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. |
| 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 | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for FLOXIN (FLOXIN).
| Breastfeeding | Ofloxacin is excreted into human breast milk; M/P ratio not well established (limited data). American Academy of Pediatrics considers it compatible with breastfeeding, but caution is advised due to potential adverse effects on infant joint development. Alternate agents may be preferred. |
| 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. |
■ 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 fluoroquinolones","History of myasthenia gravis","Concurrent administration with tizanidine","Patients with known QT prolongation or risk factors for arrhythmias (unless benefit outweighs risk)"]
| 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"] |
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| 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. |