Macrolide Antibiotics Mechanism of Action
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Questions and Answers

Which bacterial enzyme is responsible for the cross-linking of peptidoglycan molecules in the cell wall?

  • β-lactamase
  • Transpeptidase (correct)
  • Peptidase
  • Penicillinase
  • In what phase are penicillins bactericidal?

  • Growth and replication phase (correct)
  • Lag phase
  • Stationary phase
  • Decline phase
  • Which class of penicillins is effective against gram-positive organisms and remains useful if the bacteria produce penicillinase?

  • Antipseudomonal penicillin
  • Penicillinase-resistant penicillins (correct)
  • Natural penicillins
  • Extended-spectrum penicillins
  • Which drug is an irreversible inhibitor of many bacterial β-lactamases?

    <p>Clavulanic acid</p> Signup and view all the answers

    Why can high doses of penicillins lead to neurotoxicity?

    <p>They inhibit GABA receptors</p> Signup and view all the answers

    What is the most common adverse effect of penicillins?

    <p>Hypersensitivity reaction</p> Signup and view all the answers

    Which antibiotic has significant activity against anaerobes?

    <p>Cefepime</p> Signup and view all the answers

    What is the specific inhibitor of renal peptidase that prolongs the half-life of imipenem and limits renal toxicity?

    <p>Cilastatin</p> Signup and view all the answers

    Which antibiotic can cause tissue necrosis if given intramuscularly?

    <p>Vancomycin</p> Signup and view all the answers

    What is the broad-spectrum antibiotic that is effective against gram-positive organisms, including MRSA?

    <p>Ceftaroline</p> Signup and view all the answers

    Which antibiotic is specifically NOT effective against Pseudomonas aeruginosa?

    <p>Ceftaroline</p> Signup and view all the answers

    Which antibiotic may lead to risk of fetal harm and nephrotoxicity?

    <p>Telavancin</p> Signup and view all the answers

    What is the main characteristic of β-lactam antibiotics in terms of their selectivity?

    <p>They have a high degree of selective toxicity against bacteria because mammalian cells do not have cell walls.</p> Signup and view all the answers

    What is the mechanism of action of penicillins?

    <p>Inhibition of bacterial cell wall synthesis</p> Signup and view all the answers

    Why are β-lactam antibiotics able to selectively target bacteria?

    <p>They disrupt the formation of peptidoglycan in the bacterial cell wall.</p> Signup and view all the answers

    What is the primary target of β-lactam antibiotics within bacterial cells?

    <p>Peptidoglycan synthesis</p> Signup and view all the answers

    Which cellular feature makes β-lactam antibiotics ineffective against mammalian cells?

    <p>Absence of peptidoglycan in the cell membrane</p> Signup and view all the answers

    What is the key factor contributing to the high selectivity of β-lactam antibiotics for bacteria over human cells?

    <p>Differences in cell wall composition</p> Signup and view all the answers

    Which antibiotic binds to the P site of the 50S bacterial ribosomal subunit and blocks protein synthesis when a large amino acid or a polypeptide is in the P site?

    <p>Erythromycin</p> Signup and view all the answers

    Which macrolide antibiotic is much better absorbed after oral administration than erythromycin?

    <p>Clarithromycin</p> Signup and view all the answers

    Which macrolide antibiotic has the most unusual property of uptake into several tissues, maintaining high concentrations for prolonged periods?

    <p>Azithromycin</p> Signup and view all the answers

    Which antibiotic binds to the σ subunit of RNA polymerase, leading to RNA polymerase entering a 'closed clamp' conformation and inhibiting transcription and translation?

    <p>Fidaxomicin</p> Signup and view all the answers

    Which antibiotics bind to the 50S ribosomal subunit at or near the erythromycin site and have excellent activity against anaerobic bacteria?

    <p>Lincomycin and Clindamycin</p> Signup and view all the answers

    Which antibiotic preferentially binds to the 30S subunit of the microbial ribosome, interfering with binding of amino acyl-tRNA and inhibiting chain elongation and termination?

    <p>Tetracyclines</p> Signup and view all the answers

    What is the mechanism of action of tigecycline?

    <p>Reversibly binds to the 30S subunit of the microbial ribosome, inhibiting chain elongation and termination</p> Signup and view all the answers

    Which antibiotic causes deposition in bones and teeth, leading to potential damage in developing teeth and bones?

    <p>Doxycycline</p> Signup and view all the answers

    What distinguishes Amikacin from other aminoglycosides in terms of resistance?

    <p>It resists inactivation by many bacterial enzymes</p> Signup and view all the answers

    What is the serious side effect associated with chloramphenicol?

    <p>Irreversible aplastic anemia</p> Signup and view all the answers

    What is the main route of excretion for tetracyclines?

    <p>Bile/fecal</p> Signup and view all the answers

    What is the primary reason tetracyclines limit absorption and cause damage to bones and teeth?

    <p>They form insoluble complexes with cations, limiting absorption and causing deposition in bones and teeth</p> Signup and view all the answers

    Which enzyme is critical for chromosomal segregation in some bacterial strains?

    <p>DNA gyrase</p> Signup and view all the answers

    What is the main mechanism of action of fluoroquinolones (Quinolones)?

    <p>Stabilization of DNA-enzyme complex</p> Signup and view all the answers

    What effect does dietary calcium have on the absorption of Ciprofloxacin?

    <p>Reduces absorption</p> Signup and view all the answers

    Which type of bacteria are usually less susceptible to fluoroquinolones?

    <p>Gram-positive</p> Signup and view all the answers

    What is the clinical use of fluoroquinolones?

    <p>Prophylaxis and treatment of anthrax</p> Signup and view all the answers

    What is the spectrum of fluoroquinolones?

    <p>Broad</p> Signup and view all the answers

    What does DNA gyrase do in bacteria?

    <p>Introduces negative supercoils</p> Signup and view all the answers

    "Gyrase Inhibitors e.g. Fluoroquinolones (Quinolones)" are primarily bacteriostatic or bacteriocidal?

    <p>&quot;Bacteriocidal&quot;</p> Signup and view all the answers

    "Fluoroquinolones generally have good absorption and distribution, with the highest concentrations accumulating in:

    <p>&quot;Urine&quot;</p> Signup and view all the answers

    Which enzyme is responsible for the cross-linking of peptidoglycan molecules in the bacterial cell wall?

    <p>Transpeptidase</p> Signup and view all the answers

    Why are penicillins bactericidal when bacteria are in their growth and replication phase?

    <p>They inhibit cell wall synthesis by targeting transpeptidase</p> Signup and view all the answers

    What is the main mechanism of development of hypersensitivity against penicillins?

    <p>Formation of immunogenic human protein-β-lactam hapten</p> Signup and view all the answers

    Why can high doses of penicillins lead to neurotoxicity?

    <p>They bind to GABA receptors</p> Signup and view all the answers

    Which enzyme do many bacteria produce to open the β-lactam ring and destroy the activity of penicillin antibiotics?

    <p>Penicillinase</p> Signup and view all the answers

    What is the irreversible inhibitor of many bacterial β-lactamases?

    <p>Clavulanic acid</p> Signup and view all the answers

    What is the primary target of β-lactam antibiotics within bacterial cells?

    <p>Cell wall synthesis</p> Signup and view all the answers

    Why are β-lactam antibiotics able to selectively target bacteria?

    <p>They target cell wall synthesis unique to bacteria</p> Signup and view all the answers

    Which enzyme is critical for chromosomal segregation in some bacterial strains?

    <p>DNA gyrase</p> Signup and view all the answers

    What is the mechanism of action of tigecycline?

    <p>Inhibition of protein synthesis</p> Signup and view all the answers

    Which antibiotic binds to the σ subunit of RNA polymerase, leading to RNA polymerase entering a 'closed clamp' conformation and inhibiting transcription and translation?

    <p>Rifampin</p> Signup and view all the answers

    Which macrolide antibiotic has the most unusual property of uptake into several tissues, maintaining high concentrations for prolonged periods?

    <p>Azithromycin</p> Signup and view all the answers

    What is the primary mechanism of action of tetracyclines?

    <p>Inhibition of protein synthesis by binding to the 30S subunit of the microbial ribosome</p> Signup and view all the answers

    Which antibiotic is associated with a black box warning for acute pancreatitis and should only be used as a last resort?

    <p>Tigecycline</p> Signup and view all the answers

    Which antibiotic has the potential to cause irreversible aplastic anemia, reversible bone marrow depression, and 'gray baby' syndrome in neonates?

    <p>Chloramphenicol</p> Signup and view all the answers

    Which enzyme do aminoglycosides inhibit in bacteria?

    <p>Peptide synthetase</p> Signup and view all the answers

    Which antibiotic has good penetration into cerebrospinal fluid, ocular fluids, and joint fluids due to its high lipid solubility?

    <p>Chloramphenicol</p> Signup and view all the answers

    Which class of antibiotics bind to the P site of the 50S bacterial ribosomal subunit and block protein synthesis when a large amino acid or a polypeptide is in the P site?

    <p>Macrolides</p> Signup and view all the answers

    Which antibiotic binds to the σ subunit of RNA polymerase, leading to RNA polymerase entering a 'closed clamp' conformation and inhibiting transcription and translation?

    <p>Fidaxomicin</p> Signup and view all the answers

    What is the mechanism of action of chloramphenicol?

    <p>Block protein synthesis by binding to the P site of the 50S bacterial ribosomal subunit</p> Signup and view all the answers

    What makes azithromycin unusual compared to other macrolide antibiotics?

    <p>It maintains high concentrations in tissues for prolonged periods</p> Signup and view all the answers

    Which antibiotic has minimal absorption and remains mainly in the gastrointestinal tract, making its main clinical use in C. difficile infections?

    <p>Fidaxomicin</p> Signup and view all the answers

    What is the primary target of tetracyclines within bacterial cells?

    <p>30S ribosomal subunit</p> Signup and view all the answers

    Which antibiotic is chemically similar but pharmacologically different to erythromycin, and binds to the σ subunit of RNA polymerase?

    <p>Fidaxomicin</p> Signup and view all the answers

    What is the mechanism of action of vancomycin?

    <p>Inhibition of peptidoglycan synthesis through binding to D-alanine-D-alanine terminus</p> Signup and view all the answers

    Which antibiotic is specifically effective against Pseudomonas aeruginosa?

    <p>Cefepime</p> Signup and view all the answers

    What is the primary mechanism of action of daptomycin?

    <p>Disruption of bacterial cell membrane integrity</p> Signup and view all the answers

    What is the main spectrum of activity for aztreonam?

    <p>Mostly gram-negative bacteria</p> Signup and view all the answers

    Which antibiotic has the broadest spectrum of all β-lactam antibiotics?

    <p>Imipenem</p> Signup and view all the answers

    What is the specific inhibitor that prolongs the half-life of imipenem and limits its renal toxicity?

    <p>Cilastatin</p> Signup and view all the answers

    What is the primary mechanism of action of gyrase inhibitors like fluoroquinolones?

    <p>Promoting double stranded breaks and inhibiting chromosomal segregation</p> Signup and view all the answers

    Which enzyme is critical for chromosomal segregation in some bacterial strains?

    <p>Topoisomerase IV</p> Signup and view all the answers

    Why are fluoroquinolones like ciprofloxacin generally not effective against gram-positive bacteria?

    <p>They inhibit DNA gyrase in gram-negative bacteria but Topoisomerase IV in gram-positive bacteria</p> Signup and view all the answers

    What is the effect of dietary calcium on the absorption of ciprofloxacin?

    <p>It reduces the absorption of ciprofloxacin</p> Signup and view all the answers

    What is the primary clinical use of fluoroquinolones like ciprofloxacin?

    <p>Treatment of urinary tract infections</p> Signup and view all the answers

    What is the main characteristic of fluoroquinolones that allows for selective toxicity to bacteria over eukaryotic cells?

    <p>Their structural difference in bacterial vs eukaryotic topoisomerases</p> Signup and view all the answers

    What is the most common adverse effect associated with fluoroquinolones like ciprofloxacin?

    <p>Neurotoxicity</p> Signup and view all the answers

    Which type of bacteria are usually less susceptible to fluoroquinolones?

    <p>Gram-positive bacteria</p> Signup and view all the answers

    What effect does high dietary calcium have on the excretion of ciprofloxacin?

    <p>It increases excretion of ciprofloxacin</p> Signup and view all the answers

    Which bacterial enzyme can introduce negative supercoils into bacterial DNA?

    <p>DNA gyrase</p> Signup and view all the answers

    Study Notes

    Bacterial Cell Wall

    • The enzyme responsible for cross-linking peptidoglycan molecules in the bacterial cell wall is transpeptidase.

    Penicillins

    • Penicillins are bactericidal during the growth and replication phase.
    • Penicillinase-resistant penicillins are effective against gram-positive organisms and remain useful if the bacteria produce penicillinase.
    • Clavulanate is an irreversible inhibitor of many bacterial β-lactamases.
    • High doses of penicillins can lead to neurotoxicity.
    • The most common adverse effect of penicillins is hypersensitivity.
    • β-lactamases are produced by many bacteria to open the β-lactam ring and destroy the activity of penicillin antibiotics.

    β-lactam Antibiotics

    • Transpeptidase is the primary target of β-lactam antibiotics within bacterial cells.
    • β-lactam antibiotics are able to selectively target bacteria because they inhibit cell wall synthesis.
    • The key factor contributing to the high selectivity of β-lactam antibiotics for bacteria over human cells is the presence of peptidoglycan in bacterial cell walls.

    Macrolide Antibiotics

    • Azithromycin is a macrolide antibiotic with unusual properties, including uptake into several tissues, maintaining high concentrations for prolonged periods.
    • Erythromycin is a macrolide antibiotic that binds to the P site of the 50S bacterial ribosomal subunit and blocks protein synthesis.

    Other Antibiotics

    • Tigecycline binds to the 30S subunit of the microbial ribosome, interfering with binding of amino acyl-tRNA and inhibiting chain elongation and termination.
    • Tetracyclines bind to the 30S subunit of the microbial ribosome, interfering with binding of amino acyl-tRNA and inhibiting chain elongation and termination.
    • Fluoroquinolones are gyrase inhibitors that inhibit DNA replication and transcription.
    • Aminoglycosides inhibit protein synthesis by binding to the 30S subunit of the bacterial ribosome.
    • Chloramphenicol binds to the 50S subunit of the bacterial ribosome, inhibiting protein synthesis.
    • Vancomycin inhibits cell wall synthesis by binding to the terminal D-alanyl-D-alanine residue of peptidoglycan.
    • Daptomycin inhibits bacterial cell membrane function.
    • Aztreonam has a narrow spectrum of activity against gram-negative bacteria.
    • Imipenem is a broad-spectrum β-lactam antibiotic.
    • Cilastatin is a specific inhibitor that prolongs the half-life of imipenem and limits its renal toxicity.

    Fluoroquinolones

    • Gyrase is the bacterial enzyme that introduces negative supercoils into bacterial DNA.
    • Fluoroquinolones are generally not effective against gram-positive bacteria.
    • Dietary calcium decreases the absorption of ciprofloxacin.
    • The primary clinical use of ciprofloxacin is against gram-negative bacteria.
    • The main characteristic of fluoroquinolones that allows for selective toxicity to bacteria over eukaryotic cells is inhibition of DNA replication and transcription.
    • The most common adverse effect associated with fluoroquinolones is gastrointestinal disturbance.
    • Gram-positive bacteria are usually less susceptible to fluoroquinolones.
    • High dietary calcium has no effect on the excretion of ciprofloxacin.

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    Description

    Test your knowledge on the mechanism of action of macrolide antibiotics, with a focus on erythromycin. Learn about the binding to the P site of the bacterial ribosomal subunit and its effect on protein synthesis. Explore the spectrum and properties of macrolide antibiotics.

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