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28 Cards in this Set
- Front
- Back
Fluoroquinolones
-veterinary label drugs |
-enrofloxacin
-difloxacin -orbifloxacin -marbofloxacin -danofloxacin |
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Enrofloxacin
-labeled routes of administration |
-Injectable & Oral (dogs, cats)
-Injectable (cattle, swine) -don't use in dairy cattle 20 months of age or older or in veal calves |
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Difloxacin
-labeled routes of administration |
-tablets (dogs)
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Orbifloxacin
-labeled routes of administration |
-tablets (dogs)
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Marbofloxacin
-labeled routes of administration |
-tablets (dogs, cats)
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Daofloxacin
-labeled routes of administration |
-single injection regimen
-only for bovine respiratory disease in cattle not intended for dairy production and not intended to be processed for veal |
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Fluoroquinolones
-use in food animals |
-extralabel use in food animals is illegal
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Fluoroquinolone
-human labeled drug |
-ciprofloxacin
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Fluoroquinolones
-first fluoroquinolone |
-nalidixic acid
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Fluoroquinolones
-physiochemical properties |
-poor lipid solubility except in a pH 6-8
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Fluoroquinolones
-mechanism of action |
-bactericidal
-topoisomerase inhibition of 2 different bacterial enzyme targets -when altered by fluoroquinolones there is DNA strand breakage and cell death -Mammalian topoisomerase is unaffected |
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Fluoroquinolone
-spectrum |
-Aerobic bacteria
-variable with Strep -Mycoplasma -Ehrlichia -Rickettsia -Campylobacter -Lepto |
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Fluoroquinolone
-resistance development |
2 mechanisms
-alteration of target enzymes (topoisomerases) -decreased drug permeation into bacterial cells due to efflux pumps -Plasmid mediated resistance in Klebsiella and E. coli -Single-step mutations in Staph. aureus and Pseudomonas aeruginosa |
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Fluoroquinolone
-mutant selection window |
-use of fluoroquinolones in concentrations from the MIC to 10x the MIC
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Fluoroquinolone
-mutant prevention concentration |
-the concentration above which two concurrent mutations for resistance must occur for an organism to grow
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Fluoroquinolone
-bioavailability |
-high bioavailability from oral, IM, SC administration
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Fluoroquinolone
-time until peak plasma concentration reached |
-30-60 min
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Fluoroquinolone
-volume of distribution |
-very high
-can even reach therapeutic concentrations in brain and prostate |
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Fluoroquinolones
-primary route of excretion |
-kidneys
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Fluoroquinolones
-routes of excretion |
-kidneys (primary)
-de-ethylation reaction in liver biotransforming enrofloxacin to ciprofloxacin -biliary excretion |
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Fluoroquinolones
-is the same dose of cirpofloxacin and enrofloxacin equivalent? |
-no
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Fluoroquinolone
-efficacy |
-associated with peak concentration and the ratio of the area under the serum concentration curve to the pathogen MIC
-want to exceed the mutant prevention concentration and prevent proliferation of first step resistant mutants |
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Fluoroquinolone
-target for the AUC to pathogen MIC ration |
-minimum of 125
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Fluoroquinolone
-adverse reaction |
-articular cartilage damage; abnormal carriage of the carpal joint and weakness of the hind quarters (puppies (15-28 wks) on enrofloxacin at high doses for extended periods; also foals)
-retinal degeneration (cats; enrofloxacin) -increased seizure frequency (dogs on phenobarbitol) -raise serum theophylline levels (block cytochrome p450 isozyme IA-2) -irritating to the uterine mucosa |
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Enrofloxacin
-what is the dose label for dogs |
-5-20 mg/kg/day
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Enrofloxacin
-animals that get articular cartilage damage |
-puppies
-foals |
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Enrofloxacin
-possible predisposing factors to retinal degeneration in cats |
-large doses/high plasma concentration
-rapid IV administration -prolonged course of therapy -age -exposure to sunlight |
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Enrofloxacin
-dose for cats |
-5 mg/kg/day
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