CILOXAN
Clinical safety rating: caution
Comprehensive clinical and safety monograph for CILOXAN (CILOXAN).
Ciprofloxacin, a fluoroquinolone antibiotic, inhibits bacterial DNA gyrase and topoisomerase IV, blocking DNA replication and transcription.
| Metabolism | Ciprofloxacin is partially metabolized in the liver via CYP1A2, producing four metabolites: desethyleneciprofloxacin (M1), sulfociprofloxacin (M2), oxociprofloxacin (M3), and formylciprofloxacin (M4). |
| Excretion | Renal: 50-70% unchanged drug; biliary: 15-20% as metabolites; fecal: 20-35% |
| Half-life | Terminal elimination half-life approximately 4 hours in patients with normal renal function; extended to 8-12 hours in moderate renal impairment (CrCl 30-50 mL/min) and up to 24 hours in severe impairment (CrCl <30 mL/min) |
| Protein binding | 20-40% bound to serum proteins, primarily albumin |
| Volume of Distribution | 1.5-2.5 L/kg, indicating extensive tissue penetration |
| Bioavailability | Ophthalmic: negligible systemic absorption (<5% of applied dose); oral: not applicable (ophthalmic use only) |
| Onset of Action | Ophthalmic solution: within 15-30 minutes for bacterial conjunctivitis; ophthalmic ointment: within 1-2 hours |
| Duration of Action | Ophthalmic solution: 6-8 hours post-instillation; ophthalmic ointment: 8-12 hours; clinical effect sustained with q.i.d. dosing |
1-2 drops in affected eye(s) every 2 hours while awake for 2 days, then every 4 hours for 5 days; or 1-2 drops 4 times daily for 7 days. Ointment: ½-inch ribbon into conjunctival sac 3 times daily for 2 days, then 2 times daily for 5 days.
| Dosage form | SOLUTION/DROPS |
| Renal impairment | No dosage adjustment required for ophthalmic use; systemic absorption is minimal. |
| Liver impairment | No dosage adjustment required for ophthalmic use; systemic absorption is minimal. |
| Pediatric use | Children ≥1 year: Same as adult dosing. Infants <1 year: Safety and efficacy not established. |
| Geriatric use | No specific adjustment; use same dosing as general adult population. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for CILOXAN (CILOXAN).
| Breastfeeding | Ciprofloxacin is excreted into breast milk; M/P ratio approximately 0.85-2.1. Risk of infant joint toxicity. Use only if benefit outweighs risk; consider temporary cessation of breastfeeding. |
| Teratogenic Risk | CILOXAN (ciprofloxacin) is contraindicated in pregnancy. Animal studies show arthropathy in immature animals; human data insufficient but fluoroquinolones may cause cartilage damage in neonates. Avoid in all trimesters unless no alternative. |
| Fetal Monitoring |
■ FDA Black Box Warning
Fluoroquinolones, including ciprofloxacin, may exacerbate muscle weakness in persons with myasthenia gravis. Avoid use in patients with a history of myasthenia gravis.
| Serious Effects |
Hypersensitivity to ciprofloxacin, any quinolone, or any component of the formulation. Use in patients with myasthenia gravis is contraindicated due to risk of exacerbation.
| Precautions | Prolonged use may result in overgrowth of nonsusceptible organisms including fungi. Hypersensitivity reactions may occur. Use with caution in patients with corneal epithelial defects due to risk of corneal perforation. Discontinue if rash or allergic reaction occurs. |
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| Monitor for maternal gastrointestinal disturbances, CNS effects, and tendonitis. Fetal monitoring not specific; avoid use in pregnancy. |
| Fertility Effects | No specific human fertility data. Animal studies indicate no adverse effects on fertility. |