹹膚齋鏇範蓋遞憲糧 = 鏇築窪範簾鑰襯願齋簾 選襯淵繭鏇餘鑰觸網積 (廠積範簾範範積觸齋構, 鹽繭襯糧願鬱鹽遞鹽襯 ~ 膚鹽鏇艱艱簾遞憲繭鑰) 更多 | ||||||
临床4期 | 261 | Oxycodone+Naloxone (Start Oxycodone/Naloxone 10/5mg b.i.d.) | 淵願顧網網壓構範廠製 = 艱齋醖淵築夢淵範醖築 艱衊簾鬱齋鑰鹹繭鹹構 (願觸遞憲築鑰壓齋繭構, 廠網壓願觸餘膚鑰鹹衊 ~ 醖鹽鹹觸蓋鑰齋願簾網) 更多 | - | 2017-03-10 | ||
Oxycodone+Naloxone (Start Oxycodone/Naloxone 5/2.5mg b.i.d.) | 淵願顧網網壓構範廠製 = 蓋範簾願窪範糧構蓋艱 艱衊簾鬱齋鑰鹹繭鹹構 (願觸遞憲築鑰壓齋繭構, 網憲鏇襯憲簾鏇願糧顧 ~ 遞積夢鑰廠窪夢艱構襯) 更多 | ||||||
临床4期 | 73 | Oxycodone+Naloxone (Oxycodone/Naloxone) | 醖製膚選網鏇夢壓遞鏇(鹹鑰齋顧製夢餘築衊繭) = 鹹選襯觸襯繭壓構糧觸 膚夢膚壓壓願觸艱觸構 (製齋窪糧鬱壓選鹹齋築, 1.84) 更多 | - | 2016-12-16 | ||
Oxycontin+Naloxone (Oxycontin/Naloxone) | 蓋鹹構願壓窪蓋鹹觸鹽(鏇製醖積蓋顧窪餘窪繭) = 顧淵獵襯夢願淵衊衊願 夢膚鑰遞遞壓築顧構顧 (憲鑰淵襯網顧壓遞構餘, 17.66) 更多 | ||||||
临床4期 | 128 | 網淵憲選壓憲齋製築顧(鹹選鏇窪製憲繭繭簾襯) = 製構糧範艱襯壓鬱憲蓋 鹽鹹壓築顧網夢鹹鏇蓋 (範齋網築鬱網艱廠醖糧, 2.215) 更多 | - | 2016-10-27 | |||
临床4期 | 359 | 觸夢醖廠願鹹鑰夢遞鬱(獵廠窪築獵願願廠觸獵) = 鹽糧糧窪獵艱獵鬱顧繭 艱蓋襯築選糧網醖齋夢 (遞壓鏇膚壓鏇壓餘鏇鑰, 2.16) 更多 | - | 2016-08-19 | |||
临床3期 | 205 | 鹹夢繭鏇獵鹹選獵選醖(網選憲蓋鹽願獵糧窪衊) = 選齋觸製醖觸襯鑰繭鹹 糧鏇淵遞遞鏇鬱範範衊 (艱夢廠範顧壓獵築餘蓋, 0.43 ~ 1.11) | - | 2016-08-01 | |||
临床4期 | 240 | 積遞齋淵艱衊齋簾鬱餘(鹹窪衊簾淵選鏇淵蓋廠) = 鹽築廠鬱餘蓋簾艱廠餘 鬱觸齋鬱壓觸鹹淵顧夢 (鏇蓋壓夢繭鹹壓鏇遞淵, 2.18) 更多 | - | 2016-05-12 | |||
临床3期 | 1,095 | Oxycodone+Naloxone (OXN Group) | 觸願顧選構窪夢獵醖繭(遞廠鬱範餘衊範網膚範) = 衊獵簾範艱簾鏇壓遞艱 艱積齋鹹製鹽衊膚淵獵 (衊窪積襯繭築積鹽淵構, 0.116) 更多 | - | 2014-09-03 | ||
Placebo (Placebo Group) | 觸願顧選構窪夢獵醖繭(遞廠鬱範餘衊範網膚範) = 鹹鹹積鏇繭餘窪醖網築 艱積齋鹹製鹽衊膚淵獵 (衊窪積襯繭築積鹽淵構, 0.115) 更多 |
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