What it is
Levofloxacin is the active enantiomer of ofloxacin, a third-generation fluoroquinolone with a balanced spectrum: it covers Gram-negatives well and, unlike ciprofloxacin, also Gram-positives (pneumococcus) and atypical bacteria (Mycoplasma, Legionella, Chlamydia).
It is used in community-acquired pneumonia, some COPD exacerbations, prostatitis and some urinary infections. It shares the European restrictions of 2018–2019 with the other fluoroquinolones: it is not used for mild infections or when another antibiotic is appropriate, because of the risk of serious effects on tendons, nerves and the aorta.
Mechanism of action
It inhibits:
- DNA gyrase and topoisomerase IV (bacterial DNA synthesis and replication)
- Balanced cover: Gram-negative, Gram-positive and atypical bacteria
- A bactericidal effect (it actively kills bacteria)
At the counter
When to recommend it
- Community-acquired pneumonia when the doctor considers a quinolone necessary
- COPD exacerbation with a bacterial cause, if other antibiotics are not appropriate
- Bacterial prostatitis
- Complicated urinary infections, according to the culture result
When not to
- Allergy to fluoroquinolones
- History of tendinitis or tendon rupture
- Pre-existing peripheral neuropathy
- Under 18s without a clear justification
Warnings
- Important Tendinitis / tendon rupture: the same risk as ciprofloxacin. Avoid over 60 with corticosteroids.
- Important Peripheral neuropathy: rare but potentially irreversible.
- Caution Photosensitivity: less than with other fluoroquinolones, but present. Full sun protection.
- Caution Interactions: it prolongs the QT interval; caution with antiarrhythmics and other medicines that prolong it.
Pharmacokinetics
- Absorption
- Excellent oral absorption. Bioavailability of 99%. Peak at 1–2 hours. Food has minimal effect.
- Distribution
- Wide distribution. Excellent penetration into lung, prostate and urine. Protein binding of 24–38%. It crosses the placenta.
- Metabolism
- Limited metabolism. Most of it is eliminated unchanged.
- Elimination
- 87% renal elimination. Longer half-life than ciprofloxacin (6–7 hours).
Levofloxacin vs azithromycin
| Aspect | Levofloxacin | Azithromycin |
|---|---|---|
| Cover of atypical bacteria | Good | Excellent |
| Gram-negative cover | Excellent | Poor |
| Lung penetration | Good | Excellent |
| Cardiac risk (QT) | Present | Present |
| Tendinitis risk | Present | Minimal |
Levofloxacin in pneumonia when Gram-negatives are likely or other options do not work. Azithromycin for purely atypical infection or if quinolones are contraindicated.
Self-assessment
Three questions. When you check your answers you will see the explanation for each one.
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Levofloxacin is a third-generation quinolone with better balanced cover: Gram-negative, Gram-positive and atypical bacteria. Ciprofloxacin is weak against Gram-positives.
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Levofloxacin gives broader cover (Gram-negative, Gram-positive and atypical). Azithromycin is better if only an atypical bacterium is suspected or if quinolones are contraindicated.
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As with all fluoroquinolones, tendinitis and neuropathy are serious. Tendon pain or tingling should make the patient stop at once and get checked.
Training content. It does not replace the summary of product characteristics or clinical judgement.