Protein Synthesis Inhibitors
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Questions and Answers

Which of the following antibiotics is classified as a 30S inhibitor?

  • Clindamycin
  • Chloramphenicol
  • Tetracycline (correct)
  • Erythromycin
  • What is the primary action mechanism of aminoglycosides?

  • Inhibition of DNA replication
  • Inhibition of cell wall synthesis
  • Concentration dependent killing (correct)
  • Inhibition of folate synthesis
  • Which of the following antibiotics is NOT a 50S ribosomal subunit inhibitor?

  • Linezolid
  • Chloramphenicol
  • Erythromycin
  • Vancomycin (correct)
  • Aminoglycosides are often administered in a single injection for the entire daily dose mainly due to what characteristic?

    <p>Post-antibiotic effect</p> Signup and view all the answers

    Which of the following agents is a bactericidal antibiotic?

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

    What is the nature of the killing effect of chloramphenicol?

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

    Aminoglycosides are sometimes combined with which of the following to enhance their effect?

    <p>Cell-wall inhibiting antibiotics</p> Signup and view all the answers

    Which of the following is a characteristic unique to aminoglycosides?

    <p>Post-antibiotic effect</p> Signup and view all the answers

    Which of the following drugs are classified as macrolides?

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

    What is a common adverse reaction associated with erythromycin?

    <p>Gastrointestinal upset</p> Signup and view all the answers

    What effect does impaired absorption of certain antibiotics have on children?

    <p>Fluorescence in teeth</p> Signup and view all the answers

    Which of the following is a side effect linked to hepatic function impairment from antibiotic use?

    <p>Acute Cholestatic Hepatitis</p> Signup and view all the answers

    What is a significant consequence of using certain antibiotics during pregnancy?

    <p>Bone deformity</p> Signup and view all the answers

    Which of the following antibiotics is NOT classified as a GNAT?

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

    What type of inhibition is associated with GNATS?

    <p>Irreversible inhibition by binding to the 30S ribosomal unit</p> Signup and view all the answers

    Which of the following is a potential adverse effect of GNATS?

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

    Which mechanism of action describes how GNATS interfere with protein synthesis?

    <p>Interfering with the initiation complex of peptide formation</p> Signup and view all the answers

    Which statement best describes the effect of GNATS on mRNA?

    <p>They cause misreading of mRNA leading to nonfunctional proteins.</p> Signup and view all the answers

    Which of the following best explains the term 'bactericidal' in the context of GNATS?

    <p>They cause irreversible damage to bacterial cells.</p> Signup and view all the answers

    What happens to polysomes when GNATS inhibit protein synthesis?

    <p>Polysomes break up into nonfunctional monosomes.</p> Signup and view all the answers

    Which of the following is an example of a 30S ribosomal subunit inhibitor?

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

    What type of blockade can GNATS cause as an adverse effect?

    <p>Neuromuscular blockade</p> Signup and view all the answers

    In terms of ribosomal function, what is a key distinction between the 30S and 50S subunits?

    <p>The 30S subunit is associated with mRNA decoding.</p> Signup and view all the answers

    What is one of the mechanisms by which bacteria develop resistance to aminoglycosides?

    <p>Production of a transferase enzyme that inactivates aminoglycosides</p> Signup and view all the answers

    Which of the following statements correctly describes the entry mechanism of aminoglycosides into prokaryotic cells?

    <p>Mutation in porin proteins can impair aminoglycoside entry</p> Signup and view all the answers

    How are aminoglycosides typically administered to ensure proper absorption?

    <p>Intravenously over a 30 to 60-minute infusion</p> Signup and view all the answers

    What is the target ribosomal subunit of aminoglycosides in prokaryotic cells?

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

    What is the recommended dosing schedule for aminoglycosides based on their pharmacokinetics?

    <p>Administered in 2 or 3 equally divided doses per day</p> Signup and view all the answers

    Which of the following is true about the half-life of aminoglycosides?

    <p>It typically lasts between 2 to 3 hours</p> Signup and view all the answers

    Which type of bacteria is specifically targeted by aminoglycosides?

    <p>Smaller bacterial ribosomes</p> Signup and view all the answers

    What can result from mutations in the receptor protein of the 30S ribosomal subunit?

    <p>Inhibition of aminoglycoside binding</p> Signup and view all the answers

    What is the primary mechanism of action for macrolides?

    <p>Binding to 50s ribosomal subunit</p> Signup and view all the answers

    Why are aminoglycosides not typically given orally?

    <p>They are poorly absorbed in the gastrointestinal tract</p> Signup and view all the answers

    Which of the following bacteria are macrolides effective against?

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

    Which phrase best describes the actions of aminoglycosides upon bacterial ribosomes?

    <p>They prevent protein synthesis by binding to the 30S subunit</p> Signup and view all the answers

    What effect does increased metabolization by cytochrome P450 enzymes have?

    <p>Decreased drug effectiveness</p> Signup and view all the answers

    Which of the following describes the spectrum of activity of macrolides?

    <p>Broad-spectrum including Gram-negative and Gram-positive</p> Signup and view all the answers

    Which of the following is an example of a clinical use for clarithromycin?

    <p>Treatment of infections caused by Streptococcus pneumoniae</p> Signup and view all the answers

    How does the binding of macrolides to peptidyl transferase center affect protein synthesis?

    <p>It inhibits peptide chain elongation</p> Signup and view all the answers

    What is the effect of improved acid stability of clarithromycin?

    <p>Lower gastrointestinal intolerance</p> Signup and view all the answers

    Which bacterium is NOT typically treated with macrolides?

    <p>Escherichia coli</p> Signup and view all the answers

    What is the primary effect of metabolite inhibition of cytochrome P450 enzymes?

    <p>Altered drug metabolism</p> Signup and view all the answers

    Which of the following microbes can be treated with macrolides?

    <p>Streptococcus pyogenes</p> Signup and view all the answers

    Study Notes

    Protein Synthesis Inhibitors Overview

    • 30S Inhibitors: Inhibit bacterial protein synthesis, including aminoglycosides (bactericidal).
    • 50S Inhibitors: Include macrolides, clindamycin, and chloramphenicol, mostly bacteriostatic.

    Aminoglycosides

    • Typically administered as a single intramuscular or intravenous injection to optimize pharmacological effects.
    • Exhibit concentration-dependent killing, resulting in faster bacterial elimination at higher doses.
    • Possess a post-antibiotic effect, indicating prolonged antibacterial activity after drug concentration decreases below measurable levels.
    • Often combined with cell-wall inhibitors (e.g., beta-lactams, vancomycin) for enhanced synergistic efficacy.
    • Example drugs: Gentamicin, Neomycin, Amikacin, Tobramycin, Streptomycin (GNATS).

    Mechanism of Action

    • Bind irreversibly to the 30S ribosomal subunit:
      • Interfere with initiation complex formation.
      • Cause misreading of mRNA, producing nonfunctional proteins.
      • Break up polysomes into inactive monosomes.

    Pharmacokinetics

    • Poor gastrointestinal absorption; administered via IV infusion typically lasting 30-60 minutes.
    • Traditional dosing involves 2-3 equally divided doses per day.
    • Half-life of 2-3 hours; some cases (e.g., TB treatment) require intramuscular delivery.

    Adverse Effects

    • Nephrotoxicity: Damage to kidneys.
    • Ototoxicity: Potential for hearing loss.
    • Neuromuscular blockade: Risk of muscle paralysis.
    • Teratogen: Risks during pregnancy.

    Mechanism of Resistance

    • Transferase enzyme production leading to aminoglycoside inactivation.
    • Mutations in porin proteins preventing antibiotic entry.
    • Alterations in the 30S ribosomal subunit’s receptor proteins that inhibit binding.

    Macrolides

    • Characterized by the suffix "-thromycin"; examples include erythromycin, clarithromycin, and azithromycin.
    • Primarily bacteriostatic, inhibiting protein synthesis via binding to the 50S subunit.
    • Known adverse reactions include gastrointestinal upset (nausea, anorexia, diarrhea) and potential hepatotoxicity (acute cholestatic hepatitis).

    Spectrum of Activity

    • Effective against various pathogens, including:
      • Gram Positive: Streptococci, Staphylococci, Pneumococci, Corynebacteria.
      • Gram Negative: Neisseria, Bordetella pertussis, H. influenzae.
      • Atypical Bacteria: Mycoplasma, Bartonella spp.

    Summary Notes

    • Dosing for aminoglycosides leverages unique pharmacological properties to minimize toxicity while maximizing efficacy.
    • Resistance mechanisms highlight a need for monitoring and adapting treatment strategies in bacterial infections.
    • Adverse reactions necessitate careful patient selection and monitoring to mitigate risks in clinical settings.

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    Description

    This quiz explores the mechanisms of action and classifications of antibiotic inhibitors, specifically focusing on 30S and 50S inhibitors. Participants will be tested on key concepts such as aminoglycosides and chloramphenicol. Enhance your understanding of clinical scenarios involving these antibiotics.

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