LEVAQUIN IN DEXTROSE 5% IN PLASTIC CONTAINER
Clinical safety rating: caution
Comprehensive clinical and safety monograph for LEVAQUIN IN DEXTROSE 5% IN PLASTIC CONTAINER (LEVAQUIN IN DEXTROSE 5% IN PLASTIC CONTAINER).
Levofloxacin is a fluoroquinolone antibacterial that inhibits bacterial DNA gyrase (topoisomerase II) and topoisomerase IV, thereby inhibiting DNA replication and transcription.
| Metabolism | Levofloxacin is minimally metabolized; approximately 87% is excreted unchanged in urine. It undergoes limited hepatic metabolism to desmethyl-levofloxacin and N-oxide metabolites. |
| Excretion | Primarily renal excretion as unchanged drug (approximately 87% within 48 hours); less than 4% as metabolites; biliary/fecal excretion accounts for <5%. |
| Half-life | Terminal elimination half-life is approximately 6-8 hours in patients with normal renal function (creatinine clearance >80 mL/min); prolonged in renal impairment (up to 30-50 hours in severe impairment). |
| Protein binding | Approximately 24-38% bound to serum proteins, mainly albumin. |
| Volume of Distribution | Volume of distribution is approximately 1.1-1.5 L/kg, indicating extensive distribution into tissues including lung, kidney, and skin tissues. |
| Bioavailability | Intravenous: 100% bioavailability since administered directly into the bloodstream. |
| Onset of Action | Intravenous: Onset of action within 30-60 minutes for systemic infections; peak serum concentrations achieved by end of infusion (1 hour). No oral route applicable. |
| Duration of Action | Duration of action is approximately 24 hours, supporting once-daily dosing for most indications; therapeutic concentrations maintained over the dosing interval. |
750 mg intravenously every 24 hours for 5 days. Alternatively, 500 mg intravenously every 24 hours for 7-14 days depending on infection.
| Dosage form | INJECTABLE |
| Renal impairment | CrCl 20-49 mL/min: 750 mg IV every 48 hours or 500 mg IV every 24 hours (loading dose 500-750 mg). CrCl <20 mL/min or hemodialysis: 500 mg IV every 48 hours (loading dose 500 mg). Continuous ambulatory peritoneal dialysis: 500 mg IV every 48 hours. |
| Liver impairment | No dose adjustment required for mild to moderate hepatic impairment (Child-Pugh A or B). Not studied in severe hepatic impairment (Child-Pugh C); use with caution. |
| Pediatric use | Safety and effectiveness in children <18 years have not been established due to risk of musculoskeletal toxicity. Use only for inhalational anthrax or plague: 8 mg/kg IV every 12 hours (max 250 mg/dose) for 60 days (anthrax) or 14 days (plague). |
| Geriatric use | No specific dose adjustment solely based on age. Adjust dose based on renal function (CrCl). Elderly patients may have reduced CrCl; monitor renal function and consider increased risk of tendonitis and tendon rupture. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for LEVAQUIN IN DEXTROSE 5% IN PLASTIC CONTAINER (LEVAQUIN IN DEXTROSE 5% IN PLASTIC CONTAINER).
| Breastfeeding | Levofloxacin is excreted into human breast milk in small amounts. The M/P ratio is approximately 0.8. The relative infant dose is <5% of maternal weight-adjusted dose. However, because of potential adverse effects on infant bone and joint development, caution is advised. Alternative antibiotics are preferred during breastfeeding. |
| Teratogenic Risk | Fluoroquinolones, including levofloxacin, are associated with arthropathy in juvenile animals. Human data are limited but do not indicate a major teratogenic risk. However, due to potential fetal toxicity, use is not recommended during pregnancy unless no alternative exists. First trimester exposure may be associated with increased risk of spontaneous abortion; second and third trimester exposure has been linked to fetal cartilage damage theoretically, though definitive human data are lacking. |
■ FDA Black Box Warning
Fluoroquinolones, including levofloxacin, are associated with an increased risk of tendinitis and tendon rupture, especially in patients over 60 years of age, those taking corticosteroids, and those with kidney, heart, or lung transplants. They also exacerbate muscle weakness in myasthenia gravis and may cause irreversible peripheral neuropathy.
| Serious Effects |
["Hypersensitivity to levofloxacin or any other fluoroquinolone","History of tendinopathy or tendon rupture with fluoroquinolone use","Use in children under 18 years of age (except for specific indications)","Use in pregnant or breastfeeding women unless benefit outweighs risk"]
| Precautions | ["Tendon effects: Discontinue at first sign of tendon pain or inflammation.","Myasthenia gravis exacerbation: Avoid use in patients with known myasthenia gravis.","Peripheral neuropathy: May occur rapidly and become irreversible.","Central nervous system effects: May cause dizziness, confusion, and increased intracranial pressure.","QT prolongation: Use with caution in patients with risk factors for QT prolongation.","Hypersensitivity reactions: Serious and occasionally fatal reactions may occur.","Clostridioides difficile-associated diarrhea: Consider in patients presenting with diarrhea.","Photosensitivity: Avoid excessive sunlight or UV light exposure."] |
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| Fetal Monitoring | Monitor maternal renal function, pregnancy status, and fetal development via ultrasound. Assess for signs of tendonitis or tendon rupture in the mother. No specific fetal monitoring is required beyond routine prenatal care. |
| Fertility Effects | Fluoroquinolones have not been shown to adversely affect human fertility. Animal studies have not demonstrated impaired fertility at therapeutic doses. |