• Journal of Medicine and Life Science
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• 제16권2호
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• pp.46-51
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• 2019

Inflammatory bowel disease (IBD) is an immune-mediated chronic inflammatory intestinal condition. With development of various treatment options for IBD, 5-aminosalicylic acid (5-ASA) agents became the drugs of choice due to high efficacy and low risk of complication, specifically effective at inducing and maintaining remission in ulcerative colitis(UC). Pancytopenia caused by 5-ASA agents, especially by mesalazine, has been rarely reported compared with azathioprine, which is commonly used for glucocorticoid-dependent IBD and known to have risk of bone marrow suppression. In the present report, we describe the case of a 57-year-old woman diagnosed with UC, who developed pancytopenia due to adverse effect of mesalazine after recovery from azathioprine-induced pancytopenia. After withdrawal of mesalazine, the laboratory values consistent with myelosuppression continued for 3 months while pancytopenia from azathioprine remained only for 2 weeks. Since pancytopenia can be fatal due to its risk of severe bleeding and infection, close monitoring of clinical presentation is important when starting mesalazine and laboratory data should be evaluated whenever the patients present related symptoms. Furthermore, we suggest that complete blood cell counts should be considered when resuming mesalazine following the development of pancytopenia from any cause, as routinely recommended for azathioprine use.

• Tuberculosis and Respiratory Diseases
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• 제60권2호
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• pp.180-186
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• 2006

배경: 다제내성 결핵환자에서 이차약제로 구성된 처방 복약시 특히 PAS는 심한 위장장애 등의 부작용으로 환자의 치료순응도 저하에 중요한 요인이 되므로 균음전 후 PAS를 처방에서 제외한 경우의 치료경과 특히, 치료종결 후 재발율에 대한 조사를 통해 치료경과 중에 적절한 시점에 처방에서 PAS제외 가능성에 대하여 평가하고자 하였다. 방법: 2000년 1월 1일부터 2001년 12월 31일 동안에 국립마산결핵병원에서 입원 혹은 외래치료를 받았던 452명의 다제내성 결핵환자 중에서 처방에 PAS가 포함된 194명 중 심한 위장장애 등의 부작용 때문에 PAS를 중단한 환자 중 균음전 후 PAS를 제외한 처방을 12개월 이상 유지할 수 있었던 42명을 대상으로 임상적 특성 및 치료종결 후 재발율을 분석하였다. 결과: 대상환자의 남녀성비는 2.5:1, 평균나이는 56.2세였다. 1.2회의 과거치료력이 있었으며, 사용한 약제는 평균 3.9제였다. 내성약제수는 평균 4.3제였으며 처방에 포함된 감수성약제수는 평균 3.9제였다. 치료가 시작된 후 균음전시기는 평균 2.3개월째였으며, PAS 중단 시기는 균음전 후 평균 6개월째였다. 31.6개월의 추구관찰 기간 중 재발환자는 없었다. 결론: 새로운 항결핵제의 개발이 요원하고, 다제내성 결핵에 사용가능한 약제가 제한된 현 상황에서 치료순응도 개선방안을 강구하는 것은 치료효율을 높일 수 있는 최선의 방법 중 하나라고 생각되며, 다제내성 결핵환자에서 PAS가 포함된 처방으로 균음전이 되고 환자가 PAS복약에 따른 부작용을 호소하여 치료순응도가 나빠질 것으로 염려가 되면 균음전 후 6개월 즈음에는 PAS를 처방에서 제외할 수 있을 것으로 판단되었다.

• 약학회지
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• 제52권5호
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• pp.402-406
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• 2008

Previously, we have shown that 1-furan-2-yl-3-pyridin-2-yl-propenone (FPP-3) has an anti-inflammatory activity in a rat paw-edema model. In the present study, we investigated an inhibitory effect of FPP-3 on the tumor necrosis factor (TNF)-${\apha}$-induced inflammatory cytokine response in HT-29 human colon epithelial cells. Treatment with FPP-3 significantly prevented the TNF-${\apha}$-induced attachment of leukocytes to HT-29 colon epithelial cells, which is one of the pathologic hallmarks in colon inflammation. The effect of FPP-3 was markedly superior than that of 5-aminosalicylic acid (5-ASA), a commonly used drug for the treatment of inflammatory bowel disease (IBD). The pretreatment with FPP-3 inhibited TNF-${\apha}$- induced monocyte chemoattractant protein (MCP)-1, interleukin (IL)-8 mRNA expressions. In addition, FPP-3 significantly suppressed TNF-${\apha}$-induced nuclear factor (NF)-${\kappa}B$ transcription activity. These results demonstrate that FPP-3 modulates intestinal inflammation via suppressing the NF-${\kappa}B$ dependent expressions of MCP-1 and IL-8, and suggest that FPP-3 may be a valuable agent for the treatment of IBD.

• Tuberculosis and Respiratory Diseases
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• 제39권2호
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• pp.167-171
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• 1992

PTA, CS, PAS, SM (KM 또는 TUM) 4제 요법의 임상효과를 알고자 지난 5년동안 국립 공주 병원에 입원하였던 도말양성 환자중 추적 가능한 112명을 대상으로 한 조사에서 다음과 같은 결과를 얻었다. 균 도말검사상 64%가 음전을 나타내었고 그 시기는 85%가 3개월 이내에 이루어졌다. 방사선 소견은 반응이 없는 경우가 약 반 정도이었으며, 세균학적 검사를 함께 고려하여 판단할 때 62% 정도만이 양호한 결과를 나타내었다. 양호한 결과는 병력이 짧고 내성정도가 적을수록 좋았다. 그리고 병력이 오래된 환자의 재치료 처방은 적어도 3제 이상의 감수성을 가진 약제를 선택해야 되며, 두가지 이하의 감수성이 있는 경우는 INH 단독 요법등의 고려가 필요할 것으로 사료된다.

• Archives of Pharmacal Research
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• 제28권6호
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• pp.637-647
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• 2005

This work includes the synthesis of 15 final compounds (6a-h and 7b-h) as prod rugs of 5-ASA in the form of the acid itself, esters and amides linked by an amide linkage through a spacer to the endocyclic ring N of nicotinamide. Also, 15 new intermediate compounds were prepared. The target compounds (6b, 6f, 7b, and 7e-h) revealed potent analgesic and anti-inflammatory activities in comparison to sulfasalazine and 5-ASA. In addition, ulcerogenicity, $LD_{50}$, in vivo and in vitro metabolism of compound 7f were determined.

• 약학회지
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• 제52권1호
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• pp.62-66
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• 2008

In this study, we examined the inhibitory effects of propenone derivatives, 1,3-diphenyl-propenone (DPhP), 3-phenyl-1-thiophen-2-yl-propenone (PhT2P), 3-phenyl-1-thiophen-3-yl-propenone (PhT3P) and 1-furan-2-yl-3-phenyl-propenone (FPhP), on $TNF-{\alpha}$-induced nuclear factor (NF)-${\kappa}B$ activity and interleukin (IL)-8-induced monocyte adhesion to colon epithelial cells. 1-Furan-2-yl-3-pyridin-2-yl-propenone (FPP-3) that is previously reported as a $NF-{\kappa}B$ inhibitor suppressed $TNF-{\alpha}$-induced monocyte-epithelial cell adhesion in a concentration-dependent manner. The propenone derivatives, DPhP, PhT2P, PhT3P, FPhP, also inhibited $TNF-{\alpha}$-induced $NF-{\kappa}B$ activation in a similar degree to FPP-3. In a DPPH radical scavenging assay, none of the compounds showed DPPH radical scavenging activity, indicating that the inhibitory actions of the propenone derivatives on redox-sensitive $NF-{\kappa}B$ activity is not due to a simple free radical scavenging activity. In addition, the propenone derivatives also suppressed the IL-8-induced monocyte adhesion to colon epithelial cells. Furthermore, the effective concentrations of the propenone derivatives on both $NF-{\kappa}B$ activation as well as IL-8 induced monocyte-epithelial cell adhesion were 1000 times lower than 5-aminosalicylic acid (5-ASA), a clinically used drug for inflammatory bowel disease. These results suggest that the propenone derivatives may be a potential lead having a strong inhibitory activity against inflammatory cytokine-induced epithelial inflammation.

• Archives of Pharmacal Research
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• 제28권8호
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• pp.983-987
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• 2005

Hydrogels composed of glycidyl methacrylate dextran (GMD) and poly(acrylic acid, PM) were prepared by UV irradiation method for colon-specific drug delivery. GMD was synthesized by coupling of glycidyl methacrylate to dextran in the presence of 4-(N,N-dimethylamino)pyridine. GMD was photo-polymerized by ammonium peroxydisulfate as initiating system in phosphate­buffered solution (0.1 M, pH 7.4). And then, acrylic acid monomer was added and subsequently heat-polymerized by 2,2'-azobisisobutyronitrile as an initiator. The hydrogels exhibited high swelling ratio (about 20) at $37^{\circ}C$, and showed a pH-dependent swelling behavior. In addition, the swelling ratio of the hydrogel was remarkably enhanced to about 45 times in the presence of dextranase at pH 7.4. The swelling-deswelling behavior proceeded reversibly for the GMD/PM hydrogels between pH 2 and pH 7.4. Release of 5-aminosalicylic acid from the GMD/PAA hydrogels was evaluated in simulated gastrointestinal pH fluids in the absence or presence of dextranase. We concluded that the hydrogels prepared could be used as a dual-sensitive drug carrier for sequential release in gastrointestinal tract.

• Elastomers and Composites
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• 제51권3호
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• pp.175-180
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• 2016

Influence of amino acidic chemical on properties of maleic anhydride-grafted ethylene-propylene-diene terpolymer/zinc oxide (EPDM-g-MAH/ZnO) composites was investigated. 4-Aminosalicylic acid (ASA), 4-amino-2-methoxybenzoic acid (AMBA), 12-aminolauric acid (ALA), and glutamine (Gln) were employed as the amino acidic chemicals. Though small quantity (0.5 phr) of the amino acidic chemical was added to the EPDM-g-MAH/ZnO composite, the properties were notably changed. By adding the amino acidic chemical, the percent crystallinity and apparent crosslink density were reduced. Order of the percent crystallinity was related to that of the $pK_a$ values of amino acidic chemicals. By adding the amino acidic chemical, the basic tensile properties were on the whole improved. The experimental results were explained by the $pK_a$ values of amino acidic chemicals, change of zinc ionomer formation, and interactions between the additive and EPDM-g-MAH chain.

• 한국식품영양학회지
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• 제23권4호
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• pp.435-439
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• 2010

The aim of this study was to evaluate the anti-inlfammatory effects of Glycyrrhiza glabra Linne extract on ulcerative colitis induced by 3% dextran sulfate sodium in mice. The experimental animals were divided into six groups: control(normal), DSS-induced colitis(control), 1 mg/kg, 10 mg/kg, and 100 mg/kg of Glycyrrhiza glabra Linne extract, and 150 mg/kg 5-aminosalicylic acid(5-ASA)(positive control). We evaluated the pathological disease activity index(DAI), change in weight, colon mucosa damage and myeloperoxidase(MPO) in colon mucosa. Treatment with 10 mg/kg and 100 mg/kg of Glycyrrhiza glabra Linne extract led to significant loss of body weight, the decrease of MPO activity and clinical symptoms such as DAI and histological change. In particular, 100 mg/kg Glycyrrhiza glabra Linne extract led to markedly greater improvement than 150 mg/kg 5-ASA treatment. These results suggest that Glycyrrhiza glabra mediated anti-inflammatory action on colorectal sites may be a useful therapeutic approach to ulcerative colitis.

• 생약학회지
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• 제43권1호
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• pp.22-26
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• 2012

The aim of this study was to evaluate the anti-inlfammatory effect of the extract of Zanthoxylum schinifolium on ulcerative colitis induced by 3% dextran sulfate sodium in the rat. The experiment animals were divided into six groups: control (normal), DDS-induced colitis, 1 mg/kg, 15 mg/kg and 150 mg/kg of the extract of Z. schinifolium and 150 mg/kg of 5-aminosalicylic acid (5-ASA) as comparative drug. Anti-ulcerative colitis effect was evaluated pathologically by disease activity index (DAI), the change of weight and myeloperoxidase (MPO) in colon mucosa. Treatment with 15 mg/kg and 150 mg/kg of the extract of Z. schinifolium significantly improved the gain of body weight and DAI as clinical symptoms, and reduced MPO and $PGE_2$ level as biochemical index. Especially, 150 mg/kg of the extract of Z. schinifolium showed markedly more improvement than the same dose of 5-ASA in all kind of index such as MPO, $PGE_2$ and DAI. These results suggest that Z. schinifolium mediated anti-inflammatory action on colorectal sites may be a useful therapeutic approach to ulcerative colitis.