Erdman FQ Flashcards
MOA of Fluoroquinolones
inhibit DNA synthesis through binding to and inhibiting DNA topoisomerases
What are the 2 targets of FQs
DNA gyrase (topoII) and topoIV
What does inhibition of DNA gyrase do
prevents the relaxation of positively supercoiled DNA
What does inhibition of topo IV do
interferes with the separation of replicated DNA into daughter cells
DNA gyrase is the the main target for ________ bacteria
gram (-)
Topo IV is the main target for ______ bacteria
gram (+) (S. aureus)
FQs display ______ bactericidal activity
concentration-dependent
What are the 3 MOR for FQs
Alteration of binding site, increased efflux pump expression, alteration of cell wall permeability
True or False: cross-resistance is usually observed between FQs
True
Ciprofloxacin displays (good/poor) activity against gram (+) aerobes?
poor
Levo and Moxi display ______ activity against gram (+) aerobes compared to Cipro
enhanced
T/F: FQs are effective against MRSA
F - active against MSSA
What gram (+) aerobes do FQs cover
Group and viridans strep, enterococcus (limited)
Strep. pnuemoniae (including PRSP - not cipro)
MSSA
activity against enterobacteriaceae (H. influenzae, Neisseriam, M. catarrhalis)
cipro=levo activity but both > moxi
Which FQs have activity against Pseudomonas aeruginosa
Cipro and Levo
Which FQs have activity against anaerobes
Trova and Moxi - resistance is emerging for moxi
What FQs are active against atypical bacteria
most FQs are extremely active against legionella
What type of activity do FQs exhibit
rapid, concentration dependent bactericidal activity
T/F: FQs exhibit PAE against only gram(-) bacteria
False - display PAE against both gram (+) and (-) bacterial; (2hrs for gram (+), 2-4 for gram (-))
How does oral bioavailability of cipro compare to moxi/levo
Cipro - 70-75% F
Moxi/Levo - >90%
very good oral bioavailability allows for early conversion to oral therapy
how does food effect Tmax of FQs
coingestion with food delays peak serum concentrations
FQs obtain therapeutic concentrations in which tissues
prostate, lung, bronchial mucosa, sputum, bone
All FQs achieve high urinary concentrations and can be used to treat UTIs, except…?
Moxi and Gemi
T/F: FQs achieve good CSF concentrations
False: achieve minimal penetration into CSF