Lomefloxacin Clinical Pharmacokinetics

Abstract

Lomefloxacin is a quinolone antibiotic with chemical and microbiological properties similar to most commercially available agents of this class. There are differences, however, between lomefloxacin and other quinolones in activity against specific micro-organisms, a situation that is typical of most antibiotic classes. The pharmacokinetics of lomefloxacin support once- or twice-daily dosage, depending on the pathogen or site of infection. This is a result of its relatively high serum concentrations and long half-life. The outstanding pharmacokinetic features of lomefloxacin are its high degree of tissue distribution, lack of significant metabolism (and, therefore, no competitive drug interactions with other metabolised drugs showing a common metabolic pathway), and good oral absorption. Like most fluoroquinolones, lomefloxacin can chelate with heavy metals. However, this interaction can be eliminated by administering lomefloxacin 2h before the cation-containing products. Dosage adjustments are required in patients with renal dysfunction. However, patients with liver disease do not require alterations in lomefloxacin dosage regimens. The safety profile, lack of significant drug interactions and convenience of administration make lomefloxacin a useful agent in specific clinical settings.

Intestinal elimination of ofloxacin enantiomers in the rat: evidence of a carrier-mediated process

“…In humans, temafloxacin, sparfloxacin, and fleroxacin show significant fecal elimination (12,33). In rats, lomefloxacin is significantly eliminated by the intestine, and this is not influenced by probenecid, a substrate of the anionic transporter (8,38). In rats, 7% of a parenterally administered ciprofloxacin dose is eliminated via the intestine, mostly the jejunum (28).…”

Quinolone Antibacterials

“…2, this volume) which determine their physicochemical characteristics. Whereas lomefloxacin is used as the racemic compound with no available data on single enantiomer activities (FREEMAN et al 1993;MITSCHER et al 1989), sparfloxacin is used as a pure enantiomer . The (-)-and (+)-isomers differ by as much as 100-fold in activity against Gram-positive and Gramnegative bacteria HAYAKAWA 1986).…”

Kinetic Characterization of Secretory Transport of a New Ciprofloxacin Derivative (CNV97100) across Caco-2 Cell Monolayers**This work has been submitted for the partial fulfillment of the requirement for a Ph.D. Degree in Pharmaceutics at the University of Valencia, Valencia, Spain

“…In addition, these compounds appeared to have better bioavailability 4. For example, bioavailabilities of methyl fluoroquinolone analogs, such as lomefloxacin (85–90%)5 and sparfloxacin (90%),6 are higher than the bioavailability of ciprofloxacin (50–70%) 4…”