FLOXIN IN DEXTROSE 5%
Clinical safety rating: caution
Comprehensive clinical and safety monograph for FLOXIN IN DEXTROSE 5% (FLOXIN IN DEXTROSE 5%).
Inhibits bacterial DNA gyrase (topoisomerase II) and topoisomerase IV, preventing DNA replication and transcription.
| Metabolism | Hepatic metabolism via CYP1A2 and possibly other CYP enzymes; renal excretion of unchanged drug and metabolites. |
| Excretion | Primarily renal (approximately 70-90% unchanged drug), with 5-10% biliary/fecal elimination. |
| Half-life | Terminal elimination half-life: 6-8 hours (prolonged in renal impairment, up to 20-30 hours in severe impairment). |
| Protein binding | 20-32% (primarily to albumin). |
| Volume of Distribution | 2.0-3.0 L/kg (indicates extensive tissue penetration, including lung, prostate, and bone). |
| Bioavailability | Not applicable (IV administration only); oral floxin has bioavailability ~70-80%, but FLOXIN IN DEXTROSE 5% is IV. |
| Onset of Action | Intravenous: immediate (minutes); peak concentrations achieved by end of infusion. |
| Duration of Action | Approximately 12 hours (supports twice-daily dosing). |
400 mg intravenously every 12 hours.
| Dosage form | INJECTABLE |
| Renal impairment | If CrCl 20-50 mL/min: 400 mg IV every 24 hours; if CrCl <20 mL/min or hemodialysis: 400 mg IV every 48 hours. |
| Liver impairment | No dosage adjustment required for mild to moderate hepatic impairment (Child-Pugh A/B). Not studied in severe impairment (Child-Pugh C). |
| Pediatric use | Not recommended for children under 18 years due to risk of musculoskeletal adverse events. |
| Geriatric use | Use with caution; reduce dose based on renal function. Monitor for tendonitis and QT prolongation. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for FLOXIN IN DEXTROSE 5% (FLOXIN IN DEXTROSE 5%).
| Breastfeeding | Ofloxacin is excreted into human breast milk. The milk-to-plasma ratio is approximately 0.12 to 0.98. Due to potential for serious adverse reactions (arthropathy, CNS effects) in the nursing infant, breastfeeding is not recommended during therapy. |
| Teratogenic Risk | FLOXIN (ofloxacin) is contraindicated in pregnancy. Fluoroquinolones cause arthropathy in juvenile animals and may damage fetal cartilage. Use is not recommended in any trimester. There is no safe trimester for use. |
■ FDA Black Box Warning
Fluoroquinolones have been 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. May exacerbate muscle weakness in myasthenia gravis.
| Serious Effects |
Hypersensitivity to ofloxacin or any fluoroquinolone; history of tendinopathy with fluoroquinolone use; myasthenia gravis; concomitant use with tizanidine; pregnancy (category C) and nursing mothers; children under 18 years (except for specific approved indications).
| Precautions | Avoid use in patients with known aortic aneurysm or dissection; increased risk of peripheral neuropathy, CNS effects including seizures and increased intracranial pressure; photosensitivity; QT prolongation; hypoglycemia; and tendon disorders. |
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| Fetal Monitoring |
| If inadvertent exposure occurs, monitor fetal growth and joint development (ultrasound). For the mother, monitor for tendon pain, CNS effects, and gastrointestinal disturbances. No specific fetal monitoring is routinely indicated because use is avoided. |
| Fertility Effects | Fluoroquinolones have not been associated with impaired fertility in animal studies. However, ofloxacin may cause sperm DNA damage in vitro; clinical significance in humans is unknown. No specific fertility effects are documented. |