Tetracyclines

Question 1

General backgroud of tetracyclines

Static or cidal?

Money?

Commonly given? Because?

Dosing?

Resistance why?

Answer 1

• Niche Uses
• Bacteriostatic (Except Mino)
• Cheap (fermented or semi-synthetic) Commonly given orally
• IV/IM administration is painful and can lead to thrombophlebitis
• t 1/2 = 16–18 h, once-daily
• Few life-threatening toxicities
• Resistance because of misuse

Question 2

Tetracyclines examples

Answer 2

Question 3

Tetracyclines are?

MOA?

static cidal?

Answer 3

• Generally Bacteriostatic (Except Mino = ‘Cidal)
• Inhibition of protein biosynthesis:
  
  • Binding to the 30S ribosomal subparticles in bacteria
    
    • Some participation by 50S subparticle
  • Inhibition of binding of aminoacyl t-RNA to ribosomes
  • Termination of bacterial protein biosynthesis
• At low [Tetracycline], anti-anabolic effects exclusive to bacteria
• At high [Tetracycline], anti-anabolic to humans

Question 4

Binding interactions of ____ mediated by?

Answer 4

• Interaction with ribosome is mediated by MG2+ and H bonding network
• No conformational movement is needed for interaction

Question 5

Vinylogous acidity of Tetracyclines?

In ____ solutions, tetracyclines behave like?

Vinylogy?

Answer 5

Question 6

Clinical Implications of Chelation of metal ions

Answer 6

Bioavailability can be reduced

Dental SEs

Skeletal growth

Admin IV

Question 7

Epimerizations under basic conditions?

Unstable at what C and why?

how can they be inactivated?

Answer 7

Question 8

Dehydration under acidic conditions?

Answer 8

*

Question 9

Resistance to Tetracyclines?

ABC

Answer 9

Question 10

Resistance to tetracyclines

Widespread?

Mechanisms of resistance repeated

Answer 10

Question 11

Therapeutic Used?

Spectrum?

Coverage?

Skin infections?

Niche?

Answer 11

Question 12

Doxyclycine?

Absorption?

metabolism?

Excretion?

Dosing?

Answer 12

Question 13

Minocycline

Distribution?

Lipophilicity?

Stability/ Metabolism/ Excretion?

Can cross?

Answer 13

Question 14

Tigecycline

Increased __ coverage

Resistance?

Spectrum?

log p?

Answer 14

Question 15

SEs and interactions?

Answer 15

Question 16

Comparison of Different medications

Answer 16