Fisher Bioreagents Antibiotics and Antimycotics Catalog
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Resistance to Paromomycinis Conferred by Rpsl Mutations
VOL.53 NO. 12, DEC.2000 THE JOURNAL OF ANTIBIOTICS pp.1424 - 1427 COMMUNICATIONS TO THE EDITOR Resistance to Paromomycinis Conferred by paromomycin at a frequency of 10 7 or 10 8, respectively. rpsL Mutations, Accompaniedby an Out of 77 randomly selected paromomycin resistant Enhanced Antibiotic Production in mutants, 4 strains, designated as KO-347-350, were found to produce actinorhodin in 7 to 10-fold greater amounts Streptomyces coelicolor A3 (2) than the parent strain (Table 1). In our previous studies10'11>14) we established that an antibiotic- Sir: overproducing characteristic frequently appears together Aminoglycoside antibiotics interfere with bacterial with the mutation within the rpsL gene. To address this protein synthesis by binding to the 3OS ribosomal relationship weexamined for the presence of mutations in subunit1>2). Their binding is known to stabilize the tRNA- rpsL. Strikingly, all antibiotic-overproducing mutants mRNAinteraction in the A-site by decreasing the tRNA (Class I) examined had rpsL mutations, resulting in the dissociation rates3). Eventually, aminoglycoside antibiotics alteration of amino acid residue 91 from proline to serine cause a decrease in translational accuracy and inhibit (Table 1). In contrast, another group of paromomycin translocation of the ribosome. Such detrimental effects of resistant mutant, (Class II; KO-351-356) which do not aminoglycoside antibiotics can be circumvented by overproduce antibiotic, was found to have no mutation mutations altering 16S rRNA4~6) or certain ribosomal within the rpsL gene. It should be pointed out that Class I proteins6^; these mutations have been found in either the mutants displayed a higher level of resistance to nucleotide 530 or 915 regions of 16S rRNAor in ribosomal paromomycin than that of Class II mutants (Table 1). -
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. -
A New Mutation in 16S Rrna Ofescherichia Coli
464-466 Nucleic Acids Research, 1995, Vol. 23, No. 3 Q-D/ 1995 Oxford University Press A new mutation in 16S rRNA of Escherichia coli conferring spectinomycin resistance Urban Johanson and Diarmaid Hughes* Department of Molecular Biology, Uppsala University, Biomedical Center, S-751 24 Uppsala, Sweden Received September 24, 1994; Revised and Accepted December 30, 1994 ABSTRACT 1067 1089 A -U We report a novel mutation, Cl 066U in 16S rRNA which was selected for resistance to spectinomycin, an U @- G4C antibiotic which inhibits ribosomal translocation. The U,A,C e- G,U,A minimal inhibitory concentration (MIC) of spectinomy- A cin determined for this mutant (15 pg/ml) is greater U U than with the wild-type plasmid (5 ig/ml) but lower than 1062 1194 with the well known C1192U mutation (>80 pg/ml). The Cl 066U mutation also increases the cells sensitivity to Figure 1. Secondary structure of the upper part of helix 34 of 16S rRNA in fusidic acid, another antibiotic which inhibits transla- Ecoli (24) with the novel C1066U mutation indicated by an open U. In tion at the translocation stage, whereas C1192U is addition, all other known SpcR mutations are shown. The mutations are A1191G,C, Gi 193A in C.reinhardtii chloroplast (25); G1064A (20), A1191C, unchanged relative to the wild type. We discuss why Cl 192U (26) inN.tabacum chloroplast; GI 193A (20) inN.undulata chloroplast the acquisition of resistance to one of these drugs is and C1192U (1), C1192U,G,A (19), G1064U,C,A, G1064U-C1192A, often associated with hypersensitivity to the other. -
Farrukh Javaid Malik
I Farrukh Javaid Malik THESIS PRESENTED TO OBTAIN THE GRADE OF DOCTOR OF THE UNIVERSITY OF BORDEAUX Doctoral School, SP2: Society, Politic, Public Health Specialization Pharmacoepidemiology and Pharmacovigilance By Farrukh Javaid Malik “Analysis of the medicines panorama in Pakistan – The case of antimicrobials: market offer width and consumption.” Under the direction of Prof. Dr. Albert FIGUERAS Defense Date: 28th November 2019 Members of Jury M. Francesco SALVO, Maître de conférences des universités – praticien hospitalier, President Université de Bordeaux M. Albert FIGUERAS, Professeur des universités – praticien hospitalier, Director Université Autonome de Barcelone Mme Antonia AGUSTI, Professeure, Vall dʹHebron University Hospital Referee Mme Montserrat BOSCH, Praticienne hospitalière, Vall dʹHebron University Hospital Referee II Abstract A country’s medicines market is an indicator of its healthcare system, the epidemiological profile, and the prevalent practices therein. It is not only the first logical step to study the characteristics of medicines authorized for marketing, but also a requisite to set up a pharmacovigilance system, thus promoting rational drug utilization. The three medicines market studies presented in the present document were conducted in Pakistan with the aim of describing the characteristics of the pharmaceutical products available in the country as well as their consumption at a national level, with a special focus on antimicrobials. The most important cause of antimicrobial resistance is the inappropriate consumption of antimicrobials. The results of the researches conducted in Pakistan showed some market deficiencies which could be addressed as part of the national antimicrobial stewardship programmes. III Résumé Le marché du médicament d’un pays est un indicateur de son système de santé, de son profil épidémiologique et des pratiques [de prescription] qui y règnent. -
Streptomycin Sulfate PRODUCT DATA SHEET Issue Date 01/06/2020
Streptomycin Sulfate PRODUCT DATA SHEET issue date 01/06/2020 Product Name: Streptomycin Sulfate Product Number: S008 CAS Number: 3810-74-0 Molecular Formula: C21H39N7O12 · 1.5H 2SO4 Molecular Weight: 728.69 Form: Powder Appearance: A white or almost white powder Solubility: Acetone: Soluble Chloroform: Soluble Water: >20 mg/mL Source: Streptomyces Griseus pH: 4.5 - 7.0 Storage Conditions: 28°C Description: Streptomycin sulfate is a freely soluble aminocyclitol glycoside antibiotic, that was co-discovered by Salman Waksman, Albert Schatz, and Elizabeth Bugie at the Rutgers University in 1943 and was later patented in 1948. Streptomycin is isolated from Streptomyces griseus and shows bacteriostatic activity at low concentrations and bactericidal activity at higher concentrations against mycobacteria and gram-negative bacteria. It is less active against gram-positive bacteria. Streptomycin sulfate has been found to be effective against certain βlactam sensitive VRE or vancomycin resistant Enterococcus species; a glycopeptide antibiotic resistant "superbug”. Streptomycin sulfate is often used together with penicillin and other agents to inhibit bacterial contamination in cell culture applications. It is recommended for use in molecular biology applications at 2550μg/mL, in cell culture applications at 100 mg/L and in embryo culture at 50 mg/L. Streptomycin is a protein synthesis inhibitor that acts by binding to the 30S ribosomal subunit at the S12 protein thereby inducing a misreading of the genetic code, inhibiting the initiation of translation of DNA, which then results in death for a susceptible bacterium. Streptomycin has also shown activity as a miRNA inhibitor, that is capable of down-regulating miR-21, a miRNA that is overexpressed in a wide variety of cancers. -
Neomycin—Production and Antibiotic Properties
NEOMYCIN—PRODUCTION AND ANTIBIOTIC PROPERTIES Selman A. Waksman, … , Hubert A. Lechevalier, Dale A. Harris J Clin Invest. 1949;28(5):934-939. https://doi.org/10.1172/JCI102182. Research Article Find the latest version: https://jci.me/102182/pdf NEOMYCIN-PRODUCTION AND ANTIBIOTIC PROPERTIES 1, 2 3 By SELMAN A. WAKSMAN, HUBERT A. LECHEVALIER, AND DALE A. HARRIS (From the Department of Microbiology, New Jersey Agricultural Experiment Station, Rutgers University, New Brunswick, N. J.) ANTIBIOTIC SURVEYS All these cultures proved to be highly active against mycobacteria. of During the last 10 years, a large number anti- Only few of the cultures, however, that gave biotics which are active against Gram-negative good activity by the agar-streak method yielded and Gram-positive bacteria, mycobacteria, rickett- filtrates which possessed corresponding potency. siae, and certain of the larger viruses were iso- This may be due to a variety of factors, such as lated (1) from various species and strains of the the formation by a single organism of more than genus Streptomyces. This served to focus atten- one antibiotic or the production of different anti- tion on the actinomycetes as potential producers of biotics under different conditions of culture. One antimicrobial agents that might possess promising of these cultures proved to be highly promising chemotherapeutic properties. The fact that nearly and was selected for more detailed investigations. 20 to 50%o of these organisms possess antimicrobial This culture was entered into the Collection as No. activities served to heighten this interest. Numer- 3535. The nature of its antimicrobial spectrum, ous surveys have been conducted. -
(ESVAC) Web-Based Sales and Animal Population
16 July 2019 EMA/210691/2015-Rev.2 Veterinary Medicines Division European Surveillance of Veterinary Antimicrobial Consumption (ESVAC) Sales Data and Animal Population Data Collection Protocol (version 3) Superseded by a new version Superseded Official address Domenico Scarlattilaan 6 ● 1083 HS Amsterdam ● The Netherlands Address for visits and deliveries Refer to www.ema.europa.eu/how-to-find-us Send us a question Go to www.ema.europa.eu/contact Telephone +31 (0)88 781 6000 An agency of the European Union © European Medicines Agency, 2021. Reproduction is authorised provided the source is acknowledged. Table of content 1. Introduction ....................................................................................................................... 3 1.1. Terms of reference ........................................................................................................... 3 1.2. Approach ........................................................................................................................ 3 1.3. Target groups of the protocol and templates ......................................................................... 4 1.4. Organization of the ESVAC project ...................................................................................... 4 1.5. Web based delivery of data ................................................................................................ 5 2. ESVAC sales data ............................................................................................................... 5 2.1. -
MACROLIDES (Veterinary—Systemic)
MACROLIDES (Veterinary—Systemic) This monograph includes information on the following: Category: Antibacterial (systemic). Azithromycin; Clarithromycin; Erythromycin; Tilmicosin; Tulathromycin; Tylosin. Indications ELUS EL Some commonly used brand names are: For veterinary-labeled Note: The text between and describes uses that are not included ELCAN EL products— in U.S. product labeling. Text between and describes uses Draxxin [Tulathromycin] Pulmotil Premix that are not included in Canadian product labeling. [Tilmicosin Phosphate] The ELUS or ELCAN designation can signify a lack of product Erythro-200 [Erythromycin Tylan 10 [Tylosin availability in the country indicated. See the Dosage Forms Base] Phosphate] section of this monograph to confirm availability. Erythro-Med Tylan 40 [Tylosin [Erythromycin Phosphate] General considerations Phosphate] Macrolides are considered bacteriostatic at therapeutic concentrations Gallimycin [Erythromycin Tylan 50 [Tylosin Base] but they can be slowly bactericidal, especially against Phosphate] streptococcal bacteria; their bactericidal action is described as Gallimycin-50 Tylan 100 [Tylosin time-dependent. The antimicrobial action of some macrolides is [Erythromycin Phosphate] enhanced by a high pH and suppressed by low pH, making them Thiocyanate] less effective in abscesses, necrotic tissue, or acidic urine.{R-119} Gallimycin-100 Tylan 200 [Tylosin Base] Erythromycin is an antibiotic with activity primarily against gram- [Erythromycin Base] positive bacteria, such as Staphylococcus and Streptococcus Gallimycin-100P Tylan Soluble [Tylosin species, including many that are resistant to penicillins by means [Erythromycin Tartrate] of beta-lactamase production. Erythromycin is also active against Thiocyanate] mycoplasma and some gram-negative bacteria, including Gallimycin-200 Tylosin 10 Premix [Tylosin Campylobacter and Pasteurella species.{R-1; 10-12} It has activity [Erythromycin Base] Phosphate] against some anaerobes, but Bacteroides fragilis is usually Gallimycin PFC Tylosin 40 Premix [Tylosin resistant. -
ARK™ Linezolid Assay
1 NAME ARK™ Linezolid Assay 2 INTENDED USE The ARK Linezolid Assay is a homogeneous enzyme immunoassay intended for the quantitative For Export Only – Not For Sale in USA determination of linezolid in human serum on automated clinical chemistry analyzers. The measurements obtained are used in monitoring levels of linezolid to help ensure appropriate therapy. ™ ARK Linezolid Assay 3 SUMMARY AND EXPLANATION OF THE TEST This ARK Diagnostics, Inc. package insert for the ARK Linezolid Assay must be read carefully Linezolid (ZYVOX®, Pfizer, Inc.) [(S)-N-[[3-[3-Fluoro-4-(4-morpholinyl)phenyl]-2-oxo- prior to use. Package insert instructions must be followed accordingly. Reliability of the assay 5-oxazolidinyl] methyl]-acetamide] is an oxazolidinone derivative with a predominantly results cannot be guaranteed if there are any deviations from the instructions in this package bacteriostatic effect against severe infections caused by methicillin- or vancomycin-resistant insert. The ARK Linezolid Assay test system includes separately provided test kits for the ARK Gram-positive bacteria.1 Linezolid Assay, ARK Linezolid Calibrator and ARK Linezolid Control. ZYVOX is indicated in adults and children for the treatment of the following infections caused by susceptible Gram-positive bacteria: Nosocomial pneumonia; Community-acquired pneumonia; Complicated skin and skin structure infections, including diabetic foot infections, without concomitant osteomyelitis; Uncomplicated skin and skin structure infections; Vancomycin- CUSTOMER SERVICE resistant Enterococcus faecium infections.2 ARK Diagnostics, Inc. C 4 PRINCIPLES OF THE PROCEDURE 48089 Fremont Blvd Emergo Europe The ARK Linezolid Assay is a homogeneous immunoassay based on competition between drug in the specimen and linezolid labeled with recombinant enzyme glucose-6-phosphate Fremont, CA 94538 USA Prinsessegracht 20 dehydrogenase (rG6PDH) for binding to the antibody reagent. -
SEPSIS AMINOGLYCOSIDES Examples: Streptomycin, Gentamicin
SEPSIS AMINOGLYCOSIDES Examples: streptomycin, gentamicin, tobramycin Mechanism of action A bactericidal group of drugs which inhibit bacterial protein synthesis by irreversibly binding bacterial ribosomes. They require entry to Gram negative bacterial cells through outer cell membrane (via porins) and inner cytoplasmic membrane (an oxygen-dependent system) in order to exert their effect. They have difficulty penetrating Gram positive cell walls. They are therefore effective against Gram negative aerobic bacteria but not against anaerobic gram negative bacteria whose cell wall/membranes the antibiotic cannot penetrate. They have limited application against Gram positive bacteria. Synergistic with penicillins - cell wall synthesis inhibitors increase the permeability of the cell wall to aminoglycosides. They do not cross the blood brain barrier and have low concentrations in many tissues. They reach high concentrations in the inner ears and kidneys. Adverse Effects Ototoxicity - accumulates in the endolymph and perilymph of the inner ear causing deafness, tinnitus and vertigo. Increased risk with co-use of loop diuretics and cisplatin. Nephrotoxicity - retention of aminoglycosides by proximal tubular cells disrupts calcium- mediated transport processes resulting in nephrotoxicity. This ranges from mild, reversible renal impairment to severe, irreversible acute tubular necrosis. Dose, frequency and duration of therapy determine the extent of nephrotoxicity. Other adverse effects - allergy, neuromuscular blockade. They cross the placenta and may cause congenital deafness. Gentamicin Prescribing Where possible prescribe gentamicin using the Gentamicin calculator. If critically ill and gentamicin is needed prescribe 5mg/kg actual body weight (max 400mg). If critically ill and known CKD stage V give 2.5mg/kg (max 180mg). Always prescribe gentamicin on the Gentamicin prescription chart. -
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. -
Sales of Veterinary Antimicrobial Agents in 19 EU/EEA Countries in 2010
Sales of veterinary antimicrobial agents in 19 EU/EEA countries in 2010 Second 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 • We are strongly committed to public and animal Union (EU) body responsible for coordinating the health. existing scientific resources put at its disposal by • We make independent recommendations based on Member States for the evaluation, supervision and scientific evidence, using state-of-the-art knowl- pharmacovigilance of medicinal products. edge and expertise in our field. • We support research and innovation to stimulate The Agency provides the Member States and the the development of better medicines. institutions of the EU the best-possible scientific advice on any question relating to the evaluation of • We value the contribution of our partners and the quality, safety and efficacy of medicinal products stakeholders to our work. for human or veterinary use referred to it in accord • We assure continual improvement of our processes ance with the provisions of EU legislation relating to and procedures, in accordance with recognised medicinal products. quality 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 colleag network, the European Medicines Agency: ues. • We promote the wellbeing, motivation and • provides independent, sciencebased recommen ongoing professional development of every dations on the quality, safety and efficacy of member of the Agency.