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Ciprofloxacin

From Pharmacopedia
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Ciprofloxacin
Cipro, Cipro XR, Ciloxan (ophthalmic)

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Summary
Common uses
Complicated UTI / pyelonephritis0, Bacterial prostatitis0, Bacterial gastroenteritis (selected)0, Pseudomonal coverage (selected)0, Anthrax prophylaxis and treatment0, Bacterial conjunctivitis/keratitis (topical)0
Pharmacy
Starting dose
500-750 mg PO BID; 400 mg IV q8-12h
Preparations
250, 500, 750 mg IR tablets; 500, 1000 mg ER tablets (XR); 250, 500 mg/5 mL oral suspension; 200, 400 mg IV; 0.3% ophthalmic solution and ointment; 0.2% otic
US FDA Max
~1500 mg/d (oral); 1200 mg/d (IV)
Pharmacology
Routes
Oral, IV, topical ophthalmic, otic
Onset
Hours
Duration
8-12 hours
Half-life
4 hours[1]
Bioavailability
~70% (oral; reduced by divalent cations — antacids, iron, calcium, dairy)[1]
Pregnancy
Avoid in pregnancy where alternatives exist (animal cartilage toxicity; class-wide concern); use only when benefit clearly outweighs.[citation needed]
Legal status
Rx-only in US. Carries Boxed Warnings for tendinitis/tendon rupture (especially elderly, corticosteroid co-use, post-transplant), peripheral neuropathy (sometimes irreversible), CNS effects (psychosis, seizure), and worsening of myasthenia gravis[1]
Purported mechanism
Ciprofloxacin inhibits bacterial DNA gyrase (topoisomerase II, dominant in gram-negatives) and topoisomerase IV (dominant in gram-positives), preventing supercoiling and decatenation needed for DNA replication; the result is bactericidal at clinically achievable concentrations.0 CYP1A2 inhibitor — clinically meaningful interactions with theophylline, caffeine, and tizanidine. QT prolongation, hypoglycemia (especially with sulfonylureas), and aortic aneurysm/dissection signals add to the class-wide reasons FDA has progressively restricted fluoroquinolone use to indications where alternatives have failed[1].

References

  1. 1.0 1.1 1.2 1.3 FDA Prescribing Information, Cipro (ciprofloxacin), Bayer, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/019537s086,019847s060,019857s062,020780s041lbl.pdf