• Title/Summary/Keyword: Analgesic effects

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The Joins (SKI 306X) study: Effects on Arachidonic acid metabolism pathway and other inflammatory mediators

  • Ryu, Keun-Ho;Jung, Ki-Won;Han, Chang-Kyun;Kwak, Wie-Jong;Cho, Yong-Baik
    • Proceedings of the PSK Conference
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    • 2003.04a
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    • pp.143.2-144
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    • 2003
  • Joins (SKI 306X) is now clinically used for the treatment of osteoarthritis (OA). In previous reports, Joins a natural herbal product extracted from three herbs Clematis Radix. Trichosanthes Radix and Prunella Flos, was shown to have good analgesic and anti-inflammatory effects in several in vivo models. e.g., acetic acid-induced pain, carrageenan-induced paw edema and adjuvant-induced arthritis. (omitted)

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A Novel and Highly Potent Non-vanilloid VR Antagonist

  • Suh, Young-Ger;Lee, Yong-Sil;Lee, Bo-Young;Min, Kyung-Hoon;Kim, Jin-Kwan;Seung, Ho-Sun;Park, Young-Ho
    • Proceedings of the PSK Conference
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    • 2003.04a
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    • pp.239.1-239.1
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    • 2003
  • The vanilloid receptor VR has attracted great interest as a sensory transducer for capsaicin. protons, and heat. and as a therapeutic target. On the basis of the previous studies on vanilloid agonists and antagonists. we have looked for non-vanilloid VR antagonists by developing ideal vanilloid equivalents, which might provide the perfect analgesic effects without the side effects caused by vanilloid receptor agonists. (omitted)

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Synthesis and Biological Activities of New Substituted Indoles

  • Hishmat, Orchidee H.;Nakkady, Sally S.;El Shabrawy, Osama A.;Mahmoud, Sawsan S.
    • Archives of Pharmacal Research
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    • v.15 no.1
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    • pp.104-108
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    • 1992
  • 2, 3-Diphenyl-6-formyl-5-methoxyindole reacts with ethyl cyano acetate to yield the arylidene derivative which forms with urea and thiourea the corresponding pyrimidine derivatives. The arylidene derivatives react with hydrazines and with active methylenes to form the respective pyrazole derivatives and the $\alpha, \;\beta$-disubstituted acrylonitriles. Seven new compounds were tested for their effects on the arterial blood pressure of rats and analgesic activity.

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Effects of Morphine and Buprenorphine Intravenous Infusion for Postoperative Pain (Morphine과 Buprenorphine의 지속적 정주에 의한 술후 통증 억제효과의 비교)

  • Baek, Sun-Ki;So, Sang-Yoon;Han, Young-Jin;Choe, Huhn
    • The Korean Journal of Pain
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    • v.7 no.1
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    • pp.78-83
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    • 1994
  • Morphine, a $\mu$-receptor agonist, produces strong analgesic effect with some side effects such as nausea, vomiting, urinary retension, somnolence, and respiratory depression. Buprenorphine also provides strong analgesic effects, and hemodynamic changes after continuous infusion of morphine, or buprenorphine-ketorolac combination in gynecologic patients. Analgesic effect was assessed by visual analogue scale(VAS) and Prince Henry scale(PHS). Morphine group, initial 2 mg of bolus morphine was followed by 48 mg/96 ml of continuous infusion. Buprenorphine group, initial 0.1 mg of buprenorphine was followed up with infusion by 2.3 mg/100 ml. Half dose of both initial bolus and maintenance buprenorphine with ketorolac 15 mg for bolus and 60 mg for maintenance were infused in buprenorphine-ketorolac combination group. No significant hemodynamic changes were seen in any of the groups. VAS significantly decreased after 15 minutes of infusion in all three groups, and was significantly lower in morphine group than the other 2 groups, after 60 minutes. PHS was decreased significantly 15 minutes after infusion in the morphine group, and after 60 minutes in two other groups. The incidence of side effects were similar between morphine and buprenorphine groups, but significantly reduced in buprenorphine-ketorolac combination group. We concluded that buprenorphine could be an alternative to morphine for postoperative pain, and smaller dose of buprenorphine could be used if it is combined with ketorolac with less side effects.

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Effects of Preincisional Administration of Magnesium Sulfate on Postoperative Pain and Recovery of Pulmonary Function in Patients Undergoing Gastrectomy (위절제술 환자에서 술전 마그네슘 정주가 술후 통증 및 폐기능 회복에 미치는 영향)

  • Ko, Seong-Hoon;Jang, Young-Ik;Lee, Jun-Rye;Han, Young-Jin;Choe, Huhn
    • The Korean Journal of Pain
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    • v.13 no.1
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    • pp.31-37
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    • 2000
  • Background: Recent studies suggested that a preoperative block of N-methyl-D-aspartate (NMDA) receptors with NMDA antagonists may reduce postoperative pain. In this double-blind study, magnesium sulfate, a natural NMDA receptor antagonist, was administered preoperatively to investigate the effects of magnesium sulfate on postoperative pain and pulmonary function. Methods: Seventy patients who were to undergo gastrectomy under general anesthesia were randomly assigned to one of three groups. Groups 2 and 3 received intravenous magnesium, preoperatively (Group 2: 50 mg/kg bolus, 7.5 mg/kg/hr for 20 hr, Group 3: 50 mg/kg bolus, 15 mg/kg/hr for 20 hr). Group 1 received normal saline as the control group. Visual analog scale (VAS) for postoperative pain and mood, cumulative analgesic consumption, recovery of pulmonary function and side effects were evaluated at 6, 24, 48 and 72 hours after the operation. Results: In Groups 2 and 3, plasma concentration of magnesium were significantly higher than in Group 1 at 6 and 20 hours after infusion (P<0.05). There were no significant differences in the analgesic consumption, and recovery of pulmonary function and the incidence of side effects at 6, 24, 48 and 72 hours after the operation among the three groups. In Group 3, pain scores at rest measured 24 and 48 hours after operation were lower than the control group, and pain scores when deep breathing were significantly lower than the control group at postoperative 6, 24, 48, and 72 hours. Conclusions: We conclude that intravenous infusion of greater amount of magnesium has little effectiveness in reducing postoperative pain. However, further studies are needed to characterize the clinical significance of these effects on postoperative pain.

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Effects of Hyunggyeyungyotang and Kamihyunggyeyungyotang administration on the anti-inflammation, analgesia and anti-allergic reaction in mice (형개연교탕(荊芥連翹湯)과 가미형개연교탕(加味荊芥連翹湯)이 소염(消炎).진통(鎭通) 및 항(抗)알레르기에 미치는 영향(影響))

  • Park Eun-Jeong;Shin So-Young
    • The Journal of Pediatrics of Korean Medicine
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    • v.11 no.1
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    • pp.249-273
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    • 1997
  • Hyunggyeyungyotang has been used for treatment of sinusitis and otitis media in oriental medicine since ancient times. It is reported that Hyunggyeyungyotang has good effects on inflammatory and allergic diseases of otorhinolaryngology in clinical medicine. Kamihyunggyeyungyotang was made by adding several herbs to Hyunggyeyungyotang which has such good effects. To investigate the effects of Hyunggyeyungyotang and Kamihyunggyeyungyotang on inflammatory, algesic and allergic diseases, the author examined the analgesic effect by acetic acid reaction, studied the anti-inflammatory effect through the experiments of the protein thermo-denaturation and circumscribed edema. Besides researched the anti-allergic effect through the vascular permeability response to Chemical Mediator and the delayed type hypersensitivity response to Picryl Chloride. The obtained results were as follows ; 1. In the analgesic effect of Hyunggyeyungyotang and Kamihyunggyeyungyotang extract by acetic acid method, both of the sample groups showed the analgesia, but didn't show useful effect. 2. In the anti-inflammatory effect on the protein thermo-denaturation, the sample groups revealed the inhibitory effect in proportion to concentration as compared with the control group. 3. In the inhibitory action on circumscribed edema induced by Caraggeenin, both of Hyunggyeyungyotang and Kamihyunggyeyungyotang administration showed the significant effect after 4 hours in comparison to the control group. 4. In the delayed type hypersensitivity response to Picryl Chloride, both of the sample groups revealed the significant effects. 5. Both of the sample groups decreased the vascular permeability induced by Histamine in comparison with the control group, but the significancy was admitted in only Hyunggyeyungyotang administration. According to above results, Hyunggyeyungyotang and Kamihyunggyeyungyotang are considered to be used for treament of the inflammatory diseases including sinusitis.

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The Role of Spinal Dopaminergic Transmission in the Analgesic Effect of Nefopam on Rat Inflammatory Pain

  • Kim, Do Yun;Chae, Joo Wung;Lim, Chang Hun;Heo, Bong Ha;Park, Keun Suk;Lee, Hyung Gon;Choi, Jeong Il;Yoon, Myung Ha;Kim, Woong Mo
    • The Korean Journal of Pain
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    • v.29 no.3
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    • pp.164-171
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    • 2016
  • Background: Nefopam has been known as an inhibitor of the reuptake of monoamines, and the noradrenergic and/or serotonergic system has been focused on as a mechanism of its analgesic action. Here we investigated the role of the spinal dopaminergic neurotransmission in the antinociceptive effect of nefopam administered intravenously or intrathecally. Methods: The effects of intravenously and intrathecally administered nefopam were examined using the rat formalin test. Then we performed a microdialysis study to confirm the change of extracellular dopamine concentration in the spinal dorsal horn by nefopam. To determine whether the changes of dopamine level are associated with the nefopam analgesia, its mechanism was investigated pharmacologically via pretreatment with sulpiride, a dopaminergic D2 receptor antagonist. Results: When nefopam was administered intravenously the flinching responses in phase I of the formalin test were decreased, but not those in phase II of the formalin test were decreased. Intrathecally injected nefopam reduced the flinching responses in both phases of the formalin test in a dose dependent manner. Microdialysis study revealed a significant increase of the level of dopamine in the spinal cord by intrathecally administered nefopam (about 3.8 fold the baseline value) but not by that administered intravenously. The analgesic effects of intrathecally injected nefopam were not affected by pretreatment with sulpiride, and neither were those of the intravenous nefopam. Conclusions: Both the intravenously and intrathecally administered nefopam effectively relieved inflammatory pain in rats. Nefopam may act as an inhibitor of dopamine reuptake when delivered into the spinal cord. However, the analgesic mechanism of nefopam may not involve the dopaminergic transmission at the spinal level.

Sedative and Analgesic Effects of Intravenous Detomidine and Tramadol on Horses (말에서 detomidine과 tramadol의 정맥 투여에 의한 진정 및 진통효과)

  • Kim, Tae-Hoon;Jang, Min;Lee, Hang;Lee, In-Hyung
    • Journal of Veterinary Clinics
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    • v.29 no.3
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    • pp.226-232
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    • 2012
  • This study was performed to evaluate the sedative and analgesic effects of intravenous (IV) administration of detomidine (D) and tramadol (T) to horses. Six warmblood horses each received D (10 ${\mu}g/kg$), T (2 mg/kg), and a combination of DT (10 ${\mu}g/kg$ and 2 mg/kg). No significant differences in the heart rate, respiratory rate, rectal temperature, indirect arterial pressure, and gastrointestinal motility between D and DT were observed. The sedative effect was evident within 5 min after D and DT administration, but no significant difference between D and DT was observed. D and DT induced a similar analgesic effect up to 50 min after injection and DT maintained a longer analgesic effect than D. A significant increase in blood glucose was shown for D after the injection, but not for DT. A horse with T and DT showed an excited behavior within 5 min of the injection. This study suggests that the DT combination could be used for diagnostic procedures and simple surgeries in standing horses, with caution for excitement in the early phase after the administration.

Effects of Carbenoxolone and P2X recepter antagonist combined therapy on oral neuropathic pain in rat (신경병증 통증 모델에서 Carbenoxolone과 P2x receptor 길항제의 효과)

  • Ku, In-Young;Moon, Seon-Jeong;Ka, Kyung-Hwan;Park, Min-Kyoung
    • Journal of the Korea Academia-Industrial cooperation Society
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    • v.17 no.2
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    • pp.123-128
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    • 2016
  • The study was conducted to confirm the analgesic effects of the Carbenoxolone(CBX)and P2X receptor antagonist(iso-PPADS), which separates the gap junction in the facial neuropathic pain model. The experiment used white male Sprague-Dawley rats (240~280g). The second left molars on the lower jaw was extracted to induce facial neuropathic pain, and small dental implants were implanted to induce damage to the inferior alveolar nerve. When CBX was injected twice daily to the abdominal cavity, a significant analgesic effect at 5ug/kg was observed(p<0.05). In addition, when iso-PPADS was injected twice daily into the abdominal cavity, a significant analgesic reaction was observed at $25{\mu}g/kg$(p<0.05). When the two drugs were injected together at a low concentration, in which they did not display an effect, they displayed a significant analgesic reaction at CBX 1ug/kg and iso-PPADS 2.5ug/kg(p<0.05). When a gap injunction block using a low concentration of CBX and a low concentration P2X receptor antagonist was injected together, the pain suppressing effect was observed against the orofacial neuropathic pain mechanism. These results make it possible to determine that the gap junction block using CBX and the injection of the P2X receptor antagonist plays an important role in the pain management of the facial region.

Comparision of cardiovascular and analgesic effects of epidural administration of medetomidine, medetomidine-buprenorphine and medetomidine-fentanyl in dogs anesthetized with isoflurane (Isofourane으로 마취된 개에 medetomidine, medetomidine-buprenorphine, medetomidine-fentanyl의 경막외 투여 시 심혈관계 반응과 진통효과의 비교)

  • Chang, Hwa-Seok;Kim, Hye-Jin;Choi, Chi-Bong;Lee, Jung-Sun;Kim, Hwi-Yool
    • Korean Journal of Veterinary Research
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    • v.47 no.1
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    • pp.103-115
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    • 2007
  • The aim of this study was to compare the reaction of the cardiovascular system, and the anesthetic effect among 3 experimental groups, epidural administration of medetomidine as a single agent, the combination of buprenorphine and medetomidine, and the combination of fentanyl and medetomidine. Twenty one dogs were anesthetized with isoflurane and allowed to breathe spontaneously. Epidural, arterial, and venous catheters were inserted. The tip of epidural catheter was positioned at the level of the space between the sixth and seventh lumbar vertebra. After a stable plane of anesthesia was achieved, these dogs were each administered one of the following treatments epidurally : medetomidine $10{\mu}g/kg$ (Group M), a combination of medetomidine $5{\mu}g/kg$ and buprenorphine $10{\mu}g/kg$ (Group M/B), and a combination of medetomidine $5{\mu}g/kg$ and fentanyl $10{\mu}g/kg$ (Group M/F). Heart rate (HR), Respiratory rate (RR), End-tidal carbon dioxide (EtCO2), and arterial blood pressure were measured before drug administration (base line) and 5, 10, 15, 20, 25, 30, 35, 40, 45, 50, 55, and 60 min postinjection. Blood gas analysis was performed before injection and 5, 15, 25, 35, 45, 60 min postinjection. Isoflurane was discontinued 80 min postinjection and pain/motor function were evaluated up to 260 min postinjection every 15 min. At the early stage of drug introduction (until 5 min), the HR was decreased significantly in all 3 groups compared with base line. In Group M, HR was significantly decreased compared with the other 2 groups. With time (starting 20 min after drug introduction), the HR was decreased significantly in Group M/B in respect to base line. However, no significant difference was seen number-wise in all 3 groups. During 60 min after drug introduction, the systolic, diastolic and mean arterial pressures were highest in Group M and lowest in Group M/F. Among 3 groups, drug action and motor loss duration were longest in Group M/F. Analgesic effect observed in the M/F group was the most prominent and long-lasting, compared to those seen in the other 2 groups. Given the fact that the recovery of motor function takes place in a short period of time after analgesic effects disappeared, additional use of M/F depending on the patient's condition would be a good way to achieve effective pain management. However, proper care should be taken to ensure the function of cardiovascular system in the patient because the administration of M/F under isoflurane anesthesia results in a significant decline in arterial blood pressure ($65{\pm}10mmHg$).