• Title/Summary/Keyword: basic drug

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Drug Delivery into the Blood-Brain Barrier by Endogenous Substances-A Role of Amine and Monocarboxylic Acid Carrier Systems for the Drug Transport- (내인성물질의 수송계를 이용한 혈액-뇌관문에의 약물송달V-약물의 혈액-뇌관문 투과성에 대한 염기성 아민 및 모노카르본산 수송계의 역할-)

  • Kang, Young-Sook
    • Journal of Pharmaceutical Investigation
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    • v.20 no.4
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    • pp.223-228
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    • 1990
  • The contribution of endogenous transport systems to the blood-brain barrier (BBB) transport of basic and acidic drugs was studied by using a carotid injection technique in rats and an isolated bovine cerebrovascular disease state were compared between the normotensive rats (WKY) and stroke-prone spontaneously hypertensive rats (SHRSP) which have been well established as an animal model with pathogenic similarities to humans. Basic drugs such as eperisone, thiamine and scopolamine inhibited, in a concentration dependent manner the in vivo uptake of $[{^3}H]choline$ through BBB, whereas amino acids and acidic drugs such as salicylic acid and valproic acid did not inhibit the uptake. The uptake of $[^3H]choline$ by B-CAP increased with time and showed a remarkable temperature dependency. The uptake of $[^3H]choline$ by B-CAP showed the very similar inhibitory effects as observed in the in vivo brain uptake, and was competitively inhibited by a basic drug, eperisone. The in vivo BBB uptakes of $[^3H]acetic$ acid and $[^{14}C]salicylic$ acid were dependent on pH of the injectate and the concentration of drugs. Several acidic drugs such such as salicylic acid, benzoic acid and valproic acid inhibited the in vivo uptake of $[^3H]acetic$ acid, whereas amino acid, choline and a basic drug such as eperisone did not inhibit the uptake. The uptake of acetic acid by B-CAP was competitively inhibited by salicylic acid. The permeability surface area product (PS) through BBB for $[^3H]choline$ in SHRSP was significantly lower than that in WKY. The concentration of choline in the brain dialysate in SHRSP was about half of that in WKY, while no significant difference was observed in the plasma concentration of choline between SHRSP and WKY. No significant difference was observed in the transport of monocarboxylic acids, glucose and neutral amino acid through BBB between SHRSP and WKY. From these results, it was concluded that BBB transport system of choline contributes to the transport of basic drugs through BBB, that acidic drugs can be transported via a moncarboxylic acid BBB transport system and that the specific dysfuntion of the BBB choline transport in SHRSP was ascribed to the reduction of the maximum velocity of choline concentration in the brain interstitial fluids.

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Prevention and the characteristics of drug abusers among Japanese junior high school students : A comparative study of drug users and non-drug users (예방적 측면에서 본 일본 청소년의 약물남용자의 특징 -약물남용자와 비남용자의 비교 연구-)

  • Oh, Hak
    • Korean Journal of Health Education and Promotion
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    • v.11 no.2
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    • pp.57-67
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    • 1994
  • The aim of this study was to research and compare the demographic characteristics of drug abusers with non-drug abusers among junior high school students in Japan through a closed format questionnaire. The same questionnaire and face-to-face interviews were used in order to find the circumstances of drug abuser among Kyogoin(a sort of child welfare institution) students in Japan. The goal of the study was to provide basic materials for preventive education of drug abuse through the two investigations mentioned above. Between July 1993 and November 1993, the information for this study was collected from 964 students from 4 junior high schools, and also 142 students from 3 Kyogoin in Japan. A total of 1106 questionnaires were completed resulting in a following response rate of 90.4%. Information was based on the scales : family relation scale, school life scale, recognition on danger of drug abuse scale, family environment scale (Moos, 1986), self esteem inventory (Coopersmith, 1967), etc. The conclusions can be summarized as follows : 1. Drug abusers are more likely to lake communication in their families and have poorer human relations than non-drug abusers. Also their school life scores tended to be lawer non-drug abusers. 2. It was between their 6th year of elementary school and their first of Junior high school when the drug was first used. The drug of choice which they made their first attempt at using was a volatile solvent which was inhaled. It is likely that this drug is "gateway-drug" for adolescents in Japan because they then also tried other drugs (e.g. cocaine, marijuana, etc.) step by step. 3. It is therefore clearly important that greatly increasing education on the harmful effects of drug abuse before the summer vacation of the first term of the sixth year of elementary school. At the same time, intervention in the family will have an effective prevention strategy in Japan, as well., as well.

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Pseudoreceptor: Concept and an Overview

  • Kothandan, Gugan;Madhavan, Thirumurthy;Gadhe, Changdev G.;Cho, Seung Joo
    • Journal of Integrative Natural Science
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    • v.3 no.3
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    • pp.162-167
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    • 2010
  • A pseudoreceptor combines structure-based and ligand-based techniques to represent a unifying concept for both receptor mapping and ligand matching. In this molecular modeling approach, there are opportunities to construct the pseudoreceptor models using a set of small molecules. To build a reliable pseudoreceptor model, we need a set of ligand molecules with known affinity (biological activity) to generate 3D bioactive conformation for each of these ligand molecules. Several software packages are available to generate a pseudoreceptor model and this can provide an entry point for structure based drug discovery in cases where receptor structure information is not available. In this review, we presented the concept of pseudoreceptor, as well as discussed about various software packages available to generate a pseudoreceptor model.

Exploration of the Binding Mode of Indole Derivatives as Potent HIV-1 Inhibitors Using Molecular Docking Simulations

  • Balupuri, Anand;Cho, Seung Joo
    • Journal of Integrative Natural Science
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    • v.6 no.3
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    • pp.138-142
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    • 2013
  • The HIV-1 envelope glycoprotein gp120 plays a vital role in the entry of the virus into the host cells. The crucial role of the glycoprotein suggests gp120 as potential drug target for the future antiviral therapies. Identification of the binding mode of small drug like compounds has been an important goal in drug design. In the current study we attempt to propose binding mode of indole derivatives in the binding pocket of gp120. These derivatives are reported to inhibit HIV-1 by acting as attachment inhibitors that bind to gp120 and prevent the gp120-CD4 interaction and thus inhibit the infectivity of HIV-1. To elucidate the molecular basis of the small molecules interactions to inhibit the glycoprotein function we employed the molecular docking simulation approach. This study provides insights to elucidate the binding pattern of indole-based gp120 inhibitors and may help in the rational design of novel HIV-1 inhibitors with improved potency.

A Short Review on the Application of Combining Molecular Docking and Molecular Dynamics Simulations in Field of Drug Discovery

  • Kothandan, Gugan;Ganapathy, Jagadeesan
    • Journal of Integrative Natural Science
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    • v.7 no.2
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    • pp.75-78
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    • 2014
  • Computer-aided drug design uses computational chemistry to discover, enhance, or study drugs and related biologically active molecules. It is now proved to be effective in reducing costs and speeding up drug discovery. In this short review, we discussed on the importance of combining molecular docking and molecular dynamics simulation methodologies. We also reviewed the importance of protein flexibility, refinement of docked complexes using molecular dynamics and the use of free energy calculations for the calculation of accurate binding energies has been reviewed.

Drug resistance of bladder cancer cells through activation of ABCG2 by FOXM1

  • Roh, Yun-Gil;Mun, Mi-Hye;Jeong, Mi-So;Kim, Won-Tae;Lee, Se-Ra;Chung, Jin-Woong;Kim, Seung Il;Kim, Tae Nam;Nam, Jong Kil;Leem, Sun-Hee
    • BMB Reports
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    • v.51 no.2
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    • pp.98-103
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    • 2018
  • Recurrence is a serious problem in patients with bladder cancer. The hypothesis for recurrence was that the proliferation of drug-resistant cells was reported, and this study focused on drug resistance due to drug efflux. Previous studies have identified FOXM1 as the key gene for recurrence. We found that FOXM1 inhibition decreased drug efflux activity and increased sensitivity to Doxorubicin. Therefore, we examined whether the expression of ABC transporter gene related to drug efflux is regulated by FOXM1. As a result, ABCG2, one of the genes involved in drug efflux, has been identified as a new target for FOXM1. We also demonstrated direct transcriptional regulation of ABCG2 by FOXM1 using ChIP assay. Consequently, in the presence of the drug, FOXM1 is proposed to directly activate ABCG2 to increase the drug efflux activation and drug resistance, thereby involving chemoresistance of bladder cancer cells. Therefore, we suggest that FOXM1 and ABCG2 may be useful targets and important parameters in the treatment of bladder cancer.

The Needs on the Drug Free Education in Adolescents (청소년의 약물남용 예방교육 요구도 조사)

  • Jung Hyang-Mi;Lee Hwa-Za;Kim Young-Hae
    • Child Health Nursing Research
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    • v.9 no.1
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    • pp.57-65
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    • 2003
  • Purpose: This study was intended to present basic data of a more effective drug free education program by examining and analyzing the needs of drug and health education in the adolescent. Method: The study subjects were 480 students from six high schools in Pusan. The data were collected by a self-administered questionnaire between June 1 and June 10, 1999. Descriptive statistics, t-test, one-way ANOVA, Scheffe test in SPSS program were used for data analysis. Result: The scoring rate of knowledge for drug abuse of the subjects was 26.8%. For the scores of knowledge according to the type of drug, cigarettes were the highest at 38.4%, and for the scores of knowledge according to items, the abuse part was 59%, also the highest. The needs of drugs and drug education for the subjects had an average of 19.59. For the score of needs according to the items, plans to maintain and improve health was 1.72, the highest, methods to control anger and stress was 1.66, toxicity of drugs was 1.51, and medicinal use of drugs was 1.44. For the characteristics of the subject and characteristics relating to drugs, and the comparison of needs of drug education, consisted of students who said they liked or disliked their school life, those who have had drug education at school, who having received drug education by various kinds of materials, all had high needs for the education. Conclusion: It is necessary that drug free education plans including plans to maintain and improve health on the basis of the needs of drug education for the adolescent and other contents such as the methods to control anger and stress are established. Development of various kinds of audio-visual materials, publicity booklets and educational programs for parents etc. are needed in order to make the adolescent have an interest in drug free education, and recognize its importance.

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A Study on the Actual Condition of Drug Abuse by Some Juveniles in Seoul - Based on Third School Year Students of Some Senior High Schools - (서울 시내 일부 청소년의 약물남용 실태에 관한 조사 연구 - 고등학교 3학년 학생을 중심으로 -)

  • Koh, Hong-Kyeong;Kim, Myung
    • Korean Journal of Health Education and Promotion
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    • v.7 no.1
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    • pp.72-82
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    • 1990
  • The actual condition of drug abuse by some Juveniles in our country and effects of some elements on their drug abusing were observed providing basic materials for health education to juveniles to contribute to the health improvement of them and the reduction of the harmfulness of drug abuse. 1035 third school year students of some senior high schools in Seoul were subjected to the questionnaire survey. The results could be summarized as follows : 1. Among the twelve kinds of drug involved in the study, alcohol (72.0%), cigarette (44.2%), stimulants (23.9%), analgesics (7.9%) appeard abused in the order named. 2. As for the motives of using antitussives, 30.1% of students answered because of curiosity, then 28.8%, in order to get a calm condition, and then 16.4%, to get along with friends. 3. As the result from seeing how much each drug abuser is contact with his family, frends, school, social surroundings and himself, every abuser appeared having higher degree of discontentment with family, school, society and himself excepting friends. 4. And when analyzed the relationship between their misconducting and drug-abusing, a close relationship was shown : mere abusers among misconduct-experienced students, and more misconduct-experienced students among abusers.

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Analysis of Factors Affecting Medication Compliance of Outpatients (의료기관 외래 이용자의 복약순응 관련 요인분석)

  • Lee, Eui-Kyung;Park, Jeong-Young
    • Quality Improvement in Health Care
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    • v.9 no.2
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    • pp.164-175
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    • 2002
  • Background : The purpose of this study was to investigate the current status of medication compliance of outpatients and to analyze the factors contributing to medication non-compliance Methods : Telephone survey was conducted to the 1,000 outpatients who visited medical institutions during the period from January 2002 to April 2002. Subjects were randomly selected from the telephone directories of the nation, and the socio-demographic characteristics of the respondents such as age, gender and region were matched based on those of outpatients in 2001. Results : The results of survey revealed that those who complied with doctors' regimen in the right way accounted for 82.4%. The compliance increased with the strong belief in the medication, less unwanted side effects and inconvenience, more severity of disease, and lower perceived health status. Compliance rate was also higher in the patients group who experienced the drug education by the pharmacists than those who did not. Conclusion : In order to improve drug compliance, drug information on efficacy, adverse reaction, drug interactions, and basic disease information are to be provided to the patients. Drug education needs to be focused not only on providing knowledge of drugs and diseases but also changing attitude on drug use of the patients.

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A Study on Improvement Issues to Activate the Statistics Utilization of the Ministry of Food and Drug Safety (식품의약품안전처 통계 활용 활성화를 위한 개선과제 도출)

  • Jung, Daeun;Kim, Jinmin
    • Journal of Korea Society of Digital Industry and Information Management
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    • v.17 no.4
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    • pp.133-146
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    • 2021
  • In the field of food and drug, the role of the Ministry of Food and Drug Safety is becoming more important for national and public safety as well as national development and improvement of public welfare. Food and drug statistics are being used to determine the priorities and directions of policy for the promotion of public health and the development of the health industry. This study focuses on statistics from the MFDS. Through the analysis of the MFDS's statistics, the current status of the MFDS's production statistics was identified, and the survey of utilization and satisfaction of the MFDS's statistics was conducted on food and drug experts who actually use the statistics of the MFDS. In order to identify problems of the MFDS statistics, environmental factors affecting the MFDS statistics were derived, and the priorities of improvement tasks for its statistics were identified using AHP and IPA. In addition, the current situation of the statistical system, which serve as the basic coordinate for the establishment and execution of domestic food and drug policies, was identified and implications were provided.