Pefloxacin is a quinolone antibiotic used to treat bacterial infections. Pefloxacin has not been approved for use in the United States.
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| Bioavailability | 100% |
| Protein binding | 20–30% |
| Metabolism | Hepatic |
| Elimination half-life | 8.6 hours |
| Excretion | Mostly renal, also biliary |
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| ECHA InfoCard | 100.067.807 |
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| Formula | C17H20FN3O3 |
| Molar mass | 333.363 g·mol−1 |
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History
editPefloxacin was developed in 1979 and approved in France for human use in 1985.[1]
Licensed uses
edit- Uncomplicated gonococcal urethritis in males.[2]
- Bacterial infections in the gastrointestinal system.[2]
- Genitourinary tract infections.[2]
- Gonorrhoea, however, this use 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
editPefloxacin 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
editTendinitis and rupture, usually of the Achilles tendon, are 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
edit- ^ Generics (UK) Limited v. Daiichi Pharmaceutical Co. Ltd & Daiichi Sankyo Co. Ltd, 2016-07-13 (EWHC 15 October 2008), Text.
- ^ a b c "Reasons for prescribing Pefloxacin". pefloxacin.com. Archived from the original on 2016-03-05.
- ^ Centers for Disease Control and Prevention (CDC) (April 2007). "Update to CDC's sexually transmitted diseases treatment guidelines, 2006: fluoroquinolones no longer recommended for treatment of gonococcal infections". MMWR Morb. Mortal. Wkly. Rep. 56 (14): 332–6. PMID 17431378.
- ^ "Alternative uses for Pefloxacin". pefloxacin.com. Archived from the original on 2016-06-17.
- ^ Drlica K, Zhao X (1 September 1997). "DNA gyrase, topoisomerase IV, and the 4-quinolones". Microbiol Mol Biol Rev. 61 (3): 377–92. doi:10.1128/mmbr.61.3.377-392.1997. PMC 232616. PMID 9293187.
- ^ Khaliq Y, Zhanel GG (October 2005). "Musculoskeletal injury associated with fluoroquinolone antibiotics". Clin Plast Surg. 32 (4): 495–502, vi. doi:10.1016/j.cps.2005.05.004. PMID 16139623.
- ^ Casparian JM, Luchi M, Moffat RE, Hinthorn D (May 2000). "Quinolones and tendon ruptures". South. Med. J. 93 (5): 488–91. doi:10.1097/00007611-200093050-00008. PMID 10832946.