The Experts below are selected from a list of 75 Experts worldwide ranked by ideXlab platform
Jianjun Yang - One of the best experts on this subject based on the ideXlab platform.
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effects of Dezocine for the prevention of postoperative catheter related bladder discomfort a prospective randomized trial
Drug Design Development and Therapy, 2019Co-Authors: Guangfen Zhang, Jie Guo, Lili Qiu, Man Zheng, Jiangyan Xia, Jianjun YangAbstract:Purpose: To evaluate the effects of Dezocine on the prevention of postoperative catheter-related bladder discomfort (CRBD). Patients and methods: Ninety-six adult patients undergoing abdominal surgery with urinary catheterization under general anesthesia were randomized into Dezocine and control (flurbiprofen) groups. The postoperative CRBD, pain score, sedation score and adverse effects were evaluated at 0, 1, 2 and 6 hrs after tracheal extubation. Results: The primary outcome showed a lower incidence of CRBD at 1 hr post-extubation in the Dezocine group (29.17%) than the control group (58.33%, P 0.05); however, the overall severity of CRBD was decreased in the Dezocine group compared with the control group (P<0.05). Conclusion: Intraoperative Dezocine reduces the incidence and severity of postoperative CRBD without clinically relevant adverse effects.
Jiangyan Xia - One of the best experts on this subject based on the ideXlab platform.
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effects of Dezocine for the prevention of postoperative catheter related bladder discomfort a prospective randomized trial
Drug Design Development and Therapy, 2019Co-Authors: Guangfen Zhang, Jie Guo, Lili Qiu, Man Zheng, Jiangyan Xia, Jianjun YangAbstract:Purpose: To evaluate the effects of Dezocine on the prevention of postoperative catheter-related bladder discomfort (CRBD). Patients and methods: Ninety-six adult patients undergoing abdominal surgery with urinary catheterization under general anesthesia were randomized into Dezocine and control (flurbiprofen) groups. The postoperative CRBD, pain score, sedation score and adverse effects were evaluated at 0, 1, 2 and 6 hrs after tracheal extubation. Results: The primary outcome showed a lower incidence of CRBD at 1 hr post-extubation in the Dezocine group (29.17%) than the control group (58.33%, P 0.05); however, the overall severity of CRBD was decreased in the Dezocine group compared with the control group (P<0.05). Conclusion: Intraoperative Dezocine reduces the incidence and severity of postoperative CRBD without clinically relevant adverse effects.
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effect of propofol combined with opioids on cough reflex suppression in gastroscopy study protocol for a double blind randomized controlled trial
BMJ Open, 2017Co-Authors: Ning Yin, Jiangyan Xia, Yizhi Cao, Jing Yuan, Jue XieAbstract:Introduction The best methods for inducing analgesia and sedation for gastroscopy are still debated but finding an adequate regimen of sedation/analgesia is important. Stimulation of the larynx under sedation can cause reflex responses. Propofol with opioids has been recommended for gastroscopy sedation but the effects on cough reflex suppression remain unclear. This trial will evaluate the effects of propofol combined with small doses of Dezocine, oxycodone, sufentanil or fentanyl for gastroscopy. We hypothesise that better performance may be obtained with a combination of propofol and oxycodone. We will observe the incidence and degree of reflex coughing and gagging under sedation when using propofol combined with one of the above drugs or propofol alone. Methods and analysis This will be a prospective, randomised, double-blind, controlled trial. ASA I–II level patients aged 18–65 years and scheduled for gastroscopy will be included. It is planned that 500 subjects will be randomised to intravenously receive 2–2.2 mg/kg propofol plus 0.5–0.8 μg/kg fentanyl (fentanyl group), 2–2.2 mg/kg propofol plus 0.05–0.08 μg/kg sufentanil (sufentanil group), 2–2.2 mg/kg propofol plus 0.04–0.05 mg/kg Dezocine (Dezocine group), 2–2.2 mg/kg propofol plus 0.04–0.05 mg/kg oxycodone (oxycodone group), or 2.4–3 mg/kg propofol plus 2–2.5 mL saline (control group) for sedation. The primary endpoint is the incidence and degree of reflex coughing and gagging. The secondary endpoints include the occurrence of discomfort or side effects, the use of jaw thrust, assisted ventilation or additional propofol, recovery time, duration of procedure and Steward score. Ethics and dissemination This study has been approved by the Institutional Ethics Committee for Clinical Research of Zhongda Hospital, Affiliated to Southeast University (No. 2015ZDSYLL033.0). The results of the trial will be published in an international peer-reviewed journal. Trial registration This study has been registered with the Chinese Clinical Trial Register (No. ChiCTR-ICR-15006952). Trial status At the time of manuscript submission, the study was in the recruitment phase.
Mitchell J. Picker - One of the best experts on this subject based on the ideXlab platform.
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Sex-related differences in the antinociceptive effects of opioids: importance of rat genotype, nociceptive stimulus intensity, and efficacy at the µ opioid receptor
Psychopharmacology, 2000Co-Authors: Charles D. Cook, Andrew C. Barrett, Emily L. Roach, Joseph R. Bowman, Mitchell J. PickerAbstract:Rationale: Recent studies indicate that morphine is more potent as an antinociceptive agent in male than female rodents and monkeys. Objectives: To evaluate the influence of sex, nociceptive stimulus intensity and an opioid's relative efficacy on opioid-induced antinociception in rat strains (F344 and Lewis) that display differential sensitivity to morphine antinociception. Methods: Antinociceptive testing was conducted using a rat warm-water (50–56°C) tail-withdrawal procedure. Dose–response and time-course determinations were performed with various opioids. Results: Across the nociceptive stimulus intensities tested, the high-efficacy µ opioids morphine, etorphine, and levorphanol were equally effective in males and females, but on average 2.5-fold more potent in males. At moderate stimulus intensities, the low-efficacy µ opioid buprenorphine was approximately 0.4-fold more potent in males, and at higher stimulus intensities more potent and effective (greater maximal effect) in males. At low stimulus intensities, the low-efficacy µ opioid Dezocine and the µ/κ opioid butorphanol were greater than 8.9-fold more potent in males, and at moderate stimulus intensities were more potent and effective in males. At a low stimulus intensity, the µ/κ opioid nalbuphine was more potent and effective in males. At stimulus intensities in which buprenorphine, Dezocine, butorphanol, and nalbuphine produced maximal effects in males but not females, these opioids antagonized the effects of morphine in females. Genotype-related differences were noted as opioids were generally more potent in F344 than Lewis males, whereas no consistent differences were observed between F344 and Lewis females. Conclusions: That sex differences in the potency and effectiveness of opioids increased with decreases in the opioid's relative efficacy and with increases in the nociceptive stimulus intensity suggests that the relative efficacy of µ opioids as antinociceptive agents is greater in male than female rats.
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naltrexone and β funaltrexamine antagonism of the antinociceptive and response rate decreasing effects of morphine Dezocine and d propoxyphene
Psychopharmacology, 1999Co-Authors: Ellen A Walker, Michael J Tiano, Steven I Benyas, Linda A Dykstra, Mitchell J. PickerAbstract:Rationale: Patterns of competitive and insurmountable antagonism provide important data to guide the classification and characterization of different types of opioid agonists as well as infer the mechanism of action for agonists. Objective: Experiments with the competitive antagonist, naltrexone, and the insurmountable antagonist, β-funaltrexamine (β-FNA), were conducted to determine whether the antinociceptive and rate-decreasing effects of the opioid agonists Dezocine and d-propoxyphene are 1) mediated through µ opioid receptors in rats, and 2) differ from morphine with respect to relative efficacy. Methods: The rat tail-withdrawal assay was used to measure antinociception and a fixed ratio 20 (FR20) schedule of food delivery was used to measure rate suppression. Results: Naltrexone (0.01–1.0 mg/kg) was approximately equipotent as an antagonist of the antinociceptive and rate-decreasing effects of both morphine and Dezocine and as an antagonist of the antinociceptive effects of d-propoxyphene. Naltrexone failed to block the rate-decreasing effects of d-propoxyphene. β-FNA (5 and 10 mg/kg) also antagonized the antinociceptive and rate-decreasing effects of morphine and Dezocine as well as the antinociceptive effects of d-propoxyphene. β-FNA failed to produce a dose-dependent antagonism of the rate-decreasing effects of d-propoxyphene. Conclusions: These data suggest that the antinociceptive effects of morphine, Dezocine, and d-propoxyphene and the rate-decreasing effects of morphine and Dezocine are mediated through µ opioid receptors. Overall, high doses of β-FNA produced a greater degree of antagonism of the behavioral effects of Dezocine than morphine or d-propoxyphene, confirming other reports that Dezocine is a lower efficacy agonist than morphine. Additionally, the degree of antagonism produced by β-FNA was greater for the antinociceptive effects of all three compounds than for the rate-decreasing effects.
Guangfen Zhang - One of the best experts on this subject based on the ideXlab platform.
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effects of Dezocine for the prevention of postoperative catheter related bladder discomfort a prospective randomized trial
Drug Design Development and Therapy, 2019Co-Authors: Guangfen Zhang, Jie Guo, Lili Qiu, Man Zheng, Jiangyan Xia, Jianjun YangAbstract:Purpose: To evaluate the effects of Dezocine on the prevention of postoperative catheter-related bladder discomfort (CRBD). Patients and methods: Ninety-six adult patients undergoing abdominal surgery with urinary catheterization under general anesthesia were randomized into Dezocine and control (flurbiprofen) groups. The postoperative CRBD, pain score, sedation score and adverse effects were evaluated at 0, 1, 2 and 6 hrs after tracheal extubation. Results: The primary outcome showed a lower incidence of CRBD at 1 hr post-extubation in the Dezocine group (29.17%) than the control group (58.33%, P 0.05); however, the overall severity of CRBD was decreased in the Dezocine group compared with the control group (P<0.05). Conclusion: Intraoperative Dezocine reduces the incidence and severity of postoperative CRBD without clinically relevant adverse effects.
Zhi-chao Xiao - One of the best experts on this subject based on the ideXlab platform.
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Pharmacological Characterization of Dezocine, a Potent Analgesic Acting as a κ Partial Agonist and μ Partial Agonist
Scientific reports, 2018Co-Authors: Yu-hua Wang, Jing-rui Chai, Gui-ying Zan, George Yun-kun Liu, Jian-dong Long, Xiang Huang, Zhi-chao XiaoAbstract:Dezocine is becoming dominated in China market for relieving moderate to severe pain. It is believed that Dezocine’s clinical efficacy and little chance to provoke adverse events during the therapeutic process are mainly attributed to its partial agonist activity at the μ opioid receptor. In the present work, we comprehensively studied the pharmacological characterization of Dezocine and identified that the analgesic effect of Dezocine was a result of action at both the κ and μ opioid receptors. We firstly found that Dezocine displayed preferential binding to μ opioid receptor over κ and δ opioid receptors. Dezocine, on its own, weakly stimulated G protein activation in cells expressing κ and μ receptors, but in the presence of full κ agonist U50,488 H and μ agonist DAMGO, Dezocine inhibited U50,488H- and DAMGO-mediated G protein activation, indicating that Dezocine was a κ partial agonist and μ partial agonist. Then the in intro results were verified by in vivo studies in mice. We observed that Dezocine-produced antinociception was significantly inhibited by κ antagonist nor-BNI and μ antagonist β-FNA pretreatment, indicating that Dezocine-mediated antinociception was via both the κ and μ opioid receptors. When co-administrating of Dezocine with U50,488 H or morphine, Dezocine was capable of inhibiting U50,488H- or morphine-induced antinociception. Finally, κ receptor activation-associated side effect sedation was investigated. We found that Dezocine displayed limited sedative effect with a ceiling effecting at a moderate dose. Thus, our work led to a better understanding of the analgesic mechanism of action of Dezocine in vivo.