DOCSLIB.ORG

Handbook of Anti-Tuberculosis Agents

Total Page：16

File Type：pdf, Size：1020Kb

Download full-text PDF Read full-text
Handbook of Anti-Tuberculosis Agents Volume 88 Tuberculosis Number 2 2008 http://intl.elsevierhealth.com/journals/tube Pages 85–170 Handbook of Anti-Tuberculosis Agents Global Alliance for TB Drug Development 80 Broad Street New York, NY 10004, USA Amsterdam • Boston • Jena • London • New York • Oxford • Paris • Philadelphia • San Diego • St Louis Aims and Scope Tuberculosis is a speciality journal focusing on basic experimental research . pathogenesis on tuberculosis, notably on bacteriological, immunological and patho- . pathology genesis aspects. The journal publishes original research and reviews on . molecular epidemiology the host response and immunology of tuberculosis and the molecular . diagnostics biology, genetics and physiology of the organism. vaccine development Areas covered include: . drug resistance . immunology The resurgence of interest in tuberculosis has accelerated the . immunogenetics pace of relevant research and Tuberculosis has grown with it, as . pathogenetics the only journal dedicated to experimental biomedical research in . microbiology tuberculosis. Please see details of online submission at http:// . microbial physiology ees.elsevier.com/tube/ Author Enquiries e-mail: [email protected] Permissions may be sought directly For enquiries relating to the submission of To k yo: Elsevier, Customer Service Depart- from Elsevier’s Rights Department in articles (including electronic submission where ment, 4F Higashi-Azabu, 1-Chome Bldg, Oxford, UK; phone: (+44) 1865 843 830 or available) please visit this journal’s homepage 1-9-15 Higashi-Azabu, Minato-ku, (+1) 215 238 7869; fax: (+1) 215 238 2239; at http://www.elsevier.com/locate/tube/. You Tokyo 106-0044, Japan; phone: (+81) (3) e-mail: [email protected] or can track accepted articles at http://www. 5561 5037; fax: (+81) (3) 5561 5047; [email protected]. Requests may elsevier.com/trackarticle and set up e-mail e-mail: [email protected] also be completed on-line via the Elsevier alerts to inform you of when an article’s status Singapore: Elsevier, Customer Service homepage (http://www.elsevier.com/locate/ haschanged,aswellascopyrightinformation, Department, 3 Killiney Road, #08-01 Wins- permissions).In the USA, users may clear frequently asked questions and more. land House I, Singapore 239519; phone: permissions and make payments through Contact details for questions arising after (+65) 63490222; fax: (+65) 67331510; the Copyright Clearance Center, Inc., 222 acceptance of an article, especially those e-mail: [email protected] Rosewood Drive, Danvers, MA 01923, USA; relating to proofs, are provided after phone: (+1) (978) 750 8400; fax: registration of an article for publication. Advertising information (+1) (978) 750 4744,and in the UK through The full and complete Guide for Authors Advertising orders and enquiries can be sent the Copyright Licensing Agency Rapid USA, Canada and South America: can be found in the first issue of the volume to: Clearance Service (CLARCS), 90 Tottenham and the electronic version on http:// Mr Tino DeCarlo, The Advertising Court Road, London W1P 0LP, UK; phone: www.elsevier/health.com/journals/tube. Department, Elsevier Inc., 360 Park Avenue (+44) 20 7631 5555; fax: (+44) 20 7631 5500. South, New York, NY 10010-1710, USA; Other countries may have a local Publication information phone: (+1) (212) 633 3815; reprographic rights agency for payments. fax: (+1) (212) 633 3820; Tuberculosis (ISSN 1472-9792). For 2008, e-mail: [email protected]. DerivativeWorks volume 88 is scheduled for publication. Japan: The Advertising Department, Subscribers may reproduce tables of con- Subscription prices are available upon Elsevier K.K., 4F Higashi-Azabu, tents or prepare lists of articles including request from the Publisher or from the 1-Chome Bldg, 1-9-15 Higashi-Azabu, abstracts for internal circulation within their Regional Sales Office nearest you or from Minato-ku, Tokyo 106-0044, Japan; institutions. Permission of the Publisher is this journal’s website (http://www.elsevier. phone: (+81) (3) 55615037; required for resale or distribution outside com/locate/tube). Further information is fax: (+81) (3) 55615047; the institution. available on this journal and other Elsevier e-mail: [email protected] Permission of the Publisher is required products through Elsevier’s website: (http:// Europe and ROW: Fiona Macnab, for all other derivative works, including www.elsevier.com). Subscriptions are European Journal Commercial Sales, compilations and translations. accepted on a prepaid basis only and are Elsevier Ltd., 32 Jamestown Road, Camden, Electronic Storage or Usage entered on a calendar year basis. Issues are London, NW1 7BY, UK; Permission of the publisher is required to sent by standard mail (surface within phone: (+44) (0) 20 7424 4259; store or use electronically any material Europe, air delivery outside Europe). Priority fax: (+44) (0) 20 7424 4433; contained in this journal, including any rates are available upon request. Claims for e-mail: [email protected] missing issues should be made within six article or part of an article. months of the date of dispatch. Indexing and Abstracting Services Except as outlined above, no part of this publication may be reproduced, stored in a This journal is indexed, abstracted USA mailing notice: Tuberculosis (ISSN retrieval system or transmitted in any form and/or published online in the following 1472-9792) is published bimonthly by or by any means, electronic, mechanical, media: Adonis, CAB International, Elsevier Ltd. (The Boulevard, Langford Lane, photocopying, recording or otherwise, Cambridge Scientific Abstracts, Current Kidlington, Oxford OX5 1GB, UK). Annual without prior written permission of the $ Contents, Academy of Sciences Russia, subscription price in the USA US 949 Publisher. Biological Abstracts, UMI (Microfilms), (valid in North, Central and South America), Address permissions requests to: Elsevier BIOSIS, Index Medicus/Medline, NMLUS, including air speed delivery. Periodical Rights Department, at the fax and e-mail Sciences Citation Index, Scisearch, postage paid at Rahway NJ and additional addresses noted above. mailing offices. Research Alert, Medical Documentation Service, EMBASE/Exerpta Medica, Elsevier Notice USA postmaster: Send change of address: BIOBASE/Current Awareness in No responsibility is assumed by the Tuberculosis, Elsevier, 6277 Sea Harbor Biological Sciences. Publisher for any injury and/or damage to Drive, Orlando, FL 32887-4800. & 2007 Elsevier Ltd. All rights reserved persons or property as a matter of products Airfreight and Mailing in USA by liability, negligence or otherwise, or from This journal and the individual contribu- any use or operation of any methods, Mercury International Limited, 365, Blair tions contained in it are protected Road, Avenel, NJ 07001. products, instructions or ideas contained in under copyright by Elsevier Ltd, and the the material herein. Because of rapid Orders, claims, and journal enquiries: please following terms and conditions apply to advances in the medical sciences, in contact the Customer Service Department at their use: particular, independent verification of diag- the Regional Sales Office nearest you: noses and drug dosages should be made. Orlando: Elsevier, Customer Service Depart- Photocopying Although all advertising material is expected ment, 6277 Sea Harbor Drive, Orlando, FL Single photocopies of single articles may to conform to ethical (medical) standards, 32887-4800, USA; phone: (877) 8397126 or be made for personal use as allowed by inclusion in this publication does not (800) 6542452 [toll free number for US national copyright laws. Permission of the constitute a guarantee or endorsement of the customers]; (+1) (407) 3454020, (+1) (407) Publisher and payment of a fee is required quality or value of such product or of the 3639661 [customers outside US]; fax: (+1) for all other photocopying, including claims made of it by its manufacturer. (407) 3631354; e-mail: usjcs@ multiple or systematic copying, copying elsevier.com or [email protected] for advertising or promotional purposes, 1 The paper used in this publication meets Amsterdam: Elsevier, Customer Service resale, and all forms of document delivery. the requirments of ANSI/NISO Z39.48-1992 Department, PO Box 211, 1000 AE Amster- Special rates are available for educational (Permanence of Paper). dam, The Netherlands; institutions that wish to make photo- phone: (+31) (20) 4853757; copies for non-profit educational fax: (+31) (20) 4853432; classroom use. Tuberculosis has no page charges Tuberculosis Co-Editors in Chief Patrick J. Brennan Department of Microbiology, Immunology and Pathology, College of Veterinary Medicine and Biomedical Sciences, Colorado State University, Fort Collins, CO 80523-1682, USA Douglas B. Young Centre for Molecular Microbiology and Infection, 3.14 Flowers Building, South Kensington Campus, Imperial College, London SW7 2AZ, UK Deputy Editor Brian D. Robertson Centre for Molecular Microbiology and Infection, 3.41 Flowers Building, South Kensington Campus, Imperial College London SW7 2AZ, UK Section Editors Peter Andersen Ken Duncan Gilla Kaplan Staens Seruminstitut Bill and Melinda Gates Foundation Public Health Research Copenhagen, Denmark Seattle, WA, USA Institute, Newark, NJ, USA Kathleen Eisenach Stefan Kaufmann Clifton Barry III University of Arkansas Max Planck Institute for Infec- National Institutes of Health for Medical Sciences tion Biology, Rockville, MD, USA Little Rock, AR, USA Berlin, Germany Warwick
Load more

Recommended publications
  • WO 2015/179249 Al 26 November 2015 (26.11.2015) P O P C T
    (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (10) International Publication Number (43) International Publication Date WO 2015/179249 Al 26 November 2015 (26.11.2015) P O P C T (51) International Patent Classification: (81) Designated States (unless otherwise indicated, for every C12N 15/11 (2006.01) A61K 38/08 (2006.01) kind of national protection available): AE, AG, AL, AM, C12N 15/00 (2006.01) AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, (21) Number: International Application DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, PCT/US2015/031213 HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KN, KP, KR, (22) International Filing Date: KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, 15 May 2015 (15.05.2015) MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, (25) Filing Language: English SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, (26) Publication Language: English TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (30) Priority Data: (84) Designated States (unless otherwise indicated, for every 62/000,43 1 19 May 2014 (19.05.2014) US kind of regional protection available): ARIPO (BW, GH, 62/129,746 6 March 2015 (06.03.2015) US GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, (72) Inventors; and TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, (71) Applicants : GELLER, Bruce, L.
    [Show full text]
  • CLINICAL USE of RIFABUTIN, a RIFAMYCIN-CLASS ANTIBIOTIC, for the TREATMENT of TUBERCULOSIS (A Supplement to the 2008 Revision Of“ Standards for Tuberculosis Care”)
    Kekkaku Vol. 86, No. 1: 43, 2011 43 CLINICAL USE OF RIFABUTIN, A RIFAMYCIN-CLASS ANTIBIOTIC, FOR THE TREATMENT OF TUBERCULOSIS (A supplement to the 2008 revision of“ Standards for tuberculosis care”) August, 2008 The Treatment Committee of the Japanese Society for Tuberculosis The Treatment Committee of the Japanese Society for [Dosage and administration of rifabutin] Tuberculosis published statements on the“ Standards for Rifabutin, 5 mg/kg in body weight/day, maximum 300 mg/ tuberculosis care” in April 2008. Therein we referred to day, once daily. rifampicin as follows“; Use of rifampicin requires attention The dosage of rifabutin can be increased up to the maximum because of the interactions with a number of other drugs. daily dose of 450 mg in cases where decreased rifabutin serum Particularly for HIV-infected patients who need antiviral levels are expected due to anti-HIV drugs such as efavirenz, drugs, the replacement of rifampicin by rifabutin should be and in other cases if necessary. considered”. Rifabutin, belonging to rifamycin-class antibiotics In non-HIV-infected patients, rifabutin can be used for like rifampicin, causes less significant drug-drug interactions intermittent treatment with a regimen of twice or three times a than rifampicin, and can be used in combination with antiviral week, with the same dosage as daily administration. drugs mentioned above. In July 2008, rifabutin was approved as antituberculous drug, and is expected to be added to the drug [Important points for use of rifabutin] price listing in the near future*. Therefore, to the published (1) Rifabutin causes drug interactions due to induction of opinions, we add new statements concerning the use of rifabutin hepatic enzyme though less significantly than rifampicin.
    [Show full text]
  • Folic Acid Antagonists: Antimicrobial and Immunomodulating Mechanisms and Applications
    International Journal of Molecular Sciences Review Folic Acid Antagonists: Antimicrobial and Immunomodulating Mechanisms and Applications Daniel Fernández-Villa 1, Maria Rosa Aguilar 1,2 and Luis Rojo 1,2,* 1 Instituto de Ciencia y Tecnología de Polímeros, Consejo Superior de Investigaciones Científicas, CSIC, 28006 Madrid, Spain; [email protected] (D.F.-V.); [email protected] (M.R.A.) 2 Consorcio Centro de Investigación Biomédica en Red de Bioingeniería, Biomateriales y Nanomedicina, 28029 Madrid, Spain * Correspondence: [email protected]; Tel.: +34-915-622-900 Received: 18 September 2019; Accepted: 7 October 2019; Published: 9 October 2019 Abstract: Bacterial, protozoan and other microbial infections share an accelerated metabolic rate. In order to ensure a proper functioning of cell replication and proteins and nucleic acids synthesis processes, folate metabolism rate is also increased in these cases. For this reason, folic acid antagonists have been used since their discovery to treat different kinds of microbial infections, taking advantage of this metabolic difference when compared with human cells. However, resistances to these compounds have emerged since then and only combined therapies are currently used in clinic. In addition, some of these compounds have been found to have an immunomodulatory behavior that allows clinicians using them as anti-inflammatory or immunosuppressive drugs. Therefore, the aim of this review is to provide an updated state-of-the-art on the use of antifolates as antibacterial and immunomodulating agents in the clinical setting, as well as to present their action mechanisms and currently investigated biomedical applications. Keywords: folic acid antagonists; antifolates; antibiotics; antibacterials; immunomodulation; sulfonamides; antimalarial 1.
    [Show full text]
  • Clinically Isolated Chlamydia Trachomatis Strains
    ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, JUIY 1988, p. 1080-1081 Vol. 32, No. 7 0066-4804/88/071080-02$02.00/0 Copyright © 1988, American Society for Microbiology In Vitro Activities of T-3262, NY-198, Fleroxacin (AM-833; RO 23-6240), and Other New Quinolone Agents against Clinically Isolated Chlamydia trachomatis Strains HIROSHI MAEDA,* AKIRA FUJII, KATSUHISA NAKATA, SOICHI ARAKAWA, AND SADAO KAMIDONO Department of Urology, School of Medicine, Kobe University, 7-5-1 Kusunoki-cho, Chuo-ku, Kobe-city, Japan Received 9 December 1987/Accepted 29 March 1988 The in vitro activities of three newly developed quinolone drugs (T-3262, NY-198, and fleroxacin [AM-833; RO 23-6240]) against 10 strains of clinically isolated Chiamydia trachomatis were assessed and compared with those of other quinolones and minocycline. T-3262 (MIC for 90% of isolates tested, 0.1 ,ug/ml) was the most active of the quinolones. The NY-198 and fleroxacin MICs for 90% of isolates were 3.13 and 62.5 ,ug/ml, respectively. Recently, it has become well known that Chlamydia 1-ml sample of suspension was seeded into flat-bottomed trachomatis is an important human pathogen. It is respon- tubes with glass cover slips and incubated at 37°C in 5% CO2 sible not only for trachoma but also for sexually transmitted for 24 h. The monolayer was inoculated with 103 inclusion- infections, including lymphogranuloma venereum. In forming units of C. trachomatis. The tubes were centrifuged women, it causes cervicitis, endometritis, and salpingitis at 2,000 x g at 25°C for 45 min and left undisturbed at room asymptomatically (19), while in men it causes nongono- temperature for 2 h.
    [Show full text]
  • Second and Third Generation Oral Fluoroquinolones
    Therapeutic Class Overview Second and Third Generation Oral Fluoroquinolones Therapeutic Class • Overview/Summary: The second and third generation quinolones are approved to treat a variety of infections, including dermatologic, gastrointestinal, genitourinary, respiratory, as well as several miscellaneous infections.1-10 They are broad-spectrum agents that directly inhibit bacterial deoxyribonucleic acid (DNA) synthesis by blocking the actions of DNA gyrase and topoisomerase IV, which leads to bacterial cell death.11,12 The quinolones are most active against gram-negative bacilli and gram-negative cocci.12 Ciprofloxacin has the most potent activity against gram-negative bacteria. Norfloxacin, ciprofloxacin and ofloxacin have limited activity against streptococci and many anaerobes while levofloxacin and moxifloxacin have greater potency against gram-positive cocci, and moxifloxacin has enhanced activity against anaerobic bacteria.11-12 Gemifloxacin, levofloxacin and moxifloxacin are considered respiratory fluoroquinolones. They possess enhanced activity against Streptococcus pneumoniae while maintaining efficacy against Haemophilus influenzae, Moraxella catarrhalis and atypical pathogens. Resistance to the quinolones is increasing and cross-resistance among the various agents has been documented. Two mechanisms of bacterial resistance have been identified. These include mutations in chromosomal genes (DNA gyrase and/or topoisomerase IV) and altered drug permeability across the bacterial cell membranes.11-12 Clinical Guidelines support
    [Show full text]
  • Repurposing Drug Scaffolds: a Tool for Developing Novel Therapeutics with Applications in Malaria and Lung Cancer
    Repurposing Drug Scaffolds: A Tool for Developing Novel Therapeutics with Applications in Malaria and Lung Cancer A Thesis Submitted by: Hannah Elizabeth Cook In partial fulfilment of the requirements for the degree of: Doctor of Philosophy September 2018 Supervisors: Professor Matthew J. Fuchter & Professor Anthony G. M. Barrett Department of Chemistry Imperial College London 2 Declaration of Originality I, Hannah Cook, hereby confirm that the work presented within this thesis is entirely my own, conducted under the supervision of Professor Matthew J. Fuchter and Professor Anthony G. M. Barrett, at the Department of Chemistry, Imperial College London, unless otherwise stated. All work performed by others has been acknowledged within the text and referenced where appropriate. Hannah E. Cook September 2018 Copyright Declaration The copyright of this thesis rests with the author and is made available under a Creative Commons Attribution Non-Commercial No Derivatives licence. Researchers are free to copy, distribute or transmit the thesis on the condition that they attribute it, that they do not use it for commercial purposes and that they do not alter, transform or build upon it. For any reuse or redistribution, researchers must make clear to others the licence terms of this work. 3 Abstract The definition of repurposing in the context of drug discovery encompasses a variety of strategies designed to redirect current therapeutic knowledge towards new disease indications. This approach can be successful for the design of new drugs to treat diseases of the developing world such as Malaria, where there are limited resources to fund new drug discovery campaigns. Moreover, it can be used to decrease the drug development time for diseases in which there is high drug attrition rates coupled with high mortality rates, which is the case for some cancers.
    [Show full text]
  • A TWO-YEAR RETROSPECTIVE ANALYSIS of ADVERSE DRUG REACTIONS with 5PSQ-031 FLUOROQUINOLONE and QUINOLONE ANTIBIOTICS 24Th Congress Of
    A TWO-YEAR RETROSPECTIVE ANALYSIS OF ADVERSE DRUG REACTIONS WITH 5PSQ-031 FLUOROQUINOLONE AND QUINOLONE ANTIBIOTICS 24th Congress of V. Borsi1, M. Del Lungo2, L. Giovannetti1, M.G. Lai1, M. Parrilli1 1 Azienda USL Toscana Centro, Pharmacovigilance Centre, Florence, Italy 2 Dept. of Neurosciences, Psychology, Drug Research and Child Health (NEUROFARBA), 27-29 March 2019 Section of Pharmacology and Toxicology , University of Florence, Italy BACKGROUND PURPOSE On 9 February 2017, the Pharmacovigilance Risk Assessment Committee (PRAC) initiated a review1 of disabling To review the adverse drugs and potentially long-lasting side effects reported with systemic and inhaled quinolone and fluoroquinolone reactions (ADRs) of antibiotics at the request of the German medicines authority (BfArM) following reports of long-lasting side effects systemic and inhaled in the national safety database and the published literature. fluoroquinolone and quinolone antibiotics that MATERIAL AND METHODS involved peripheral and central nervous system, Retrospective analysis of ADRs reported in our APVD involving ciprofloxacin, flumequine, levofloxacin, tendons, muscles and joints lomefloxacin, moxifloxacin, norfloxacin, ofloxacin, pefloxacin, prulifloxacin, rufloxacin, cinoxacin, nalidixic acid, reported from our pipemidic given systemically (by mouth or injection). The period considered is September 2016 to September Pharmacovigilance 2018. Department (PVD). RESULTS 22 ADRs were reported in our PVD involving fluoroquinolone and quinolone antibiotics in the period considered and that affected peripheral or central nervous system, tendons, muscles and joints. The mean patient age was 67,3 years (range: 17-92 years). 63,7% of the ADRs reported were serious, of which 22,7% caused hospitalization and 4,5% caused persistent/severe disability. 81,8% of the ADRs were reported by a healthcare professional (physician, pharmacist or other) and 18,2% by patient or a non-healthcare professional.
    [Show full text]
  • 2019 National Library of Medicine Classification Schedules
    National Library of Medicine Classification 2019 Schedule S-1 QS Human Anatomy Classify here general works on normal human anatomy. Works that treat men, women, or children separately are classed here. • Classify works on anatomy of a part of the body with the part. • Classify works on surgical anatomy in WO 101. • Classify works on artistic anatomy of human or animal in NC 760-783.8. • Classify works on anatomy of animals in QL or SF. QS 1-132 Anatomy QS 504-532 Histology QS 604-681 Embryology Anatomy Note that form numbers are also used under Histology (QS 504-539) and under Embryology (QS 604-681). QS 1 Organizations. Societies (General or not elsewhere classified) (Cutter from name of organization or society) (Table G) (Used for both monographs and serials) Includes membership lists issued serially or separately. Classify directories in QS 22. Classify annual reports, journals, etc., in W1. For academies and institutes, see QS 23-24. QS 4 General works Classify here works on regional anatomy. If written for the surgeon, classify in WO 101 Surgical anatomy. Classify material on comparative anatomy in QS 124. Collected works QS 5 By several authors QS 7 By individual authors QS 9 Addresses. Essays. Lectures QS 11 History (Table G) QS 11.1 General coverage (Not Table G) QS 13 Dictionaries. Encyclopedias QS 15 Classification. Terminology (Used for both monographs and serials) QS 16 Tables. Statistics. Surveys (Table G) (Used for both monographs and serials) QS 16.1 General coverage (Not Table G) (Used for both monographs and serials) QS 17 Atlases.
    [Show full text]
  • Pharmaceutical Applications Notebook
    Pharmaceutical Applications Notebook Antibiotics Table of Contents Index of Analytes .......................................................................................................................................................................3 Introduction to Pharmaceuticals ................................................................................................................................................4 UltiMate 3000 UHPLC+ Systems .............................................................................................................................................5 IC and RFIC Systems ................................................................................................................................................................6 MS Instruments .........................................................................................................................................................................7 Chromeleon 7 Chromatography Data System Software ..........................................................................................................8 Process Analytical Systems and Software ................................................................................................................................9 Automated Sample Preparation ..............................................................................................................................................10 Analysis of Antibiotics ...........................................................................................................................................................11
    [Show full text]
  • G Genito Urinary System and Sex Hormones
    WHO/EMP/RHT/TSN/2018.2 © World Health Organization 2018 Some rights reserved. This work is available under the Creative Commons Attribution-NonCommercial-ShareAlike 3.0 IGO licence (CC BY-NC-SA 3.0 IGO; https://creativecommons.org/licenses/by-nc-sa/3.0/igo). Under the terms of this licence, you may copy, redistribute and adapt the work for non-commercial purposes, provided the work is appropriately cited, as indicated below. In any use of this work, there should be no suggestion that WHO endorses any specific organization, products or services. The use of the WHO logo is not permitted. If you adapt the work, then you must license your work under the same or equivalent Creative Commons licence. If you create a translation of this work, you should add the following disclaimer along with the suggested citation: “This translation was not created by the World Health Organization (WHO). WHO is not responsible for the content or accuracy of this translation. The original English edition shall be the binding and authentic edition”. Any mediation relating to disputes arising under the licence shall be conducted in accordance with the mediation rules of the World Intellectual Property Organization. Suggested citation. Learning clinical pharmacology with the use of INNs and their stems. Geneva: World Health Organization; 2018 (WHO/EMP/RHT/TSN/2018.2). Licence: CC BY-NC-SA 3.0 IGO. Cataloguing-in-Publication (CIP) data. CIP data are available at http://apps.who.int/iris. Sales, rights and licensing. To purchase WHO publications, see http://apps.who.int/bookorders. To submit requests for commercial use and queries on rights and licensing, see http://www.who.int/about/licensing.
    [Show full text]
  • P147-Bioorgchem-Kanamycin Nucleotidyltransferase-1999.Pdf
    Bioorganic Chemistry 27, 395±408 (1999) Article ID bioo.1999.1144, available online at http://www.idealibrary.com on Kinetic Mechanism of Kanamycin Nucleotidyltransferase from Staphylococcus aureus1 Misty Chen-Goodspeed,* Janeen L. Vanhooke,² Hazel M. Holden,² and Frank M. Raushel*,2 *Department of Chemistry, Texas A&M University, College Station, Texas 77843; and ²Department of Biochemistry, Institute for Enzyme Research, University of Wisconsin, Madison, Wisconsin 53705 Received December 16, 1998 Kanamycin nucleotidyltransferase (KNTase) catalyzes the transfer of the adenyl group from MgATP to either the 4Ј or 4Љ-hydroxyl group of aminoglycoside antibiotics. The steady state kinetic parameters of the enzymatic reaction have been measured by initial velocity, product, and dead-end inhibition techniques. The kinetic mechanism is ordered where the antibiotic binds prior to MgATP and the modified antibiotic is the last product to be released. The effects of altering the relative solvent viscosity are consistent with the release of the products as the rate-limiting step. The pH profiles for Vmax and V/KATP show that a single ionizable group with apK of ϳ8.9 must be protonated for catalysis. The V/K profile for kanamycin as a function of pH is bell-shaped and indicates that one group must be protonated with a pK value of 8.5, while another group must be unprotonated with a pK value of 6.6. An analysis of the kinetic constants for 10 different aminoglycoside antibiotics and 5 nucleotide triphosphates indicates very little difference in the rate of catalysis or substrate binding among these substrates. ᭧ 1999 Academic Press Key Words: kanamycin nucleotidyltransferase; antibiotic modification.
    [Show full text]
  • Para-Aminosalicylic Acid – Biopharmaceutical, Pharmacological
    Para-aminosalicylic acid – biopharmaceutical, pharmacological... PHARMACIA, vol. 62, No. 1/2015 25 PARA-AMINOSALICYLIC ACID – BIOPHARMACEUTICAL, PHARMACO- LOGICAL, AND CLINICAL FEATURES AND RESURGENCE AS AN ANTI- TUBERCULOUS AGENT G. Momekov*, D. Momekova, G. Stavrakov, Y. Voynikov, P. Peikov Faculty of Pharmacy, Medical University of Sofia, 2 Dunav Str., 1000 Sofia, Bulgaria Summary: Para-aminosalicylic acid (INN aminosalicylic acid; PAS) is a bacteriostatic chemo- therapeutic agent used in the therapy of all forms of tuberculosis, both pulmonary and extrapul- monary, caused by sensitive strains of the mycobacteria resistant to other antituberculotics or if the patient is intolerant towards other drugs. Since its clinical introduction in the late 1940s aminosalicylic acid (PAS) has been a mainstay in the treatment of TB into the 1960s. Along with isoniazid and streptomycin, it was a ‘first-line’ agent for tuberculosis. However, it was plagued by poor gastro-intestinal tolerance and rare but severe allergic reactions. Ethambutol was later shown to be approximately equivalent to PAS in potency, and generally better tolerated than PAS when ethambutol was used at dosages of 25 mg/kg/day or less. Therefore, PAS was replaced by etham- butol as a primary TB drug. However, because of the relative lack of use of PAS over the past 3 decades, most isolates of TB remain susceptible to it. Thus, PAS has experienced a renaissance in the management of patients with multi-drug resistant tuberculosis. Key words: Aminosalicylic acid, Antituberculous agents, MDR-TB, XDR-TB Introduction of treatment the cure rate improved up to 90%. The In 1943 the Swedish chemist Jörgen Lehmann combination of both drugs reduced the selection of (1898-1989) addressed a letter to the managers of resistant strains tremendously [3].
    [Show full text]