Levofloxacin, levo-isomer of the D,L-racemate ofloxacin, is a new fluo
roquinolone antibiotic approved for use in the United States in Decemb
er 1996. It has an extended spectrum of activity compared with older-g
eneration fluoroquinolones (ciprofloxacin, ofloxacin), with improved a
ctivity against gram-positive bacteria and excellent activity against
gram-negative bacteria and atypical organisms. Although its activity a
gainst anaerobic organisms is improved over that of earlier fluoroquin
olones, levofloxacin should not be considered a first-line anaerobic a
gent. It is available in an injectable form, as well as an oral formul
ation with virtually 100% oral bioavailability. The plasma elimination
half-life ranges from 6-8 hours in individuals with normal renal func
tion. Approximately 80% of drug is eliminated unchanged in urine throu
gh glomerular filtration and tubular secretion. The pharmacokinetics a
re not appreciably affected by age, gender, or race when differences i
n renal function and body mass and composition are taken into account.
Levofloxacin had impressive efficacy in clinical studies of community
-acquired pneumonia, acute bacterial exacerbations of chronic bronchit
is, acute sinusitis, skin and skin structure infections, and complicat
ed urinary tract infections and pyelonephritis. It is well tolerated;
its adverse event profile is similar to that of other fluoroquinolones
, with gastrointestinal and central nervous system effects reported mo
st commonly. Drug interactions are uncommon with levofloxacin; however
, coadministration with antacids or with other agents containing dival
ent or trivalent cations reduces levofloxacin absorption. The agent sh
ould prove to be more effective than older fluoroquinolones, especiall
y for infections caused by pneumococci highly resistant to penicillin.