Levofloxacin

Levofloxacin is a broad-spectrum fluoroquinolone antibiotic. It is used for severe bacterial infections, including complicated urinary tract infections and kidney infections.

Important note: Due to the risk of serious side effects (tendons, nerves, mental health), the EMA and the BfArM have restricted the use of fluoroquinolones for uncomplicated infections. Levofloxacin should only be used for severe infections when no suitable alternatives are available.

Mechanism of action:

• Inhibits bacterial DNA gyrase (topoisomerase II) and topoisomerase IV
• Prevents bacterial DNA replication and transcription
• Bactericidal effect (kills bacteria)

Spectrum of activity:

• Very broad spectrum against gram-positive and gram-negative pathogens
• Also atypical pathogens (mycoplasma, chlamydia, legionella)
• Good tissue penetration (kidney, prostate, lung)

Pharmacokinetics:

• High oral bioavailability (~99%)
• Once-daily dosing is sufficient
• Excreted via the kidneys (good urinary tract concentrations)

Levofloxacin is suitable for:

• Complicated urinary tract infections including pyelonephritis
• Complicated prostatitis
• Severe infections when other antibiotics are not suitable

NOT suitable for:

• Uncomplicated bladder infection, unless other commonly recommended antibiotics are unsuitable (Rote-Hand-Brief!)
• Mild to moderately severe infections for which alternatives are available
• Children and adolescents (cartilage damage)
• Pregnancy and breastfeeding
• History of tendon disorders while taking fluoroquinolones

Urinary tract infections:

• Uncomplicated (only if there is no alternative): 250 mg once daily for 3 days
• Complicated incl. pyelonephritis: 500 mg once daily for 7–14 days

Available strengths:

• 250 mg, 500 mg film-coated tablets

Dose adjustment in renal insufficiency (with 500 mg once daily):

• GFR 20–49 ml/min: 250 mg every 24 hours (after the initial dose)
• GFR 10–19 ml/min: 125 mg every 24 hours

How to take:

• Once daily, regardless of meals
• With sufficient water (at least 1 glass)
• At least 2 hours apart from: antacids, iron supplements, zinc, magnesium, dairy products

Important notes:

• Avoid sun and UV radiation (phototoxicity!)
• If tendon pain occurs, stop taking it immediately and contact a doctor
• Drink sufficient fluids
• Complete the full course of antibiotics

Levofloxacin must not be taken in cases of:

• Hypersensitivity to fluoroquinolones
• Tendon disorder after previous fluoroquinolone therapy
• Epilepsy (lowering of the seizure threshold)
• Pregnancy and breastfeeding
• Children and adolescents under 18 years of age

Caution in:

• Elderly patients (increased risk of tendon rupture)
• Renal insufficiency (dose adjustment)
• G6PD deficiency (risk of hemolysis)
• QT interval prolongation or medications that prolong the QT interval
• Myasthenia gravis (worsening possible)
• Diabetes (blood sugar dysregulation possible)

Tendon warning: Fluoroquinolones can cause tendon inflammation and tendon ruptures, particularly of the Achilles tendon. The risk increases with concomitant corticosteroid therapy and in older people.

Common (1–10%):

• Nausea, diarrhea
• Headache, dizziness
• Sleep disturbances
• Elevated liver enzymes

Uncommon (0.1–1%):

• Skin rash, phototoxicity
• Fungal infections
• Anxiety, confusion
• Muscle and joint pain

Rare but serious (Rote-Hand-Brief):

• Tendinitis
• Tendon rupture (especially of the Achilles tendon)
• Peripheral neuropathy (tingling, numbness)
• Psychiatric disorders (depression, suicidal thoughts, psychosis)
• Aortic aneurysm/dissection
• QT interval prolongation
• Hypoglycemia, up to and including coma

FQAD (fluoroquinolone-associated disability): In rare cases, side effects affecting the tendons, nerves, and mental health can be long-lasting.