Levofloxacin. A review of its antibacterial activity, pharmacokinetics and therapeutic efficacy

Drugs. 1994 Apr;47(4):677-700. doi: 10.2165/00003495-199447040-00008.


Levofloxacin, an oral fluoroquinolone antibacterial agent, is the optical S-(-) isomer of ofloxacin. In vitro it is generally twice as potent as ofloxacin. Levofloxacin is active against most aerobic Gram-positive and Gram-negative organisms and demonstrates moderate activity against anaerobes. Drug penetration into body tissues and fluids is rapid and widespread after oral administration. In clinical trials conducted in Japan, oral levofloxacin has demonstrated antibacterial efficacy against a variety of infections, including upper and lower respiratory tract, genitourinary, obstetric, gynaecological and skin and soft tissues. In comparative trials with ofloxacin, levofloxacin, at half the daily dosage of ofloxacin, showed equivalent efficacy and a reduced incidence of adverse effects in the treatment of lower respiratory tract and complicated urinary tract infections. Levofloxacin has a tolerability profile similar to that of other oral fluoroquinolones, with gastrointestinal and central nervous system effects reported most commonly. Theophylline dosage adjustment does not appear to be necessary in patients receiving concomitant levofloxacin. Coadministration with antacids or with other drugs containing divalent or trivalent cations reduces levofloxacin absorption. Thus, levofloxacin has potential as a broad spectrum antibacterial drug in the treatment of a variety of infections. However, clinical trials recruiting non-Japanese patients are in progress and these results will form a basis on which future recommendations for the broader use of levofloxacin can be made.

Publication types

  • Review

MeSH terms

  • Administration, Oral
  • Aging / metabolism
  • Bacteria / drug effects*
  • Bacterial Infections / drug therapy*
  • Biological Availability
  • Drug Interactions
  • Female Urogenital Diseases / drug therapy*
  • Half-Life
  • Humans
  • Levofloxacin*
  • Male Urogenital Diseases*
  • Microbial Sensitivity Tests
  • Ofloxacin* / pharmacokinetics
  • Ofloxacin* / pharmacology
  • Ofloxacin* / therapeutic use
  • Respiratory Tract Infections / drug therapy*
  • Stereoisomerism


  • Levofloxacin
  • Ofloxacin