levofloxacin

Brand: Levaquin

⚠ BBW Beers Criteria Prototype: ciprofloxacin
Drug Class: fluoroquinolone antibiotic
Drug Family: antibiotic
Subclass: respiratory fluoroquinolone (third-generation)
Organ Systems: infectious-diseaserespiratory

Mechanism of Action

Inhibits DNA gyrase and topoisomerase IV, preventing DNA supercoiling relaxation and strand separation required for replication; bactericidal with concentration-dependent killing. Enhanced gram-positive activity vs. ciprofloxacin including S. pneumoniae.

DNA gyrase (topoisomerase II)topoisomerase IV

Indications

  • community-acquired pneumonia
  • hospital-acquired pneumonia
  • acute exacerbation of chronic bronchitis
  • sinusitis
  • urinary tract infections
  • pyelonephritis
  • skin/soft tissue infections
  • anthrax prophylaxis and treatment

Contraindications

  • fluoroquinolone hypersensitivity
  • children (relative — damage to growing cartilage)
  • concurrent QTc-prolonging drugs (relative)

Adverse Effects

Common

  • nausea
  • diarrhea
  • headache
  • insomnia

Serious

  • tendinopathy/tendon rupture (especially Achilles)
  • peripheral neuropathy (irreversible)
  • CNS effects (seizures, psychosis, hallucinations)
  • QTc prolongation
  • aortic aneurysm/dissection
  • hypoglycemia/hyperglycemia
  • C. difficile colitis
  • photosensitivity

Pharmacokinetics (ADME)

Absorption 99% oral bioavailability; IV and oral dosing are interchangeable
Distribution widely distributed; high tissue concentrations; crosses BBB
Metabolism minimal hepatic
Excretion renal (87% unchanged); dose adjustment in CKD
Half-life 6–8 hours
Onset rapid (1 hour)
Peak 1–2 hours (oral)
Duration 24 hours (once-daily dosing)
Protein Binding 24–38%
Vd large

Drug Interactions

Drug / Agent Mechanism Severity
antacids/sucralfate/iron/zinc chelation of fluoroquinolone; separate by 2 hours before or 6 hours after major
warfarin inhibits CYP1A2; increases INR major
QTc-prolonging drugs additive QTc prolongation major
NSAIDs increased CNS adverse effects including seizure risk moderate
sulfonylureas/insulin disrupts glucose homeostasis; hypoglycemia or hyperglycemia moderate

Nursing Considerations

  1. Screen patients for contraindications before administration: prior fluoroquinolone tendinopathy, myasthenia gravis, QTc prolongation, or use of QTc-prolonging drugs.
  2. Instruct patients to stop levofloxacin and notify the provider immediately if tendon pain or swelling develops — Achilles tendon rupture can be permanent.
  3. Monitor glucose in diabetic patients; fluoroquinolones can cause both hypoglycemia and hyperglycemia.
  4. Obtain baseline ECG in patients on QTc-prolonging drugs, those with hypokalemia, or hypomagnesemia.

Clinical Pearls

  • Levofloxacin has near-100% oral bioavailability, enabling seamless IV-to-oral step-down without pharmacokinetic changes in dosing — a major advantage for stewardship-conscious practitioners.
  • Fluoroquinolone use should be reserved for situations without safer alternatives per FDA guidance; the FDA updated black box warnings in 2016 and 2018 to include peripheral neuropathy, CNS effects, aortic aneurysm risk, and myasthenia gravis exacerbation.

Safety Profile

Pregnancy avoid
Lactation avoid
Renal Adjustment Required
Hepatic Adjustment Not required
TDM Not required
Guideline Update pending