indication

For the treatment of uncomplicated gonococcal urethritis in males and for gram-negative-bacterial infections in the gastrointestinal system and the genitourinary tract.

pharmacology

Pefloxacin is a fluoroquinolone antibiotic. Flouroquinolones such as pefloxacin 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

The bactericidal action of pefloxacin 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.

toxicity

Adverse reactions include peripheral neuropathy, nervousness, agitation, anxiety, and phototoxic events (rash, itching, burning) due to sunlight exposure.

biotransformation

Hepatic. Primary metabolites are pefloxacin N-oxide and norfloxacin.

absorption

Well absorbed by the oral route.

half life

8.6 hours

drug interactions

Aminophylline: Pefloxacin may increase the effect of aminophylline.

Calcium: Formation of non-absorbable complexes

Iron Dextran: Formation of non-absorbable complexes

Magnesium: Formation of non-absorbable complexes

Oxtriphylline: Pefloxacin may increase the effect of oxtriphylline.

Theophylline: Pefloxacin may increase the effect of theophylline.