FLOXIN
Clinical safety rating: caution
Comprehensive clinical and safety monograph for FLOXIN (FLOXIN).
Inhibition of bacterial DNA gyrase and topoisomerase IV, preventing DNA replication, transcription, repair, and recombination.
| Metabolism | Primarily hepatic metabolism via CYP450 isoenzymes (not major pathway); approximately 70-80% of drug excreted unchanged in urine via glomerular filtration and tubular secretion. |
| Excretion | Approximately 70-90% excreted unchanged in urine via glomerular filtration and tubular secretion; about 10-30% eliminated in feces via biliary excretion. |
| Half-life | Terminal elimination half-life of 10-14 hours in patients with normal renal function; prolonged in renal impairment (up to 40-50 hours in severe cases). |
| Protein binding | Approximately 30% bound to serum proteins, primarily albumin. |
| Volume of Distribution | 2.5-3.5 L/kg, indicating extensive tissue penetration, including into pleural fluid, bronchial mucosa, and bone. |
| Bioavailability | Oral: 95-100% (well absorbed); Ophthalmic: negligible systemic absorption; Intravenous: 100%. |
| Onset of Action | Oral: 1-2 hours; Ophthalmic: 30 minutes; Intravenous: within 30 minutes. |
| Duration of Action | Approximately 24 hours; dosing interval adjusted based on renal function. |
| Molecular Weight | 397.3 |
| Action Class | Selective Seretonin Reuptake inhibitors (SSRIs) |
| Brand Substitutes | Dedep 20mg Tablet, Fluget 20mg Tablet, Arkadep 20mg Tablet, Syine 20mg Tablet, Depilox 20mg Tablet, Fluchem 60mg Tablet, Maxitin 60mg Tablet, Bardep-TS Tablet, Flutop 60mg Tablet, Fastgen 60mg Tablet, Tariflox 200mg Tablet, Oflotas 200mg Tablet, Olox 200mg Tablet, Zenflox 200 Tablet, Onoff 200mg Tablet, Minimax 400mg Tablet, Ofloter 400mg Tablet, Ojen 400mg Tablet, Oflabin 400mg Tablet, Oxa 400mg Tablet, Fluget 10mg Tablet, Fluoxet 10mg Tablet, Bardep-H Tablet, Fluoxer 10mg Tablet, Maxitin 10mg Tablet |
400 mg orally every 12 hours for 10-14 days; ophthalmic solution: 1-2 drops in affected eye(s) every 2-4 hours for 2 days, then 1-2 drops 4 times daily for 10 days; otic solution: 5-10 drops in affected ear(s) twice daily for 10-14 days.
| Dosage form | TABLET |
| Renal impairment | CrCl <20 mL/min: 400 mg orally every 24 hours. Hemodialysis: 400 mg after dialysis on dialysis days. Peritoneal dialysis: 400 mg every 24 hours. |
| Liver impairment | No adjustment required for mild to moderate hepatic impairment (Child-Pugh A or B). Not studied in severe impairment (Child-Pugh C); use with caution. |
| Pediatric use | For ophthalmic use: Children ≥1 year: same as adult. For otic use: Children ≥6 months: same as adult. Systemic use not recommended for children <18 years due to risk of arthropathy. |
| Geriatric use | No specific adjustment required, but monitor renal function; adjust dose if CrCl <20 mL/min. Avoid use in elderly with tendon disorders or on corticosteroids due to increased risk of tendon rupture. |
| 1st trimester | Contraindicated due to risk of arthropathy and cartilage damage in developing fetus. |
| 2nd trimester | Contraindicated; potential for fetal harm based on animal studies. |
| 3rd trimester | Contraindicated; may cause fetal harm and increase risk of infantile diarrhea. |
Clinical note
Comprehensive clinical and safety monograph for FLOXIN (FLOXIN).
| Placental transfer | Extensive transfer across placenta; achieves therapeutic concentrations in fetal serum. |
| Breastfeeding | Excreted in small amounts into breast milk; potential for serious adverse reactions in nursing infants (e.g., cartilage damage, gastrointestinal effects). Use only if benefits outweigh risks. |
| Lactation Rating |
■ FDA Black Box Warning
Fluoroquinolones, including FLOXIN, are associated with an increased risk of tendinitis and tendon rupture, especially in patients over 60 years, those taking corticosteroids, and those with kidney, heart, or lung transplants. FLOXIN may also exacerbate muscle weakness in persons with myasthenia gravis. Avoid use in patients with a history of myasthenia gravis.
| Serious Effects |
Hypersensitivity to fluoroquinolonesTendonitis or tendon rupture historyChildren and adolescents <18 yearsPregnancyBreastfeeding (relative)
| Precautions | Tendinopathy and tendon rupture risk, Exacerbation of myasthenia gravis, Peripheral neuropathy, Central nervous system effects including seizures and increased intracranial pressure, QT prolongation and arrhythmias, Phototoxicity, Hypersensitivity reactions, Clostridium difficile-associated diarrhea, Blood glucose disturbances, Renal impairment dosing adjustment, Avoid excessive sunlight/UV exposure |
| Food/Dietary | No significant food interactions; absorption unaffected by food. Avoid caffeine-containing foods if excessive CNS stimulation occurs. |
Loading safety data…
| L3 - Moderately Safe |
| Teratogenic Risk | Fluoroquinolones (including ofloxacin) are generally avoided in pregnancy due to potential risk of arthropathy in animal studies and case reports of infant joint abnormalities. The FDA classifies ofloxacin as Pregnancy Category C. There is no adequate human data for first trimester; second and third trimester use is not recommended unless no alternative, due to risk of fetal cartilage damage. However, definitive teratogenicity in humans is not established. |
| Fetal Monitoring | Monitor for maternal adverse effects including tendonitis, tendon rupture, neuropathy, CNS effects. In pregnancy, fetal ultrasound monitoring for joint development if exposure occurs. No specific fetal monitoring required for short-term use, but avoid in pregnant women unless benefit outweighs risk. |
| Fertility Effects | No significant fertility effects reported in animal studies or human data. Ofloxacin does not appear to impair fertility in either sex. |
| Clinical Pearls | FLOXIN (ofloxacin) has oral bioavailability exceeding 95%; adjust dose in renal impairment (CrCl <50 mL/min). Avoid concurrent NSAIDs due to increased CNS stimulation risk. Reserve for infections with proven susceptibility to limit resistance. Prolonged use may cause phototoxicity; sun avoidance advised. |
| Patient Advice | Take at the same time each day with or without food; take missed doses when remembered unless near next dose. · Complete full course even if feeling better; do not skip doses. · Avoid excessive sun or tanning beds; use sunscreen and protective clothing due to photosensitivity. · Report tendon pain or swelling immediately; stop drug if tendinitis occurs. · May cause dizziness or lightheadedness; avoid driving until tolerance known. · Do not take with antacids, sucralfate, iron, or zinc supplements within 2 hours. · Use effective contraception during treatment; may reduce oral contraceptive efficacy. |