Fluoroquinolones Flashcards
What is the mechanism of action of FQs?
Inhibit DNA gyrase and topoisomerase
Are FQ bacteriostatic or bactericidal?
Bactericidal (due to inhibition of 2 enzymes)
What is the spectrum of the FQs?
Gram (+) and gram (-), but NO ANAEROBES
Nalidixic acid is the non-fluorinated precursor that only kills some gram (-). What is added to extend the spectrum of FQs to gram (+)s?
Fluorine
What is the most common method of resistance to FQs?
Point mutation in DNA gyrase genes
Which bug has the fastest development of resistance against the FQs?
Campylobacter
Are FQs time, concentration, or AUC/MIC-dependent?
AUC/MIC-dependent
What is the MPC?
Mutation prevention concentration
What is the MPC for gram (+)?
x5
What is the MPC for gram (-)?
x10
In what 3 tissues do the FQs concentrate?
- WBCs
- Prostate
- Brain
Are FQs water soluble or lipid soluble?
Lipid soluble (high Vd)
True or False: FQs are not absorbed well orally.
FALSE
True or False: FQs are excreted mostly unchanged in the urine.
TRUE
What toxicities are associated with the use of FQs?
- Chondrotoxicity in neonates/juveniles
- Retinopathies in cats
- Exacerbates seizures in epileptic dogs
- Herxhimer’s reaction
- Inhibit p450 enzymes