Tetracycline AB - 5Qs Flashcards
Are Tetracyclines acidic/basic?
Neither.
They’re amphoteric that is, they can be acidic, basic/ neutral depending on the solution.
What carbons are modifiable?
4, 5, 6, 7
What may lead to inactivity of Tetracyclines?
Epimerization at C-4 leads to loss of activity
What also occurs at C-4?
Dehydration
What’s the toxic metabolite of tetracycline?
Epianhydrotetracycline
Which tetracyclines are not prone to dehydration
Minocycline and Doxycycline
What chelates tetracyclines that are prone to chelation?
Mg2+ Ca2+ Fe2+ Al3+ Diary pdts Antacids Mineral supplements
MOA of tetracyclines
BacterioSTATIC
What are the Target for tetracyclines?
Inh protein synthesis after binding to bacterial 30s ribosomal subunit
What are tetracyclines to human in high concentrations?
Antianabolic in humans
What are the other targets of tetracycline?
Cytoplasmic membranes causing leakage into the cell
How’s resistance dev to tetracyclines?
R-factor mediated
Efflux pump
Oxidative enzymes (in some strains)
Are tetracyclines still popular?
Not anymore.
Minocycline and doxycycline are the ones most commonly used
When’s tetracycline considered 1st line?
Chlamydia, Mycoplasma and Ureaplasma inf Lyme dx Cholera Rocky Mountain spotted fever Scrub typhus
When are tetracyclines used as prophylaxis?
Traveller’s diarrhea
Malaria