• Title/Summary/Keyword: diclofenac

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Synthesis and Antiinflammatory Activity of Novel Indazolones

  • Abouzid, Khaled-A.M.;EI-Abhar, H.S.
    • Archives of Pharmacal Research
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    • v.26 no.1
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    • pp.1-8
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    • 2003
  • In this study, a series of new $N^2$ substituted 1,2-dihydro-3H-indazol-3-ones (3a-d) as well as their condensed pyrazolo, pyridazino derivatives such as pyridazino[1,2-a]indazole-6,9,11-triones (4a-h) and 3,9-dioxo-3H,9H-pyrazolo[1,2-a]indazole (7) were synthesized. The antiinflammatory activity of some synthesized compounds was determined by carrageenan-induced rat paw edema technique using diclofenac as reference drug. The pharmacological data showed that most of the tested compounds exhibited a significant long lasting antiinflammatory activity, which in the case of compound 3b was superior to that of diclofenac.

The Joins (SKI 306X) study: Effects on gastric mucosa and the diclofenac-induced gastric lesions

  • Kim, Joo-Hyon;Lee, Hae-In;Jung, In-Ho;Jung, Ki-Won;Han, Chang-Kyun;Kwak, Wie-Jong;Cho, Yong-Baik;Joo, Hee-Jae
    • Proceedings of the PSK Conference
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    • 2003.04a
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    • pp.146.1-146.1
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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 and cartilage protective effects in several experimental models. In this study we characterized the effects of Joins on the gastric mucosa and compared to that of diclofenac. (omitted)

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Hepatotoxic mechanism of diclofenac sodium on broiler chicken revealed by iTRAQ-based proteomics analysis

  • Sun, Chuanxi;Zhu, Tianyi;Zhu, Yuwei;Li, Bing;Zhang, Jiaming;Liu, Yixin;Juan, Changning;Yang, Shifa;Zhao, Zengcheng;Wan, Renzhong;Lin, Shuqian;Yin, Bin
    • Journal of Veterinary Science
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    • v.23 no.4
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    • pp.56.1-56.17
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    • 2022
  • Background: At the therapeutic doses, diclofenac sodium (DFS) has few toxic side effects on mammals. On the other hand, DFS exhibits potent toxicity against birds and the mechanisms remain ambiguous. Objectives: This paper was designed to probe the toxicity of DFS exposure on the hepatic proteome of broiler chickens. Methods: Twenty 30-day-old broiler chickens were randomized evenly into two groups (n = 10). DFS was administered orally at 10mg/kg body weight in group A, while the chickens in group B were perfused with saline as a control. Histopathological observations, serum biochemical examinations, and quantitative real-time polymerase chain reaction were performed to assess the liver injury induced by DFS. Proteomics analysis of the liver samples was conducted using isobaric tags for relative and absolute quantification (iTRAQ) technology. Results: Ultimately, 201 differentially expressed proteins (DEPs) were obtained, of which 47 were up regulated, and 154 were down regulated. The Gene Ontology classification and Kyoto Encyclopedia of Genes and Genomes pathway analysis were conducted to screen target DEPs associated with DFS hepatotoxicity. The regulatory relationships between DEPs and signaling pathways were embodied via a protein-protein interaction network. The results showed that the DEPs enriched in multiple pathways, which might be related to the hepatotoxicity of DFS, were "protein processing in endoplasmic reticulum," "retinol metabolism," and "glycine, serine, and threonine metabolism." Conclusions: The hepatotoxicity of DFS on broiler chickens might be achieved by inducing the apoptosis of hepatocytes and affecting the metabolism of retinol and purine. The present study could provide molecular insights into the hepatotoxicity of DFS on broiler chickens.

Analysis of Repeated Measured VAS in a Clinical Trial for Evaluating a New NSAID with GEE Method (퇴행성 관절염 환자를 대상으로 새로운 진통제 평가를 위한 임상시험자료의 GEE 분석)

  • Lim, Hoi-Jeong;Kim, Yoon-I;Jung, Young-Bok;Seong, Sang-Cheol;Ahn, Jin-Hwan;Roh, Kwon-Jae;Kim, Jung-Man;Park, Byung-Joo
    • Journal of Preventive Medicine and Public Health
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    • v.37 no.4
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    • pp.381-389
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    • 2004
  • Objective : To compare the efficacy between SKI306X and Diclofenac by using generalized estimating equations (GEE) methodology in the analysis of correlated bivariate binary outcome data in Osteoarthritis (OA) diseases. Methods : A randomized, double-blind, active comparator-controlled, non-inferiority clinical trial was conducted at 5 institutions in Korea with the random assignment of 248 patients aged 35 to 75 years old with OA of the knee and clinical evidence of OA. Patients were enrolled in this study if they had at least moderate pain in the affected knee joint and a score larger than 35mm as assessed by VAS (Visual Analog Scale). The main exposure variable was treatment (SKI 306X vs. Diclofenac) and other covariates were age, sex, BMI, baseline VAS, center, operation history (Yes/No), NSAIDS (Y/N), acupuncture (Y/N), herbal medicine (Y/N), past history of musculoskeletal disease (Y/N), and previous therapy related with OA (Y/N). The main study outcome was the change of VAS pain scores from baseline to the 2nd and 4th weeks after treatment. Pain scores were obtained as baseline, 2nd and 4th weeks after treatment. We applied GEE approach with empirical covariance matrix and independent(or exchangeable) working correlation matrix to evaluate the relation of several risk factors to the change of VAS pain scores with correlated binary bivariate outcomes. Results : While baseline VAS, age, and acupuncture variables had protective effects for reducing the OA pain, its treatment (Joins/Diclofenac) was not statistically significant through GEE methodology (ITT:aOR=1.37, 95% CI=(0.8200, 2.26), PP:aOR=1.47, 95% CI=(0.73, 2.95)). The goodness-of-fit statistic for GEE (6.55, p=0.68) was computed to assess the adequacy of the fitted final model. Conclusions : Both ANCOVA and GEE methods yielded non statistical significance in the evaluation of non-inferiority of the efficacy between SKI306X and Diclofenac. While VAS outcome for each visit was applied in GEE, only VAS outcome for the fourth visit was applied in ANCOVA. So the GEE methodology is more accurate for the analysis of correlated outcomes.

A randomized, double-dummy, multicenter non-inferiority clinical trials to evaluate the efficacy and the safety of SKI 306X compared to diclofenac in patients with osteoarthritis of the knee (양측 눈가림, 무작위배정, 다기관공동 제 3상 임상시험 결과 - 퇴행성 관절염에 대한 SKI 306X정과 Diclofenac과의 비열등성 임상시험)

  • Jung Y.B.;Seong S.C.;Lee M.C.;Shin Y.U.;Kim D.H.;Kim J.M.;Jung Y.K.;Ahn J.H.;Seo J.G.;Park Y.S.;Lee C.S.;Roh K.J.;Han C.K.
    • 대한임상약리학회:학술대회논문집
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    • 2001.12a
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    • pp.24-25
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    • 2001
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