A simple and rapid liquid chromatography-tandem mass spectrometry （LC-MS/MS） method was de- veloped and validated for simultaneous determination of acetaminophen and oxycodone in human plasma. Acetaminophen-d4 and o...A simple and rapid liquid chromatography-tandem mass spectrometry （LC-MS/MS） method was de- veloped and validated for simultaneous determination of acetaminophen and oxycodone in human plasma. Acetaminophen-d4 and oxycodone-d3 were used as internal standards. The challenge en- countered in the method development that the high plasma concentration level of acetaminophen made the MS response saturated while the desired lower limit of quantification （LLOQ,） for oxycodone was hard to reach was well solved. The analytes were extracted by protein precipitation using acetonitrile. The matrix effect of the analytes was avoided by chromatographic separation using a hydrophilic C18 column coupled with gradient elution. Multiple reaction monitoring in positive ion mode was performed on tandem mass spectrometer employing electrospray ion source. The calibration curves were linear over the concentration ranges of 40.0-8000 ng/mL and 0.200-40.0 ng/mL for acetaminophen and oxycodone, respectively. This method, which could contribute to high throughput analysis and better clinical drug monitoring, was successfully applied to a pharmacokinetic study in healthy Chinese volunteers.展开更多
BACKGROUND:To describe trends in oxycodone and oxycodone-containing analgesic prescribing for the treatment of back pain among adults in emergency departments(EDs) in the USA from 2007 to 2018.METHODS:Data were gather...BACKGROUND:To describe trends in oxycodone and oxycodone-containing analgesic prescribing for the treatment of back pain among adults in emergency departments(EDs) in the USA from 2007 to 2018.METHODS:Data were gathered from the National Hospital Ambulatory Medical Care Survey(NHAMCS) from 2007 to 2018.The study population included individuals of all ages presenting to USA EDs.The NHAMCS reasons for visit and oxycodone drug ID codes were used to isolate patients with back pain.The main outcome was the proportion of oxycodone and oxycodone-containing analgesics prescribed for back pain in the EDs over the specified time period.RESULTS:There was a relative decrease in the overall administration of oxycodone for back pain in the EDs by 62.3% from 2007(244,000 visits) to 2018(92,000 visits).The proportion of ED patients prescribed with oxycodone-containing analgesics for back pain increased among patients aged 45 years and older(from 43.8% to 57.6%),female patients(from 54.5% to 62.0%),black patients(from 22.5% to 30.4%),and Hispanic/Latino patients(from 9.4% to 19.6%).Oxycodone/acetaminophen was most prescribed and accounted for 90.2% of all oxycodone-containing analgesics in 2007,with a decrease to 68.5% in 2018.Pure oxycodone was the second most prescribed medication,accounting for 6.1% in 2007 and 31.5% in 2018.CONCLUSION:The overall number of oxycodone-containing analgesics decreased significantly from 2007 to 2018.However,that number trended upward in 45-year-old and older,female,black,or Hispanic/Latino patients from 2007 to 2018.The total amount of pure oxycodone increased significantly from 2007 to 2008.展开更多
BACKGROUND High levels of acetaminophen(APAP)consumption can result in significant liver toxicity.Mogroside V(MV)is a bioactive,plant-derived triterpenoid known for its various pharmacological activities.However,the i...BACKGROUND High levels of acetaminophen(APAP)consumption can result in significant liver toxicity.Mogroside V(MV)is a bioactive,plant-derived triterpenoid known for its various pharmacological activities.However,the impact of MV on acute liver injury(ALI)is unknown.AIM To investigate the hepatoprotective potential of MV against liver damage caused by APAP and to examine the underlying mechanisms.METHODS Mice were divided into three groups:Saline,APAP and APAP+MV.MV(10 mg/kg)was given intraperitoneally one hour before APAP(300 mg/kg)administration.Twenty-four hours after APAP exposure,serum transaminase levels,liver necrotic area,inflammatory responses,nitrotyrosine accumulation,and c-jun-N-terminal kinase(JNK)activation were assessed.Additionally,we analyzed reactive oxygen species(ROS)levels,JNK activation,and cell death in alpha mouse liver 12(AML12)cells.RESULTS MV pre-treatment in vivo led to a reduction in the rise of aspartate transaminase and alanine transaminase levels,mitigated liver damage,decreased nitrotyrosine accumulation,and blocked JNK phosphorylation resulting from APAP exposure,without affecting glutathione production.Similarly,MV diminished the APAP-induced increase in ROS,JNK phosphorylation,and cell death in vitro.CONCLUSION Our study suggests that MV treatment alleviates APAP-induced ALI by reducing ROS and JNK activation.展开更多
Background: Controlled-release oxycodone/naloxone(OXN-CR) maintains the effect of opioid-induced analgesia through oxycodone while reducing the occurrence rate of opioid-induced constipation through naloxone. The pres...Background: Controlled-release oxycodone/naloxone(OXN-CR) maintains the effect of opioid-induced analgesia through oxycodone while reducing the occurrence rate of opioid-induced constipation through naloxone. The present study was designed to assess the non-inferiority of OXN-CR to controlled-release oxycodone(OX-CR) for the control of cancer-related pain in Korean patients.Methods: In this randomized, open-labeled, parallel-group, phase IV study, we enrolled patients aged 20 years or older with moderate to severe cancer-related pain [numeric rating scale(NRS) pain score ≥4] from seven Korean oncology/hematology centers. Patients in the intention-to-treat(ITT) population were randomized(1:1) to OXNCR or OX-CR groups. OXN-CR was administered starting at 20 mg/10 mg per day and up-titrated to a maximum of80 mg/40 mg per day for 4 weeks, and OX-CR was administered starting at 20 mg/day and up-titrated to a maximum of 80 mg/day for 4 weeks.The primary efficacy endpoint was the change in NRS pain score from baseline to week4, with non-inferiority margin of-1.5. Secondary endpoints included analgesic rescue medication intake, patientreported change in bowel habits, laxative intake, quality of life(QoL), and safety assessments.Results: Of the ITT population comprising 128 patients, 7 with missing primary efficacy data and 4 who violated the eligibility criteria were excluded from the efficacy analysis. At week 4, the mean change in NRS pain scores was not significantly different between the OXN-CR group(n = 58) and the OX-CR group(n = 59)(-1.586 vs.-1.559,P = 0.948). The lower limit of the one-sided 95% confidence interval(-0.776 to 0.830) for the difference exceeded the non-inferiority margin(P < 0.001). The OXN-CR and OX-CR groups did not differ significantly in terms of analgesic rescue medication intake, change in bowel habits, laxative intake, QoL, and safety assessments.Conclusions: OXN-CR was non-inferior to OX-CR in terms of pain reduction after 4 weeks of treatment and had a similar safety profile. Studies in larger populations of Korean patients with cancer-related pain are needed to further investigate the effectiveness of OXN-CR for long-term pain control and constipation alleviation.Trial registration ClinicalTrials.gov NCT01313780, registered March 8。展开更多
To review the research progress of pure opioid receptor agonist oxycodone.The research progress of oxycodone in terms of pharmacokinetics,pharmacodynamics,adverse reactions,clinical application,combined medication and...To review the research progress of pure opioid receptor agonist oxycodone.The research progress of oxycodone in terms of pharmacokinetics,pharmacodynamics,adverse reactions,clinical application,combined medication and new progress in clinical application was summarized by referring to the literature.Oxycodone is a semi-synthetic thebaine derivative of opioid alkaloids,and is a pure opioidμandκreceptor agonist.The main action sites are the central nervous system and visceral smooth muscle.Due to its advantages of low adverse reactions,good analgesic effects,and a wide range of safe doses,the drug has been widely used in the control of acute and chronic postoperative pain,as well as malignant and non-malignant pain.Since the end of the 20^(th) century,researchers have begun to formulate antipyretic analgesics,opioid receptor agonists,opioid receptor antagonists,dopamine receptor antagonists and other drugs with oxycodone in different proportions to enhance the analgesic effect.At the same time,it can reduce the dosage of oxycodone and reduce its adverse reactions,so as to achieve the purpose of limiting opioid abuse.With the continuous research on the efficacy and safety of oxycodone in the perioperative period at home and abroad,oxycodone has become the only dual-opioid potent analgesic that can be used in clinical work.展开更多
Objective:To study the effect of dexmedetomidine combined with oxycodone on systemic stress response in recovery period of gynecological laparoscopic operation.Methods:A total of 86 patients who received laparoscopic ...Objective:To study the effect of dexmedetomidine combined with oxycodone on systemic stress response in recovery period of gynecological laparoscopic operation.Methods:A total of 86 patients who received laparoscopic operation in the Second Affiliated Hospital of Kunming Medical University between June 2014 and December 2016 were selected and randomly divided into the dexmedetomidine combined with oxycodone group (DO group) and control group (C group). Before anesthesia induction (T1), at the end of the surgery and before micro pump injection of dexmedetomidine and oxycodone hydrochloride (T2) and in recovery period (T3), serum levels of pituitary-target gland axis-related hormones, vascular activity-related hormones and oxidative stress-related molecules were determined.Results: At T1 and T2, serum TSH, T3, T4, ACTH, Cor, NE, E, ADH, AT-II, ROS, MDA, SOD and HO-1 levels of DO group were not significantly different from those of C group;at T3, serum TSH, T3, T4, ACTH, Cor, NE, E, ADH, AT-II, ROS and MDA levels of DO group were significantly lower than those of C group while SOD and HO-1 levels were significantly higher than those of C group.Conclusions: Dexmedetomidine combined with oxycodone can inhibit the systemic stress response in recovery of gynecological laparoscopic operation.展开更多
Background: Post-craniotomy pain has been reported to be moderate to severe. Management of post-craniotomy pain is often inadequate, yet limited by the side effects of opioids. We aim to find out the efficacy of oral ...Background: Post-craniotomy pain has been reported to be moderate to severe. Management of post-craniotomy pain is often inadequate, yet limited by the side effects of opioids. We aim to find out the efficacy of oral oxycodone as compared to oral codeine for the treatment of post-craniotomy pain in our institution. Methods: A randomized, double-blinded controlled trial was used to evaluate the efficacy of oral oxycodone versus oral codeine. 40 patients were randomized to the control group of codeine (n = 20) or the experimental group receiving oxycodone (n = 20) in addition to regular oral paracetamol for both groups of patients. Results: There was no difference in the visual analogue scale scores at 24 hours (2.78 versus 1.85, p = 0.11) or side effects in the oxycodone group compared with the codeine group. Conclusions: Oral oxycodone had similar efficacy as oral codeine in the management of post-craniotomy pain.展开更多
Oxycodone hydrochloride is a semi-synthetic opioid agonist that provides very effective relief for moderate to severe pain in cancer and post-operative patients. Controlled release oxycodone formulations have been stu...Oxycodone hydrochloride is a semi-synthetic opioid agonist that provides very effective relief for moderate to severe pain in cancer and post-operative patients. Controlled release oxycodone formulations have been studied to enhance the therapeutic effect by providing constant release over the whole dosing interval and improve patient’s convenience by reducing the frequency of administration as well.展开更多
Backgroud:Intravenous opioid patient-controlled analgesia(IV-PCA)has been suggested as an effective method in postoperative pain management.There are several randomized controlled trials(RCTs)of comparison of oxycodon...Backgroud:Intravenous opioid patient-controlled analgesia(IV-PCA)has been suggested as an effective method in postoperative pain management.There are several randomized controlled trials(RCTs)of comparison of oxycodone and fentanyl for IV-PCA in surgical patients.The purpose of this study was to perform a meta-analysis to compare the efficacy and safety of oxycodone and fentanyl for IV-PCA in surgical patients from current data.Methods:The RCTs of oxycodone versus fentanyl for IV-PCA were gathered from PubMed,Embase,Cochrane library,CNKI and VIP data.After data extraction and quality assessment of the included RCTs,the RevMan 5.3 software was applied for meta-analysis of numerical rating scale(NRS)scores,accumulated IV-PCA consumption of oxycodone and fentanyl,patient satisfaction,postoperative nausea and vomiting(PONV),and other adverse events(AEs).Results:Results reported from eight RCTs involving 600 patients are included in the meta-analysis.The NRS score at rest and upon movement of group oxycodone was significantly lower than that of group fentanyl(WMD=-3.85,95%CI-4.93^-2.76,P<0.00001;WMD=-4.31,95%CI-5.79^-2.84,P<0.00001);however,the incidence of PONV and dizziness was obviously increased in group oxycodone than in group fentanyl(OR=2.41,95%CI 1.60~3.63,P<0.0001;OR=3.69,95%CI 2.17~6.26,P<0.00001).Accumulated IV-PCA consumption in group oxycodone was less than in group fentanyl overall the 48 hours postoperatively(WMD=-12.11,95%CI-18.42^-5.80,P=0.0002).There was no significant difference in patient satisfaction between oxycodone and fentanyl(OR=0.73,95%CI 0.11~5.04,P=0.75).Conclusion:According to the evidence,this meta-analysis suggest that oxycodone for IV-PCA is superior to fentanyl in postoperative pain relief,whereas the higher incidence of PONV and dizziness was accompanied with oxycodone.Further large-scale,prospective,observational studies are needed to summarize and analyse the data to draw a fair conclusion.展开更多
Objective:To study the effects of oxycodone and fentanyl patient-controlled intravenous analgesia on pain, immune response and stress response after laparoscopic surgery.Methods:Patients undergoing laparoscopic surger...Objective:To study the effects of oxycodone and fentanyl patient-controlled intravenous analgesia on pain, immune response and stress response after laparoscopic surgery.Methods:Patients undergoing laparoscopic surgery in Xianning Central Hospital between June 2015 and February 2017 were selected and randomly divided into oxycodone group and fentanyl group who received postoperative oxycodone and fentanyl patient-controlled intravenous analgesia respectively. 3 d after surgery and 5 d after surgery, the serum contents of pain-related transmitters, immune indexes, stress-related molecules as well as peripheral blood contents of immune cells were measured.Results: 3 d after surgery and 5 d after surgery, CRP, TNF-α, IL-8, sICAM-1, YKL-40, Cor, C-P, FT3, FT4 and HO-1 contents in serum of oxycodone group were significantly lower than those of fentanyl group whereas CD3+CD4+T cell and CD3+CD8+T cell contents in peripheral blood as well as C3 and C4 contents in serum were significantly higher than those of fentanyl group.Conclusion:oxycodone patient-controlled intravenous analgesia after laparoscopic surgery is better than fentanyl and can reduce the pain degree, inhibit the stress response and improve the immune response.展开更多
Objective： To study the effect of the transdermal preparation of traditional Chinese medicine in treating cancer pain. Methods： From October 2016 to January 2018, 126 patients with cancer pain were enrolled and divi...Objective： To study the effect of the transdermal preparation of traditional Chinese medicine in treating cancer pain. Methods： From October 2016 to January 2018, 126 patients with cancer pain were enrolled and divided into 4 groups, 39 patients in group A （directed TCM permeation）, 26 patients in group B （oxycodone sustained-release tablets）, 32 patients in group C （Chinese medicine directed drug penetration ＋ oxycodone sustained-release tablets）, and 29 patients group D （Chinese medicine directed drug penetration ＋ oxycodone sustained-release tablets ＋ nimesulide sustained release tablets）, according to KPS scores. Results： Transdermal preparations of traditional Chinese medicine can significantly alleviate cancer pain. For the treatment of moderate to severe cancer pain, the Chinese medicine transdermal preparation can reduce the dosage of oxycodone sustained-release tablets. At the same time, the patient＇s KPS and NRS scores were significantly reduced. Moreover, the transdermal preparation of traditional Chinese medicine has a better therapeutic effect on visceral pain. Conclusion： The traditional Chinese medicine tra_nsdermal preparation combined with western medicine for the treatment of cancer pain may be a new method for the treatment of cancer pain.展开更多
Objective: To discuss the analgesic effect of oxycodone combined with parecoxib sodium after laparoscopic cholecystectomy and its influence on inflammatory stress response. Methods:A total of 260 patients with chronic...Objective: To discuss the analgesic effect of oxycodone combined with parecoxib sodium after laparoscopic cholecystectomy and its influence on inflammatory stress response. Methods:A total of 260 patients with chronic cholecystitis who accepted laparoscopic cholecystectomy in this hospital between December 2016 and May 2017 were divided into control group (n=130) and oxycodone group (n=130) by random number table method. Control group received morphine combined with parecoxib sodium analgesia after operation, and oxycodone group received oxycodone combined with parecoxib sodium analgesia after operation. The differences in serum levels of pain mediators, inflammatory mediators and stress hormones were compared between the two groups immediately after operation (T0), 12 h after operation (T1) and 24 h after operation (T3). Results: At T0, there was no statistically significant difference in serum levels of pain mediators, inflammatory mediators and stress hormones between the two groups. At T1 and T2, serum pain mediators PGE2, NPY, SP and NGF levels of oxycodone group were lower than those of control group whereas β-EP levels were higher than those of control group;serum inflammatory mediators CRP, IL-1β, IL-6 and TNF-αlevels were lower than those of control group;serum stress hormones Cor, NE and INS levels were lower than those of control group. Conclusion: Oxycodone combined with parecoxib sodium analgesia after laparoscopic cholecystectomy can effectively relieve the pain perception and inhibit the systemic inflammatory response and stress response.展开更多
Objective:To investigate the effect of oxycodone hydrochloride injection preemptive analgesia on serum inflammatory factors, neurotransmitter index and immune function in patients with laparoscopic cholecystectomy.Met...Objective:To investigate the effect of oxycodone hydrochloride injection preemptive analgesia on serum inflammatory factors, neurotransmitter index and immune function in patients with laparoscopic cholecystectomy.Methods: According to random data table, 113 patients undergoing laparoscopic cholecystectomy were divided into control group (n=57) and observation group (n=56), patients in the control group were treated with sufentanil citrate injection analgesia, and the observation group patients were given oxycodone hydrochloride injection analgesia, level of serum inflammatory factors [tumor necrosis factor-α (TNF-α), interleukin-6 (IL-6)], neurotransmitter index [5-hydroxy tryptamine (5-HT), P substance] and immune function index [CD4+, CD8+, CD4+/CD8+] of two groups between preoperative and postoperative 1d were compared.Results: There were no significant difference in level of TNF-α, IL-6, 5-HT, P substance, CD4+, CD8+ and CD4+/CD8+ between the two groups preoperative. Compared with the level of the same group preoperative, at postoperative 1 d level of TNF-α, IL-6, 5-HT, P substance, CD8+were significantly increased, moreover level in the observation group were significantly lower compared with the control group, the difference was statistically significant;Postoperative 1 d, level of CD4+, CD4+/CD8+ in the two groups were significantly lower than the preoperative level within the group, and the observation group was significantly higher than the control group.Conclusion: Oxycodone hydrochloride injection preemptive analgesia in laparoscopic cholecystectomy can effectively reduce serum inflammatory factors and neurotransmitter index release, improve immune function, has an important clinical value.展开更多
Acetaminophen(APAP),the most frequently used mild analgesic and antipyretic drug worldwide,is implicated in causing 46%of all acute liver failures in the USA and between 40%and 70%in Europe.The predominant pharmacolog...Acetaminophen(APAP),the most frequently used mild analgesic and antipyretic drug worldwide,is implicated in causing 46%of all acute liver failures in the USA and between 40%and 70%in Europe.The predominant pharmacological intervention approved for mitigating such overdose is the antioxidant N-acetylcysteine(NAC);however,its efficacy is limited in cases of advanced liver injury or when administered at a late stage.In the current study,we discovered that treatment with a moderate intensity static magnetic field(SMF)notably reduced the mortality rate in mice subjected to high-dose APAP from 40%to 0%,proving effective at both the initial liver injury stage and the subsequent recovery stage.During the early phase of liver injury,SMF markedly reduced APAPinduced oxidative stress,free radicals,and liver damage,resulting in a reduction in multiple oxidative stress markers and an increase in the antioxidant glutathione(GSH).During the later stage of liver recovery,application of vertically downward SMF increased DNA synthesis and hepatocyte proliferation.Moreover,the combination of NAC and SMF significantly mitigated liver damage induced by high-dose APAP and increased liver recovery,even 24 h post overdose,when the effectiveness of NAC alone substantially declines.Overall,this study provides a noninvasive non-pharmaceutical tool that offers dual benefits in the injury and repair stages following APAP overdose.Of note,this tool can work as an alternative to or in combination with NAC to prevent or minimize liver damage induced by APAP,and potentially other toxic overdoses.展开更多
文摘A simple and rapid liquid chromatography-tandem mass spectrometry （LC-MS/MS） method was de- veloped and validated for simultaneous determination of acetaminophen and oxycodone in human plasma. Acetaminophen-d4 and oxycodone-d3 were used as internal standards. The challenge en- countered in the method development that the high plasma concentration level of acetaminophen made the MS response saturated while the desired lower limit of quantification （LLOQ,） for oxycodone was hard to reach was well solved. The analytes were extracted by protein precipitation using acetonitrile. The matrix effect of the analytes was avoided by chromatographic separation using a hydrophilic C18 column coupled with gradient elution. Multiple reaction monitoring in positive ion mode was performed on tandem mass spectrometer employing electrospray ion source. The calibration curves were linear over the concentration ranges of 40.0-8000 ng/mL and 0.200-40.0 ng/mL for acetaminophen and oxycodone, respectively. This method, which could contribute to high throughput analysis and better clinical drug monitoring, was successfully applied to a pharmacokinetic study in healthy Chinese volunteers.
文摘BACKGROUND:To describe trends in oxycodone and oxycodone-containing analgesic prescribing for the treatment of back pain among adults in emergency departments(EDs) in the USA from 2007 to 2018.METHODS:Data were gathered from the National Hospital Ambulatory Medical Care Survey(NHAMCS) from 2007 to 2018.The study population included individuals of all ages presenting to USA EDs.The NHAMCS reasons for visit and oxycodone drug ID codes were used to isolate patients with back pain.The main outcome was the proportion of oxycodone and oxycodone-containing analgesics prescribed for back pain in the EDs over the specified time period.RESULTS:There was a relative decrease in the overall administration of oxycodone for back pain in the EDs by 62.3% from 2007(244,000 visits) to 2018(92,000 visits).The proportion of ED patients prescribed with oxycodone-containing analgesics for back pain increased among patients aged 45 years and older(from 43.8% to 57.6%),female patients(from 54.5% to 62.0%),black patients(from 22.5% to 30.4%),and Hispanic/Latino patients(from 9.4% to 19.6%).Oxycodone/acetaminophen was most prescribed and accounted for 90.2% of all oxycodone-containing analgesics in 2007,with a decrease to 68.5% in 2018.Pure oxycodone was the second most prescribed medication,accounting for 6.1% in 2007 and 31.5% in 2018.CONCLUSION:The overall number of oxycodone-containing analgesics decreased significantly from 2007 to 2018.However,that number trended upward in 45-year-old and older,female,black,or Hispanic/Latino patients from 2007 to 2018.The total amount of pure oxycodone increased significantly from 2007 to 2008.
基金Supported by Guangxi Natural Science Foundation of China,No.2024GXNSFAA010040Special Fund of the Central Government Guiding Local Scientific and Technological Development by Guangxi Science and Technology Department,No.GuikeZY21195024National Natural Science Foundation of China,No.82260499 and No.82460463.
文摘BACKGROUND High levels of acetaminophen(APAP)consumption can result in significant liver toxicity.Mogroside V(MV)is a bioactive,plant-derived triterpenoid known for its various pharmacological activities.However,the impact of MV on acute liver injury(ALI)is unknown.AIM To investigate the hepatoprotective potential of MV against liver damage caused by APAP and to examine the underlying mechanisms.METHODS Mice were divided into three groups:Saline,APAP and APAP+MV.MV(10 mg/kg)was given intraperitoneally one hour before APAP(300 mg/kg)administration.Twenty-four hours after APAP exposure,serum transaminase levels,liver necrotic area,inflammatory responses,nitrotyrosine accumulation,and c-jun-N-terminal kinase(JNK)activation were assessed.Additionally,we analyzed reactive oxygen species(ROS)levels,JNK activation,and cell death in alpha mouse liver 12(AML12)cells.RESULTS MV pre-treatment in vivo led to a reduction in the rise of aspartate transaminase and alanine transaminase levels,mitigated liver damage,decreased nitrotyrosine accumulation,and blocked JNK phosphorylation resulting from APAP exposure,without affecting glutathione production.Similarly,MV diminished the APAP-induced increase in ROS,JNK phosphorylation,and cell death in vitro.CONCLUSION Our study suggests that MV treatment alleviates APAP-induced ALI by reducing ROS and JNK activation.
文摘Background: Controlled-release oxycodone/naloxone(OXN-CR) maintains the effect of opioid-induced analgesia through oxycodone while reducing the occurrence rate of opioid-induced constipation through naloxone. The present study was designed to assess the non-inferiority of OXN-CR to controlled-release oxycodone(OX-CR) for the control of cancer-related pain in Korean patients.Methods: In this randomized, open-labeled, parallel-group, phase IV study, we enrolled patients aged 20 years or older with moderate to severe cancer-related pain [numeric rating scale(NRS) pain score ≥4] from seven Korean oncology/hematology centers. Patients in the intention-to-treat(ITT) population were randomized(1:1) to OXNCR or OX-CR groups. OXN-CR was administered starting at 20 mg/10 mg per day and up-titrated to a maximum of80 mg/40 mg per day for 4 weeks, and OX-CR was administered starting at 20 mg/day and up-titrated to a maximum of 80 mg/day for 4 weeks.The primary efficacy endpoint was the change in NRS pain score from baseline to week4, with non-inferiority margin of-1.5. Secondary endpoints included analgesic rescue medication intake, patientreported change in bowel habits, laxative intake, quality of life(QoL), and safety assessments.Results: Of the ITT population comprising 128 patients, 7 with missing primary efficacy data and 4 who violated the eligibility criteria were excluded from the efficacy analysis. At week 4, the mean change in NRS pain scores was not significantly different between the OXN-CR group(n = 58) and the OX-CR group(n = 59)(-1.586 vs.-1.559,P = 0.948). The lower limit of the one-sided 95% confidence interval(-0.776 to 0.830) for the difference exceeded the non-inferiority margin(P < 0.001). The OXN-CR and OX-CR groups did not differ significantly in terms of analgesic rescue medication intake, change in bowel habits, laxative intake, QoL, and safety assessments.Conclusions: OXN-CR was non-inferior to OX-CR in terms of pain reduction after 4 weeks of treatment and had a similar safety profile. Studies in larger populations of Korean patients with cancer-related pain are needed to further investigate the effectiveness of OXN-CR for long-term pain control and constipation alleviation.Trial registration ClinicalTrials.gov NCT01313780, registered March 8。
基金Supported by The National Key Research and Development Program,No.2020YFC2005303.
文摘To review the research progress of pure opioid receptor agonist oxycodone.The research progress of oxycodone in terms of pharmacokinetics,pharmacodynamics,adverse reactions,clinical application,combined medication and new progress in clinical application was summarized by referring to the literature.Oxycodone is a semi-synthetic thebaine derivative of opioid alkaloids,and is a pure opioidμandκreceptor agonist.The main action sites are the central nervous system and visceral smooth muscle.Due to its advantages of low adverse reactions,good analgesic effects,and a wide range of safe doses,the drug has been widely used in the control of acute and chronic postoperative pain,as well as malignant and non-malignant pain.Since the end of the 20^(th) century,researchers have begun to formulate antipyretic analgesics,opioid receptor agonists,opioid receptor antagonists,dopamine receptor antagonists and other drugs with oxycodone in different proportions to enhance the analgesic effect.At the same time,it can reduce the dosage of oxycodone and reduce its adverse reactions,so as to achieve the purpose of limiting opioid abuse.With the continuous research on the efficacy and safety of oxycodone in the perioperative period at home and abroad,oxycodone has become the only dual-opioid potent analgesic that can be used in clinical work.
文摘Objective:To study the effect of dexmedetomidine combined with oxycodone on systemic stress response in recovery period of gynecological laparoscopic operation.Methods:A total of 86 patients who received laparoscopic operation in the Second Affiliated Hospital of Kunming Medical University between June 2014 and December 2016 were selected and randomly divided into the dexmedetomidine combined with oxycodone group (DO group) and control group (C group). Before anesthesia induction (T1), at the end of the surgery and before micro pump injection of dexmedetomidine and oxycodone hydrochloride (T2) and in recovery period (T3), serum levels of pituitary-target gland axis-related hormones, vascular activity-related hormones and oxidative stress-related molecules were determined.Results: At T1 and T2, serum TSH, T3, T4, ACTH, Cor, NE, E, ADH, AT-II, ROS, MDA, SOD and HO-1 levels of DO group were not significantly different from those of C group;at T3, serum TSH, T3, T4, ACTH, Cor, NE, E, ADH, AT-II, ROS and MDA levels of DO group were significantly lower than those of C group while SOD and HO-1 levels were significantly higher than those of C group.Conclusions: Dexmedetomidine combined with oxycodone can inhibit the systemic stress response in recovery of gynecological laparoscopic operation.
文摘Background: Post-craniotomy pain has been reported to be moderate to severe. Management of post-craniotomy pain is often inadequate, yet limited by the side effects of opioids. We aim to find out the efficacy of oral oxycodone as compared to oral codeine for the treatment of post-craniotomy pain in our institution. Methods: A randomized, double-blinded controlled trial was used to evaluate the efficacy of oral oxycodone versus oral codeine. 40 patients were randomized to the control group of codeine (n = 20) or the experimental group receiving oxycodone (n = 20) in addition to regular oral paracetamol for both groups of patients. Results: There was no difference in the visual analogue scale scores at 24 hours (2.78 versus 1.85, p = 0.11) or side effects in the oxycodone group compared with the codeine group. Conclusions: Oral oxycodone had similar efficacy as oral codeine in the management of post-craniotomy pain.
文摘Oxycodone hydrochloride is a semi-synthetic opioid agonist that provides very effective relief for moderate to severe pain in cancer and post-operative patients. Controlled release oxycodone formulations have been studied to enhance the therapeutic effect by providing constant release over the whole dosing interval and improve patient’s convenience by reducing the frequency of administration as well.
文摘Backgroud:Intravenous opioid patient-controlled analgesia(IV-PCA)has been suggested as an effective method in postoperative pain management.There are several randomized controlled trials(RCTs)of comparison of oxycodone and fentanyl for IV-PCA in surgical patients.The purpose of this study was to perform a meta-analysis to compare the efficacy and safety of oxycodone and fentanyl for IV-PCA in surgical patients from current data.Methods:The RCTs of oxycodone versus fentanyl for IV-PCA were gathered from PubMed,Embase,Cochrane library,CNKI and VIP data.After data extraction and quality assessment of the included RCTs,the RevMan 5.3 software was applied for meta-analysis of numerical rating scale(NRS)scores,accumulated IV-PCA consumption of oxycodone and fentanyl,patient satisfaction,postoperative nausea and vomiting(PONV),and other adverse events(AEs).Results:Results reported from eight RCTs involving 600 patients are included in the meta-analysis.The NRS score at rest and upon movement of group oxycodone was significantly lower than that of group fentanyl(WMD=-3.85,95%CI-4.93^-2.76,P<0.00001;WMD=-4.31,95%CI-5.79^-2.84,P<0.00001);however,the incidence of PONV and dizziness was obviously increased in group oxycodone than in group fentanyl(OR=2.41,95%CI 1.60~3.63,P<0.0001;OR=3.69,95%CI 2.17~6.26,P<0.00001).Accumulated IV-PCA consumption in group oxycodone was less than in group fentanyl overall the 48 hours postoperatively(WMD=-12.11,95%CI-18.42^-5.80,P=0.0002).There was no significant difference in patient satisfaction between oxycodone and fentanyl(OR=0.73,95%CI 0.11~5.04,P=0.75).Conclusion:According to the evidence,this meta-analysis suggest that oxycodone for IV-PCA is superior to fentanyl in postoperative pain relief,whereas the higher incidence of PONV and dizziness was accompanied with oxycodone.Further large-scale,prospective,observational studies are needed to summarize and analyse the data to draw a fair conclusion.
文摘Objective:To study the effects of oxycodone and fentanyl patient-controlled intravenous analgesia on pain, immune response and stress response after laparoscopic surgery.Methods:Patients undergoing laparoscopic surgery in Xianning Central Hospital between June 2015 and February 2017 were selected and randomly divided into oxycodone group and fentanyl group who received postoperative oxycodone and fentanyl patient-controlled intravenous analgesia respectively. 3 d after surgery and 5 d after surgery, the serum contents of pain-related transmitters, immune indexes, stress-related molecules as well as peripheral blood contents of immune cells were measured.Results: 3 d after surgery and 5 d after surgery, CRP, TNF-α, IL-8, sICAM-1, YKL-40, Cor, C-P, FT3, FT4 and HO-1 contents in serum of oxycodone group were significantly lower than those of fentanyl group whereas CD3+CD4+T cell and CD3+CD8+T cell contents in peripheral blood as well as C3 and C4 contents in serum were significantly higher than those of fentanyl group.Conclusion:oxycodone patient-controlled intravenous analgesia after laparoscopic surgery is better than fentanyl and can reduce the pain degree, inhibit the stress response and improve the immune response.
文摘Objective： To study the effect of the transdermal preparation of traditional Chinese medicine in treating cancer pain. Methods： From October 2016 to January 2018, 126 patients with cancer pain were enrolled and divided into 4 groups, 39 patients in group A （directed TCM permeation）, 26 patients in group B （oxycodone sustained-release tablets）, 32 patients in group C （Chinese medicine directed drug penetration ＋ oxycodone sustained-release tablets）, and 29 patients group D （Chinese medicine directed drug penetration ＋ oxycodone sustained-release tablets ＋ nimesulide sustained release tablets）, according to KPS scores. Results： Transdermal preparations of traditional Chinese medicine can significantly alleviate cancer pain. For the treatment of moderate to severe cancer pain, the Chinese medicine transdermal preparation can reduce the dosage of oxycodone sustained-release tablets. At the same time, the patient＇s KPS and NRS scores were significantly reduced. Moreover, the transdermal preparation of traditional Chinese medicine has a better therapeutic effect on visceral pain. Conclusion： The traditional Chinese medicine tra_nsdermal preparation combined with western medicine for the treatment of cancer pain may be a new method for the treatment of cancer pain.
文摘Objective: To discuss the analgesic effect of oxycodone combined with parecoxib sodium after laparoscopic cholecystectomy and its influence on inflammatory stress response. Methods:A total of 260 patients with chronic cholecystitis who accepted laparoscopic cholecystectomy in this hospital between December 2016 and May 2017 were divided into control group (n=130) and oxycodone group (n=130) by random number table method. Control group received morphine combined with parecoxib sodium analgesia after operation, and oxycodone group received oxycodone combined with parecoxib sodium analgesia after operation. The differences in serum levels of pain mediators, inflammatory mediators and stress hormones were compared between the two groups immediately after operation (T0), 12 h after operation (T1) and 24 h after operation (T3). Results: At T0, there was no statistically significant difference in serum levels of pain mediators, inflammatory mediators and stress hormones between the two groups. At T1 and T2, serum pain mediators PGE2, NPY, SP and NGF levels of oxycodone group were lower than those of control group whereas β-EP levels were higher than those of control group;serum inflammatory mediators CRP, IL-1β, IL-6 and TNF-αlevels were lower than those of control group;serum stress hormones Cor, NE and INS levels were lower than those of control group. Conclusion: Oxycodone combined with parecoxib sodium analgesia after laparoscopic cholecystectomy can effectively relieve the pain perception and inhibit the systemic inflammatory response and stress response.
文摘Objective:To investigate the effect of oxycodone hydrochloride injection preemptive analgesia on serum inflammatory factors, neurotransmitter index and immune function in patients with laparoscopic cholecystectomy.Methods: According to random data table, 113 patients undergoing laparoscopic cholecystectomy were divided into control group (n=57) and observation group (n=56), patients in the control group were treated with sufentanil citrate injection analgesia, and the observation group patients were given oxycodone hydrochloride injection analgesia, level of serum inflammatory factors [tumor necrosis factor-α (TNF-α), interleukin-6 (IL-6)], neurotransmitter index [5-hydroxy tryptamine (5-HT), P substance] and immune function index [CD4+, CD8+, CD4+/CD8+] of two groups between preoperative and postoperative 1d were compared.Results: There were no significant difference in level of TNF-α, IL-6, 5-HT, P substance, CD4+, CD8+ and CD4+/CD8+ between the two groups preoperative. Compared with the level of the same group preoperative, at postoperative 1 d level of TNF-α, IL-6, 5-HT, P substance, CD8+were significantly increased, moreover level in the observation group were significantly lower compared with the control group, the difference was statistically significant;Postoperative 1 d, level of CD4+, CD4+/CD8+ in the two groups were significantly lower than the preoperative level within the group, and the observation group was significantly higher than the control group.Conclusion: Oxycodone hydrochloride injection preemptive analgesia in laparoscopic cholecystectomy can effectively reduce serum inflammatory factors and neurotransmitter index release, improve immune function, has an important clinical value.
基金supported by the National Key R&D Program of China(2023YFB3507004)National Natural Science Foundation of China(U21A20148)+5 种基金International Partnership Program of Chinese Academy of Sciences(116134KYSB20210052)Anhui Provincial Natural Science Foundation(2308085QE183,2308085QE181)CASHIPS Director’s Fund(YZJJ2024QN44,YZJJ2023QN43)Heye Health Technology Chong Ming Project(HYCMP2021010)China Post-doctoral Science Foundation(2023M743536)Science Research Fund for Postdoctoral in Anhui Province(2023B669)。
文摘Acetaminophen(APAP),the most frequently used mild analgesic and antipyretic drug worldwide,is implicated in causing 46%of all acute liver failures in the USA and between 40%and 70%in Europe.The predominant pharmacological intervention approved for mitigating such overdose is the antioxidant N-acetylcysteine(NAC);however,its efficacy is limited in cases of advanced liver injury or when administered at a late stage.In the current study,we discovered that treatment with a moderate intensity static magnetic field(SMF)notably reduced the mortality rate in mice subjected to high-dose APAP from 40%to 0%,proving effective at both the initial liver injury stage and the subsequent recovery stage.During the early phase of liver injury,SMF markedly reduced APAPinduced oxidative stress,free radicals,and liver damage,resulting in a reduction in multiple oxidative stress markers and an increase in the antioxidant glutathione(GSH).During the later stage of liver recovery,application of vertically downward SMF increased DNA synthesis and hepatocyte proliferation.Moreover,the combination of NAC and SMF significantly mitigated liver damage induced by high-dose APAP and increased liver recovery,even 24 h post overdose,when the effectiveness of NAC alone substantially declines.Overall,this study provides a noninvasive non-pharmaceutical tool that offers dual benefits in the injury and repair stages following APAP overdose.Of note,this tool can work as an alternative to or in combination with NAC to prevent or minimize liver damage induced by APAP,and potentially other toxic overdoses.
