• 제목/요약/키워드: cholinesterase inhibitor

검색결과 29건 처리시간 0.023초

혈관성치매에 대한 한.양방 치료약물의 처방 사례연구 (A Case Study on Drug Prescription for Vascular Dementia in Western and Oriental Medicine)

  • 최성훈;전우현;백경민;한창현;전원경;감철우;이영준
    • 대한예방한의학회지
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    • 제15권3호
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    • pp.39-49
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    • 2011
  • Objectives : Vascular dementia is the second common cause of dementia after Alzheimer's disease. It assumed that the ratio of prescription drugs on vascular dementia are quite different from each hospital in Western medicine or Oriental medicine, respectively. The aim of this research is to collect and analyze the ratio of prescription drugs on vascular dementia in Western medicine or Oriental medicine in university hospitals. Methods : We collected and analyzed the data related to prescriptions on vascular dementia in the department of neurology in three university hospitals(A, B, C) and in the department of internal medicine in two Oriental medicine hospitals(Daegu Haany Oriental Hospital, Dong Eui Oriental Hospital). Results : In the department of neurology in A university hospital, donepezil(69.1%), memantine(14.0%), rivastigmine(12.3%), galantamine(4.5%) were prescribed in order. In B university hospital, galantamine(57.8%) donepezil(33.3%), rivastigmine(6.7%), donepezil with memantine(4.4%) were prescribed. In C university hospital, donepezil(62.0%), rivastigmine(25.0%), galantamine(7.0%) memantine(6.0%) were prescribed. The average frequencies of prescribed medication in the department of neurology in A, B, C university hospitals were donepezil(54.8%), galantamine(23.1%), rivastigmine(14.7%), memantine(7.4%). In Oriental medicine hospitals, various prescriptions have been used for vascular dementia. Among them, Ansincheongnoetang (安神淸腦湯) and Gamijihangeumja(加味地黃飮子) were often prescribed in Daegu Haany Oriental Hospital, and Bojungikgitang(補中益氣湯) in Dong Eui Oriental Hospital, too. Conclusions : Cholinesterase inhibitors such as donepezil, galantamine, rivastigmine and NMDA receptor inhibitor like memantine have been used as a drug of choice for vascular dementia in all surveyed university hospitals. In oriental hospitals, various prescriptions have been used for vascular dementia.

Selective Butyrylcholinesterase Inhibitors Using Polyphenol-polyphenol Hybrid Molecules

  • Woo, Yeun-Ji;Lee, Bo-Hyun;Yeun, Go-Heum;Kim, Hyun-Ju;Won, Moo-Ho;Kim, Sang-Hern;Lee, Bong-Ho;Park, Jeong-Ho
    • Bulletin of the Korean Chemical Society
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    • 제32권8호
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    • pp.2593-2598
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    • 2011
  • Polyphenols (PPs) are known as antioxidant compounds having benign biological activities. In this paper, a series of hybrid molecules between the free or acetyl protected polyphenol compounds were synthesized and their in vitro antioxidant activity (DPPH assay) and cholinesterase [acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE)] inhibition activities were evaluated. As expected, free phenolic hybrid compounds (6 and 8) showed better antioxidant activity than acetyl protected hybrid compounds (5 and 7) from DPPH assay. But the contrast result was obtained from BuChE inhibition assay. Acetyl protected hybrid compounds (5 and 7) showed better inhibition activity for BuChE than free phenolic hybrid compounds (6 and 8). Specifically, 10 (AcFA-AcFA) were shown as an effective inhibitor of BuChE ($IC_{50}=2.3{\pm}0.3{\mu}M$) and also had a great selectivity for BuChE over AChE (more than 170 fold). Inhibition kinetic studies with acetyl protected compounds (5, 7, 9, and 10) indicated that 5, 7 and 10 are a hyperbolic mixed-type inhibition and 10 is a competitive inhibition type. The binding affinity (Ki) value of 10 to BuChE is $2.32{\pm}0.15{\mu}M$.

Synthesis of Selective Butyrylcholinesterase Inhibitors Coupled between α-Lipoic Acid and Polyphenols by Using 2-(Piperazin-1-yl)ethanol Linker

  • Yeun, Go Heum;Lee, Seung Hwan;Lim, Yong Bae;Lee, Hye Sook;Won, Moo-Ho;Lee, Bong Ho;Park, Jeong Ho
    • Bulletin of the Korean Chemical Society
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    • 제34권4호
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    • pp.1025-1029
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    • 2013
  • In the previous paper (Bull. Korean Chem. Soc., 2011, 32, 2997), the hybrid molecules between ${\alpha}$-lipoic acid (ALA) and polyphenols (PPs) connected with neutral 2-(2-aminoethoxy)ethanol linker (linker-1) showed new biological activity such as butyrylcholinesterase (BuChE) inhibition. In order to increase the binding affinity of the hybrid compounds to cholinesterase (ChE), the neutral 2-(2-aminoethoxy)ethanol (linker 1) was switched to the cationic 2-(piperazin-1-yl)ethanol linker (linker 2). The $IC_{50}$ values of the linker-2 hybrid molecules for BuChE inhibition were lower than those of linker-1 hybrid molecules (except 9-2) and they also had the same great selectivity for BuChE over AChE (> 800 fold) as linker-1 hybrid molecules. ALA-acetyl caffeic acid (10-2, ALA-AcCA) was shown as an effective inhibitor of BuChE ($IC_{50}=0.44{\pm}0.24{\mu}M$). A kinetic study using 7-2 showed that it is the same mixed type inhibition as 7-1. Its inhibition constant (Ki) to BuChE is $4.3{\pm}0.09{\mu}M$.

대동맥 판막 치환술 후 만기에 발생한 상행 대동맥 박리증 (Ascending Aortic Dissection Late After Aortic Valve Replacement)

  • 오정훈;이동협;이정철;정태은;이장훈;한승세
    • Journal of Chest Surgery
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    • 제34권8호
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    • pp.630-633
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    • 2001
  • 선천성 다발성 판막질환(Congenital Polyvalvular Disease)은 결체조직의 이상으로 인해 한 개 이상의 심장판막에 비정상적 기형을 초래하는 질환으로 그 원인은 아직 확실히 알려져 있지 않다. 이 질환은 제 18번 또는 13∼15번 삼염색체 증후군에서 자주 관찰되며, 심실중격결손증, 동맥과 개존증 등의 심장기형을 동반하기도 한다. 환아는 산전 초음파 검사에서 우심방내의 종괴가 발견되고, 출생 후 시행한 심초음파 검사에서 삼첨판위의 혈종 또는 점액종이 의심되어 수술을 시행하였다. 종괴는 삼첨판막의 전판막첨과 중격판막첨으로부터 완전히 제거되었고 병리학적 검사에서 불규clr하게 두꺼워지고 결절화되어 있었으며, 석회화와 골화의 소견을 보였다. 태아의 산전 심초음파 검사에서 판막에 석회화 소견이 관찰될 때 선천성 다발성 판막질환도 염두에 두어야 할 의미 있는 소견이라고 생각된다. 저자들은 선천성 다발성 판막질환 1예를 경험하여 임상 및 조직소견을 문헌 고찰과 함께 보고하고자 한다.

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Oxyfluoren이 함유된 입제 glyphosate 제초제(대장군) 급성 중독 1예 (A Case of Acute Intoxication with Glyphosate and Oxyfluorfen Containing Powder Herbicide ($Daejangun^{(R)}$))

  • 이승희;이금호;유성수;노형근
    • 대한임상독성학회지
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    • 제3권2호
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    • pp.110-113
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    • 2005
  • Glyphosate containing herbicides are an alternative to paraquat and have been widely used with increasing frequency in suicide attempts throughout Asia. It is an organophosphorus compound that is not a cholinesterase inhibitor. Daejangun powder consists of glyphosate ammonium, surfactant and another herbicide, oxyfluorfen. A 60-year-old man ingested about 300 g of Daejangun powder with 500 ml of water in a suicide attempt. He was brought to emergency room 6 hours after the ingestion and showed severe metabolic acidosis (pH 6.75), marked leukocytosis (WBC 35,800/$mm^3$), hypoglycemia (glucose 13 mg/dL) and increased liver enzymes (AST/ALT 1,683/418 IU/L). Later he developed aspiration pneumonia, acute renal failure and hyperchloremic acidosis. Upper gastrointestinal endoscopy which performed 5 days after the ingestion revealed corrosive injuries (grade 1) in both esophagus and stomach. However, intensive treatment with supportive measures improved the abnormal findings almost completely 4 weeks after the ingestion.

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Development of donepezil-induced hypokalemia following treatment of cognitive impairment

  • Kim, Dongryul;Yoon, Hye Eun;Park, Hoon Suk;Shin, Seok Joon;Choi, Bum Soon;Kim, Byung Soo;Ban, Tae Hyun
    • Journal of Yeungnam Medical Science
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    • 제38권1호
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    • pp.65-69
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    • 2021
  • Donepezil is a cholinesterase inhibitor used extensively to treat Alzheimer disease. The increased cholinergic activity is associated with adverse effects, therefore gastrointestinal symptoms, including nausea, vomiting, and diarrhea, are common. Hypokalemia is a rare adverse event that occurs in less than 1% of donepezil-treated patients. Although hypokalemia of mild and moderate grade does not present serious signs and symptoms, severe hypokalemia often results in prolonged hospitalization and mortality. Herein, we report a case of hypokalemia developed after the initiation of donepezil therapy for cognitive impairment.

비전형적 치매양상을 보이는 후부대뇌피질위축 증례보고 (A case of Posterior Cortical Atrophy Presenting with Features of Atypical Dementia)

  • 박기형;김성완;신동진;박현미;이영배;성영희
    • 생물정신의학
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    • 제15권1호
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    • pp.46-53
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    • 2008
  • Posterior cortical atrophy(PCA) is a presenile dementia that presents primarily with signs and symptoms of cortical visual dysfunction, while memory is relatively preserved until the late stage of the disease. We report a patient with PCA, confirmed by brain magnetic resonance imaging (MRI) and $F^{18}$-fluorodeoxyglucose positron emission tomography(FDG PET). A 58-year-old right-handed woman presented initially with visual dimness and difficulty finding things around her. She had partial Balint's syndrome, partial Gerstmann syndrome, and idiomotor apraxia. She also had a mild memory disturbance, but preserved insight of her disease. Neuropsychological evaluation showed decreased parietal and left temporal functions bilaterally. Brain MRI and $F^{18}$-FDG PET revealed typical bilateral occipitoparietal atrophy and hypometabolism, which were slightly worse on the right side. Cholinesterase inhibitor administration for 6 months improved the memory impairment slightly, but not the cortical visual dysfunction. This is a typical case of PCA, confirmed by neurologic signs and imaging findings.

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Effect of Panax ginseng on Latency of Passive Avoidance Response and Neuronal Damage of Hippocampus

  • Cho, So-Hyun;Choi, Sang-Hyun;Choi, Jae-Won;Kim, Dong-Hoon;Shin, Kyung-Ho;Chun, Yeon-Sook;Chun, Boe-Gwun
    • The Korean Journal of Physiology and Pharmacology
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    • 제1권4호
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    • pp.345-353
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    • 1997
  • The effects of crude saponin (SAP) and alkaloid (ALK) fractions of Panax ginseng C.A. Meyer on the detrimental effects of electroconvulsive shock (ECS) and scopolamine on passive avoidance response (PAR) were studied in male Sprague-Dawley rats, referring their effects on the neuronal injury and plasticity of hippocampus in response to electrolytic lesion of left entorhinal cortex (ECL). The detrimental ECS effect on PAR was attenuated by pre- and post-treatments with SAP and ALK, respectively, or by pretreatment with aminoguanidine (AG), an inhibitor of diamine oxidase and NO synthase. And the detrimental scopolamine effect on PAR was also inhibited by pre-treatment with ALK or AG, and by post- treatment with SAP or ALK, respectively. On the 7th day after ECL, the brain sections stained by cresyl violet and by acetylcholinesterase (AChE) histochemistry, respectively, showed the chromatolysis and numeral decrease of neurons and the reduction of AChE reactivity in the hippocampus CA1 area and to a lesser extent, in the dentate gyrus. The neuronal cell death of the CA1 area was significantly reduced by SAP, ALK, or AG, and the reduction of AChE reactivity was significantly attenuated by SAP or ALK and to a lesser extent by AG. These results suggests that the protective effect of ginseng SAP and ALK fractions on ECS- or scopolamine-induced impairment of PAR may be ascribed in part to preservation of hippocampal neurons, particularly cholinergic neurons.

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흰쥐 적출 배뇨근에서 콜린성 및 퓨린성 수용체의 존재 (Existence of Cholinergic and Purinergic Receptor on the Detrusor Muscle of Rat Urinary Bladder)

  • 최태수;권오철;하정희;이광윤;김원준
    • Journal of Yeungnam Medical Science
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    • 제8권2호
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    • pp.138-149
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    • 1991
  • 흰쥐(Sprague-Dawley)의 방광에서 적출한 배뇨근절편을 적출 근편 실험조에 현수하고, 등척성 장력 측정기를 사용하여 그 수축력을 묘기하였다. 배뇨근 절편은 전기장자극에 의해 수축하였으며, 이 수축반응은 콜린에스테라제 억제약물인 physostigmine에 의해 증가하였고 신경말단에서의 choline 재흡수를 방해하는 hemicholinium에 의해 억제되었으며, 신경절봉쇄약물인 hexamethonium에 의해서는 영향을 받지 않았으나 신경축색전도 억제제인 tetrodotoxin에 의해서 소실되었다. 이러한 전기장자극유발 수축은 콜린성 무스카린성 수용체봉쇄약물인 atropine에 의해 부분적으로 길항되었으며, atropine에 의해 길항되지 않는 부분은 ATP 탈감작에 의해 완전히 소실되었다. 배뇨근 절편은 콜린성 무스카린성 수용체 흥분제인 bethanechol과 퓨린성 수용체 흥분제인 ATP에 의하여 농도의존적 수축력 증가를 나타내었으며, 이중 bethanechol 유발수축은 ATP 탈감작에 의해 영향을 받지 않았고, ATP 유발수축은 tetrodotoxin에 의하여 영향을 받지 않았다. 이상의 결과로 보아 흰쥐의 적출배뇨근에는 흥분성 신경전달체계로서 퓨린성 수용체와 콜린성 수용체가 존재하며, 이들은 서로 영향을 미침이 없이 독자적으로 배뇨근 수축에 기여하고 있다고 사료된다.

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