Pefloxacin

Pefloxacin

Pefloxacin
Systematic (IUPAC) name
1-ethyl-6-fluoro-7-(4-methylpiperazin-1-yl)-4-oxo-quinoline-3-carboxylic acid
Pharmacokinetic data
Bioavailability 100%
Protein binding 20–30%
Metabolism Hepatic
Biological half-life 8.6 hours
Excretion Mostly renal, also biliary
Identifiers
CAS Registry Number  YesY
ATC code J01
PubChem CID:
DrugBank  YesY
ChemSpider  YesY
UNII  YesY
KEGG  YesY
ChEBI  YesY
ChEMBL  YesY
Chemical data
Formula C17H20FN3O3
Molecular mass 333.358 g/mol
 YesY   

Pefloxacin is a quinolone drug used to treat bacterial infections. Pefloxacin has not been approved for use in the United States.

Contents

  • History 1
  • Licensed uses 2
  • Mode of action 3
  • Adverse effects 4
  • References 5
  • External links 6

History

Pefloxacin was developed in 1979 and approved in France for human use in 1985.[1]

Licensed uses

  • Uncomplicated gonococcal urethritis in males.[2]
  • Bacterial infections in the gastrointestinal system.[2]
  • Genitourinary tract infections.[2]
  • Gonorrhoeae. however this indication is no longer effective due to bacterial resistance.[3]

Pefloxacin has been increasingly used as a veterinary medicine to treat microbial infections.[4]

Mode of action

Pefloxacin is a broad-spectrum antibiotic that is active against both Gram-positive and Gram-negative bacteria. It functions by inhibiting DNA gyrase, a type II topoisomerase, and topoisomerase IV,[5] which is an enzyme necessary to separate, replicated DNA, thereby inhibiting cell division.

Adverse effects

Tendinitis and rupture, usually of the Achilles tendon, are a class-effects of the fluoroquinolones, most frequently reported with pefloxacin.[6] 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.[7]

References

  1. ^ http://www.bailii.org/ew/cases/EWHC/Patents/2008/2413.html
  2. ^ a b c http://www.pefloxacin.com/pefloxacin_usage.htm
  3. ^
  4. ^ http://www.pefloxacin.com/pefloxacin_other.html
  5. ^
  6. ^
  7. ^

External links

  • How Stuff Works - Cipro
  • Package insert information