Objective:To evaluate the antinociceptive activity of perillyl acetate in mice and in silico simulations.Methods:The vehicle,perillyl acetate(100,150 and/or 200 mg/kg,i.p.),diazepam(2 mg/kg,i.p.)or morphine(6 mg/kg,i....Objective:To evaluate the antinociceptive activity of perillyl acetate in mice and in silico simulations.Methods:The vehicle,perillyl acetate(100,150 and/or 200 mg/kg,i.p.),diazepam(2 mg/kg,i.p.)or morphine(6 mg/kg,i.p.)was administered to mice,respectively.Rotarod test,acetic acidinduced abdominal writhing,formalin-induced nociception,hot plate test,and tail-flick test were performed.Opioid receptorsinvolvement in perillyl acetate antinociceptive effect was also investigated.Results:Perillyl acetate did not affect the motor coordination of mice.However,it reduced the number of acetic acid-induced abdominal twitches and licking times in the formalin test.There was an increase of latency time in the tail-flick test of 30 and 60minutes.Pretreatment with naloxone reversed the antinociceptive effect of perillyl acetate(200 mg/kg).In silico analysis demonstrated that perillyl acetate could bind toμ-opioid receptors.Conclusions:Perillyl acetate has antinociceptive effect at the spinal level in animal nociception models,without affecting the locomotor integrity and possibly throughμ-opioid receptors.In silico studies have suggested that perillyl acetate can act as aμ-opioid receptor agonist.展开更多
Introduction: Pain is the sensory and emotional experience, which altered human health and well-being. When pain does not resolve, it may be associated with a serious disease, condition, or injury that needs timely me...Introduction: Pain is the sensory and emotional experience, which altered human health and well-being. When pain does not resolve, it may be associated with a serious disease, condition, or injury that needs timely medical care and also irrational prescribing of analgesics, which is possible to lead to unwanted side effects. Therefore, this study has been intended to evaluate the prescribing pattern of analgesics drugs at Boru Meda Hospital. Method: A retrospective cross sectional descriptive study was conducted. A total of 200 prescriptions containing analgesic were systematically collected by using well designed and pretested Data collection format. The necessary information was extracted from the prescription sheets by trained pharmacists and later analyzed using SPSS version 20 software. Result: Regarding prescribed analgesic acetaminophen 115 (36.9%) was the most prescribed, and then followed diclofenac 83 (26.6%) and Ibuprofen 64 (20.5%). The maximum number of analgesic drugs was administered to patients by oral rout (75%), which is followed by parenteral (19%). About dosing approach 94% acetaminophen prescribed as needed (PRN) based, whereas ibuprofen 59.4% and tramadol 40% were prescribed as twice a day (bid) based. Acute fibril illness (13.6%) was the highest reason for prescribing analgesics. Conclusion: Majority of the prescription analgesics drugs were prescribed as PRN dosing approaches with a very large percentage of oral medications. Some of the prescriptions revealed irrational prescribing of analgesics, in accordance of clinical indication, frequency of administration and combination of analgesic.展开更多
AIM: To evaluate the opioid-sparing effect of selective cyclooxygenase-2(COX-2) inhibitors on short-term surgical outcomes after open colorectal surgery.METHODS: Patients undergoing open colorectal resection within an...AIM: To evaluate the opioid-sparing effect of selective cyclooxygenase-2(COX-2) inhibitors on short-term surgical outcomes after open colorectal surgery.METHODS: Patients undergoing open colorectal resection within an enhanced recovery after surgery protocol from 2011 to 2015 were reviewed. Patients with combined general anesthesia and epidural anesthesia, and those with acute colonic obstruction or perforation were excluded. Patients receiving selective COX-2 inhibitor were compared with well-matched individuals without such a drug. Outcome measures included numeric pain score and morphine milligram equivalent(MME) consumption on postoperative day(POD) 1-3, gastrointestinal recovery(time to tolerate solid diet and time to defecate), complications and length of postoperative stay.RESULTS: There were 75 patients in each group. Pain score on POD 1-3 was not significantly different between two groups. However, MME consumption and MME consumption per kilogram body weight on POD 1-3 was significantly less in patients receiving a selective COX-2 inhibitor(P < 0.001). Median MME consumption per kilogram body weight on POD 1-3 was 0.09, 0.06 and nil, respectively in patients receiving a selective COX-2 inhibitor and 0.22, 0.25 and 0.07, respectively in the comparative group(P < 0.001), representing at least 59% opioidreduction. Patients prescribing a selective COX-2 inhibitor had a shorter median time to resumption of solid diet [1(IQR 1-2) d vs 2(IQR 2-3) d; P < 0.001] and time to first defecation [2(IQR 2-3) d vs 3(IQR 3-4) d; P < 0.001]. There was no significant difference in overall postoperative complications between two groups. However, median postoperative stay was significantly 1-d shorter in patients prescribing a selective COX-2 inhibitor [4(IQR 3-5) d vs 5(IQR 4-6) d; P < 0.001]. CONCLUSION: Perioperative administration of oral selective COX-2 inhibitors significantly decreased intravenous opioid consumption, shortened time to gastrointestinal recovery and reduced hospital stay after open colorectal surgery.展开更多
Between the illicit use of opioids and attendant overdoses, and accidental overdoses with prescribed drugs, overuse of opioids has become a serious problem. At the same time, finding that fine balance between minimizi...Between the illicit use of opioids and attendant overdoses, and accidental overdoses with prescribed drugs, overuse of opioids has become a serious problem. At the same time, finding that fine balance between minimizing the risk of opioid misuse and abuse while at the same time providing access to treatment for patients who need pain control presents an ongoing challenge. Efforts to discover and develop better agents have led to what we term “new-look” opioids. We summarize here one such approach—known as biased ligands. By targeting a subset of GPCR signal transduction, this approach attempts to increase the separation between therapeutic and adverse effects.展开更多
The incidence of prescription opioid misuse in Canada is increasing. Initiatives for safe prescribing practices for opioid medications include risk assessment for current and future opioid misuse. A clinical screening...The incidence of prescription opioid misuse in Canada is increasing. Initiatives for safe prescribing practices for opioid medications include risk assessment for current and future opioid misuse. A clinical screening tool that can be universally applied to all patient populations is currently not available. Our objective was to provide a brief narrative review on opioid misuse from a Canadian perspective as well as a critical appraisal of the available clinical screening tools for detecting aberrant behaviors associated with opioid misuse. The Drug Abuse Screening Test, Addiction Behaviors Checklist, Diagnosis, Intractability, Risk and Efficacy Inventory, Pain Assessment and Documentation Tool, Prescription Drug Use Questionnaire, Prescription Opioid therapy Questionnaire, Screener and Opioid Assessment for Patients with Pain(SOAPP), Revised SOAPP, Pain Medication Questionnaire, Opioid Risk Tool and Current Opioid Misuse Measure were included in the following review. Overall, a wide variability in quality, sensitivity and specificity was observed between screening tools. There is an overall lack of applicability to diverse patient populations as the majority of screening tools have been validated in pain clinic populations only. To conclude, there is a great need for a validated and convenient aberrant behaviors risk assessment tool that can be applied to a diverse patient population in a clinical setting.展开更多
Given the rising incidence of opioid misuse and opioid-related deaths worldwide, it is imperative to find nonopioid analgesic adjuncts for perioperative pain management. Perioperative opioid exposure in opioid-na<s...Given the rising incidence of opioid misuse and opioid-related deaths worldwide, it is imperative to find nonopioid analgesic adjuncts for perioperative pain management. Perioperative opioid exposure in opioid-na<span style="color:#4F4F4F;font-family:-apple-system, "font-size:14px;white-space:normal;background-color:#F7F7F7;">ï</span>ve patients for even minor surgical procedures may result in significant opioid dependence. Although the use of intravenous lidocaine in the perioperative period is not novel, recently it has been proposed as an important adjunct to multimodal analgesia. In addition to improving acute pain, lidocaine may reduce the incidence of chronic post-operative pain syndrome (CPPS), improve bowel function, and decrease post-operative nausea and vomiting (PONV) thereby speeding up the post-operative recovery process. Furthermore, lidocaine has efficacy in a variety of procedures including abdominal, gynecological, and urological surgeries. The aim of this narrative review is to evaluate the effects of intravenous lidocaine compared to traditional analgesic methods on post-operative pain control and recovery for various surgical procedures.展开更多
Pain is a sensation related to potential or actual damage in some tissue of the body. The mainstay of medical pain therapy remains drugs that have been around for decades, like non-steroidal anti-inflammatory drugs （...Pain is a sensation related to potential or actual damage in some tissue of the body. The mainstay of medical pain therapy remains drugs that have been around for decades, like non-steroidal anti-inflammatory drugs （NSAIDs）, or opiates. However, adverse effects of opiates, particularly tolerance, limit their clinical use. Several lines of investigations have shown that systemic （intraperitoneal） administration of NSAIDs induces antinociception with some effects of tolerance. In this review, we report that repeated microinjection of NSAIDs analgin, clodifen, ketorolac and xefocam into the central nucleus of amygdala, the midbrain periaqueductal grey matter and nucleus raphe magnus in the following 4 days result in progressively less antinociception compared to the saline control testing in the tail-flick reflex and hot plate latency tests. Hence, tolerance develops to these drugs and cross-tolerance to morphine in male rats. These findings strongly support the suggestion of endogenous opioid involvement in NSAIDs antinociception and tolerance in the descending pain-control system. Moreover, the periaqueductal grey-rostral ventro-medial part of medulla circuit should be viewed as a pain-modulation system. These data are important for human medicine. In particular, cross-tolerance between non-opioid and opioid analgesics should be important in the clinical setting.展开更多
Objective： To investigate the analgesic effects of Nourishing yin and Unblocking meridians Receipe （NUR） combined with opioid analgesics in managing cancer pain. Methods： All the patients enrolled were differentia...Objective： To investigate the analgesic effects of Nourishing yin and Unblocking meridians Receipe （NUR） combined with opioid analgesics in managing cancer pain. Methods： All the patients enrolled were differentiated as of yin deficiency and meridian blocked syndrome type of TCM. Forty-one of them in the treated group were treated with NUR combined with opioid analgesics, while 43 of them in the control group were given opioid analgesics alone with successive 14 days as one treatment course for both groups. Results： The indexes of the treated group were superior to those in the control group as to the degree of pain-relieving, the therapeutic effect of analgesia, the occurrence frequency of cancer pain every day and its duration each time, the analgesic initial time, and the quality of life. Conclusion： NUR combined with opioid analgesics in cancer pain management was more effective than opioid analgesics alone. KEY WORDS展开更多
基金supported by funds from the Coordination for the Improvement of Higher Education Personnel(CAPES)National Council for Scientific and Technological Development(CNPq)。
文摘Objective:To evaluate the antinociceptive activity of perillyl acetate in mice and in silico simulations.Methods:The vehicle,perillyl acetate(100,150 and/or 200 mg/kg,i.p.),diazepam(2 mg/kg,i.p.)or morphine(6 mg/kg,i.p.)was administered to mice,respectively.Rotarod test,acetic acidinduced abdominal writhing,formalin-induced nociception,hot plate test,and tail-flick test were performed.Opioid receptorsinvolvement in perillyl acetate antinociceptive effect was also investigated.Results:Perillyl acetate did not affect the motor coordination of mice.However,it reduced the number of acetic acid-induced abdominal twitches and licking times in the formalin test.There was an increase of latency time in the tail-flick test of 30 and 60minutes.Pretreatment with naloxone reversed the antinociceptive effect of perillyl acetate(200 mg/kg).In silico analysis demonstrated that perillyl acetate could bind toμ-opioid receptors.Conclusions:Perillyl acetate has antinociceptive effect at the spinal level in animal nociception models,without affecting the locomotor integrity and possibly throughμ-opioid receptors.In silico studies have suggested that perillyl acetate can act as aμ-opioid receptor agonist.
文摘Introduction: Pain is the sensory and emotional experience, which altered human health and well-being. When pain does not resolve, it may be associated with a serious disease, condition, or injury that needs timely medical care and also irrational prescribing of analgesics, which is possible to lead to unwanted side effects. Therefore, this study has been intended to evaluate the prescribing pattern of analgesics drugs at Boru Meda Hospital. Method: A retrospective cross sectional descriptive study was conducted. A total of 200 prescriptions containing analgesic were systematically collected by using well designed and pretested Data collection format. The necessary information was extracted from the prescription sheets by trained pharmacists and later analyzed using SPSS version 20 software. Result: Regarding prescribed analgesic acetaminophen 115 (36.9%) was the most prescribed, and then followed diclofenac 83 (26.6%) and Ibuprofen 64 (20.5%). The maximum number of analgesic drugs was administered to patients by oral rout (75%), which is followed by parenteral (19%). About dosing approach 94% acetaminophen prescribed as needed (PRN) based, whereas ibuprofen 59.4% and tramadol 40% were prescribed as twice a day (bid) based. Acute fibril illness (13.6%) was the highest reason for prescribing analgesics. Conclusion: Majority of the prescription analgesics drugs were prescribed as PRN dosing approaches with a very large percentage of oral medications. Some of the prescriptions revealed irrational prescribing of analgesics, in accordance of clinical indication, frequency of administration and combination of analgesic.
文摘AIM: To evaluate the opioid-sparing effect of selective cyclooxygenase-2(COX-2) inhibitors on short-term surgical outcomes after open colorectal surgery.METHODS: Patients undergoing open colorectal resection within an enhanced recovery after surgery protocol from 2011 to 2015 were reviewed. Patients with combined general anesthesia and epidural anesthesia, and those with acute colonic obstruction or perforation were excluded. Patients receiving selective COX-2 inhibitor were compared with well-matched individuals without such a drug. Outcome measures included numeric pain score and morphine milligram equivalent(MME) consumption on postoperative day(POD) 1-3, gastrointestinal recovery(time to tolerate solid diet and time to defecate), complications and length of postoperative stay.RESULTS: There were 75 patients in each group. Pain score on POD 1-3 was not significantly different between two groups. However, MME consumption and MME consumption per kilogram body weight on POD 1-3 was significantly less in patients receiving a selective COX-2 inhibitor(P < 0.001). Median MME consumption per kilogram body weight on POD 1-3 was 0.09, 0.06 and nil, respectively in patients receiving a selective COX-2 inhibitor and 0.22, 0.25 and 0.07, respectively in the comparative group(P < 0.001), representing at least 59% opioidreduction. Patients prescribing a selective COX-2 inhibitor had a shorter median time to resumption of solid diet [1(IQR 1-2) d vs 2(IQR 2-3) d; P < 0.001] and time to first defecation [2(IQR 2-3) d vs 3(IQR 3-4) d; P < 0.001]. There was no significant difference in overall postoperative complications between two groups. However, median postoperative stay was significantly 1-d shorter in patients prescribing a selective COX-2 inhibitor [4(IQR 3-5) d vs 5(IQR 4-6) d; P < 0.001]. CONCLUSION: Perioperative administration of oral selective COX-2 inhibitors significantly decreased intravenous opioid consumption, shortened time to gastrointestinal recovery and reduced hospital stay after open colorectal surgery.
文摘Between the illicit use of opioids and attendant overdoses, and accidental overdoses with prescribed drugs, overuse of opioids has become a serious problem. At the same time, finding that fine balance between minimizing the risk of opioid misuse and abuse while at the same time providing access to treatment for patients who need pain control presents an ongoing challenge. Efforts to discover and develop better agents have led to what we term “new-look” opioids. We summarize here one such approach—known as biased ligands. By targeting a subset of GPCR signal transduction, this approach attempts to increase the separation between therapeutic and adverse effects.
文摘The incidence of prescription opioid misuse in Canada is increasing. Initiatives for safe prescribing practices for opioid medications include risk assessment for current and future opioid misuse. A clinical screening tool that can be universally applied to all patient populations is currently not available. Our objective was to provide a brief narrative review on opioid misuse from a Canadian perspective as well as a critical appraisal of the available clinical screening tools for detecting aberrant behaviors associated with opioid misuse. The Drug Abuse Screening Test, Addiction Behaviors Checklist, Diagnosis, Intractability, Risk and Efficacy Inventory, Pain Assessment and Documentation Tool, Prescription Drug Use Questionnaire, Prescription Opioid therapy Questionnaire, Screener and Opioid Assessment for Patients with Pain(SOAPP), Revised SOAPP, Pain Medication Questionnaire, Opioid Risk Tool and Current Opioid Misuse Measure were included in the following review. Overall, a wide variability in quality, sensitivity and specificity was observed between screening tools. There is an overall lack of applicability to diverse patient populations as the majority of screening tools have been validated in pain clinic populations only. To conclude, there is a great need for a validated and convenient aberrant behaviors risk assessment tool that can be applied to a diverse patient population in a clinical setting.
文摘Given the rising incidence of opioid misuse and opioid-related deaths worldwide, it is imperative to find nonopioid analgesic adjuncts for perioperative pain management. Perioperative opioid exposure in opioid-na<span style="color:#4F4F4F;font-family:-apple-system, "font-size:14px;white-space:normal;background-color:#F7F7F7;">ï</span>ve patients for even minor surgical procedures may result in significant opioid dependence. Although the use of intravenous lidocaine in the perioperative period is not novel, recently it has been proposed as an important adjunct to multimodal analgesia. In addition to improving acute pain, lidocaine may reduce the incidence of chronic post-operative pain syndrome (CPPS), improve bowel function, and decrease post-operative nausea and vomiting (PONV) thereby speeding up the post-operative recovery process. Furthermore, lidocaine has efficacy in a variety of procedures including abdominal, gynecological, and urological surgeries. The aim of this narrative review is to evaluate the effects of intravenous lidocaine compared to traditional analgesic methods on post-operative pain control and recovery for various surgical procedures.
基金supported by the grant from Georgian National Science Foundation,No.GNSF/ST07/6-234
文摘Pain is a sensation related to potential or actual damage in some tissue of the body. The mainstay of medical pain therapy remains drugs that have been around for decades, like non-steroidal anti-inflammatory drugs （NSAIDs）, or opiates. However, adverse effects of opiates, particularly tolerance, limit their clinical use. Several lines of investigations have shown that systemic （intraperitoneal） administration of NSAIDs induces antinociception with some effects of tolerance. In this review, we report that repeated microinjection of NSAIDs analgin, clodifen, ketorolac and xefocam into the central nucleus of amygdala, the midbrain periaqueductal grey matter and nucleus raphe magnus in the following 4 days result in progressively less antinociception compared to the saline control testing in the tail-flick reflex and hot plate latency tests. Hence, tolerance develops to these drugs and cross-tolerance to morphine in male rats. These findings strongly support the suggestion of endogenous opioid involvement in NSAIDs antinociception and tolerance in the descending pain-control system. Moreover, the periaqueductal grey-rostral ventro-medial part of medulla circuit should be viewed as a pain-modulation system. These data are important for human medicine. In particular, cross-tolerance between non-opioid and opioid analgesics should be important in the clinical setting.
文摘Objective： To investigate the analgesic effects of Nourishing yin and Unblocking meridians Receipe （NUR） combined with opioid analgesics in managing cancer pain. Methods： All the patients enrolled were differentiated as of yin deficiency and meridian blocked syndrome type of TCM. Forty-one of them in the treated group were treated with NUR combined with opioid analgesics, while 43 of them in the control group were given opioid analgesics alone with successive 14 days as one treatment course for both groups. Results： The indexes of the treated group were superior to those in the control group as to the degree of pain-relieving, the therapeutic effect of analgesia, the occurrence frequency of cancer pain every day and its duration each time, the analgesic initial time, and the quality of life. Conclusion： NUR combined with opioid analgesics in cancer pain management was more effective than opioid analgesics alone. KEY WORDS
