• Title/Summary/Keyword: ANALGESIC EFFECT

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Enhancement of Antinociception by Co-administrations of Nefopam, Morphine, and Nimesulide in a Rat Model of Neuropathic Pain

  • Saghaei, Elham;Zanjani, Taraneh Moini;Sabetkasaei, Masoumeh;Naseri, Kobra
    • The Korean Journal of Pain
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    • v.25 no.1
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    • pp.7-15
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    • 2012
  • Background: Neuropathic pain is a chronic pain due to disorder in the peripheral or central nervous system with different pathophysiological mechanisms. Current treatments are not effective. Analgesic drugs combined can reduce pain intensity and side effects. Here, we studied the analgesic effect of nimesulide, nefopam, and morphine with different mechanisms of action alone and in combination with other drugs in chronic constriction injury (CCI) model of neuropathic pain. Methods: Male Wistar rats (n = 8) weighing 150-200 g were divided into 3 different groups: 1- Saline-treated CCI group, 2- Saline-treated sham group, and 3- Drug-treated CCI groups. Nimesulide (1.25, 2.5, and 5 mg/kg), nefopam (10, 20, and 30 mg/kg), and morphine (1, 3, and 5 mg/kg) were injected 30 minutes before surgery and continued daily to day 14 post-ligation. In the combination strategy, a nonanalgesic dose of drugs was used in combination such as nefopam + morphine, nefopam + nimesulide, and nimesulide + morphine. Von Frey filaments for mechanical allodynia and acetone test for cold allodynia were, respectively, used as pain behavioral tests. Experiments were performed on day 0 (before surgery) and days 1, 3, 5, 7,10, and 14 post injury. Results: Nefopam (30 mg/kg) and nimesulide (5 mg/kg) blocked mechanical and thermal allodynia; the analgesic effects of morphine (5 mg/kg) lasted for 7 days. Allodynia was completely inhibited in combination with nonanalgesic doses of nefopam (10 mg/kg), nimesulide (1.25 mg/kg), and morphine (3 mg/kg). Conclusions: It seems that analgesic drugs used in combination, could effectively reduce pain behavior with reduced adverse effects.

The Experimental study on the Anti-inflammatory and Analgesic Effects of Gold injection Aqua-acupuncture (금주사액약침자극(金注射液藥鍼刺戟)의 항염증(抗炎症) 및 진통(鎭痛)에 관한 실험적(實驗的) 연구(硏究))

  • Hong, Seong-Hun;Choi, Do-young
    • Journal of Acupuncture Research
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    • v.18 no.2
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    • pp.200-213
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    • 2001
  • Objectives : This study was purposed to investigate the Anti-inflammatory and Analgesic Effects of Gold injection Aqua-acupuncture on the experimental model of rheumatoid arthritis. Methods : The experimental groups were divided into 4 groups : Control group (group injected with normal saline), J-NS (group injected with normal saline into bilateral Choksamni(ST36)), J-GS (group injected with Gold Injection into bilateral Choksamni(ST36)), and N-GS (injected with Gold Injection into the blank locus of the root of mouse tail). In addition, Diclofenac-Na as a comparative medicine is injected into bilateral Choksamni(ST36) and the blank locus of the root of mouse tail. So we measured the mice paw edema induced by Carrageenin and Dextran, the chronic rat paw edema induced by adjuvant, vascular permeability induced by Acetic acid in mice, the writhing syndrome induced by Acetic acid in mice, the heat-induced pain threshold in mice. Results : The following result have been obtained. 1. The mice paw edema induced by Carrageenin was significantly decreased in J-GS as compared with the control group. 2. The mice paw edema induced by Dextran was significantly decreased in J-GS and N-GS as compared with the control group. 3. The chronic rat paw edema induced by Adjuvant was significantly decreased in J-GS and N-GS as compared with the control group. Serum Iron content was significantly decreased in J-GS and N-GS as compared with the control group. But the effect on the Serum Copper contents has no significance statistically. 4. Vascular permeability induced by Acetic acid in mice was significantly decreased in J-GS and N-GS as compared with the control group. 5. The level of Acetic acid-induced Writhing syndrome and Heat-induced Pain Threshold in mice were all significantly decreased in J-GS and N-GS as compared with the control group. Conclusion : According to the result, gold injection aqua-acupuncture has significant anti-inflammatory and analgesic effects on the experimental model of rheumatiod arthiritis.

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The Analgesic Effects of Apitoxin and its Mechanism via JOR and Measuring Expression of mRNA in Phospholipase and TPH using RT-PCR (Jaw Opening Reflex 및 RT-PCR을 이용한 봉독의 진통효과)

  • Cho, Kwang-Ho;Lee, Jae-Dong;Park, Dong-Suk;Ahn, Byoung-Choul
    • Journal of Pharmacopuncture
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    • v.3 no.1
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    • pp.35-51
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    • 2000
  • The purpose of this study is to prove the analgesic effects of apitoxin and its mechanism via jaw-opening reflex(JOR) and measuring expression of mRNA in Phospholipase and Tryptophan hydroxylase(TPH) using RT-PCR. The experiments were carried out on Sprague-Dawley rats(300-400g) and mastocytoma(P-185 HTR) for JOR and RT-PCR, respectively. Rats anesthetized with thiopental sodium (80mg/kg) were used in the Tooth Pulp stimulation induced JOR. The amplitude of a digastric electromyogram (dEMG) was recorded during the stimulation at an intensity of 1.5 times the threshold for JOR. Apitoxin used in this experiment was diluted with normal saline by 1:1000. Apitoxin was injected intravenously into the test group while normal saline to the control group. However, it was injected directly into the cell of mastocytoma. We referred to base sequence registered in Genbank in designing primers for RT-PCR. The results were as follows; (1)Compared with control group, analgesic effect started to show right after Sprague-Dawely rats were treated with apitoxin($71.50{\pm}8.08$) and lasted for 50 minutes. (2)As a result of the experiment of RT-PCR, we witnessed significant changes in the degree of expression of phospholipase or rate-limiting enzyme of biosynthesis of prostaglandins with $10{\mu}g/ml$ apitoxin.($31.74{\pm}18.98%$, P<0.05) (3)As a result of the experiment of RT-PCR, we witnessed significant changes in the degree of expression of TPH or rate-limiting enzyme in biosynthesis of serotonin with $10{\mu}g/ml$ apitoxin.($131.37{\pm}16.87%$, P<0.05). These results suggest that $10{\mu}g/ml$ apitoxin have the most analgesic effects. This study showed that apitoxin has analgesic effects and held good for 50 minutes. The injection of apitoxin has brought out changes in the degree of expression of phospholipase and TPH. These results strongly suggest that analgesic mechanism by apitoxin is closely related to prostaglandins and serotonin.

Acupuncture on ST36 Increases c-Fos Expression in vlPAG of Visceral Pain-induced Mice

  • Choo, Jin-Suk;Song, Yun-Kyung;Lim, Hyung-Ho
    • The Journal of Korean Medicine
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    • v.29 no.1
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    • pp.39-46
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    • 2008
  • Background : Acupuncture has been used as a clinical treatment in Oriental medicine for various diseases including pain relief. The descending pain control system of periaqueductal gray (PAG) is a powerful pain control system in mammalians. Expression of c-Fos is used as a marker for stimuli-induced metabolic changes of neurons. Objective : In the present study, the effects of acupuncture on analgesic effect in visceral pain were investigated through the writhing reflex and c-Fos expression in ventrolateral PAG (vlPAG) area using immunohistochemistry in mice. Method : For the writhing test, mice were divided into five groups. Immediately after finishing the behavioral test, the animals were weighed and overdosed with Zoletil. After a complete lack of response was observed, the brains of the mice were dissected into serial coronal sections, and c-Fos immunohistochemistry was performed. Statistical analysis of all data was performed using one-way ANOVA. Result : The present results showed that acupuncture affected the writhing reflex and that Choksamni (zusnali) acupoint and aspirin significantlysuppressed acetic acid treatment-induced increased writhing reflex, and the expression of c-Fos in vlPAG was significantly increased in the acupunctured group. Conclusion : The present study suggests that acupuncture has an antinociceptive effect on acetic acid-induced visceral pain by increase of c-Fos expression in mice. Aspirin also showed analgesic effect, however the mechanism is different from the acupuncture.

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Pharmaceutical Study on Ketoprofen Lysinate (Ketoprofen Lysinate의 약제학적(藥劑學的) 연구(硏究))

  • Lee, Wan-Ha;Kim, Jang-Bae;Jee, Ung-Kil;Rhyu, Byung-Tae
    • Journal of Pharmaceutical Investigation
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    • v.12 no.2
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    • pp.37-44
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    • 1982
  • In order to enhance water solubility, ketoprofen was made as lysine salt, such as acetylsalicylic acid lysine salt, ibuprofen lysine salt and amino acid salt of phenylbutazone. The purpose of this study was to make a comparison between ketoprofen lysine salt in aspects of analgesic, anti-inflammatory, and antipyretic effect. The experimental results were summerized as followings. 1. Ketoprofen lysinate was composed of one molecule of ketoprofen and one molecule of lysine. The product was water soluble and melting point was $92^{\circ}C{\sim}94^{\circ}C$. 2. Ketoprofen lysinate showed about 2 times stronger analgesic effect than that of ketoprofen while no difference in antipyretic effect was observed. 3. $LD_{50}$ of ketoprofen lysinate was higher than that of ketoprofen, suggesting ketoprofen lysinate as safer drug. 4. Blood concentration of ketoprofen lysinate was $156{\mu}g/ml$ while the concentration of ketoprofen was $116{\mu}g/ml$ in 30 min., suggesting long acting as well as high blood concentration.

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Synthesis of Mefenamic Acid Derivatives and Antioxidative and Anticoagulant Activities

  • Cha, Bae-Cheon
    • Biomolecules & Therapeutics
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    • v.8 no.4
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    • pp.349-353
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    • 2000
  • Mefenamic acid has been widely used as clinical drug for anti-inflammatory and analgesic. This drug was known to non-steroidal anti-inflammatory drugs (NSAIDs) such as aspirin, ibuprofen and indomethacin. Although the drugs which comprise this group are of diverse chemical structures, they all share the antipyretic, analgesic and anti-inflammatory actions which are characteristic of aspirin. Action of this drugs is caused by inhibitory effect of biosynthesis of prostaglandin that are synthesized from arachidonic acid via the endoperoxide biosynthesis pathway, the initial step of which is catalysed by cyclooxygenase. Mefenamic acid has more potent inhibitory action of prostaglandin biosynthesis than aspirin. Therefore, mefenamic acid is expected to have anticoagulant activity as aspirin-like drugs. This study was carried out to investigate the sinthesis of mefenamic acid derivatives from mefenamic acid and aromatic compound of antioxidant and its antioxidative and anticoagulant activities. Synthesis of mefenamic acid derivatives was conformed by conjugation as using esterification method. Biological activities was examined using effect of anticoagulant on bleeding time and effect of antioxidant by TBA method. As a result, SJ-202 showed strong antioxidative activity and anticoagulant activity among tested 4 compounds and exhibited similar activity to aspirin at anticoagulant activity.

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Systematic Studies on Galgeun-tang(gegen-tang, kakkon-to) for Establishment of Evidence Based Medicine (표준한방처방의 EBM 구축을 위한 갈근탕(葛根湯) 문헌 분석 연구)

  • Lee, Jun-Kyoung;Kim, Jung-Hoon;Shin, Hyeun-Kyoo
    • Herbal Formula Science
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    • v.19 no.1
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    • pp.103-111
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    • 2011
  • Objectives : The purpose of this report was to provide the information of activity and safety of galgeun-tang by analyzing domestic/international papers and theses about galgeun-tang. Methods : Domestic/international papers and theses related to galgeun-tang were reviewed and analyzed. These papers were then classified by efficacy, or clinical trials. Results : The basic pharmacological experiment showed antipyretic, analgesic and anti-virus and anti-oxidant efficacy of galgeun-tang. In the case report of galgeun-tang, it showed therapeutic effect for patient with chronic rhinitis. But administration of galgeun-tang induced pruritic eruption in the two case report as a side effects of galgeun-tang. Conclutions : galgeun-tang showed tantipyretic, analgesic and anti-virus and anti-oxidant efficacy in the basic pharmacological experiment. Also, galgeun-tang showed therapeutic effect for patient with chronic rhinitis. But it was reported that galgeun-tang induced pruritic eruption in two case report, so physicians should be aware of the potential side effects.

Inhibitory Effects of the Essential Oil from Nardostachys intamansi on Central Nervous System after Inhalation and Oral Administration (감송향 정유성분의 흡입 및 경구투여시의 중추신켱 억제효과)

  • Koo Byung-Soo;Kim Dae-kun;Choi Jung-Hyun;Lee Dong-Ung
    • Journal of Life Science
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    • v.16 no.1
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    • pp.156-161
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    • 2006
  • The essential oil of Nardostachys jatamansi (Valerianaceae), which has been used for a long time in aroma therapy, was investigated after inhalation or oral administration for its analgesic effect, anticonvulsant action, hypnotic effect and in vitro inhibitory activity on monoamine oxidase. This fragrance oil showed a significant analgesic effect in the phenylquinone-induced .writhing test, suppressed the convulsion induced by pentylenetetrazole and lengthened the pentobarbital-induced sleeping time in a time-dependent manner after fragrance inhalation or dose-independently by oral administration. Its inhibitory activity on monoamine oxidase was remarkable, showing $49.4\%$ inhibition at a concentration of 5.0 mg/ml. Six new terpenes with seven known compounds were detected by our GC-MS analytical conditions used. As a result, the essential oil fragrance of Nardostachys jatamansi would be clinically useful for a sedative by either inhalation or oral administration.

Effect of preoperative pregabalin on postoperative pain after gastrectomy

  • Park, Chan Yoon;Park, Sol Hee;Lim, Dong Gun;Choi, Eun Kyung
    • Journal of Yeungnam Medical Science
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    • v.35 no.1
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    • pp.40-44
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    • 2018
  • Background: Pregabalin has been studied as a single or multimodal analgesic drug for postoperative pain management in different types of surgeries. We evaluated the analgesic effect of 150 mg of pregabalin in resolving post-gastrectomy pain. Methods: Forty-four patients were randomized into two groups: a pregabalin group that received oral pregabalin (150 mg) 2 h before anesthetic induction, and a control group that received placebo tablets at the same time. Data on postoperative pain intensity (visual analog scale [VAS], at 30 min, 2 h, 4 h, and 24 h), consumption of fentanyl in patient-controlled analgesia (PCA), and the proportion of patients requiring rescue analgesics at different time intervals (0-2 h, 2-4 h, and 4-24 h) were collected during the 24 h postoperative period. Results: The VAS scores did not show significant differences at any time point and consumption of fentanyl in PCA and the proportion of patients requiring rescue analgesics did not differ between the two groups. The groups did not differ in the occurrence of dizziness, sedation, and dry mouth. Conclusion: A preoperative 150 mg dose of pregabalin exerts no effect on acute pain after gastrectomy.

Screening of Medicinal Plants on the Anti-inflammatory Effect and Active Component (전남지역 자생식물들의 소염활성검색 및 활성화합물)

  • 박종철;이효연
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.25 no.3
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    • pp.523-528
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    • 1996
  • The anti-inflammatory effect of the methanolic extracts of some medicinal plants was investigated on the hydrolysis of N-benzoylarginine-p-nitroanilide by trypsin in vitro, the writhing syndrome induced by acetic acid in mice, and the carrageenin-induced paw edema in rats. Among tested medicinal plants, the methanoilc extract of Angelica keiskei, Rosa rugosa and Cudrania tricuspidata showed significant inhibitory effect. And we also found that adenosine, isolated from A. keiskei was identified as one active components.

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