Certain fluoroquinolones have been shown to elevate the serum concentr
ations of the immunosuppressant cyclosporine. It is th us important to
investigate the potential interaction between levofloxacin, a new flu
oroquinolone anitmicrobial agent, and the pharmacokinetics of cyclospo
rine. Twelve healthy subjects (6 men, 6 women) were enrolled in and co
mpleted a placebo-controlled, randomized, double-blind, two-phase cros
sover study. Subjects were given a single oral 10-mg/kg dose of cyclos
porine solution during multiple-dose twice-daily oral treatment with p
lacebo or 500 mg of levofloxacin. Blood cyclosporine concentrations we
re measured for 48 hours after each cyclosporine dose for pharmacokine
tic evaluation. Cyclosporine pharmacokinetic parameters were comparabl
e and not significantly different in the absence and presence of levof
loxacin. Results of this study suggest that a clinically important pha
rmacokinetic interaction between levofloxacin and cyclosporine is unli
kely to occur during concurrent therapy.