Levofloxacin

Description: Levofloxacin is a synthetic broad-spectrum antibacterial agent. Chemically, levofloxacin, a chiral fluorinated carboxyquinilone, is the pure (-)-(S)-enantiomer of the racemic drug substance ofloxacin with a chemical name of: (-)-(S)-9-fluoro-2, 3-dihydro-3-methyl-10-(4-methyl-piperazinyl)-7-oxo-7Hpyrido [1,2,3,-de] [1,4] benzoxazine-6-carboxylic acid. Class: Levofloxacin is a member of the fluoroquinolone class of antibacterial agents Structure: The molecular formula is C18H20FN3O4, and the structural formula is:

Mechanism of action: Levofloxacin is the L-isomer of the racemate, ofloxacin, a quinolone antimicrobial agent. The antibacterial activity ofloxacin resides primarily in the L-isomer. The main mechanism of action of levofloxacin involves the inhibition of bacterial topoisomerase IV and DNA gyrase (both of which are type ii topoisomerases), enzymes required for DNA replication, transcription, repair and recombination. Levofloxacin has an in vitro activity against the following gram-negative and gram-positive microorganism. It is often bactericidal at concentrations equal to or slightly greater than inhibitory concentration. It is generally considered to be about twice as active as its isomer, ofloxacin. Mechanism of Resistance Fluoroquinolone resistance can arise through mutations in defined regions of DNA gyrase or topoisomerase IV, termed the Quinolone-Resistance Determining Regions (QRDRs), or through altered efflux. Fluoroquinolones, including levofloxacin, differ in chemical structure and mode of action from aminoglycosides, macrolides and -lactam antibiotics, including penicillins. Fluoroquinolones may, therefore, be active against bacteria resistant to these antimicrobials. Resistance to levofloxacin due to spontaneous mutation in vitro is a rare occurrence (range: 10-9 to 10-10). Cross-resistance has been observed between levofloxacin and some other fluoroquinolones, some microorganisms resistant to other fluoroquinolones may be susceptible to levofloxacin.

Microbiology: Levofloxacin has been shown to be active against most strains of the following microorganisms both in vitro and in clinical infections. Aerobic gram-positive microorganisms Enterococcus faecalis (Moderately susceptible) Staphylococcus aureus (methicillin-susceptible strains) Staphylococcus epidermidis (methicillin-susceptible strains) Staphylococcus saprophyticus Streptococcus pneumonia (including penicillin-resistant strains) Streptococcus pyogenes Aerobic gram-negative microorganisms Enterobacter cloacae Escherichia coli Haemophilus influenzae Haemophilus parainfluenzae Klebsiella pneumoniae Legionella pneumophila Salmonella species Moraxella catarrhalis Proteus mirabilis Pseudomonas auruginosa (Some strains of Pseudomonas aeruginosa may develop resistance rapidly during treatment with levofloxacin) Serratia marcescens Anaerobic microorganisms Bacteroides fragilis Clostridium perfringens Peptostreptococcus Other microorganism: Chlamydia pneumonia Mycoplasma pneumonia