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    Antimicrobial Drugs

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    rolandagyei65

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    © All Rights Reserved
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    Antimicrobial Drugs

    Uploaded by

    rolandagyei65
    3 views43 pages

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    3 views43 pages

    Antimicrobial Drugs

    Uploaded by

    rolandagyei65

    Copyright:

    © All Rights Reserved
    Download as PDF, TXT or read online from Scribd
    Download as pdf or txt
    of 43

    Antimicrobial Drugs

    Chemotherapy
    • The use of drugs to treat a disease

    • Selective toxicity: A drug that kills harmful


    microbes without damaging the host
    Antibiotic/Antimicrobial
    • Antibiotic: Chemical produced by a microorganism
    that kills or inhibits the growth of another
    microorganism
    • Antimicrobial agent: Chemical that kills or inhibits
    the growth of microorganisms
    Microbial
    Sources of
    Antibiotics
    Antibiotic Spectrum of Activity

    • No antibiotic is effective against all microbes


    Mechanisms of Antimicrobial Action

    • Bacteria have their own enzymes for


    • Cell wall formation
    • Protein synthesis
    • DNA replication
    • RNA synthesis
    • Synthesis of essential metabolites
    Mechanisms of Antimicrobial Action

    • Viruses use host enzymes inside host cells


    • Fungi and protozoa have own eukaryotic
    enzymes

    • The more similar the pathogen and host


    enzymes, the more side effects the
    antimicrobials will have
    Modes of Antimicrobial Action
    Antibacterial Antibiotics
    Inhibitors of Cell Wall Synthesis
    • Penicillin (over 50 compounds)
    • Share 4-sided ring (b lactam ring)
    • Natural penicillins
    • Narrow range of action
    • Susceptible to penicillinase (b lactamase)
    Prokaryotic Cell Walls

    Gram +ve
    Gram -ve
    Penicillins
    Penicillinase (b Lactamase)
    Semisynthetic Penicillins

    • Penicilinase-resistant penicillins
    • Carbapenems: very broad spectrum
    • Monobactam: Gram negative
    • Extended-spectrum penicillins
    • Penicillins + b-lactamase inhibitors
    Other Inhibitors of Cell Wall Synthesis

    • Cephalosporins
    • 2nd, 3rd, and 4th generations
    more effective against
    gram-negatives
    Other Inhibitors of Cell Wall Synthesis
    • Polypeptide antibiotics
    • Bacitracin
    • Topical application
    • Against gram-positives
    • Vancomycin
    • Glycopeptide
    • Important "last line" against antibiotic resistant S. aureus
    Other Inhibitors of Cell Wall
    Synthesis
    • Antibiotics effective against Mycobacteria:
    interfere with mycolic acid synthesis or
    incorporation
    • Isoniazid (INH)
    • Ethambutol
    Inhibitors of Protein Synthesis
    • Broad spectrum, toxicity problems
    • Examples
    • Chloramphenicol (bone marrow)
    • Aminoglycosides: Streptomycin, neomycin, gentamycin
    (hearing, kidneys)
    • Tetracyclines (Rickettsias & Chlamydia; GI tract)
    • Macrolides: Erythromycin (gram +, used in children)
    Injury to the Plasma Membrane

    • Polymyxin B (Gram negatives)


    • Topical
    • Combined with bacitracin and neomycin (broad spectrum) in
    over-the-counter preparation
    Inhibitors of Nucleic Acid Synthesis

    • Rifamycin
    • Inhibits RNA synthesis
    • Antituberculosis
    • Quinolones and fluoroquinolones
    • Ciprofloxacin
    • Inhibits DNA gyrase
    • Urinary tract infections
    Competitive Inhibitors
    • Sulfonamides (Sulfa drugs)
    • Inhibit folic acid synthesis
    • Broad spectrum
    Antifungal Drugs

    • Fungi are eukaryotes


    • Have unique sterols in their cell walls
    • Pathogenic fungi are often outside the
    body
    Antiviral Drugs
    • Viruses are composed of nucleic acid, protein capsid, and
    host membrane containing virus proteins
    • Viruses live inside host cells and use many host enzymes
    • Some viruses have unique enzymes for DNA/RNA
    synthesis or protein cutting in virus assembly
    Antiviral Drugs
    Nucleoside and Nucleotide Analogs
    Analogs Block DNA Synthesis
    Antiviral Drugs Enzyme Inhibitors
    • Inhibit assembly
    • Indinavir (HIV)
    • Inhibit attachment
    • Zanamivir (Influenza)
    • Inhibit uncoating
    • Amantadine (Influenza)
    • Interferons prevent spread of viruses to new cells (Viral
    hepatitis)
    • Natural products of the immune system in viral infections
    Antiprotozoan Drugs

    • Protozoa are eukaryotic cells


    • Many drugs are experimental
    and their mode of action is
    unknown
    Antihelminthic Drugs
    • Helminths are macroscopic
    multicellular eukaryotic
    organisms: tapeworms,
    roundworms, pinworms,
    hookworms
    Antihelminthic Drugs
    • Prevent ATP generation (Tapeworms)
    • Alters membrane permeability (Flatworms)
    • Neuromuscular block (Intestinal roundworms)
    • Inhibits nutrient absorption (Intestinal
    roundworms)
    • Paralyzes worm (Intestinal roundworms)
    Measuring Antimicrobial Sensitivity

    • E Test
    • MIC: Minimal inhibitory
    concentration
    Measuring Antimicrobial Sensitivity: Disk
    Diffusion
    Antibiotic Resistance
    Antimicrobial Resistance
    • Relative or complete lack of effect of
    antimicrobial against a previously susceptible
    microbe
    • Increase in MIC
    Mechanisms of Antibiotic Resistance
    •Enzymatic destruction of drug
    •Prevention of penetration of drug
    •Alteration of antibiotic or target
    site
    •Rapid ejection of the drug
    Antibiotic Selection for Resistant Bacteria
    What Factors Promote Antimicrobial Resistance?

    • Exposure to sub-optimal levels of antimicrobial


    • Exposure to microbes carrying resistance genes
    Inappropriate Antimicrobial Use
    • Prescription not taken correctly
    • Antibiotics for viral infections
    • Antibiotics sold without medical supervision
    • Spread of resistant microbes in hospitals due to lack of
    hygiene
    • Lack of quality control in manufacture or outdated
    antimicrobial
    • Inadequate surveillance or defective susceptibility assays
    • Poverty or war
    • Use of antibiotics in foods
    Antibiotics in Foods
    • Antibiotics are used in animal feeds and sprayed
    on plants to prevent infection and promote
    growth
    • Multi drug-resistant Salmonella typhi has been
    found in 4 states in 18 people who ate beef fed
    antibiotics
    Consequences of Antimicrobial Resistance

    • Infections resistant to
    available antibiotics
    • Increased cost of
    treatment
    Multi-Drug Resistant TB
    MRSA “mer-sah”
    • Methicillin-Resistant Staphylococcus aureus
    • Most frequent nosocomial (hospital-acquired)
    pathogen
    • Usually resistant to several other antibiotics
    Proposals to Combat Antimicrobial Resistance
    • Speed development of new antibiotics
    • Track resistance data nationwide
    • Restrict antimicrobial use
    • Direct observed dosing (TB)
    • Use more narrow spectrum antibiotics
    • Use antimicrobial cocktails
    The Future of Chemotherapeutic Agents

    • Antimicrobial peptides
    • Broad spectrum antibiotics from plants and animals
    • Squalamine (sharks)
    • Protegrin (pigs)
    • Magainin (frogs)
    • Antisense agents
    • Complementary DNA or peptide nucleic acids that binds to a
    pathogen's virulence gene(s) and prevents transcription

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