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Antibiotics: Penicillins and Bacterial Enzymes

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48 Questions

Which of the following bacteria produces penicillinases that degrade natural penicillins?

Bacteroides fragilis

What is a limitation of natural penicillins?

They are ineffective against bacteria with altered PBPs

Which of the following bacteria is susceptible to natural penicillins?

All of the above

What is the mechanism of resistance of methicillin-resistant S.aureus (MRSA) to antistaphylococcal penicillins?

Altered PBPs

What is the characteristic of antistaphylococcal penicillins?

They have bulky R side chains

Which of the following is NOT a limitation of natural penicillins?

Resistance to gram-negative bacteria

Which of the following bacteria is resistant to antistaphylococcal penicillins?

Methicillin-resistant S.aureus (MRSA)

What is the mechanism of action of antistaphylococcal penicillins?

Inhibition of cell wall synthesis

What is an important feature of extended-spectrum penicillins?

They are active against even more enteric gram-negative rods and P. aeruginosa

What is the effect of adding a β-lactamase inhibitor to an aminopenicillin?

It expands the spectrum of these agents to include many aerobic gram-negative bacilli and anaerobes

What is a characteristic of antistaphylococcal penicillins?

They are useful in treating infections caused by Staphylococcus

What is a difference between natural penicillins and aminopenicillins?

Aminopenicillins have improved activity against aerobic gram-negative bacilli

What is a characteristic of extended-spectrum penicillins?

They have improved activity against aerobic gram-negative bacilli, including P. aeruginosa

What is the result of using extended-spectrum penicillins in combination with β-lactamase inhibitors?

They are among the most powerful antibacterial agents available today

What is a feature of natural penicillins?

They have moderate activity against aerobic gram-positive bacteria and anaerobic bacteria

What is the mechanism of action of penicillins?

They bind to enzymes that function to assemble bacterial cell walls

What is the source of the first members of the cephalosporin class of antibiotics?

Fungus Cephalosporium acremonium

What is the categorization scheme used to organize cephalosporins?

By generation

What do cephalosporins have in common with penicillins?

Both are beta-lactam antibiotics

What is the common feature of the structure of cephalosporins?

Two side chains

What is the name of the fungus that was the source of the first members of the cephalosporin class of antibiotics?

Cephalosporium acremonium

What is the benefit of categorizing cephalosporins by generation?

Easier to remember the properties of the many cephalosporins

What is the name of the antibiotic class that cephalosporins belong to?

Beta-lactam

What is the common feature of cephalosporins and penicillins?

Both are beta-lactam antibiotics

What is the source of the first members of the cephalosporin class of antibiotics?

Cephalosporium acremonium

What do cephalosporins and penicillins have in common?

They are both beta-lactam antibiotics

What is the common feature of the structure of cephalosporins?

They have a nucleus with two side chains

What is the benefit of categorizing cephalosporins by generation?

It helps to predict their antibacterial spectrum

What is the name of the antibiotic class that cephalosporins belong to?

Beta-lactam antibiotics

What is the characteristic of cephalosporins that allows them to be categorized by generation?

Their antibacterial spectrum

What is the common feature of cephalosporins and penicillins?

They are both beta-lactam antibiotics

What is the categorization scheme used to organize cephalosporins?

By generation

What is the primary addition that extends the activity of extended-spectrum penicillins to include most enteric gram-negative bacilli?

A -lactamase inhibitor

Which type of bacteria are natural penicillins moderately active against?

Anaerobic bacteria

What is the primary mechanism of action of penicillins?

Binding to bacterial enzymes that assemble peptidoglycan

What is the primary advantage of aminopenicillins over natural penicillins?

Improved activity against aerobic gram-negative bacteria

Which bacteria do not make peptidoglycan and therefore are not affected by the natural penicillins?

Mycoplasma spp.

Which type of bacteria is P. aeruginosa?

Aerobic gram-negative bacteria

What is the main reason why some bacteria are resistant to natural penicillins?

They produce enzymes that break down penicillins.

Which bacteria remain susceptible to penicillin despite being gram-negative?

Neisseria meningitidis

What is the primary feature of extended-spectrum penicillins?

Activity against P. aeruginosa

What is the result of combining extended-spectrum penicillins with -lactamase inhibitors?

Activity against most aerobic gram-negative bacteria, aerobic gram-positive bacteria, and anaerobes

What is the characteristic of antistaphylococcal penicillins that makes them effective against staphylococcal infections?

They are resistant to beta-lactamases.

What is the primary function of the bacterial enzymes that penicillins bind to?

To assemble peptidoglycan

Which of the following bacteria is NOT affected by natural penicillins due to the production of penicillinases?

Streptococcus pneumoniae

What is the main difference between natural penicillins and antistaphylococcal penicillins?

Antistaphylococcal penicillins are resistant to beta-lactamases.

Which of the following bacteria is susceptible to natural penicillins despite being anaerobic?

Actinomyces israelii

What is the common feature of the bacteria that are susceptible to natural penicillins?

They all have a peptidoglycan layer in their cell walls.

Study Notes

Penicillins

  • Act by binding to PBPs, which are bacterial enzymes that function to assemble peptidoglycan.
  • Natural penicillins have moderate activity against aerobic gram-positive bacteria and anaerobic bacteria, but poor activity against aerobic gram-negative bacteria and most atypical bacteria.
  • Limitations of natural penicillins include:
    • Producing penicillinases that degrade natural penicillins (e.g., some anaerobes, such as Bacteroides fragilis).
    • Some bacteria produce PBPs that do not bind natural penicillins with high affinity (e.g., some strains of Streptococcus pneumoniae).
    • Some bacteria do not make peptidoglycan and are not affected by natural penicillins (e.g., Mycoplasma and Chlamydia spp.).

Antistaphylococcal Penicillins

  • Have bulky residues on their R side chains that prevent binding by staphylococcal β-lactamases.
  • Useful in treating infections caused by S. aureus and Staphylococcus epidermidis, but not effective against methicillin-resistant S. aureus (MRSA) and methicillin-resistant S. epidermidis (MRSE).

Extended-Spectrum Penicillins

  • Active against even more enteric gram-negative rods and importantly, Pseudomonas aeruginosa.
  • Addition of a β-lactamase inhibitor to an extended-spectrum penicillin extends its activity to include most enteric gram-negative bacilli.

Cephalosporins

  • Constitute a large extended family of antibiotics within the β-lactam group.
  • Can be categorized by "generation", with each generation having similar spectra of activity.
  • Each cephalosporin is composed of a nucleus with two side chains.

Penicillins

  • Act by binding to PBPs, which are bacterial enzymes that function to assemble peptidoglycan.
  • Natural penicillins have moderate activity against aerobic gram-positive bacteria and anaerobic bacteria, but poor activity against aerobic gram-negative bacteria and most atypical bacteria.
  • Limitations of natural penicillins include:
    • Producing penicillinases that degrade natural penicillins (e.g., some anaerobes, such as Bacteroides fragilis).
    • Some bacteria produce PBPs that do not bind natural penicillins with high affinity (e.g., some strains of Streptococcus pneumoniae).
    • Some bacteria do not make peptidoglycan and are not affected by natural penicillins (e.g., Mycoplasma and Chlamydia spp.).

Antistaphylococcal Penicillins

  • Have bulky residues on their R side chains that prevent binding by staphylococcal β-lactamases.
  • Useful in treating infections caused by S. aureus and Staphylococcus epidermidis, but not effective against methicillin-resistant S. aureus (MRSA) and methicillin-resistant S. epidermidis (MRSE).

Extended-Spectrum Penicillins

  • Active against even more enteric gram-negative rods and importantly, Pseudomonas aeruginosa.
  • Addition of a β-lactamase inhibitor to an extended-spectrum penicillin extends its activity to include most enteric gram-negative bacilli.

Cephalosporins

  • Constitute a large extended family of antibiotics within the β-lactam group.
  • Can be categorized by "generation", with each generation having similar spectra of activity.
  • Each cephalosporin is composed of a nucleus with two side chains.

Learn about the mechanism of action of penicillins, their activity against various bacteria, and their limitations. Understand how penicillinases and PBPs affect their efficacy.

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