Pefloxacin Mesilate

(BANM, rINNM)
Pefloxacin Mesilate Chemical formula
Synonyms: EU-5306 (pefloxacin); Mesilato de pefloxacino; Pefloksacino mesilatas dihidratas; Pefloksacyny mezylan dwuwodny; Pefloksasiinimesilaattidihydraatti; Pefloxacin Mesilate Dihydrate; Pefloxacin mesylát dihydrát; Pefloxacin Mesylate late de; Péfloxacine (mésilate de) dihydraté; Pefloxacini Mesilas; Pefloxacini mesilas dihydricus; Pefloxacinmesilatdihydrat; Pefloxacin-mezilát-dihidrát; 1589RB (pefloxacin); 41982-RP. 1Ethyl-6-fluoro-1,4-dihydro-7-(4-methyl-1-piperazinyl)-4-oxo-3quinolinecarboxylic acid methanesulphonate dihydrate.
Cyrillic synonym: Пефлоксацина Мезилат.

💊 Chemical information

Chemical formula: C17H20FN3O3,CH4O3S,2H2O = 465.5.
CAS — 70458-92-3 (pefloxacin); 70458-95-6 (pefloxacin mesilate).
ATC — J01MA03.
ATC Vet — QJ01MA03.

Pharmacopoeias.

In Chin. and Eur..

Ph. Eur. 6.2

(Pefloxacin Mesilate Dihydrate). A fine, white or almost white powder. Freely soluble in water; slightly soluble in alcohol; very slightly soluble in dichloromethane. A 1% solution in water has a pH of 3.5 to 4.5. Store in airtight containers. Protect from light.

💊 Profile

Pefloxacin is a fluoroquinolone antibacterial with actions and uses similar to those of ciprofloxacin. It also has bactericidal activity against Mycobacterium leprae and has been tried in the treatment of leprosy. Pefloxacin has a longer plasma half-life than ciprofloxacin (about 8 to 13 hours) and is also extensively metabolised, the principal metabolite being N-desmethylpefloxacin. Pefloxacin is given orally or by intravenous infusion as the mesilate in the treatment of susceptible infections. Doses are expressed in terms of the base; pefloxacin mesilate 558.5 mg is equivalent to about 400 mg of pefloxacin. The usual dose is 400 mg twice daily. A single oral dose of 800 mg may be used in the treatment of gonococcal urethritis in men and acute uncomplicated cystitis in women. Fluoroquinolones have caused adverse effects on the musculoskeletal system and in the case of pefloxacin this has led to restrictions in some countries.

Adverse effects.

References to adverse effects with pefloxacin.
1. Chevalier X, et al. A case of destructive polyarthropathy in a 17year-old youth following pefloxacin treatment. Drug Safety 1992; 7: 310–14
2. Al-Hedaithy MA, Noreddin AM. Hypersensitivity anaphylactoid reaction to pefloxacin in a patient with AIDS. Ann Pharmacother 1996; 30: 612–14
3. Chang H, et al. Pefloxacin-induced arthropathy in an adolescent with brain abscess. Scand J Infect Dis 1996; 28: 641–3.

Pharmacokinetics.

References to the pharmacokinetics of pefloxacin.
1. Bressolle F, et al. Pefloxacin clinical pharmacokinetics. Clin Pharmacokinet 1994; 27: 418–46.

💊 Preparations

Proprietary Preparations

Braz.: Floxinon†; Peflacin; Pefloxidina†; Cz.: Abaktal; Fr.: Peflacine; Gr.: Idrostamin; Labocton; Londoman†; Peflacin†; Hung.: Abaktal; Peflacine; India: Ifipef†; Pefbid; Pelox; Proflox; Qucin; Indon.: Dexaflox; Noflexin; Peflacine; Ital.: Peflacin; Peflox; Malaysia: Peflacine†; Perti†; Mex.: Nopriken†; Peflacina; Philipp.: Floxin; Pol.: Abaktal; Peflacine; Port.: Peflacine; Rus.: Abaktal (Абактал); Pelox (Пелокс); Perti (Перти); Unikpef (Юникпеф); Spain: Azuben†; Peflacine†; Thai.: Abaktal†; Peflacine†; Turk.: Peflacine; Venez.: Peflacina†; Perti†.
Published May 08, 2019.