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μμ© κΈ°μ : Difloxacin is a concentration-dependent bactericidal agent. * It actively enters the bacterial cell and targets **DNA-gyrase** (a type-II topoisomerase) and topoisomerase IV. * Inhibition of these enzymes β prevents DNA supercoiling and uncoiling β halts DNA synthesis and transcription. * The net result is rapid disruption of bacterial cell replication and subsequent cell death.
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- Susceptible infections (MIC β€ 0.25 micrograms/mL) Β· 7.5 mg/kg Β· PO Β· q24h Β· Administer non-fasted. Appears safe and adequately absorbed, but further investigation is warranted. Unknown if it should be avoided in young, growing horses.
- Susceptible infections Β· 5-10 mg/kg Β· PO Β· q24h Β· 2-3 days beyond the cessation of clinical signs (maximum 30 days) Β· Administer preferably on an empty stomach, unless GI upset occurs.
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- Hypersensitivity to difloxacin or other quinolones
- Immature dogs during the rapid growth phase (2-8 months in small/medium breeds; up to 18 months in large/giant breeds)
- Cats (relative contraindication due to nausea/vomiting and unknown ophthalmic/retinal safety)
- Food-producing animals (extra-label use prohibited by federal law)
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- Anorexia
- Vomiting
- Diarrhea
- Cartilage abnormalities (arthropathies) in growing animals
- CNS stimulation or seizures (rare)
- Facial erythema and edema (at high doses)
- Weight loss (at high doses)
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- Antacids (Mg++, Al+++, Ca++) Β· May bind to difloxacin and prevent its absorption; separate doses by at least 2 hours.
- Dairy Products Β· Calcium content may decrease absorption; separate doses by at least 2 hours.
- Aminoglycosides, 3rd-gen Cephalosporins, Extended-spectrum Penicillins Β· Unpredictable synergism may occur against some bacteria, particularly Pseudomonas aeruginosa.
- Cyclosporine Β· May exacerbate nephrotoxicity and reduce the metabolism of systemic cyclosporine.
- Glyburide Β· Severe hypoglycemia is possible.
- Iron and Zinc supplements Β· Decreased difloxacin absorption; separate doses by at least 2 hours.
- Methotrexate Β· Increased methotrexate levels possible, resulting in toxicity.
- Nitrofurantoin Β· May antagonize the antimicrobial activity of fluoroquinolones; concomitant use is not recommended.
- Phenytoin Β· Difloxacin may alter phenytoin blood levels.
- Probenecid Β· May block tubular secretion and increase the blood level and half-life of difloxacin.
- Sucralfate Β· May inhibit absorption of difloxacin; separate doses by at least 2 hours.
- Theophylline Β· Difloxacin may increase theophylline blood levels, potentially leading to toxicity.
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- Clinical efficacy (resolution of infection)
- Gastrointestinal signs (appetite, vomiting, diarrhea)
- CNS signs (especially in patients with a history of seizures)
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In dogs, doses up to 2.5X the maximum recommended dose (25 mg/kg) for 30 days did not cause overly significant adverse effects. Observed signs included facial erythema/edema, diarrhea, decreased appetite, and weight loss. Treatment should be supportive and symptomatic.
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