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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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