Norfloxacin: clinical pharmacology and clinical use

Norfloxacin, a nalidixic acid analog, is the first of the fluorinated quinolinecarboxylic acids to be marketed in the United States. It demonstrates potent antibacterial activity against aerobic, gram-negative bacteria including the Enterobacteriaceae, gentamicin-resistant Pseudomonas aeruginosa, and penicillin-resistant Neisseria gonorrhoeae. Norfloxacin exhibits good activity against methicillin-resistant and -sensitive Staphylococcus aureus, but less activity against most other aerobic, gram-positive organisms. Anaerobic bacteria are resistant to the drug. Resistance to norfloxacin is not plasmid mediated, but is secondary to bacterial mutation, and occurs less frequently than nalidixic acid resistance. Its pharmacokinetic properties after a 400-mg oral dose consist of a peak serum concentration of 1.3-1.58 micrograms/ml, an elimination half-life of 3-7 hours, and good penetration into kidney and prostatic tissues. Renal excretion is the major route of elimination. Norfloxacin is highly effective in the treatment of uncomplicated and complicated urinary tract infections, and gonococcal urethritis. Adverse effects are generally well tolerated and usually do not require discontinuation of therapy.