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    Antimicrobials PDF

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    Davis Kallan
    The document discusses several classes of antimicrobial agents including: 1. Lipopeptides like daptomycin that are bactericidal against gram-positive organisms. 2. Macrolides like erythromycin that bind to the 50S ribosome and are bacteriostatic or bactericidal depending on the agent. 3. Beta-lactam antibiotics like penicillins and cephalosporins that inhibit cell wall synthesis. Resistance can develop through beta-lactamases or altered penicillin-binding proteins.

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    Antimicrobials PDF

    Uploaded by

    Davis Kallan
    75 views1 page
    The document discusses several classes of antimicrobial agents including: 1. Lipopeptides like daptomycin that are bactericidal against gram-positive organisms. 2. Macrolides like erythromycin that bind to the 50S ribosome and are bacteriostatic or bactericidal depending on the agent. 3. Beta-lactam antibiotics like penicillins and cephalosporins that inhibit cell wall synthesis. Resistance can develop through beta-lactamases or altered penicillin-binding proteins.

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    The document discusses several classes of antimicrobial agents including: 1. Lipopeptides like daptomycin that are bactericidal against gram-positive organisms. 2. Macrolides like erythromycin that bind to the 50S ribosome and are bacteriostatic or bactericidal depending on the agent. 3. Beta-lactam antibiotics like penicillins and cephalosporins that inhibit cell wall synthesis. Resistance can develop through beta-lactamases or altered penicillin-binding proteins.

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    Attribution Non-Commercial (BY-NC)
    Download as PDF, TXT or read online from Scribd
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    75 views1 page

    Antimicrobials PDF

    Uploaded by

    Davis Kallan
    The document discusses several classes of antimicrobial agents including: 1. Lipopeptides like daptomycin that are bactericidal against gram-positive organisms. 2. Macrolides like erythromycin that bind to the 50S ribosome and are bacteriostatic or bactericidal depending on the agent. 3. Beta-lactam antibiotics like penicillins and cephalosporins that inhibit cell wall synthesis. Resistance can develop through beta-lactamases or altered penicillin-binding proteins.

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    Bind Bact Mem Depol - Inabil Syn Prot Bacteriocidal against Gram+ Org No Resistance Very New

    Daptomycin cyclic lipopeptide

    Lipopeptides

    Quinupristin Dalfopristin Combo

    Streptgramins

    PO Gram + Cocci Anaerobes Clindamycin Lincomycin

    Lincosamides

    4 Fused Cyclic Rings Bind to Ribosome Bacteria selective Growing teeth stained yellow Resistance due to Pump

    Tetracyclines

    Similar Axn Macrolides

    Erythromycin Clarithromycin Azithromycin Dirithromycin Telithromycin (mod ML)

    PO Bacteriostatic Bacteriocidal Respiratory Inf Bind 50S

    Macrolides

    Protein Synthesis Inhibitors

    Nephrotoxicity -most frequent -mild/rev Ototoxicity -perm AGonly used in serious inf

    Toxicity Vent Tachy if given H1-Ant Astemizole/Terfenadine Erythromycin Lots N&V Bacteriocidal at high conc Quinolones (nalidixic acid) Fluoroquinolones (ciprooxacin) Metronidazole - anaerobes Standard Penecillin NOT in Children/Preg Aminoglycosides Dihydrofolate reductase inhibitor Anti-staphylococcal Toxicity PennG = IV Penn V - PO Streptococci Meningococci Syphilis Resistant Degredation Methicillin*/Nafcillin IV Oxacillin, Cloxacillin, Dicloxacillin mecA gene Codes for PBP2a low aff B-L PBP2a takes over cell wall synthesis

    Inhibitors of DNA Synthesis


    Enter cells via O2 dep trans Anaerobes resistant Bind to 30S and prevent 50S Also misreading code Amino sugars by glycosidic bonds Bactericidal against aerobic Gram IV only Resistance Used with sulphamethoxazole Trimethoprim Axions

    H. INuenza, E. Coli, Salmonella/Shigella

    Methicillin Resistance Staphylococcal Inf

    Gentamicin Streptomycin Amikacin Neomycin

    Leprosy

    Only sulphone = Dapsone Bacteria must syn folate

    Antimicrobials
    Anti-folates
    Adverse Effects

    Low toxicity Diarrhoea seizures if intrathecal Allergic rxn 2% Peneillin metabolites

    Penicilins

    Aminopenicillins No Staph Yes Gram Amino Group Ampicillin (IV-PO) Amoxicillin (PO) Anti-pseudomonal penicillins

    Decreased Permeability Xenobiotic pump AG Mod E (Acetyl/Adenyl)

    Sulphonamides very allergenic

    10% cross rxn cephalosporins Nephrotoxicity

    Hepatotoxicity or Fever Similar to Pens Less allergy Rifam ind microsomal enzymes causing drug interaction Rifampicin Rifabutin

    Carboxypenicillins

    Carbenicillin Ticarcillin Piperacillin Azlocillin Mezlocillin

    Inhibitors RNA Synthesis


    2nd Gen

    Activity against H. Inuenza

    Cefaclor Cefamandole Cefonicid

    Ureidopenicillins Actions

    No Staph Yes Pseudomonas Aeruginosa Mimetic of Ala-Ala sub TP

    Tuberculosis treatment

    Respiratory tract Inf Cefmetazole Cefotetan Activity against Bacteroides fragilis Abdominal INf Leg ulcers

    Cell Wall Synthesis Inhibitors B-lactams

    Irr i TP prev cell wall llink Dec Sec lipotechtoic acid i autolysin Uninhibited autolysin

    Cephalosporin Incr Act Gram- CSF Enterobactericaceae H. inuenza Pseudomonas aeruginosa Cexime Cefpodoxime Ceftibuten Oral Extended Spectrum

    3rd Gen

    Ceotaxime Ceftizaxime Ceftriaxone Ceftazidime Cefepime

    1.5kDa glycopeptide Streptomyces orientalis

    Vancomycin

    Less activity GramNo act P. aeruginosa & S. aureus Enterobacteriaceae 1965 Resistant Staph Broadest spectrum activity Gram -/+ aerobic/anaerobic Carbapenems Imipenem Meropenem - Meningitis Anti-gram- activity increases and anti-staph act decreases from 1 - 3 generation 1st gen Polyinfection Resistance developing Active against staphylococci & e.coli cefodroxil cephazolin cephalexin

    Gram + infection

    Gram + Staph Aureus IV IM Less Toxic than Vanco

    Teicoplanin

    IV PO=GI infection

    Most often used for skin infection, surgical prophylaxis, and penicillin allergy Hydrolyses ring

    Glycopeptides
    Effective in MRSA Variable Resistance V Sensitivity to T VanB phen B-lactamases

    Specic Renal B-lactamas

    Inhib by Cilistatin Aztreonam Gram- aerobic rods Monobactam Non-allergenic

    Type I Chromosomal B-lactamase specic for cephalosporins Clavulante Sulbactam Tazobactam Inhibitors! No Anti-microbe activity

    VanD and VanE exist

    Ind Resistance low V Senitive to Teicoplanin

    VanC phen Resistance Enterococci (VRE) Glycopeptide resistance Mutations PBP Red Perm GramS. aureus VISA GISA Xenobiotic Pumps

    Used in Combo therapy Amoxicillin-clavulanate (po) Ampcillin-sulbactam (iv) Ticarcillin-clavulanate (iv) Piperacillin-tazobactam (iv)

    Do not inhibit cephalosporinase

    Inducible High Resistance V+T Van H = pyr to lac

    VanA phen Cephalosporins are resistant to B-lactamase

    VanA/B prod A-ala-lac NOT D-ala-alanine VanX hydorlyses D-ala-alanine

    Activate VanH,VanA/B,VanX

    Cell have VanR VanS Detect Vancomycin

    Vancomcin Resistance Genes

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