Expert Opin Pharmacother. 1999 Nov;1(1):109-19. doi: 10.1517/14656566.1.1.109.


Levofloxacin (DR-3355, Daiichi) is a new fluoroquinolone antibiotic which is the active isomer of ofloxacin (DL-8280, Daiichi). By removing the inactive isomer, the in vitro activity of levofloxacin is 8-128 times higher than that of ofloxacin. This means that bacterial species, which have borderline susceptibility to ofloxacin and other first generation fluoroquinolones (e.g., pneumococci and organisms causing atypical pneumonia), are considerably more sensitive to levofloxacin. The pharmacokinetics of levofloxacin, which is available for both oral and i.v. administration, are characterised by a very high bioavailability, low (30-40%) protein binding, high tissue concentrations and elimination via the kidneys with minimal liver metabolism. As a consequence of the low degree of metabolism, levofloxacin does not interact with other drugs to any major extent. The safety and efficacy of levofloxacin are well documented in lower respiratory tract infections, skin and soft tissue infections, and urinary tract infections. The safety profile seems advantageous and the risks of phototoxicity, CNS toxicity and cardiac reactions (prolongation of QT-time) are low. Serious liver toxicity, leading to the recent withdrawal of trovafloxacin, has not been a problem in levofloxacin studies. Levofloxacin is a valuable addition to the group of fluoroquinolone antibiotics.

Publication types

  • Review

MeSH terms

  • Animals
  • Anti-Infective Agents / adverse effects
  • Anti-Infective Agents / pharmacokinetics
  • Anti-Infective Agents / pharmacology
  • Anti-Infective Agents / therapeutic use*
  • Bacteria / drug effects
  • Bacterial Infections / drug therapy*
  • Bacterial Infections / microbiology
  • Clinical Trials as Topic
  • Humans
  • Levofloxacin*
  • Ofloxacin / adverse effects
  • Ofloxacin / pharmacokinetics
  • Ofloxacin / pharmacology
  • Ofloxacin / therapeutic use*


  • Anti-Infective Agents
  • Levofloxacin
  • Ofloxacin