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. |
| Molecular Weight | 370.38 |
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 | Avoid in first trimester unless no safer alternative; associated with arthropathy and tendon damage in juvenile animals, but human data limited; use only if benefit justifies potential risk. |
| 2nd trimester | Avoid unless necessary; potential risk of fetal tendon damage; consider alternative antibiotics. |
| 3rd trimester | Avoid near term; theoretical risk of fetal tendon damage and central nervous system effects. |
Clinical note
Comprehensive clinical and safety monograph for LEVAQUIN IN DEXTROSE 5% IN PLASTIC CONTAINER (LEVAQUIN IN DEXTROSE 5% IN PLASTIC CONTAINER).
| Placental transfer | Levofloxacin crosses the placenta; fetal concentrations approximately 30-50% of maternal serum levels. No evidence of accumulation. |
| Breastfeeding | Levofloxacin is excreted into breast milk in small amounts (approximately 2% of maternal dose). Risk of infant arthropathy and tendon damage is theoretical but caution advised; alternative antibiotics preferred during breastfeeding. Monitor infant for signs of gastrointestinal disturbance or rash. |
■ 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 quinoloneHistory of tendinopathy with fluoroquinolonesMyasthenia gravis (may exacerbate weakness)Epilepsy or history of CNS disorders (increased seizure risk)Prolonged QT interval or concurrent use with QT-prolonging drugs
| 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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| Lactation Rating | L3 (Moderately Safe) – Use with caution, monitor infant. |
| 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. |
| 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. |
| Food/Dietary | Levofloxacin absorption is not significantly affected by food; however, concurrent intake of dairy products (milk, yogurt) or calcium-fortified juices may reduce absorption. Separate administration by at least 2 hours from antacids containing magnesium or aluminum, sucralfate, iron supplements, or zinc. |
| Clinical Pearls | Levofloxacin in D5W is a fluoroquinolone antibiotic used for infections including pneumonia, UTI, and skin infections. Monitor for QT prolongation, especially with concurrent QT-prolonging drugs or electrolyte abnormalities. Avoid in patients with myasthenia gravis due to risk of exacerbation. Use caution in elderly, renal impairment (adjust dose), and those with history of tendon disorders. Infuse over 60-90 minutes to reduce risk of infusion reactions. |
| Patient Advice | Complete the full course even if feeling better; skipping doses may reduce effectiveness. · Report symptoms like tendon pain, swelling, or rupture, especially in the Achilles tendon. · Avoid excessive sun exposure and use sunscreen; photosensitivity may occur. · Take with or without food; stay well hydrated. · Avoid concurrent use with dairy products, antacids, or iron supplements within 2 hours. · Inform your doctor of any history of seizures, arrhythmias, or myasthenia gravis. |