Antibiotics for Research
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The Diverse Search for Synthetic, Semisynthetic and Natural Product Antibiotics from the 1940S and up to 1960 Exemplified by a Small Pharmaceutical Player
The Diverse Search for Synthetic, Semisynthetic and Natural Product Antibiotics From the 1940s and Up to 1960 Exemplified by a Small Pharmaceutical Player Leisner, Jørgen J. Published in: Frontiers in Microbiology DOI: 10.3389/fmicb.2020.00976 Publication date: 2020 Document version Publisher's PDF, also known as Version of record Document license: CC BY Citation for published version (APA): Leisner, J. J. (2020). The Diverse Search for Synthetic, Semisynthetic and Natural Product Antibiotics From the 1940s and Up to 1960 Exemplified by a Small Pharmaceutical Player. Frontiers in Microbiology, 11, [976]. https://doi.org/10.3389/fmicb.2020.00976 Download date: 29. Sep. 2021 fmicb-11-00976 June 10, 2020 Time: 21:55 # 1 REVIEW published: 12 June 2020 doi: 10.3389/fmicb.2020.00976 The Diverse Search for Synthetic, Semisynthetic and Natural Product Antibiotics From the 1940s and Up to 1960 Exemplified by a Small Pharmaceutical Player Jørgen J. Leisner* Department of Veterinary and Animal Sciences, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen, Denmark The 1940s and 1950s witnessed a diverse search for not just natural product antibiotics but also for synthetic and semisynthetic compounds. This review revisits this epoch, using the research by a Danish pharmaceutical company, LEO Pharma, as an example. LEO adopted a strategy searching for synthetic antibiotics toward specific bacterial Edited by: Rustam Aminov, pathogens, in particular Mycobacterium tuberculosis, leading to the discovery of a University of Aberdeen, new derivative of a known drug. Work on penicillin during and after WWII lead to the United Kingdom development of associated salts/esters and a search for new natural product antibiotics. -
Data on Before and After the Traceability System of Veterinary Antimicrobial Prescriptions in Small Animals at the University Veterinary Teaching Hospital of Naples
animals Article Data on before and after the Traceability System of Veterinary Antimicrobial Prescriptions in Small Animals at the University Veterinary Teaching Hospital of Naples Claudia Chirollo , Francesca Paola Nocera , Diego Piantedosi, Gerardo Fatone , Giovanni Della Valle, Luisa De Martino * and Laura Cortese Department of Veterinary Medicine and Animal Productions, University of Naples, “Federico II”, Via Delpino 1, 80137 Naples, Italy; [email protected] (C.C.); [email protected] (F.P.N.); [email protected] (D.P.); [email protected] (G.F.); [email protected] (G.D.V.); [email protected] (L.C.) * Correspondence: [email protected]; Tel.: +39-081-253-6180 Simple Summary: Veterinary electronic prescription (VEP) is mandatory by law, dated 20 November 2017, No. 167 (European Law 2017) Article 3, and has been implemented in Italy since April 2019. In this study, the consumption of antimicrobials before and after the mandatory use of VEP was analyzed at the Italian University Veterinary Teaching Hospital of Naples in order to understand how the traceability of antimicrobials influences veterinary prescriptions. The applicability and utility of VEP may present an effective surveillance strategy able to limit both the improper use of Citation: Chirollo, C.; Nocera, F.P.; antimicrobials and the spread of multidrug-resistant pathogens, which have become a worrying Piantedosi, D.; Fatone, G.; Della Valle, threat both in veterinary and human medicine. G.; De Martino, L.; Cortese, L. Data on before and after the Traceability Abstract: Over recent decades, antimicrobial resistance has been considered one of the most relevant System of Veterinary Antimicrobial issues of public health. -
Neomycin and Polymyxin B Sulfates Solution for Irrigation, USP Rx Only
NEOMYCIN AND POLYMYXIN B SULFATES- neomycin and polymyxin b sulfates solution X-GEN Pharmaceuticals, Inc. ---------- Neomycin and Polymyxin B Sulfates Solution for Irrigation, USP Rx Only NOT FOR INJECTION DESCRIPTION Neomycin and Polymyxin B Sulfates Solution for Irrigation is a concentrated sterile antibiotic solution to be diluted for urinary bladder irrigation. Each mL contains neomycin sulfate equivalent to 40 mg neomycin base, 200,000 units polymyxin B sulfate, and Water for Injection, inactive ingredient: sulfuric acid. The 20-mL multiple dose vial contains, in addition to the above, 1 mg methylparaben (0.1%) added as a preservative. Neomycin sulfate, an antibiotic of the aminoglycoside group, is the sulfate salt of neomycin B and C produced by Streptomyces fradiae It has a potency equivalent to not less than 600 mcg of neomycin per mg. The structural formulae are: Polymyxin B sulfate, a polypeptide antibiotic, is the sulfate salt of polymyxin B1 and B2 produced by the growth of Bacillus polymyxa. It has a potency of not less than 6,000 polymyxin B units per mg. The structural formulae are: CLINICAL PHARMACOLOGY After prophylactic irrigation of the intact urinary bladder, neomycin and polymyxin B are absorbed in clinically insignificant quantities. A neomycin serum level of 0.1 mcg/mL was observed in three of 33 patients receiving the rinse solution. This level is well below that which has been associated with neomycin-induced toxicity. When used topically, polymyxin B sulfate and neomycin are rarely irritating. Microbiology: The prepared Neomycin and Polymyxin B Sulfates Solution for Irrigation is bactericidal. The aminoglycosides act by inhibiting normal protein synthesis in susceptible microorganisms. -
Antibiotic Use Guidelines for Companion Animal Practice (2Nd Edition) Iii
ii Antibiotic Use Guidelines for Companion Animal Practice (2nd edition) iii Antibiotic Use Guidelines for Companion Animal Practice, 2nd edition Publisher: Companion Animal Group, Danish Veterinary Association, Peter Bangs Vej 30, 2000 Frederiksberg Authors of the guidelines: Lisbeth Rem Jessen (University of Copenhagen) Peter Damborg (University of Copenhagen) Anette Spohr (Evidensia Faxe Animal Hospital) Sandra Goericke-Pesch (University of Veterinary Medicine, Hannover) Rebecca Langhorn (University of Copenhagen) Geoffrey Houser (University of Copenhagen) Jakob Willesen (University of Copenhagen) Mette Schjærff (University of Copenhagen) Thomas Eriksen (University of Copenhagen) Tina Møller Sørensen (University of Copenhagen) Vibeke Frøkjær Jensen (DTU-VET) Flemming Obling (Greve) Luca Guardabassi (University of Copenhagen) Reproduction of extracts from these guidelines is only permitted in accordance with the agreement between the Ministry of Education and Copy-Dan. Danish copyright law restricts all other use without written permission of the publisher. Exception is granted for short excerpts for review purposes. iv Foreword The first edition of the Antibiotic Use Guidelines for Companion Animal Practice was published in autumn of 2012. The aim of the guidelines was to prevent increased antibiotic resistance. A questionnaire circulated to Danish veterinarians in 2015 (Jessen et al., DVT 10, 2016) indicated that the guidelines were well received, and particularly that active users had followed the recommendations. Despite a positive reception and the results of this survey, the actual quantity of antibiotics used is probably a better indicator of the effect of the first guidelines. Chapter two of these updated guidelines therefore details the pattern of developments in antibiotic use, as reported in DANMAP 2016 (www.danmap.org). -
Comparative Activity of Newer Antibiotics Against Gram-Negative Bacilli
CONTRIBUTION • Comparative activity of newer antibiotics against gram-negative bacilli CYNTHIA C. KNAPP, MS AND JOHN A. WASHINGTON, MD • The in vitro activities of cefoperazone, cefotaxime, ceftriaxone, ceftazidime, azlocillin, mezlocillin, piperacillin, ticarcillin/clavulanate, aztreonam, imipenem, and ciprofloxacin were concurrently deter- mined against over 1,000 isolates of gram-negative bacilli from clinical specimens of patients at the Cleve- land Clinic. Cephalosporins, penicillins, and aztreonam were active against species of Enterobacteriaceae other than Citrobacter freundii, Enterobacter aerogenes, and Enterobacter cloacae. Ceftazidime was the most active cephalosporin against Pseudomonas aeruginosa. Against the Enterobacteriaceae, the rank order of activity of penicillins was ticarcillin/clavulanate > piperacillin > mezlocillin > azlocillin. Against P. aer- uginosa, the rank order of activity of penicillins was piperacillin > ticarcillin/clavulanate > azlocillin > mezlocillin. Aztreonam was less active v P. aeruginosa than ceftazidime, cefoperazone, or piperacillin. The most active antimicrobials against all isolates tested were imipenem and ciprofloxacin. • INDEX TERMS: ANTIBIOTICS, LACTAM; GRAM-NEGATIVE BACTERIA • CLEVE CLIN J MED 1989; 56:161-166 HE RECENT introduction of ciprofloxacin for and penicillins, as well as the monobactam, aztreonam, clinical use follows closely a period of active re- and the carbapenem, imipenem.1-3 search in and development of expanded spec- We compared the susceptibility of more than 1,000 trum p-lactam antibiotics, including cephalo- clinical bacterial isolates to four expanded spectrum Tsporins, penicillins, monobactams, and carbapenems. cephalosporins (cefoperazone, cefotaxime, ceftriaxone, Although numerous published studies compare the ac- and ceftazidime), four expanded spectrum penicillins tivity of ciprofloxacin with other quinolones, only a (azlocillin, mezlocillin, piperacillin, and ticarcil- limited number of studies compare the activity of ci- lin/clavulanate), aztreonam, imipenem, and ciproflox- acin. -
Treatment of Extended-Spectrum Β-Lactamase
F1000Research 2018, 7(F1000 Faculty Rev):1347 Last updated: 17 JUL 2019 REVIEW Treatment of extended-spectrum β-lactamase-producing Enterobacteriaceae (ESBLs) infections: what have we learned until now? [version 1; peer review: 2 approved] Zoi Dorothea Pana1, Theoklis Zaoutis 2 1Infectious Diseases Department, 3rd Department of Pediatrics, Hippokration General Hospital Aristotle University, Thessaloniki, Greece 2Infectious Diseases Department, The Children’s Hospital of Philadelphia, Perelman School of Medicine at the University of Pennsylvania, Philadelphia, PA, USA First published: 29 Aug 2018, 7(F1000 Faculty Rev):1347 ( Open Peer Review v1 https://doi.org/10.12688/f1000research.14822.1) Latest published: 29 Aug 2018, 7(F1000 Faculty Rev):1347 ( https://doi.org/10.12688/f1000research.14822.1) Reviewer Status Abstract Invited Reviewers The spread of extended-spectrum β-lactamase (ESBL)-producing 1 2 Enterobacteriaceae (ESBL-PE) has dramatically increased worldwide, and this “evolving crisis” is currently regarded as one of the most important version 1 public health threats. The growing problem of ESBL-PE antimicrobial published resistance seems to have a dual face between “Scylla and Charybdis”: on 29 Aug 2018 one hand the potential for rapid spread and dissemination of resistance mechanisms and on the other hand the injudicious overuse of antimicrobial agents and the inadequate infection control measures, especially in the F1000 Faculty Reviews are written by members of health-care setting. Given the World Health Organization’s warning against the prestigious F1000 Faculty. They are a “post antibiotic era”, health-care providers are at a critical standpoint to commissioned and are peer reviewed before find a “balance” between safe and effective ESBL-PE treatment and publication to ensure that the final, published version avoidance of inducing further resistance mechanisms. -
Third ESVAC Report
Sales of veterinary antimicrobial agents in 25 EU/EEA countries in 2011 Third ESVAC report An agency of the European Union The mission of the European Medicines Agency is to foster scientific excellence in the evaluation and supervision of medicines, for the benefit of public and animal health. Legal role Guiding principles The European Medicines Agency is the European Union • We are strongly committed to public and animal (EU) body responsible for coordinating the existing health. scientific resources put at its disposal by Member States • We make independent recommendations based on for the evaluation, supervision and pharmacovigilance scientific evidence, using state-of-the-art knowledge of medicinal products. and expertise in our field. • We support research and innovation to stimulate the The Agency provides the Member States and the development of better medicines. institutions of the EU the best-possible scientific advice on any question relating to the evaluation of the quality, • We value the contribution of our partners and stake- safety and efficacy of medicinal products for human or holders to our work. veterinary use referred to it in accordance with the • We assure continual improvement of our processes provisions of EU legislation relating to medicinal prod- and procedures, in accordance with recognised quality ucts. standards. • We adhere to high standards of professional and Principal activities personal integrity. Working with the Member States and the European • We communicate in an open, transparent manner Commission as partners in a European medicines with all of our partners, stakeholders and colleagues. network, the European Medicines Agency: • We promote the well-being, motivation and ongoing professional development of every member of the • provides independent, science-based recommenda- Agency. -
(3H) Tobramycin Was Synthesized As Described Previously3) and Had a Specific Radioac- Tivity of 5,000 Ci/Mole
VOL. XXXIII NO. 8 THE JOURNAL OF ANTIBIOTICS 895 HAVE DEOXYSTREPTAMINE AMINOGLYCOSIDE ANTIBIOTICS THE SAME BINDING SITE ON BACTERIAL RIBOSOMES ? FRANCOIS LE GOFFIC, MARIE-LOUISE CAPMAU, EREDERIC TANGY and ELIANE CAMINADE C.N.R.S.-C.E.R.C.O.A. 2 a 8, rue Henry Dunant, 94320 Thiais, France (Received for Publication January 22, 1980) (3H) Tobramycin was used as a probe to determine the relationship between the structure of aminoglycoside antibiotics and their ability to remove this drug from its higher affinity bind- ing site on the ribosome. The dissacharide moieties (neamine, tobramine, gentamine) appeared to have a common binding site, whereas the kanosamine, garosamine and ribose moieties determined the specificity of this binding. Amikacin and butikacin behaved in an anomalous manner in spite of their close structural relationship to tobramycin. Biochemical experiments have recently demonstrated that those aminoglycoside antibiotics with deoxystreptamine and kanosamine moieties possess two types of binding sites on the bacterial ribo- some.1,2) When the binding experiments were carried out with the ribosomal subunits two types of binding sites were also found on the 50 S subunit whereas only one type of binding site was located on the 30 S particle.3) The question then arises as to whether all aminoglycoside antibiotics possessing a deoxystreptamine moiety glycosidically bound to other aminosugar residues have the same receptor site. The present study tries to answer this important question. Materials and Methods Chemicals: (3H) Tobramycin was synthesized as described previously3) and had a specific radioac- tivity of 5,000 Ci/mole. Putrescine and spermidine were from Sigma. -
Chemistry Classification Pharmacokinetics Clinical Uses And
Available online www.jocpr.com Journal of Chemical and Pharmaceutical Research, 2014, 6(11):28-58 ISSN : 0975-7384 Review Article CODEN(USA) : JCPRC5 Chemistry, classification, pharmacokinetics, clinical uses and analysis of beta lactam antibiotics: A review Mamdouh S. Masoud a, Alaa E. Ali b* and Nessma M. Nasr c aChemistry Department, Faculty of Science, Alexandria University, Alexandria, Egypt bChemistry Department, Faculty of Science, Damanhour University, Damanhour, Egypt cStudents’ Hospital, Alexandria University, Alexandria, Egypt _____________________________________________________________________________________________ ABSTRACT This review attempts to pinpoint the importance of betalactam antibiotics, which encompass penicillins, cephalosporins, cephamycins, carbapenems and monobactams from its chemistry, classification, pharmacokinetics, clinical uses and analysis. β- lactam antibiotics have been used for treatment of bacterial infections. Most antibacterials are chemically semisynthetic modifications of various natural compounds and classified on the basis of chemical /biosynthetic origin into natural, semisynthetic, and synthetic. Also, this classification system is based on biological activity; that antibacterials are divided into two broad groups according to their biological effect on microorganisms, bactericidal agents kill bacteria, and bacteriostatic agents slow down bacterial growth. Keywords: Beta lactam Antibiotics, Classification, Pharmacokinetics, Clinical uses, Analysis. _____________________________________________________________________________________________ -
Treatment of Drug-Resistant Tuberculosis an Official ATS/CDC/ERS/IDSA Clinical Practice Guideline Payam Nahid, Sundari R
AMERICAN THORACIC SOCIETY DOCUMENTS Treatment of Drug-Resistant Tuberculosis An Official ATS/CDC/ERS/IDSA Clinical Practice Guideline Payam Nahid, Sundari R. Mase, Giovanni Battista Migliori, Giovanni Sotgiu, Graham H. Bothamley, Jan L. Brozek, Adithya Cattamanchi, J. Peter Cegielski, Lisa Chen, Charles L. Daley, Tracy L. Dalton, Raquel Duarte, Federica Fregonese, C. Robert Horsburgh, Jr., Faiz Ahmad Khan, Fayez Kheir, Zhiyi Lan, Alfred Lardizabal, Michael Lauzardo, Joan M. Mangan, Suzanne M. Marks, Lindsay McKenna, Dick Menzies, Carole D. Mitnick, Diana M. Nilsen, Farah Parvez, Charles A. Peloquin, Ann Raftery, H. Simon Schaaf, Neha S. Shah, Jeffrey R. Starke, John W. Wilson, Jonathan M. Wortham, Terence Chorba, and Barbara Seaworth; on behalf of the American Thoracic Society, U.S. Centers for Disease Control and Prevention, European Respiratory Society, and Infectious Diseases Society of America THIS OFFICIAL CLINICAL PRACTICE GUIDELINE WAS APPROVED BY THE AMERICAN THORACIC SOCIETY, THE EUROPEAN RESPIRATORY SOCIETY, AND THE INFECTIOUS DISEASES SOCIETY OF AMERICA SEPTEMBER 2019, AND WAS CLEARED BY THE U.S. CENTERS FOR DISEASE CONTROL AND PREVENTION SEPTEMBER 2019 Background: The American Thoracic Society, U.S. Centers for was judged to be very low, because the data came Disease Control and Prevention, European Respiratory Society, and from observational studies with significant loss to follow-up Infectious Diseases Society of America jointly sponsored this new and imbalance in background regimens between comparator practice guideline on the treatment of drug-resistant tuberculosis groups. Good practices in the management of MDR-TB are (DR-TB). The document includes recommendations on the described. On the basis of the evidence review, a clinical strategy treatment of multidrug-resistant TB (MDR-TB) as well as tool for building a treatment regimen for MDR-TB is also isoniazid-resistant but rifampin-susceptible TB. -
Review Article UDC: 615.281.015.8:616.9 Doi:10.5633/Amm.2019.0412
Review article UDC: 615.281.015.8:616.9 doi:10.5633/amm.2019.0412 THE IMPORTANCE OF OLD ANTIBIOTICS IN OVERCOMING RESISTANCE TO ANTIBIOTICS Zorica Jović1, Lidija Ristić2,3, Dane Krtinić1,4, Gorana Nedin-Ranković1, Ana Cvetanović4,5, Dušan Simić6 Antibiotics are medications used to prevent or cure infections caused by bacteria. Discovery and introduction of antibiotics into medical practice brought about revolutionary changes in therapy and eradication of infectious diseases. There is a rise of interest for usage of old antibiotics. These drugs could be invaluable in the treatment of certain infections and, in order for them to remain effective, it is necessary to conduct certain measures which would prove their worth. The aim of antibiotic therapy is to deliver the antibiotic to the place of infection and to retain it in the place of infection for a long period of time. Most of all, it is of utmost importance to educate about this all medical personnel in health care system, especially physicians. The fact that the availability of these drugs remains low in comparison to the efforts made in attempt of discovering new antibiotics, imposes the need for national regulatory agencies to get involved in regulating the usage of these drugs. Acta Medica Medianae 2019;58(4):80-84. Key words: antibiotics, resistance, infections 1University of Niš, Faculty of Medicine, Department of pletely different from contemporary industrially pro- Pharmacology and Toxicology, Niš, Serbia duced ones. Nevertheless, this does not diminish the 2 University of Niš, Faculty of Medicine, Department of Internal fact that certain herbal medicines which have anti- Medicine, Niš, Serbia 3Clinic of Pulmonary Diseases, Clinical center Niš, Niš, Serbia biotic properties were known to ancient Greeks and 4Clinic of Oncology, Clinical center Niš, Niš, Serbia Romans and that they constituted an important part 5University of Niš, Faculty of Medicine, Department of of their medical practices (1). -
Swedres-Svarm 2005
SVARM Swedish Veterinary Antimicrobial Resistance Monitoring Preface .............................................................................................4 Summary ..........................................................................................6 Sammanfattning................................................................................7 Use of antimicrobials (SVARM 2005) .................................................8 Resistance in zoonotic bacteria ......................................................13 Salmonella ..........................................................................................................13 Campylobacter ...................................................................................................16 Resistance in indicator bacteria ......................................................18 Escherichia coli ...................................................................................................18 Enterococcus .....................................................................................................22 Resistance in animal pathogens ......................................................32 Pig ......................................................................................................................32 Cattle ..................................................................................................................33 Horse ..................................................................................................................36 Dog