Fluoroquinolones
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Fluoroquinolones | •Ciprofloxacin – Cipro
•Levofloxacin – Levaquin
•Moxifloxacin – Avelox
•Gemifloxacin – Factive
These are the first line drugs against Atypicals (weird bugs)!
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Quinolone MoA | Selectively inhibit type II topoisomerases
Topoisomerase IV target for G+
DNA gyrase target for G-
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Mech of resistance to Quinolones | Chromosomal (gyr A/B or Par C/E mutations)
Permeability alterations
Efflux
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Quinolone PK | Concentration dependent
Rapidly Cidal
Widely distrib. into most body tissues including lungs (pneumonia), prostate, and CSF
Has Post-antiBx effect, but not clinically used b/c toxic in high doses
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Clinical use of Cipro | UTIs: Cipro & Levo. Cipro used when SPACE suspected
Systemic infect: Cipro (except for Pneumococcus & enterococcus).
Intra-abdominal infect: Cipro+Flagyl
Cipro (& maybe Levo) are the only ORAL drugs for pseudomonas
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Clinical Use of Levo, Moxi, and Gemi | Levo, Moxi, Gemi: MSSA, sometimes MRSA. Cover S. pneumo (unlike Cipro) and E. faecalis, but not faecium.
Listeria
Moxi has increased anaerobe coverage. Good for some IA infections.
Gemi & Moxi for CAP, AECB (acute exacer of chron bronchitis), DRS
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Quinolone best activity: | Enterobacteriaceae, H. ducreyii, H. influenza, M. catarrhalis moxi, gemi & increased Strep, N. gonorrhoeae resistance has increased and coverage is not as excellent as in the past, ‘atypicals’ Chlamydia, Mycoplasma, Legionella
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Quinolone activity against Pseudomonas | Ciprofloxacin > gemifloxacin=moxifloxacin> levofloxacin
UTI only, cipro & levo are adequate alone
Pyelonephritis: Cipro
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Quinolone activity against S. pneumoniae (Pneumococcus) | Gemifloxacin > moxifloxacin> levofloxacin (No Cipro!)
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Quinolone activity against S. aureus | Moxifloxacin> levofloxacin
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Quinolone activity against Anaerobes (eg. B. fragilis) | Moxifloxacin is the best against anaerobes such as B. frag.
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Alternative Quinolone uses |
Alternative Uses:
•Traveler’s diarrhea
•Osteomyelitis
•Otitis media
•Bioterrorism related anthrax post exposure prophylaxis
•Empiric therapy for severe CAP in a high risk patient or those requiring hospitalization
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Quinolone counseling tips | finish all medication
minimize UV exposure, sunlight
water/hydration
bioavailability issues (Don't take with Ensure, calcium, antacids, etc.)
arthropathy (joint pain) & tendon rupture risk
hypo/hyperglycemia
teratogenicity
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Ciprofloxacin IV dose | 750mg Q12h
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Quinolone ADRs | Tendonitis & arthropathy
hyper/hypglycemia when used with antidiabetic agents
QT prolongation
Cipro: vasculitis
Teratogenicity
Many DDIs: Multivalent cations, sucralfate, cimetidine, didanosine, caffeine, theophylline, warfarine, foscarnet,
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Primary Use of Quinolones | •Multi drug resistant Streptococcus pneumoniae (5% decade ago 35-45% today)
•Complicated UTI with P. aeruginosa in which Cipro PO would be preferred over IV therapy
•Prostate infections
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