Aminoglycosides and Streptogramins Quiz
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Questions and Answers

What is a unique feature of quinupristin's action compared to macrolides?

  • It induces lysis of the bacterial cell wall.
  • It only inhibits the initiation of protein synthesis.
  • It is bactericidal for Staphylococcus and most organisms. (correct)
  • It exclusively targets Enterococcus faecium.

Which of the following correctly describes the mechanism of resistance to streptogramins B?

  • Hydrolysis of the antibiotic via the vgb gene. (correct)
  • Mutation of the vgb gene affecting antibiotic binding.
  • Decreased synthesis of 30S ribosomal subunits.
  • Inhibition of the ermB gene activity.

What does the term MLSB resistance refer to in relation to specific antibiotic classes?

  • Resistance that can only be conferred by the ermB gene.
  • Resistance to streptogramins that is exclusively carried by the ermA gene.
  • Constitutive or inducible resistance linked to methylation of rRNA and cross-resistance. (correct)
  • Activity exclusively related to lincosamides and macrolides only.

Which ribosomal component is modified to confer resistance to MLS antibiotics?

<p>23S rRNA through methylation. (C)</p> Signup and view all the answers

What characteristic prolonged effect does quinupristin exhibit against Staphylococcus aureus?

<p>It has a prolonged post-antibiotic effect lasting up to 10 hours. (B)</p> Signup and view all the answers

What is the primary mechanism through which arbekacin exerts its antibacterial effects?

<p>Interfering with bacterial protein synthesis at both 30S and 50S ribosomal subunits (B)</p> Signup and view all the answers

Which of the following statements accurately describes arbekacin's effectiveness against resistant bacteria?

<p>Effective against certain resistant strains including Pseudomonas aeruginosa (D)</p> Signup and view all the answers

How does arbekacin contribute to the treatment of MRSA infections specifically?

<p>By causing significant alterations in the biofilm and inflammatory response (A)</p> Signup and view all the answers

Which combinations with aminoglycosides are most effective against Gram-positive bacteria?

<p>Aminoglycosides combined with beta-lactams or glycopeptides (C)</p> Signup and view all the answers

What is one of the key advantages of using arbekacin over other aminoglycosides?

<p>It resists inactivation by many aminoglycoside-modifying enzymes (C)</p> Signup and view all the answers

In combination therapy for serious infections, what is a primary benefit of using aminoglycosides?

<p>Improved penetration by disrupting cell walls (C)</p> Signup and view all the answers

What specific effect does linezolid have on bacterial protein synthesis?

<p>It binds to the 23S rRNA of the 50S ribosomal subunit (D)</p> Signup and view all the answers

What is the primary mechanism by which tetracyclines inhibit bacterial growth?

<p>Binding to the 30S ribosomal subunit (D)</p> Signup and view all the answers

Which of the following is a characteristic of third-generation tetracyclines?

<p>They include Eravacycline and Omadacycline. (A)</p> Signup and view all the answers

Which of the following bacteria is NOT typically targeted by tetracyclines?

<p>Bacillus anthracis (B)</p> Signup and view all the answers

What is a significant property of tetracyclines regarding their action on bacterial cells?

<p>Their effect is reversible upon cessation of administration. (C)</p> Signup and view all the answers

Which of the following statements about tetracyclines is correct?

<p>They exhibit broad-spectrum activity. (B)</p> Signup and view all the answers

Which of the following defines the term 'bacteriostatic' as it relates to tetracyclines?

<p>They inhibit the growth and reproduction of bacteria. (C)</p> Signup and view all the answers

Which of the following is a property of tetracyclines at high dosages?

<p>They can become bactericidal. (C)</p> Signup and view all the answers

What is the primary usage of Eravacycline?

<p>Complicated intra-abdominal infections (C)</p> Signup and view all the answers

The term 'hydrophilicity' in the context of tetracyclines refers to which characteristic?

<p>Their capacity to penetrate bacterial cells easily. (C)</p> Signup and view all the answers

What role do aminoacyl-tRNA molecules play in the action of tetracyclines?

<p>They deliver amino acids to the growing peptide chain. (A)</p> Signup and view all the answers

Which antibiotics are classified as third-generation tetracyclines?

<p>Eravacycline, Omadacycline, and Sarecycline (A)</p> Signup and view all the answers

What route of administration is used for Sarecycline?

<p>Oral only (C)</p> Signup and view all the answers

What resistance mechanism is associated with Omadacycline?

<p>Mutations in 16S rRNA and ribosome protective proteins (D)</p> Signup and view all the answers

Which of the following describes the spectrum of activity for Sarecycline?

<p>Narrow spectrum, reducing impact on gut microbiota (D)</p> Signup and view all the answers

What is the prototype macrolide antibiotic mentioned?

<p>Erythromycin (A)</p> Signup and view all the answers

Which bacteria are macrolides effective against?

<p>Pneumococci, Streptococci, and Staphylococci (D)</p> Signup and view all the answers

What advantage does Omadacycline offer in its treatment capabilities?

<p>It is specifically designed to overcome tetracycline resistance (C)</p> Signup and view all the answers

What could result from separate intake of certain antibiotics?

<p>Contribution to osteoporosis risk (B)</p> Signup and view all the answers

What type of infections is Eravacycline specifically effective against?

<p>Complicated intra-abdominal infections (C)</p> Signup and view all the answers

What is the primary mechanism of action of chloramphenicol against bacteria?

<p>Inhibits protein synthesis at the peptidyl transferase reaction (A)</p> Signup and view all the answers

Which of the following bacteria are known to be bactericidal to chloramphenicol?

<p>Haemophilus influenzae (D)</p> Signup and view all the answers

Which type of infections is chloramphenicol ineffective against?

<p>Chlamydial infections (B)</p> Signup and view all the answers

In which situation is chloramphenicol considered as an alternative treatment?

<p>For meningococcal meningitis in patients allergic to penicillin (D)</p> Signup and view all the answers

Which statement regarding chloramphenicol's antimicrobial activity is correct?

<p>It is primarily bacteriostatic but may be bactericidal to some strains. (D)</p> Signup and view all the answers

Which of the following is a clinical use for chloramphenicol?

<p>Treatment of serious rickettsial infections (B)</p> Signup and view all the answers

Chloramphenicol inhibits the attachment of which component to the bacterial ribosome?

<p>Aminoacyl-tRNA in the A site (A)</p> Signup and view all the answers

Which of the following statements best describes the activity of chloramphenicol against Salmonella infections?

<p>It is more effective than tetracyclines. (D)</p> Signup and view all the answers

What prevents the peptidyl transferase enzyme from functioning properly when chloramphenicol is present?

<p>Improper alignment of tRNA molecules (B)</p> Signup and view all the answers

Which microorganism is specifically mentioned as being resistant to chloramphenicol?

<p>S. pneumoniae (B)</p> Signup and view all the answers

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Flashcards

Arbekacin's Mechanism of Action

Arbekacin targets both the 30S and 50S ribosomal subunits in bacteria, disrupting protein synthesis. It also directly damages bacterial membranes, leading to a dual attack on bacterial cells.

Arbekacin's Resistance to Inactivation

Arbekacin is resistant to inactivation by enzymes that normally break down other aminoglycosides, making it effective against bacteria that have developed resistance to those antibiotics.

Arbekacin's Effect on MRSA Biofilms

Arbekacin, when used against MRSA infections, effectively disrupts the biofilm structure and reduces inflammation. This leads to eradication of the biofilm and resolution of the infection.

Arbekacin's Spectrum of Activity

Arbekacin is highly effective against MRSA and other resistant Staphylococcus and Enterococcus species. It also shows activity against some resistant Pseudomonas aeruginosa and Acinetobacter baumannii strains.

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Aminoglycosides Effective Against Pseudomonas

Tobramycin, Gentamycin, and Arbekacin are all effective against Pseudomonas infections.

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Aminoglycosides Effective Against Mycobacterium tuberculosis

Streptomycin, Kanamycin, and Amikacin are effective against Mycobacterium tuberculosis infections.

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Aminoglycosides in Combination Therapy

Aminoglycosides are often combined with beta-lactams or glycopeptides (like cephalosporins or penicillin) to enhance their effectiveness against Gram-positive bacteria. This synergistic effect increases the permeability of the bacterial cell wall, allowing greater entry of aminoglycosides.

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What are tetracyclines?

Tetracyclines are a group of bacteriostatic antibiotics with a broad spectrum of activity against Gram-positive and Gram-negative bacteria, as well as certain pathogens like Rickettsia and Chlamydia.

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Why are tetracyclines called 'tetracyclines'?

They are named for their four hydrocarbon rings.

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How do tetracyclines work?

They reversibly bind to the 30S ribosomal subunit of bacteria, preventing the addition of amino acids to the growing peptide chain, thereby inhibiting protein synthesis.

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What type of bacteria are tetracyclines effective against?

Tetracyclines are active against multiplying bacteria, effectively stopping their growth and preventing further spread of infection.

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What is the primary effect of tetracyclines on bacteria?

Tetracyclines are bacteriostatic, meaning they inhibit bacterial growth but don't directly kill them. However, at high dosages, they can exhibit bactericidal activity.

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What makes tetracyclines 'broad-spectrum' antibiotics?

Tetracyclines have a broad spectrum of activity, meaning they can target a wide range of bacteria, including both aerobic and anaerobic, Gram-positive and Gram-negative types.

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How do tetracyclines enter bacterial cells?

They penetrate bacterial cells using both passive and active mechanisms, depending on their hydrophilicity and energy dependence.

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What are some common uses of tetracyclines?

Tetracyclines are used to treat a variety of infections caused by susceptible bacteria.

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What are some examples of infections treated with tetracyclines?

They are effective against a wide range of bacteria, including those responsible for acne, Lyme disease, and certain sexually transmitted infections.

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What are third-generation tetracyclines and their primary use?

A group of antibiotics with a broad spectrum of activity, including against some resistant strains like Acinetobacter spp. They are primarily used for treating complicated intra-abdominal infections. Eravacycline is administered intravenously.

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What is Omadacycline?

A third-generation tetracycline antibiotic with broad-spectrum activity, including against anaerobic bacteria. It's available in both oral and IV formulations.

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What is Sarecycline and its use?

A fourth-generation tetracycline with a narrow spectrum of activity. It's specifically used for treating moderate to severe acne vulgaris. Sarecycline is administered orally.

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What defines macrolide antibiotics and key examples?

A family of antibiotics characterized by their macrocyclic lactone rings and deoxy sugars. Erythromycin is a naturally occurring macrolide, often used for patients allergic to penicillin. Derivatives include clarithromycin, ketolides, and azithromycin.

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Who's macrolides' enemies?

Macrolide Antibiotics are active against which bacterial groups?

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How can bacteria become immune to third-generation tetracyclines?

Resistance mechanisms for third-generation tetracyclines include upregulation of the multidrug efflux system AcrA-AcrB-TolC and presence of adeB genes in VRE and CRE.

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How does Omadacycline resistance occur?

Ribosome protective proteins (RPPs) and mutations in 16SRNA contribute to resistance against Omadacycline.

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Why does Sarecycline cause fewer side effects than other tetracyclines?

The narrow spectrum of Sarecycline minimizes the impact on gut microbiota, leading to fewer gastrointestinal side effects.

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What are the key characteristics of Eravacycline?

Eravacycline is primarily used for treating complicated intra-abdominal infections (anaerobes).

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What is Sarecycline's particular usage?

Sarecycline is specifically used for treating moderate to severe acne vulgaris.

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Quinupristin's Mechanism of Action

Quinupristin binds to the 50S ribosomal subunit, preventing polypeptide elongation and causing incomplete chains to be released. It acts similarly to macrolides but is bactericidal against Staphylococcus and most organisms except Enterococcus faecium. A prolonged post-antibiotic effect lasts up to 10 hours for Staphylococcus aureus.

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Streptogramin B Resistance Mechanisms

Resistance to Streptogramin B can arise from two main mechanisms: Hydrolysis of the antibiotic by the vgb gene, initially observed in Staphylococcus aureus, or modification of the ribosomal target by a 23S rRNA methylase encoded by the ermB gene, leading to the MLSB phenotype.

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MLS Resistance Mechanisms

The MLS (Macrolides-Lincosamides- Streptogramins B) resistance is observed primarily due to three mechanisms: 1. Methylation of rRNA (target modification), 2. Active efflux (M and L only), 3. Inactivation of the antibiotic (M and L only).

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MLSB Resistance Phenotype

The most prevalent resistance phenotype is MLSB (constitutive or inducible), mainly attributed to the presence of ermA and ermC genes. This phenotype shows cross-resistance to Macrolides, Lincosamides, and Streptogramin B.

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ErmA and ErmC Genes and MLSB Resistance

ErmA and ErmC genes are responsible for encoding proteins that modify the ribosomal target, leading to the MLSB phenotype, where bacteria become resistant to Macrolides, Lincosamides, and Streptogramin B.

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Chloramphenicol's Mechanism of Action

Chloramphenicol binds to the bacterial 50S ribosomal subunit preventing the attachment of aminoacyl tRNA to the 50S subunit, thus inhibiting protein synthesis.

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Chloramphenicol's Bacteriostatic/Bactericidal Activity

It is primarily bacteriostatic, meaning it inhibits the growth of bacteria, but can be bactericidal, meaning it kills bacteria, against certain strains like H. influenzae, N. meningitidis, N. gonorrhea, and Bacteroides fragilis.

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Chloramphenicol's Spectrum of Activity

Effective against a wide range of bacteria including S. epidermidis, S. aureus, M. pneumoniae, L. monocytogenes, Corynebacterium diphtheriae, P. multocida, Salmonella sp., Shigella sp., E. coli, Rickettsia and Anaerobes.

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Chloramphenicol's Ineffectiveness against Chlamydia

Chloramphenicol is not effective against Chlamydia infections.

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Chloramphenicol's Effectiveness against Typhoid Fever

Chloramphenicol is more effective than Tetracyclines in treating Typhoid Fever and other Salmonella infections.

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Chloramphenicol's Use in Rickettsial Infections

Chloramphenicol can treat serious rickettsial infections like typhus and Rocky Mountain spotted fever.

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Chloramphenicol's Use in Meningococcal Meningitis

Chloramphenicol is an alternative to beta-lactams for treating meningococcal meningitis in patients allergic to penicillin.

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Chloramphenicol's Use as a Backup Drug

Chloramphenicol is used as a last resort for severe infections caused by Salmonella Typhi and Paratyphi.

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Chloramphenicol's Use in Anaerobic Infections

Chloramphenicol can be used to treat infections caused by anaerobes, such as Bacteroides.

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Chloramphenicol's Side Effects

Chloramphenicol should be used with caution due to its potential for serious side effects, such as aplastic anemia.

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Study Notes

Antimicrobials

  • Antimicrobials are broadly divided into: antibiotics, antivirals, antifungals, antiparasitic, and non-antibiotic antimicrobials.

Antibiotics

  • Antibiotics are substances produced by microorganisms that selectively suppress microbial growth or kill other microorganisms at deficient concentrations.

  • They are chemical entities with selective toxicity against infections affecting bacteria, protozoa, fungi, viruses, and helminths

Antibacterial Agents

  • An antibacterial agent interferes with the growth and reproduction of bacteria.

  • An antibiotic is a product (by a microorganism or chemical synthesis) that inhibits the growth of other microorganisms at low concentrations.

  • Bactericidal agents kill bacteria directly by damaging susceptible cell targets.

  • Bacteriostatic agents inhibit bacterial growth by inhibiting protein synthesis.

Antimicrobial Resistance (AMR)

  • Antimicrobial resistance (AMR) occurs when bacteria, viruses, fungi, and parasites no longer respond to antimicrobial medicines.

  • This can lead to difficult or impossible-to-treat infections, increasing the risk of severe illness, disability, and death.

  • The emergence and spread of AMR are accelerated by human activity, especially the misuse and overuse of antimicrobials.

Classification of Antimicrobials

  • Antimicrobials are classified by: chemical structure, mechanism of action, type of organisms, spectrum of activity, type of action (bacteriostatic or bactericidal), source of antibiotics.

Narrow and Broad Spectrum Antimicrobials

  • Narrow spectrum antimicrobials target a limited number of microbial species.
  • Broad spectrum antimicrobials target a wide range of species.

Mechanisms of Resistance

  • Permeability: alteration in outer membrane chemical nature.
  • Production of enzymes: enzymes destroying the drug.
  • Altered structure target: alterations to target site.
  • Altered metabolic pathways: Bypassing drug reactions.

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Test your knowledge on the unique features and mechanisms of action of quinupristin and arbekacin compared to other antibiotic classes. This quiz covers resistance mechanisms, effectiveness against MRSA, and the advantages of using aminoglycosides in combination therapies.

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