Tetracyclines Flashcards
General backgroud of tetracyclines
Static or cidal?
Money?
Commonly given? Because?
Dosing?
Resistance why?
- 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
Tetracyclines examples
Tetracyclines are?
MOA?
static cidal?
- 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
- Binding to the 30S ribosomal subparticles in bacteria
- At low [Tetracycline], anti-anabolic effects exclusive to bacteria
- At high [Tetracycline], anti-anabolic to humans
Binding interactions of ____ mediated by?
- Interaction with ribosome is mediated by MG2+ and H bonding network
- No conformational movement is needed for interaction
Vinylogous acidity of Tetracyclines?
In ____ solutions, tetracyclines behave like?
Vinylogy?
Clinical Implications of Chelation of metal ions
Bioavailability can be reduced
Dental SEs
Skeletal growth
Admin IV
Epimerizations under basic conditions?
Unstable at what C and why?
how can they be inactivated?
Dehydration under acidic conditions?
*
Resistance to Tetracyclines?
ABC
Resistance to tetracyclines
Widespread?
Mechanisms of resistance repeated
Therapeutic Used?
Spectrum?
Coverage?
Skin infections?
Niche?
Doxyclycine?
Absorption?
metabolism?
Excretion?
Dosing?
Minocycline
Distribution?
Lipophilicity?
Stability/ Metabolism/ Excretion?
Can cross?
Tigecycline
Increased __ coverage
Resistance?
Spectrum?
log p?
SEs and interactions?
Comparison of Different medications
