|
Absorption
Oral
T max is 1 to 2 h. Food slightly prolongs T max (1 h) and decreases C max 14%. Can be administered with or without food. About 99% bioavailable. Steady state is reached within 48 h following 500 mg dose. C max is 5.7 mcg/mL and C min is 0.5 mcg/mL following multiple oral doses of 500 mg; for multiple doses of 750 mg, C max is 8.6 mcg/mL and C min is 1.1 mcg/mL.
Oral solution
Peak concentration decreased 25% when taken with food. Take 1 h before or 2 h after eating.
Injection
C max is about 6.2 mcg/mL after 500 mg dose infused over 60 min and about 11.5 mcg/mL after 750 mg dose infused over 90 min. Steady state is reached within 48 h following a once-daily (500 or 750 mg) regimen.
Oral and IV formulations are equivalent in AUC; therefore, route of administration is interchangeable.
Distribution
Vd is 74 to 112 L. Protein binding is approximately 24% to 38%.
Metabolism
Undergoes limited metabolism. Desmethyl and N-oxide, the only metabolites identified in humans, have little relevant pharmacological activity.
Elimination
Total body Cl is 144 to 226 mL/min. Renal Cl is 96 to 142 mL/min. Terminal t ½ is 6 to 8 h.
Oral
Primarily (87%) excreted as unchanged drug in urine, less than 4% in the feces.
Special Populations
Renal Function Impairment
Cl is reduced and t ½ prolonged in patients with CrCl less than 50 mL/min. Dosage adjustment required. Hemodialysis and peritoneal dialysis do not remove levofloxacin from the body.
Hepatic Function Impairment
Pharmacokinetics not expected to be affected by hepatic function impairment.
|
