ANTIBAC 2: GLYCOPEPTIDES, AMINOGLYCOSIDE

• What are the categories of antibacterials mentioned?

  • Glycopeptides
  • Aminoglycosides
  • Macrolides & Ketolides
• Why are carbohydrate-containing natural products significant in medicine?

  They are biologically active with pharmaceutical applications
• What types of biological activity are most common in carbohydrate-containing natural products?

  Antibiotic and anti-tumour activity
• What is the nature of glycan-lectin interactions?

  They influence the biological activity of carbohydrates
• What are the main types of antibiotics mentioned in the context of carbohydrates in medicine?

  • Anti-tumour/anti-cancer
  • Anti-parasitic
  • Anti-fungal
• What are glycopeptides characterized by?

  Complex polypeptides with saccharides
• What is the primary use of glycopeptides?

  Treatment of Gram-positive bacterial infections
• What is the significance of vancomycin?

  It is a "drug of last resort"
• What type of infections is vancomycin used to treat?

  Bacterial infections resistant to other antibiotics
• What are the problems associated with vancomycin?

  Size and resistance issues
• What is teicoplanin?

  A mixture of five similar glycopeptide structures
• How does teicoplanin compare to vancomycin?

  Less toxic and does not dimerize
• What is dalbavancin?

  A second-generation teicoplanin
• What was dalbavancin designed to improve upon?

  The natural glycopeptide analogue teicoplanin
• When was dalbavancin approved for use in the USA?

  February 2015
• What is the significance of oritavancin?

  It has potent bactericidal activity against Gram-positive bacteria
• What is the mechanism of action of oritavancin?

  Inhibits bacterial cell-wall synthesis

  
• What are the three mechanisms of action of oritavancin?

  1. Inhibiting transglycosylation
  2. Inhibiting transpeptidation
  3. Disruption of bacterial membrane integrity

  
• What is the half-life of dalbavancin?

  147 to 258 hours
• What is the half-life of oritavancin?

  393 hours
• What is the mechanism of action of tetracyclines?

  They impair bacterial translation
• What are tetracyclines characterized by?

  Broad-spectrum, bacteriostatic agents
• What is the role of ribosomes in bacteria?

  They synthesize proteins through translation

  
• How do aminoglycosides work best?

  At slightly alkaline pH, positively charged
• What is the mechanism of action of chloramphenicol?

  It binds to the A-site of the 50S ribosomal subunit

  
• What is the significance of aminoglycoside-modifying enzymes (AMEs)?

  They contribute to resistance against aminoglycosides

  
• What are the mechanisms of resistance to aminoglycosides?

  • Aminoglycoside-modifying enzymes (AMEs)
  • Mutations in target binding site
  • Structural changes in outer membrane
  • More effective efflux pumps
  • Action of membrane proteases

  
• What is the first aminoglycoside discovered?

  Streptomycin
• What is the FDA approval status of plazomicin?

  Approved for treatment of cUTIs
• What is the significance of aminoglycosides working best at slightly alkaline pH?

  It aids absorption through Gram-negative bacteria
• What is the role of aminoglycosides in treating infections?

  They are bactericidal agents

  
• What is the mechanism of action of aminoglycosides?

  They disrupt protein synthesis in bacteria

  
• How do aminoglycosides accumulate inside bacterial cells?

  Through an energy-dependent transport process

  
• What is the significance of the aminoglycoside paromomycin?

  Approved as an orphan drug for leishmaniasis
• What is the role of aminoglycoside-modifying enzymes in resistance?

  They modify aminoglycosides to reduce effectiveness

  
• What is the first resistance warning for apramycin?

  Issued in 1986
• What is the significance of the aminoglycoside amikacin?

  It has better stability than gentamicin
• What is the mechanism of action of tetracyclines?

  They inhibit bacterial protein synthesis

  
• What is the significance of the structure of tetracyclines?

  It shows two distinct regions

  
• What is the mechanism of action of chloramphenicol?

  It inhibits peptidyl-transferase activity