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Ofloxacin

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From Pharmacopedia
Ofloxacin
Floxin (oral, US brand discontinued); Ocuflox (ophthalmic); Floxin Otic (otic)

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Titration strategies

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Summary
Common uses
Bacterial conjunctivitis/keratitis (ophthalmic)0, Otitis externa0, Acute otitis media with tympanostomy tubes (otic)0, Complicated UTI / pyelonephritis (oral; declining use)0, Bacterial prostatitis (oral)0
Pharmacy
Starting dose
Oral 200-400 mg BID; ophthalmic 1-2 drops in affected eye(s) q2-4h initially, then taper; otic 5-10 drops in affected ear BID
Preparations
200, 300, 400 mg tablets (mostly generic now); 0.3% ophthalmic solution; 0.3% otic solution
US FDA Max
800 mg/d
Pharmacology
Routes
Oral, ophthalmic, otic
Onset
Hours
Duration
12 hours
Half-life
~9 hours[1]
Bioavailability
~95% (oral)[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/levofloxacin[1]
Purported mechanism
Ofloxacin (racemic; the L-enantiomer levofloxacin is marketed separately and accounts for most antibacterial activity) inhibits bacterial DNA gyrase and topoisomerase IV, blocking DNA replication; the racemic form has fallen out of routine systemic use as levofloxacin's purified L-enantiomer supplanted it.0 Topical ophthalmic and otic formulations remain widely used in ENT and ophthalmology. Subject to all fluoroquinolone-class restrictions (tendinitis/rupture, peripheral neuropathy, QT prolongation)[1].

References

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  1. 1.0 1.1 1.2 1.3 FDA Prescribing Information, Floxin (ofloxacin), Janssen, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019735s058lbl.pdf