Levofloxacin

Products

Levofloxacin is commercially available as film-coated tablets and as an infusion solution (Tavanic, generic). It was approved in many countries in 1998. Generics came on the market in 2011. In 2018, a solution for a nebulizer was registered (Quinsair). The racemate ofloxacin is available as tablets (Tarivid), eye drops, and eye ointment (Floxal).

Structure and properties

Levo-Ofloxacin is the active -enantiomer of the racemate ofloxacin (C18H20FN3O4, Mr = 361.4 g/mol). It is a pale yellow to light yellow crystalline powder that is sparingly soluble in water. In drugs, it is present as levofloxacin hemihydrate (levofloxacin – 0.5 H2O).

Effects

Levofloxacin (ATC J01MA12, ATC S01AX19) has bactericidal properties against Gram-positive and Gram-negative pathogens. The effects are due to inhibition of bacterial topoisomerases II and IV, enzymes involved in DNA replication, transcription, and DNA repair.

Indications

For the treatment of bacterial infectious diseases with susceptible germs. Levofloxacin is used for respiratory, urinary, skin, and soft tissue infections, among others. Possible indications include acute sinusitis, acute bronchitis, pneumonia, and complicated urinary tract infections.

Dosage

According to the drug label. Intake is independent of meals. However, interactions with drugs taken at the same time are possible (see below). Excessive sun exposure should be avoided because of the risk for photosensitization.

Contraindications

Full precautions can be found in the drug label.

Interactions

Di- or trivalent metal ions such as iron, copper, zinc, magnesium, and aluminum may form poorly soluble complexes with levofloxacin and reduce its absorption. Appropriate drugs should be taken at least two hours apart. Levofloxacin is excreted mainly unchanged by the kidney. Other interactions have been described with vitamin K antagonists, antidiabetic agents, NSAIDs, sucralfate, probenecid, cimetidine, and ciclosporin.

Adverse effects

The most common potential adverse effects include insomnia, headache, dizziness, nausea, vomiting, and diarrhea, as well as elevated liver enzyme levels. Quinolones are known to cause sometimes severe, rare adverse reactions in various organs, which are listed below (discussion e.g., Liu, 2010). Therefore, attention to precautions is important.