Pefloxacin is a
quinolone antibiotic
Quinolone antibiotics constitute a large group of broad-spectrum bacteriocidals that share a bicyclic core structure related to the substance 4-quinolone. They are used in human and veterinary medicine to treat bacterial infections, as wel ...
used to treat bacterial infections. Pefloxacin has not been approved for use in the United States.
History
Pefloxacin was developed in 1979 and approved in France for human use in 1985.
Licensed uses
*Uncomplicated gonococcal urethritis in males.
*Bacterial infections in the gastrointestinal system.
[
*Genitourinary tract infections.][
*Gonorrhoea, however, this use is no longer effective due to bacterial resistance.
Pefloxacin has been increasingly used as a veterinary medicine to treat microbial infections.
]
Mode of action
Pefloxacin is a broad-spectrum antibiotic
A broad-antimicrobial spectrum, spectrum antibiotic is an antibiotic that acts on the two major bacterial groups, Gram-positive and Gram-negative, or any antibiotic that acts against a wide range of disease-causing bacteria. These medications are ...
that is active against both Gram-positive
In bacteriology, gram-positive bacteria are bacteria that give a positive result in the Gram stain test, which is traditionally used to quickly classify bacteria into two broad categories according to their type of cell wall.
The Gram stain is ...
and Gram-negative
Gram-negative bacteria are bacteria that, unlike gram-positive bacteria, do not retain the crystal violet stain used in the Gram staining method of bacterial differentiation. Their defining characteristic is that their cell envelope consists ...
bacteria. It functions by inhibiting DNA gyrase
DNA gyrase, or simply gyrase, is an enzyme within the class of topoisomerase and is a subclass of Type II topoisomerases that reduces topological strain in an ATP dependent manner while double-stranded DNA is being unwound by elongating RNA-po ...
, a type II topoisomerase
DNA topoisomerases (or topoisomerases) are enzymes that catalyze changes in the topological state of DNA, interconverting relaxed and supercoiled forms, linked (catenated) and unlinked species, and knotted and unknotted DNA. Topological issues in ...
, and topoisomerase IV, which is an enzyme necessary to separate, replicated DNA, thereby inhibiting cell division.
Adverse effects
Tendinitis and rupture, usually of the Achilles tendon, are class-effects of the fluoroquinolones, most frequently reported with pefloxacin. The estimated risk of tendon damage during pefloxacin therapy has been estimated by the French authorities in 2000 to be 1 case per 23,130 treatment days as compared to ciprofloxacin where it has been estimated to be 1 case per 779,600.
References
External links
How Stuff Works - Cipro
Package insert information
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1,4-di-hydro-7-(1-piperazinyl)-4-oxo-3-quinolinecarboxylic acids
Fluoroquinolone antibiotics
4-Methylpiperazin-1-yl compounds