Drug Detail

Levofloxacin

Last Updated June 10, 2016

Trade Names

Tavanic, Levofloxacin-Winthrop, Spec Levofloxacin, Aspen Levofloxacin, Austell-Levofloxacin, Mylan-Levofloxacin, Sandoz Levofloxacin, Tavaloxx, Zybact

Drug Classification

Fluoroquinolone broad-spectrum antimicrobial

Formulations

250 mg, 500 mg, 750 mg tablets; 250 mg/50 mL, 500 mg/100 mL, 750 mg/150 mL for intravenous infusion

Indications and Pharmacology

Indication: treatment of mild, moderate, and severe infections caused by susceptible bacterial strains; can be used in sinusitis, lower respiratory tract, urinary tract, and soft-tissue infections; used in treatment of multidrug-resistant tuberculosis in combination with other second-line drugs.*

Recommended for multidrug-resistant tuberculosis patients < 8 years and adults who may not tolerate moxifloxacin.*

Mechanism of action: inhibition of topoisomerase IV and DNA gyrase enzymes, disrupting bacterial DNA replication, transcription, repair, recombination.*

Pharmacokinetics: rapidly absorbed from gastrointestinal tract and widely distributed throughout body; Tmax 1-2 hours; half-life 6-9 hours.*

Dosage

Adult Dose: 250-1000 mg daily orally; 750 mg daily generally preferred for most patients with normal renal function.

Patients should be cautioned to maintain an adequate fluid intake.

Can also be given intramuscularly or intravenously.

Use in Renal or Hepatic Insufficiency: 

  • Renal insufficiency: normal initial dose then reduced dose and frequency; creatinine clearance 20-50 mL/min, 50% of initial dose; creatinine clearance 10-19 mL/min, 125 mg every 12-48 hours; < 10 mL/min or on haemodialysis or peritoneal dialysis, 125 mg every 24-48 hrs after dialysis.
  • No adjustments needed for hepatic insufficiency.

Use in Pregnancy and Breastfeeding*: US Pregnancy Category C; use only if benefits outweigh potential risk to the foetus. Likely excreted in breast milk, with potential for serious adverse reactions in breast-fed infants.

Some recommend avoiding in pregnancy and lactation; others recommend using with caution.

Use in Children: (younger than 8 years of age) 10-15 mg/kg/day orally (maximum 1g)

Warnings

Contraindicated in patients with hypersensitivity to levofloxacin or any other quinolone antimicrobials.

Associated with increased risk of tendinitis and tendon rupture, especially in patients > 60 years, taking corticosteroid drugs, or with kidney, heart, or lung transplantations.*

Anaphylactic and/or hypersensitivity reactions may occur after the first dose; fever, rash, severe dermatologic reactions, vasculitis, arthralgia, myalgia, serum sickness, allergic pneumonitis, renal toxicity, hepatic toxicity, anaemia, thrombocytopenia, leucopenia, and other haematologic abnormalities may occur after multiple doses.*

Reports of other reactions and adverse events including central nervous system effects, Clostridium difficile–associated diarrhoea, peripheral neuropathy, prolongation of the QT interval, musculoskeletal disorders in paediatric patients, blood glucose disturbances, photosensitivity/phototoxicity, development of drug resistant bacteria.*

Patients should be cautioned to maintain an adequate fluid intake.

If given with warfarin, monitor prothrombin time, international normalised ratio.

Discontinue with signs of peripheral neuropathy to avoid irreversible damage.

Rapid or bolus intravenous infusion can cause hypotension, levofloxacin should be infused intravenous slowly over 60- 90 minutes.

Avoid prolonged sunlight exposure during treatment.

Drug–Drug Interactions

Potentiation of hypoglycaemic actions of oral hypoglycaemia drugs (glyburide, glibenclamide) or insulin.*

Possible increased QTc interval of electrocardiogram with concomitant class IA or class III antiarrhythmics.*

Decreased absorption of levofloxacin with multivalent cation-containing products (eg, magnesium/aluminium antacids, sucralfate, didanosine chewable/buffered tablets or paediatric powder, highly buffered drugs, products containing calcium, zinc, or iron) within 2 hours.*

Possible increased concentration or effects of concomitant warfarin (see Warnings).

Possible increased risk of central nervous system stimulation and convulsive seizures with concomitant nonsteroidal antiinflammatory.

Caution should be used with concomitant use of theophylline; theophylline levels should be monitored and dose adjustments made appropriately.*

Possible false-positive urine screening tests for opiates.

Considerations for Special Populations

Geriatric: increased risk of severe hepatotoxicity, tendinopathy, especially with concomitant corticosteroid use, and prolongation of QT interval.*

Paediatric: limited safety information, only indicated for treatment of anthrax exposure and plague; increased incidence of musculoskeletal disorders in paediatric patients, causes arthropathy and osteochondrosis in juvenile animals.*

Diabetics receiving insulin or an oral hypoglycaemic drug should discontinue levofloxacin immediately in event of a hypoglycaemic reaction.*

Renal insufficiency: may require dose reduction.

Use with caution in patients with predisposition to seizures or lower seizure threshold.

QT interval: avoid using in patients with known QT prolongation, uncorrected hypokalemia or receiving class IA or class III antiarrhythmics; caution should be used in patients receiving other drugs known to prolong the QT interval or with congenital QT prolongation.*

See above for pregnancy and lactation.

Adverse Effects

Nausea, diarrhoea, abnormal liver function tests, vomiting, rash, abdominal pain, pain in extremities, convulsions, increased intracranial pressure, toxic psychosis, central nervous system events (headache, nervousness, agitation, restlessness, drowsiness, insomnia, anxiety, nightmares, paranoia, dizziness, confusion, tremor, hallucination, depression, suicidal thoughts or acts), hypersensitivity reactions, cardiac disturbances (QT prolongation and Torsades de points), hepatic necrosis, interstitial nephritis, blood disorders, pseudomembranous colitis, peripheral neuropathy, tendonitis and tendon ruptures, phototoxicity.*

Seizures may occur in patients with underlying central nervous system disease.

*Information from US prescribing information.
Information from Aurum Institute Drugs on the Go.