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Levofloxacin

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From Pharmacopedia
Levofloxacin
Levaquin (US brand discontinued); generic and ophthalmic Quixin/Iquix

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Summary
Common uses
Community-acquired pneumonia0, Acute bacterial sinusitis0, Complicated UTI / pyelonephritis0, Bacterial prostatitis0, Anthrax prophylaxis and treatment0, Bacterial conjunctivitis/keratitis (topical)0
Pharmacy
Starting dose
500-750 mg PO/IV once daily
Preparations
250, 500, 750 mg tablets; 25 mg/mL oral solution; 25 mg/mL IV (premix bags 250, 500, 750 mg); 0.5%, 1.5% ophthalmic solutions
US FDA Max
750 mg/d
Pharmacology
Routes
Oral, IV, topical ophthalmic
Onset
Hours
Duration
24 hours
Half-life
~6-8 hours[1]
Bioavailability
~99% (oral; matched 1:1 IV-to-PO conversion)[1]
Pregnancy
Avoid in pregnancy where alternatives exist (animal cartilage toxicity; class-wide concern).[citation needed]
Legal status
Rx-only in US. Carries the same fluoroquinolone-class Boxed Warnings as ciprofloxacin: tendinitis/tendon rupture (especially elderly, corticosteroid co-use), peripheral neuropathy, CNS effects, worsening of myasthenia gravis[1]
Purported mechanism
Levofloxacin (the L-enantiomer of ofloxacin) inhibits bacterial DNA gyrase (topoisomerase II) and topoisomerase IV, blocking supercoiling and decatenation required for DNA replication; the result is bactericidal.0 Among "respiratory fluoroquinolones" (with moxifloxacin and gemifloxacin) — broader S. pneumoniae and atypical coverage than ciprofloxacin, making it more useful in CAP. QT prolongation, hypoglycemia, and aortic dissection signals are recognized class effects[1].

References

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  1. 1.0 1.1 1.2 1.3 FDA Prescribing Information, Levaquin (levofloxacin), Janssen, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020634s072,020635s075,021721s041lbl.pdf