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Randomized, Double Blind, Double-Masked, Parallel-Group Clinical Study to Compare the Effectiveness of Oral Transmucosal Fentanyl 200 µg vs Morphine Hydrochloride 2 mg IV in the Treatment of Postoperative Pain
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作者 Hernan Figueredo Vicente Bozza +1 位作者 Maria Gonzalez Yibirin David Alberto Rincón Matute 《Open Journal of Anesthesiology》 2025年第2期48-58,共11页
Postoperative pain is an acute pain that appears due to the surgical act, reaching its maximum intensity in the first 24 - 48 hours after surgery. Postoperative pain control reduces possible postoperative complication... Postoperative pain is an acute pain that appears due to the surgical act, reaching its maximum intensity in the first 24 - 48 hours after surgery. Postoperative pain control reduces possible postoperative complications, as well as the patient’s stay in the medical institution. Objective: This study compared the effectiveness and side effects of oral transmucosal fentanyl citrate (OTFC) with IV morphine in the control of postoperative pain. Methods: Seventy-three patients (Fentanyl group: 27, morphine group: 46) were included. Changes in pain were evaluated with Visual Analog Scale (VAS) and Pain Relief Scale, Pain Intensity Differences (PID), Sum of Pain Intensity Differences (SPID), and Total Pain Relief (TOTPAR). At time zero, 15, 30, 45 min and 1, 2, 3, 4, 5 and 6 h. Results: The decrease in pain intensity measured by VAS was similar in both groups with no significant differences at any of the measurement points. Both products produced a significant increase in the Pain Relief scale, with no differences between groups at any of the measurement times. There were no differences between groups when comparing PID. Comparing SPID between groups, there were no differences at 15, 30 minutes, then there were significant differences in favor of the Fentanyl group up to 6 hours. Both products produced a significant increase in the TOPAR scale, with no differences between groups at any of the measurement times. The appearance of adverse effects was similar in both groups. Conclusions: Both products produced a significant reduction in the measures of pain intensity (VAS), increase of SPID, as well as a significant increase in the Pain Relief scale, a significant increase in the TOPAR scale, with no differences between the groups. The number of adverse effects was similar. The convenience of OTFC administration allows its administration without the special conditions needed for the administration of IV morphine. 展开更多
关键词 Postoperative Pain VAS PR PID SPID TOTPAR fentanyl MORPHINE
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Fentanyl may not be necessary for adequate endoscopic moderate sedation
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作者 Greg S Cohen Kwang-Youn A Kim 《World Journal of Gastrointestinal Endoscopy》 2025年第5期61-66,共6页
BACKGROUND Although the majority of gastrointestinal(GI)endoscopies in the United States are now performed with propofol sedation,a substantial minority are performed with midazolam and fentanyl sedation.Despite the u... BACKGROUND Although the majority of gastrointestinal(GI)endoscopies in the United States are now performed with propofol sedation,a substantial minority are performed with midazolam and fentanyl sedation.Despite the ubiquity of conscious sedation with midazolam and fentanyl in the United States,there is scant evidence specifically supporting the superiority of midazolam plus fentanyl over single agent midazolam sedation in GI endoscopy.We hypothesize that single agent sedation with midazolam is noninferior to sedation with midazolam plus fentanyl in GI endoscopy.AIM To investigate whether sedation with midazolam alone is noninferior to sedation with midazolam plus fentanyl in GI endoscopy.METHODS We conducted a randomized,single-blind study to compare the safety and effectiveness of single agent midazolam vs.standard fentanyl/midazolam moderate sedation in 300 outpatients presenting for upper endoscopy and/or colonoscopy at a tertiary care hospital.Primary outcomes were patient satisfaction as measured by the previously validated Procedural Sedation Assessment Survey.Secondary outcomes were procedure quality measures and adverse events.Statistical analysis was performed by a biomedical statistician using theχ^(2) test,Fisher’s exact test,and Welch’s 2-sample t-test.RESULTS There was no difference in patient satisfaction between sedation groups,as measured by a less than 1 point difference between groups in Procedural Sedation Assessment Survey scores for discomfort during the procedure,and for preference for level of sedation with future procedures.There were no differences in adverse events or procedure quality measures.Cecal intubation time was 1 minute longer in the single agent midazolam group,and an average of 2.7 mg more midazolam was administered when fentanyl was not included in the sedation regimen.The recruitment goal of 772 patients was not reached.CONCLUSION It may be possible to minimize or avoid using fentanyl in endoscopist administered moderate sedation for GI endoscopy.We hope these findings spur further work in this under-researched area. 展开更多
关键词 COLONOSCOPY Conscious sedation ENDOSCOPY fentanyl MIDAZOLAM
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Fentanyl and xylazine crisis:Crafting coherent strategies for opioid overdose prevention
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作者 Lakshit Jain Jasleen Kaur +4 位作者 Shahana Ayub Danya Ansari Rizwan Ahmed Abdul Qadir Dada Saeed Ahmed 《World Journal of Psychiatry》 SCIE 2024年第6期760-766,共7页
The United States is in the throes of a severe opioid overdose epidemic,primarily fueled by the pervasive use of fentanyl and the emerging threat of xylazine,a veterinary sedative often mixed with fentanyl.The high po... The United States is in the throes of a severe opioid overdose epidemic,primarily fueled by the pervasive use of fentanyl and the emerging threat of xylazine,a veterinary sedative often mixed with fentanyl.The high potency and long duration of fentanyl is compounded by the added risks from xylazine,heightening the lethal danger faced by opioid users.Measures such as enhanced surveillance,public awareness campaigns,and the distribution of fentanylxylazine test kits,and naloxone have been undertaken to mitigate this crisis.Fentanyl-related overdose deaths persist despite these efforts,partly due to inconsistent policies across states and resistance towards adopting harm reduction strategies.A multifaceted approach is imperative in effectively combating the opioid overdose epidemic.This approach should include expansion of treatment access,broadening the availability of medications for opioid use disorder,implementation of harm reduction strategies,and enaction of legislative reforms and diminishing stigma associated with opioid use disorder. 展开更多
关键词 fentanyl XYLAZINE Opioid overdose EPIDEMIC Opioid use disorder BUPRENORPHINE Medications for opioid use disorder
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Comparison of Propofol and Fentanyl for Preventing Emergence Agitation Following Sevoflurane Anesthesia in Pediatric Patients: A Single-Center Study in Bangladesh
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作者 Md. Saiful Islam Khan Md. Abir Tazim Chowdhury +8 位作者 Farzana Fardousi Munama Magdum Md. Ahaduzzaman Taneem Mohammad Shamima Akter Suriya Akter Md. Saiful Islam Azad Md. Mozaffer Hossain M. Abdur Rahman 《Pharmacology & Pharmacy》 2024年第6期223-235,共13页
Background: Emergence agitation (EA) is a common phenomenon observed in pediatric patients following general anesthesia. This study aimed to assess the efficacy of propofol and fentanyl in preventing EA and to compare... Background: Emergence agitation (EA) is a common phenomenon observed in pediatric patients following general anesthesia. This study aimed to assess the efficacy of propofol and fentanyl in preventing EA and to compare their associated complications or side effects. Methods: This prospective randomized observational comparative study was conducted at Dhaka Medical College Hospital from July 2013 to June 2014. The study aimed to evaluate the effects of propofol and fentanyl on EA in children aged 18 to 72 months undergoing circumcision, herniotomy, and polypectomy operations. Ninety children were included in the study, with 45 in each group. Patients with psychological or neurological disorders were excluded. Various parameters including age, sex, weight, American Society of Anesthesiologists (ASA) class, duration of anesthesia, Saturation of Peripheral Oxygen (SPO2), heart rate (HR), respiratory rate (RR), Pediatric Anesthesia Emergence Delirium (PAED) score, duration of post-anesthesia care unit (PACU) stay, incidence of laryngospasm, nausea, vomiting, and rescue drug requirement were compared between the two groups. Results: Age, sex, weight, ASA class, and duration of anesthesia were comparable between the two groups. Perioperative SpO2 and HR were similar in both groups. However, the PAED score was significantly higher in the fentanyl group during all follow-ups except at 30 minutes postoperatively. The mean duration of PACU stay was significantly longer in the fentanyl group. Although the incidence of laryngospasm was higher in the fentanyl group, it was not statistically significant. Conversely, nausea or vomiting was significantly higher in the fentanyl group. The requirement for rescue drugs was significantly higher in the fentanyl group compared to the propofol group. Conclusion: Both propofol and fentanyl were effective in preventing emergence agitation in pediatric patients undergoing various surgical procedures under sevoflurane anesthesia. However, propofol demonstrated a better safety profile with fewer incidences of nausea, vomiting, and rescue drug requirements compared to fentanyl. 展开更多
关键词 Emergence Agitation (EA) General Anesthesia PROPOFOL fentanyl Pediatric Patients Pediatric Anesthesia Emergence Delirium (PAED) Score BANGLADESH
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Neonatal Cord Tox Panel and Maternal Perinatal Fentanyl Exposure: A Retrospective Chart Review 被引量:1
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作者 Joseph Jones Donna Coy +2 位作者 Ryan Mitacek Stephanie Thompson Stefan Maxwell 《American Journal of Analytical Chemistry》 2021年第9期324-331,共8页
<strong>Objective:</strong> The specific aim of this study was to determine if the currently available cutoff for fentanyl in umbilical cord (UC) was appropriate to distinguish illicit fentanyl exposure fr... <strong>Objective:</strong> The specific aim of this study was to determine if the currently available cutoff for fentanyl in umbilical cord (UC) was appropriate to distinguish illicit fentanyl exposure from therapeutic in-hospital administration of fentanyl. <strong>Study Design</strong><strong>:</strong> Medical record review was conducted for perinatal administration of fentanyl and the detection of fentanyl in the corresponding routine UC toxicology. Specimens were initially tested with immunoassay followed by mass spectrometry (n = 62). <strong>Result:</strong> Excluding a single specimen that was confirmed positive, specimens were below the assays’ limit of quantification. The immunoassay’s mean b/b<sub>0</sub> for the cases that received and did not receive fentanyl prior to delivery was 91.3% ± 10.6% and 98.2% ± 6.5%, respectively (p = 0.003). <strong>Conclusion:</strong> We demonstrated that UC is a suitable specimen type for the detection of fentanyl and that the cutoff selected adequately identifies illicit fentanyl use while not flagging cases where fentanyl was administered by the hospital prior to birth. 展开更多
关键词 fentanyl Norfentanyl Umbilical Cord Prenatal fentanyl Exposure
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Transdermal Fentanyl for Management of Cancer Pain in Elderly Patients in China 被引量:2
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作者 于世英 孙燕 +5 位作者 张海春 吴一龙 秦叔逵 谢广茹 刘淑俊 隋广杰 《The Chinese-German Journal of Clinical Oncology》 CAS 2004年第2期85-89,125,共6页
Objective: Objective: To assess the effect and adverse effects of transdermal fentanyl for elderly patients with cancer pain in China. Methods: A total of 1664 elderly patients (aged 65-90 with mean age of 72.6) with ... Objective: Objective: To assess the effect and adverse effects of transdermal fentanyl for elderly patients with cancer pain in China. Methods: A total of 1664 elderly patients (aged 65-90 with mean age of 72.6) with cancer pain enrolled in the multicenter study from 136 institutes in China. Of them, 408 (28.8%) patients were 75 years old or older. All patients received transdermal fentanyl for the management of cancer pain. The patients were asked to record the attacks of pain, quality of life, and any side effects of the treatment. Results: Baseline mean of pain intensity was 7.34. On day 1, 3, 6, 9 15, and 30, the pain mean scores were decreased to 3.82, 2.80, 2.43, 2.11, 1.83, 1.64 (P=0.000). The effective rate was 97.18%. The mean doses of fentanyl was 31.34 g/h (25-150 g/h) initially, and 40.59 g/h and 47.50 g/h (25-200 g/h) at day 15 and day 30. At treatment day 15, the dose of fentanyl was ranger from 25 to 50 g/h in 91.8% of patients, 75 to 100 g/h in 7.5% patients, and 125 to 200 g/h only in 0.8% patients. The fine quality of life was in 25.4% patients before treatment, and was 71.15% and 73.04% at day 15 and day 30 respectively (P=0.0000). The common side effects were constipation (10.70%), nausea (11.96%), dizzy (6.85%), vomiting (3.85%), sedation (2.40%), Respiratory depression (0.12%). 86.2% patients preferred continue treated by transdermal fentanyl. Conclusions: Transdermal fentanyl for the elderly with cancer pain is effective, safe, convenient, and can improve the quality of life. Transdermal fentanyl can be recommended as a first-line drug for the treatment of elderly patients with moderate to severe cancer pain, and the initial doses is recommended as 25 g/h. 展开更多
关键词 ELDERLY cancer pain transdermal fentanyl pain management
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The Effect of Test Dose Fentanyl on Predicting Postoperative Respiratory Depression in Patients with Continuous Intravenous Morphine Analgesia 被引量:3
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作者 丁正年 王忠云 惠宁宁 《Journal of Nanjing Medical University》 2003年第6期283-287,303,共6页
Objective: To evaluate the effect of test dose fentanyl on predictingpostoperative analgesia and respiratory depression. Methods: Preoperatively the lowest pulseoximeter saturation (SpO_2) under room air breathing was... Objective: To evaluate the effect of test dose fentanyl on predictingpostoperative analgesia and respiratory depression. Methods: Preoperatively the lowest pulseoximeter saturation (SpO_2) under room air breathing was measured after 2 μg/kg of fentanyl givenintravenously in 35 patients who were scheduled with continuous intravenous morphine analgesia (12μg·kg^(-1)·h^(-1)) postoperatively. Results: The test dose fentanyl resulted in respiratorydepression in 19 of 35 cases, while 8 (42.1%) of the 19 cases developed respiratory depressionpostoperatively. However in the rest 16 patients, no patient (0) developed respiratory depression (P< 0.01). The fentanyl-induced lowest SpO_2 significantly correlated with the lowest SpO_2postoperatively (P < 0.01). The analgesia effect in terms of verbal analogue scale was correlatedneither with the fentanyl-induced lowest SpO_2 nor with the lowest SpO_2 postoperatively (P > 0.05).Conclusion: The patient who was sensitive to fentanyl-induced respiratory depression would take ahigh risk to develop postoperative respiratory depression with intravenous morphine analgesia andthe patient with respiratory depression does not always go with satisfactory analgesia. 展开更多
关键词 ANALGESIA respiratory depression OPIOID fentanyl test
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4-取代Fentanyl类化合物电子结构及构效关系研究 被引量:1
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作者 陈常英 李玉林 陈冀胜 《化学学报》 SCIE CAS 1988年第8期734-739,共6页
本文对十一个4-取代Fentanyl类化合物进行了量子化学(INDO)计算,研究了它们的电子结构及构效关系.结果表明,这些化合物同其他Fentanyl类化合物在主要活性部位和电子结构趋势上基本相同.酰胺氧原子是最重要的负电中心,哌啶氮原子在季铵... 本文对十一个4-取代Fentanyl类化合物进行了量子化学(INDO)计算,研究了它们的电子结构及构效关系.结果表明,这些化合物同其他Fentanyl类化合物在主要活性部位和电子结构趋势上基本相同.酰胺氧原子是最重要的负电中心,哌啶氮原子在季铵化后发挥正电中心作用.4-取代基的极性基团可能以电荷转移作用或氢键接受体形式与受体极性部位结合,并能影响其他活性部位电子密度,另外,4-取代基的立体因素与疏水因素同生物活性相关. 展开更多
关键词 化合物 电子密度 电子浓度 fentanyl 氧原子 前沿轨道 镇痛活性 轨道能级 分子轨道 氮原子 量子化学 HOMO 构效关系
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Unique Pharmacology,Brain Dysfunction,and Therapeutic Advancements for Fentanyl Misuse and Abuse 被引量:4
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作者 Ying Han Lu Cao +3 位作者 Kai Yuan Jie Shi Wei Yan Lin Lu 《Neuroscience Bulletin》 SCIE CAS CSCD 2022年第11期1365-1382,共18页
Fentanyl is a fully synthetic opioid with analgesic and anesthetic properties.It has become a primary driver of the deadliest opioid crisis in the United States and elsewhere,consequently imposing devastating social,e... Fentanyl is a fully synthetic opioid with analgesic and anesthetic properties.It has become a primary driver of the deadliest opioid crisis in the United States and elsewhere,consequently imposing devastating social,economic,and health burdens worldwide.However,the neural mechanisms that underlie the behavioral effects of fentanyl and its analogs are largely unknown,and approaches to prevent fentanyl abuse and fentanyl-related overdose deaths are scarce.This review presents the abuse potential and unique pharmacology of fentanyl and elucidates its potential mechanisms of action,including neural circuit dysfunction and neuroinflammation.We discuss recent progress in the development of pharmacological interventions,anti-fentanyl vaccines,anti-fentanyl/heroin conjugate vaccines,and monoclonal antibodies to attenuate fentanyl-seeking and prevent fentanyl-induced respiratory depression.However,translational studies and clinical trials are still lacking.Considering the present opioid crisis,the development of effective pharmacological and immunological strategies to prevent fentanyl abuse and overdose are urgently needed. 展开更多
关键词 fentanyl abuse Neural mechanisms Pharmacological interventions fentanyl vaccines
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Using Umbilical Cord Tissue to Identify Prenatal Exposure to Fentanyl and Other Commonly Abused Drugs 被引量:1
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作者 Shanthi Hariharan Donna Coy Joseph Jones 《Open Journal of Obstetrics and Gynecology》 2022年第5期434-442,共9页
Background: Prenatal exposure to fentanyl may lead to Neonatal Abstinence Syndrome (NAS), a constellation of symptoms observed when newborns begin withdrawing from addictive substances such as opioids. The use of umbi... Background: Prenatal exposure to fentanyl may lead to Neonatal Abstinence Syndrome (NAS), a constellation of symptoms observed when newborns begin withdrawing from addictive substances such as opioids. The use of umbilical cord tissue segments (UC) for newborn toxicology has been increasing due to its apparent long detection window, sensitivity, and ease of collection. However, very little has been reported in the literature concerning the prevalence of in utero exposure to fentanyl and co-exposure with other commonly abused substances. Specific aim: The specific aims of this retrospective study are twofold. We will report prevalence of neonatal exposure to fentanyl for a nationwide high-risk population using UC submitted to a national reference laboratory for routine forensic toxicology analysis and the co-exposure patterns observed for these fentanyl-exposed neonates. Methods: A secondary analysis was performed using historical data for UC received between January 1, 2020 and December 31, 2020 for routine forensic toxicology analysis. Results: During the study period, our laboratory received 23,104 UC for analysis and 9667 (41.8%) of those UC were positive for at least one drug. The prevalence of fentanyl detection was 1.9% (n = 429). Of these 429 specimens there were 407 UC where both fentanyl and norfentanyl were detected. There were 14 UC where only fentanyl was detected and 8 UC where only norfentanyl was detected. When detected, the median concentrations of fentanyl and norfentanyl were 4029 pg/g (IQR: 1696, 9230 pg/g) and 10,756 pg/mg (IQR: 3925, 25,288 pg/g), respectively. Of the 429 positive fentanyl and/or norfentanyl UC, 33 (7.7%) were only positive for fentanyl and/or norfentanyl. Of the 396 polypositive UC, morphine was the highest co-exposure with 243 UC (56.6%) being positive for both fentanyls and morphine. The second most prevalent co-exposure observed was methamphetamine/amphetamine (n = 173;40.3%) followed by cannabinoids (n = 113;26.3%) and benzoylecgonine (cocaine metabolite;n = 106;24.7%). Conclusions: Nonmedical use of fentanyl is an alarming trend in this country including this maternal demographic reported here. Fentanyl was typically found with other commonly abused substances. 展开更多
关键词 fentanyl Norfentanyl Umbilical Cord Neonatal Abstinence Syndrome NAS Newborn Toxicology Prenatal Drug Exposure Polysubstance Abuse
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Effects of Morphine,Fentanyl and Tramadol on Human Immune Response 被引量:7
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作者 刘志恒 高峰 田玉科 《Journal of Huazhong University of Science and Technology(Medical Sciences)》 SCIE CAS 2006年第4期478-481,共4页
Summary: Morphine has been reported to suppress human immune response. We aimed to observe the effects of morphine, fentanyl and tramadol on NF- K B and IL-2 from both laboratory and clinical perspective. Jurkat cell... Summary: Morphine has been reported to suppress human immune response. We aimed to observe the effects of morphine, fentanyl and tramadol on NF- K B and IL-2 from both laboratory and clinical perspective. Jurkat cells were incubated with ten times clinically relevant concentrations of morphine, fentanyl and tramadol before being stimulated with PMA. NF- κB binding activity and IL-2 levels were measured, In the clinical study, 150 consenting patients were randomized into 3 groups according to the analgesics used in them, namely, group morphine (M), group fentanyl (F) and group tramadol (T). IL-2 was measured preoperatively and 1, 3 and 24 h after operation. Consequently, NF-κB activation was suppressed by morphine and fentanyl but not by tramadol. IL-2 was significantly decreased by morphine and fentanyl but not by tramadol in vitro. In the PCA patients, IL-2 was decreased in group M and increased in group F postoperatively. Whereas in group T, IL-2 was unchanged 1 h after operation but was significantly elevated 3 and 24 h after operation. Our results showed that the inhibition of morphine on IL-2 was most probably related to its suppression on NF-κB, Fentanyl had different effects on human immune response in vitro and in vivo. Tramadol may have immune enhancing effect. 展开更多
关键词 MORPHINE fentanyl TRAMADOL NF-κB IL-2
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Multicenter Clinical Study for Evaluation of Efficacy and Safety of Transdermal Fentanyl Matrix Patch in Treatment of Moderate to Severe Cancer Pain in 474 Chinese Cancer Patients 被引量:6
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作者 Yu-lin Zhu Guo-hong Song +17 位作者 Duan-qi Liu Xi Zhang Kui-feng Liu Ai-hua Zang Ying Cheng Guo-chun Cao Jun Liang Xue-zhen Ma Xin Ding Bin Wang Wei-lian Li Zuo-wei Hu Gang Feng Jiang-jin Huang Xiao Zheng Shun-chang Jiao Rong Wu Jun Ren 《Chinese Journal of Cancer Research》 SCIE CAS CSCD 2011年第4期317-322,共6页
Objective: Although a new matrix formulation fentanyl has been used throughout the world for cancer pain management, few data about its efficacy and clinical outcomes associated with its use in Chinese patients have b... Objective: Although a new matrix formulation fentanyl has been used throughout the world for cancer pain management, few data about its efficacy and clinical outcomes associated with its use in Chinese patients have been obtained. This study aimed to assess the efficacy and safety of the new system in Chinese patients with moderate to severe cancer pain. Methods: A total of 474 patients with moderate to severe cancer pain were enrolled in this study and were treated with the new transdermal fentanyl matrix patch (TDF) up to 2 weeks. All the patients were asked to record pain intensity, side effects, quality of life (QOL), adherence and global satisfaction. The initial dose of fentanyl was 25 ?g/h titrated with opioid or according to National Comprehensive Cancer Network (NCCN) guidelines. Transdermal fentanyl was changed every three days. Results: After 2 weeks. The mean pain intensity of the 459 evaluated patients decreased significantly from 5.63?1.26 to 2.03?1.46 (P<0.0001). The total remission rate was 91.29%, of which moderate remission rate 53.16%, obvious remission rate 25.49% and complete remission rate 12.64%. The rate of adverse events was 33.75%, 18.78% of which were moderate and 3.80% were severe. The most frequent adverse events were constipation and nausea. No fatal events were observed. The quality of life was remarkably improved after the treatment (P<0.0001). Conclusion: The new TDF is effective and safe in treating patients with moderate to severe cancer pain, and can significantly improve the quality of life. 展开更多
关键词 Transdermal fentanyl matrix patch (TDF) Cancer pain EFFICACY Safety Quality of life
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Fentanyl inhibits glucose-stimulated insulin release from β-cells in rat pancreatic islets 被引量:6
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作者 Tao-Lai Qian Xin-Hua Wang +2 位作者 Sheng Liu Liang Ma Ying Lu 《World Journal of Gastroenterology》 SCIE CAS CSCD 2009年第33期4163-4169,共7页
AIM: TO explore the effects of fentanyl on insulin release from freshly isolated rat pancreatic islets in static culture. METHODS: Islets were isolated from the pancreas of mature Sprague Dawley rats by common bile ... AIM: TO explore the effects of fentanyl on insulin release from freshly isolated rat pancreatic islets in static culture. METHODS: Islets were isolated from the pancreas of mature Sprague Dawley rats by common bile duct intraductal collagenase V digestion and were purified by discontinuous Ficoll density gradient centrifugation. The islets were divided into four groups according to the fentanyl concentration: control group (0 ng/mL), group I (0.3 ng/mL), group I (3.0 ng/mL), and group III (30 ng/mL). In each group, the islets were co-cultured for 48 h with drugs under static conditions with fentanyl alone, fentanyl + 0.1 μg/mL naloxone or fentanyl + 1.0 μg/mL naloxone. Cell viability was assessed by the MTT assay. Insulin release in response to low and high concentrations (2.8 mmol/L and 16.7 mmol/L, respectively) of glucose was investigated and electron microscopy morphological assessment was performed. RESULTS: Low- and high-glucose-stimulated insulin release in the control group was significantly higher than in groups I and II (62.33 ± 9.67 μIU vs 47.75 ± 8.47 μIU, 39.67 ± 6.18 μIU and 125.5 ± 22.04 μIU vs 96.17 ± 14.17 μIU, 75.17 ± 13.57 μIU, respectively, P 〈 0.01) and was lowest in group III (P 〈 0.01). After adding 1 μg/mL naloxone, insulin release in groups II and II was not different from the control group. Electron microscopy studies showed that the islets were damaged by 30 ng/ml fentanyl. CONCLUSION: Fentanyl inhibited glucose-stimulated insulin release from rat islets, which could be prevented by naloxone. Higher concentrations of fentanyl significantly damaged β-cells of rat islets. 展开更多
关键词 fentanyl INHIBITION Insulin release ISLETS
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Determination of structure-activity relationships between fentanyl analogs and human μ-opioid receptors based on active binding site models 被引量:3
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作者 Ming Liu Xiaoli Liu +2 位作者 Ping Wan Qiangsan Wu Wenxiang Hu 《Neural Regeneration Research》 SCIE CAS CSCD 2011年第4期267-276,共10页
Fentanyl is a potent and widely used clinical narcotic analgesic, as well as a highly selective IJ-opioid agonist. The present study established a homologous model of the human μ-opioid receptor; an intercomparison o... Fentanyl is a potent and widely used clinical narcotic analgesic, as well as a highly selective IJ-opioid agonist. The present study established a homologous model of the human μ-opioid receptor; an intercomparison of three types of μ-opioid receptor protein sequence homologous rates was made. The secondary receptor structure was predicted, the model reliability was assessed and verified using the Ramachandran plot and ProTab analysis. The predictive ability of the CoMFA model was further validated using an external test set. Using the Surflex-Dock program, a series of fentanyl analog molecules were docked to the receptor, the calculation results from Biopolymer/SitelD showed that the receptor had a deep binding area situated in the extracellular side of the transmembrane domains (TM) among TM3, TM5, TM6, and TMT. Results suggested that there might be 5 active areas in the receptor. The important residues were Asp147, Tyr148, and Tyr149 in TM3, Trp293, and His297 in TM6, and Trp318, His319, Ile322, and Tyr326 in TM7, which were located at the 5 active areas. The best fentanyl docking orientation position was the piperidine ring, which was nearly perpendicular to the membrane surface in the 7 TM domains. Molecular dynamic simulations were applied to evaluate potential relationships between ligand conformation and fentanyl substitution. 展开更多
关键词 μ-opioid receptor fentanyl analogs AGONIST active site structure-activity relationship
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Membrane Separator Interface for Mass-Spectrometric Analysis of Desflurane, Propofol and Fentanyl in Plasma and Cerebrospinal Fluid 被引量:3
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作者 V. Yu. Cherebillo V. N. Sokolov +3 位作者 V. A. Elokhin V. I. Nikolaev A. V. Polegaev A. Yu. Elizarov 《International Journal of Medical Physics, Clinical Engineering and Radiation Oncology》 2015年第4期263-267,共5页
Mass-spectrometric interface for the measurement of anaesthetic agent concentration in biological fluids (blood plasma and cerebrospinal fluid) is described. Sampling of biological fluids was performed during balanced... Mass-spectrometric interface for the measurement of anaesthetic agent concentration in biological fluids (blood plasma and cerebrospinal fluid) is described. Sampling of biological fluids was performed during balanced inhalational (desflurane, fentanyl) anaesthesia and total intravenous (propofol, fentanyl) anaesthesia. The described method for drug concentration measurement in biologic fluids does not require long-term sample processing before injecting the sample into mass-spectrometer interface, in contrast to chromatographic methods. A hydrophobic membrane was used in the interface to separate anaesthetic agents from biological fluids: inhalational anaesthetic desflurane, hypnotic propofol, analgesic fentanyl. A possibility to use the interface for measurement of desflurane and propofol absolute concentration in blood plasma and cerebrospinal fluid was demonstrated for the study of blood-brain barrier (BBB) properties. 展开更多
关键词 MEMBRANE MASS-SPECTROMETER ANESTHESIA DESFLURANE fentanyl
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Conversing Rate from Morphine to Continuous Infusion of Fentanyl in Patients Suffering Cancer Pain 被引量:1
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作者 王文萍 安达勇 《Chinese Journal of Cancer Research》 SCIE CAS CSCD 2007年第3期216-221,共6页
Objective: To investigate the proper conversing rate from morphine to continuous infusion of fentanyl in patients suffering cancer pain. Methods: A retrospective study was carried on in 20 patients with cancer pain ... Objective: To investigate the proper conversing rate from morphine to continuous infusion of fentanyl in patients suffering cancer pain. Methods: A retrospective study was carried on in 20 patients with cancer pain in Shizuoka Cancer Center from Sep. 2002 to Nov. 2003. Pain intensity, adverse reactions, and satisfaction index of patients were evaluated. Results: The pain intensity was stable in 17 patients indicating good pain-control within 1 week after conversion and unstable in 3 patients after conversion suggesting poor pain-control. Fentanyl injection could alleviate side effects and increase the satisfaction index of patients. Conclusion: The equipotent ratio for conversion of low dose morphine to fentanyl injection was established as 72:1, and for non low dose morphine a ratio less than 72:1 was proposed to get stable pain-relieving effect. But the equipotent ratio for conversion of morphine to continuous infusion of fentanyl could not be determined. We must consider the morphine dose before the confirmation of the conversing rate. 展开更多
关键词 cancer pain MORPHINE fentanyl administration clinical study
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Efficacy and Safety of Transdermal Fentanyl(TDF)in Treatment of Pain Caused by Interventional Embolization Therapy 被引量:1
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作者 朱旭 杨仁杰 陈辉 《Chinese Journal of Cancer Research》 SCIE CAS CSCD 2008年第4期316-319,共4页
Objective: Interventional embolization therapy is well accepted in cancer treatment, but patient may suffer from a moderate-to-severe pain after therapy and its quality of life (QoL) is influenced, this study is to... Objective: Interventional embolization therapy is well accepted in cancer treatment, but patient may suffer from a moderate-to-severe pain after therapy and its quality of life (QoL) is influenced, this study is to observe the efficacy and safety of transdermal fentanyl (TDF) in the management of pain caused by interventional embolization therapy. Methods: Morphine 10mg and TDF 25μg/h were immediately used in 52 patients who had moderate-to-severe pain complicated by interventional embolization therapy, the pain intensity was evaluated by visual analogue scale (VAS). If VAS≥4 at t2 h after treatment, the dosage of TDF added into 50 μg/h. At 0h, 12h, 24h, 72h, 1 week, 2 weeks after TD, the vas and adverse events were observed respectively. Result: There was an obvious decrease in VAS at 12h after TDF treatment in the patients of which only 9 patients used 50ug/h dosage after partial splenic embolization (PSE) therapy. Most patients got satisfactory pain relief both the TDF 25 μg/h and TDF 50 μg/h group (VAS 0-1). The adverse events were nausea, vomiting and dizzy, especially in the TDF 50 μg/h group. No respiratory depression was observed and only one patient got retention of urine. Conclusion: TDF was effective and safe in the treatment of moderate-to-severe pain after interventional embolizafion therapy. 展开更多
关键词 Transdermal fentanyl Interventional embolization therapy Pain relief
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Three-dimensional pharmacophore screening for fentanyl derivatives 被引量:1
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作者 Ming Liu Zhiguo Sun Wenxiang HU 《Neural Regeneration Research》 SCIE CAS CSCD 2012年第18期1398-1405,共8页
Fentanyl is a highly selective u-opioid receptor agonist with high analgesic activity. Three-dimensional pharmacophore models were built from a set of 50 fentanyl derivatives. These were employed to elucidate ligand-r... Fentanyl is a highly selective u-opioid receptor agonist with high analgesic activity. Three-dimensional pharmacophore models were built from a set of 50 fentanyl derivatives. These were employed to elucidate ligand-receptor interactions using information derived only from the ligand structure to identify new potential lead compounds. The present studies demonstrated that three hydrophobic regions, one positive ionizable region and two hydrogen bond acceptor region sites located on the molecule seem to be essential for analgesic activity. The results of the comparative molecular field analysis model suggested that both steric and electrostatic interactions play important roles. The contributions from steric and electrostatic fields for the model were 0.621 and 0.379, respectively. The pharmacophore model provides crucial information about how well the common features of a subject molecule overlap with the hypothesis model, which is very valuable for designing and optimizing new active structures. 展开更多
关键词 fentanyl genetic algorithm with linear assignment of hypermolecular alignment of datasets PHARMACOPHORE ANALGESIC comparative molecular field analysis
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Comparison between intravenous morphine versus fentanyl in acute pain relief in drug abusers with acute limb traumatic injury 被引量:1
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作者 Hojat Sheikh Motahar Vahedi Hadi Hajebi +2 位作者 Elnaz Vahidi Amir Nejati Morteza Saeedi 《World Journal of Emergency Medicine》 SCIE CAS CSCD 2019年第1期27-32,共6页
BACKGROUND: Rapid and effective pain relief in acute traumatic limb injuries(ATLI) is one of the most important roles of emergency physicians. In these situations, opioid addiction is an important concern because of t... BACKGROUND: Rapid and effective pain relief in acute traumatic limb injuries(ATLI) is one of the most important roles of emergency physicians. In these situations, opioid addiction is an important concern because of the dependency on opioids. The study aims to compare the effectiveness of intravenous(IV) fentanyl versus morphine in reducing pain in patients with opioid addiction who suffered from ATLI.METHODS: In this double-blind randomized clinical trial, 320 patients with ATLI, who presented to the emergency department(ED) from February 2016 to April 2016, were randomly divided into two groups. One group(160 patients) received 0.1 mg/kg IV morphine. The other group(160 patients) received 1 mcg/kg IV fentanyl. Patients' demographic data, pain score at specif ic intervals, vital signs, side effects, satisfaction and the need for rescue analgesia were recorded.RESULTS: Eight patients in the morphine group and five patients in the fentanyl group were excluded. Pain score in the fentanyl group had a significant decrease at 5-minute follow-up(P value=0.00). However, at 10, 30, and 60-minute follow-ups no signifi cant differences were observed between the two groups in terms of pain score reduction. The rescue analgesia was required in 12(7.7%) patients in the fentanyl group and in 48(31.6%) patients in the morphine group(P value=0.00). No signifi cant difference was observed regarding side effects, vital signs and patients' satisfaction between the two groups.CONCLUSION: Fentanyl might be an effective and safe drug in opioid addicts suffering from ATLI. 展开更多
关键词 fentanyl MORPHINE Opioid addiction Acute traumatic limb injury Pain score
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Effect of pretreatment with different concertrations of morphine, fentanyl and tramadol on the differentiation of human helper T cells in vitro 被引量:1
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作者 Yanning Qian Wenjie Jin +4 位作者 Ping Chen Ling Wang Huijuan Wang Yuke Tian Xuejun Zhou 《Journal of Nanjing Medical University》 2005年第6期313-315,共3页
Objective: To investigate and compare the .effects of different concentrations of morphine, fentanyl and tramadol on the differentiation of human adult helper T cells in vitro. Methods: Twenty out-patients without i... Objective: To investigate and compare the .effects of different concentrations of morphine, fentanyl and tramadol on the differentiation of human adult helper T cells in vitro. Methods: Twenty out-patients without immune disease were selected and their peripheral blood was collected. Then the Whole blood of peripheral blood mononuclear cells (PBMCs) were pretreated with different concentration of morphine, fentanyl and tramadol for 24 h. The level of CD4^+ IFN-γ^+ IL-2^+/CD4^+ IL-4^+ IL-10^+ was analyzed by three-color flow cytometry, and the CD4^+ CCR5^+ and CD4^+ CCR3 ^+ cells were counted to observe the imbalance of Th2/Th2. Results: The number of Th2 increased significantly and the ratio of Th2/Th2 decreased dramatically compared with the control group, and there was a dose-dependent fashion in all drugs. Conclusion: Morphine, fentanyl and tramadol can direct Th0 cells toward Th2 differentiation, especially morphine and fentanyl. 展开更多
关键词 MORPHINE fentanyl TRAMADOL helper T cells CYTOKINES
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