Term
synthetic antimicrobials similar in structure to nalidixic acid, a quinolone |
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Definition
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Most widely employed floroquinolones |
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Definition
levofloxacin, ciprofloxacin |
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fluoroquinolones besides levofloxacin and ciprofloxacin are mainly used for treatment of |
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Definition
urinary tract and respiratory tract infections |
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interfere with bacterial DNA replication, transcription, and repair through inhibition of DNA gyrase (topoisomerase II) during bacterial prolieration. |
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Inhibits topoisomerase IV, essential for chromosomal DNA partitioning during bacterial cell division. |
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Definition
Third and Fourth generation fluoroquinolones |
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induce bacterial cell death by evoking cleavage of bacterial DNA |
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may exhibit synergism with B-lactams |
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Bactericidial vs. gram negatives, atypical, variable G+ activity |
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active vs. gram negative organisms: -Proteus, E. Coli, Klebsiella (PECK) -Shigella, Salmonella -Enterobacter -Pseudomonas -Haemophilus influenze -Moraxella ctarrhalis -Campylobacter -Neisseria gonorrhoeae -Citrobacter -Serratia -Vibrio -Legionella
-Mycoplasma, Chlamydia, Mycobacteriua variable G+ |
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most commonly prescribed 2nd gen fluoroquinolone |
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Definition
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Common indications: UTIs (Enterococcus, E. Coli, Enterobacter, Proteus, Pseudomonas, Klebsiella, etc) Prostatitis (PECK + pseudomonas) RTI (Moraxella, Haemophilus, Pseudomonas, Klebsiella) etc. Bacterial conjunctivitis and corneal ulcers Otitis externa |
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Definition
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bacterial conjunctivitis and corneal ulcers |
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Definition
Ciloxan Opthalmic Solution, Ointment |
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Definition
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First line agent for E. Coli (UTIs, prostatitis, bacteremia) |
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Definition
Ciprofloxacin, Levofloxacin |
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First line Enterobacter infections (UTIs etc.) (also SMX-TMX) |
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First line for Pseudomonas UTIs (Most active FQ vs. Pseudomonas) |
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First line for Pseudomonas infections associated w/ cystic fibrosis (also aztreonam?) |
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First line for Shigella infections |
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First line for Campylobacter infections (enteritis) |
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First line for Vibrio cholera (also doxycycline) |
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Other indications: Chancroid Plague Tularemia Anthrax Legionella pneumophila Mycobacterium avium intracellular complex (MAC) |
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Definition
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UTIs (PECK + Citrobacter) Prostatitis (E.Coli) Chlamydia trachomatis (urethritis) Skin infections (staph, streph, proteus) RTIs (Haemophilus influenze) Bacterial conjunctivitis and corneal ulcers (Ocuflox Opthalmic solution) Poor activity vs. psuedomoans |
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Definition
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Poor activity vs pseudomonas for second gen fluoroquinolone |
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Definition
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Similar spectrum to ciprofloxacin Least active fluoroquinolone, not for systemic infections |
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Definition
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UTIs (PECK+ pseudomonas, enterobacter, citrobacter) Prostatitis (E. COli) |
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Definition
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Third generation fluoroquinolones |
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Definition
Levofloxacin, Gemifloxacin |
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Most commonly prescribed fluoroquinolone |
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Definition
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Increased gram positive activity due to inhibition of topoisomerase IV Staph aureus, Strep pneumo, MDRSP, Strep pyogenes |
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Common indications: Sinusitis (moraxella, Haemophilus, Strep pneumo) Pneumonia and bronchitis (Moraxella, Haemophilus, Pseudomonas, Klebsiella, Legionella, Mycoplasma, Chlamydia, Strep pneumo, Staph aureus,etc.) UTIS Prostatitsi Skin and skin structure infections (staph aureus Strep pyo) Bacterial conjunctivitis |
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Other indications: Mycobacterium leprae (Hansen's disease) Cervicitis (Chlamydia trachomatis) |
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Gram negative spectrum of cirpofloxacin Increased gram positive activity vs. S. aurus, strep pneumo, MDRSP, Strep pyogenes) |
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Pneumonia and bronchitis (Moraxella, Haemophilus, Klebsiella, Mycoplasma, Chlamydia, Streptococcus pneumo, Staphylococcus aureus) |
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Fourth generation fluoroquinolones |
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Definition
Moxifloxacin, Gatifloxacin |
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Common fluroquinolone, lacks skin/soft tissue coverage, no pneumoniae |
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Only second generation that can do skin infections (Staph aureus, Strep pyo, Proteus mirabilis) |
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adds sinusitis, pneumonia and bronchitis |
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Definition
third generation (levofloxacin, gemifloxacin) |
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dubbed respiratory fluoroquinolone |
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Definition
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Adds increased activity vs. anerobes: Bacteroides fragilis, Fusobacterium, Peptostreptococcus) |
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Definition
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Vigamox, Moxeza, Zymaxid Opthalmic solutions for bacterial conjunctivitis |
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Resistance due to chromosomal mutations two mechanisms 1) altered target sites (DNA gyrase, topoisomerase IV) 2) decreased accumulation due to reduced premability or increased efflux |
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Cross resistance exists between |
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Only 35-75% absorbed orally low serum levels |
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Best oral bioavailability |
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Definition
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Cipro, ofloxacin, Lefofloxacin, moxifloxacin |
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Definition
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absorption decreased by multivalent cations (sucralfate, antacids, or dietary supplements) due to chelation |
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well distributed high concen. bone, urine, kidney, lung, prostatic tissue
accumulate sin macrophages and PMNs thereore useful in treatment of intracellular organisms (Legionella, Chlamydia, Mycoplasma) |
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which is fluoroquinolone is minimally metabolized? |
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parent and metabolites excreted to urine primary route of elimination for... half life extended during renal failure |
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Excreted primarily in bile |
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Gi intolerandce, CNS effeets (dizziness, headache, nausea) TENDINITIS NEPRHOTOXICITY (Crystalluria) Cardiac effects: PROLONGED QT interval Phototoxicity (SUN) |
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Contraindicated during PREGNANCY, nursing mothers, children under 18, due to potential for articular cartilage erosion |
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may enhance serum concentrations of theophylline, warfarin, cyclosproine through metabolic inhibition |
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