| Indication |
For the treatment of bacterial infections of the respiratory tract
(chronic bronchitis) and urinary tract, and as a pre-operative
prophylactic to prevent urinary tract infection caused by: S.pneumoniae, H.influenzae, S.aureus, P.aeruginosa, E. cloacae, P. mirabilis, C. civersus, S. asprphyticus, E.coli, and K.pneumoniae. |
| Pharmacodynamics |
Lomefloxacin is a fluoroquinolone antibiotic used to treat
chronic bronchitis, as well as complicated and uncomplicated urinary
tract infections. It is also used as a prophylactic or preventative
treatment to prevent urinary tract infections in patients undergoing
transrectal or transurethral surgical procedures. Flouroquinolones such
as lomefloxacin possess excellent activity against gram-negative aerobic
bacteria such as E.coli and Neisseria gonorrhoea as well as gram-positive bacteria including S. pneumoniae and Staphylococcus aureus.
They also posses effective activity against shigella, salmonella,
campylobacter, gonococcal organisms, and multi drug resistant
pseudomonas and enterobacter. |
| Mechanism of action |
Lomefloxacin is a bactericidal fluoroquinolone agent with activity
against a wide range of gram-negative and gram-positive organisms. The
bactericidal action of lomefloxacin results from interference with the
activity of the bacterial enzymes DNA gyrase and topoisomerase IV, which
are needed for the transcription and replication of bacterial DNA. DNA
gyrase appears to be the primary quinolone target for gram-negative
bacteria. Topoisomerase IV appears to be the preferential target in
gram-positive organisms. Interference with these two topoisomerases
results in strand breakage of the bacterial chromosome, supercoiling,
and resealing. As a result DNA replication and transcription is
inhibited. |
| Absorption |
Rapid and nearly complete with approximately 95% to 98% of a single oral dose being absorbed. |
| Volume of distribution |
Not Available |
| Protein binding |
10% |
| Metabolism |
Minimally metabolized although 5 metabolites have been
identified in human urine. 65% appears as the parent drug in urine and
9% as the glucuronide metabolite. |
| Route of elimination |
The urinary excretion of lomefloxacin was virtually complete
within 72 hours after cessation of dosing, with approximately 65% of the
dose being recovered as parent drug and 9% as its glucuronide
metabolite. |
| Half life |
8 hours |
| Clearance |
- 271 mL/min/1.73 m2 [creatinine clearance of 110 mL/min/1.73 m2]
- 31 mL/min/1.73 m2 [creatinine clearance of 0 mL/min/1.73 m2]
|
| Toxicity |
Adverse reactions include peripheral neuropathy, nervousness,
agitation, anxiety, and phototoxic events (rash, itching, burning) due
to sunlight exposure. |
