Norfloxacin Pivoxil

(BANM, rINNM)
Synonyms: Norfloxacine, Pivoxil de; Norfloxacini Pivoxil; Norfloxacino pivoxilo. Pivaloyloxymethyl 1-ethyl-6-fluoro-1,4-dihydro-4-oxo7-(piperazin-1-yl)quinoline-3-carboxylic acid.
Cyrillic synonym: Норфлоксацина Пивоксил.

💊 Chemical information

Chemical formula: C22H28FN3O5 = 433.5.

💊 Adverse Effects and Precautions

As for Ciprofloxacin.

💊 Interactions

As for Ciprofloxacin.

💊 Antimicrobial Action

As for Ciprofloxacin, although norfloxacin is less potent in vitro. Norfloxacin is not active against Chlamydiaceae, mycoplasmas, or mycobacteria.

💊 Pharmacokinetics

About 30 to 40% of an oral dose of norfloxacin is absorbed. Peak plasma concentrations of about 1.5 micrograms/mL occur about 1 to 2 hours after a 400-mg oral dose; the presence of food can delay absorption. Norfloxacin is about 14% bound to plasma proteins. It is probably widely distributed, but information is limited. Norfloxacin penetrates well into tissues of the genito-urinary tract. It crosses the placenta. Relatively high concentrations are achieved in bile. The plasma half-life is 3 to 4 hours and may be prolonged in renal impairment; a value of 6.5 hours or more has been reported when creatinine clearance is below 30 mL/minute per 1.73 m 2 . About 30% of a dose is excreted unchanged in the urine within 24 hours, producing high urinary concentrations; norfloxacin is least soluble at a urinary pH of 7.5. Urinary excretion is by tubular secretion and glomerular filtration and is reduced by probenecid, although plasma concentrations of norfloxacin are not generally affected. Some metabolism occurs, possibly in the liver, and several metabolites have been identified in urine, some with antibacterial activity. About 30% of an oral dose is recovered from the faeces.

💊 Uses and Administration

Norfloxacin is a fluoroquinolone antibacterial with properties similar to those of ciprofloxacin, but it is generally less potent in vitro. Norfloxacin is used mainly in the treatment of urinarytract infections and for the treatment of gonorrhoea. Norfloxacin is given orally at least 1 hour before, or 2 hours after, food or milk. In urinary-tract infections the usual dose is 400 mg twice daily for 3 to 10 days. Treatment may need to be continued for up to 12 weeks in chronic relapsing urinary-tract infections; it may be possible to reduce the dose to 400 mg once daily if there is an adequate response within the first 4 weeks. A 28-day course of treatment with a dose of 400 mg twice daily should be given for acute or chronic bacterial prostatitis. For details of reduced doses to be used in renal impairment, see below. A single oral dose of 800 mg is given in the treatment of uncomplicated gonorrhoea. Eye drops containing 0.3% of norfloxacin are used to treat eye infections. The pivaloyloxymethyl salt of norfloxacin, norfloxacin pivoxil, is also used in some countries.

Administration in renal impairment.

Doses of norfloxacin may need to be reduced in renal impairment; for urinary-tract infections, 400 mg once daily should be given to patients with a creatinine clearance of 30 mL/minute per 1.73 m2 or less.

💊 Preparations

BP 2008: Norfloxacin Eye Drops; Norfloxacin Tablets; USP 31: Norfloxacin Ophthalmic Solution; Norfloxacin Tablets.

Proprietary Preparations

Arg.: Bio Tarbun; Chibroxin†; Floxamicin; Floxatral; Memento NF; Norflol; Noroxin; Norsol; Parcetin; Ritromine; Uro-Linfol; Urofos; Uronovag; Uroseptal; Urotem; Uroxacin; Wenflox; Yanurax†; Austral.: Insensye; Norflohexal; Noroxin; Nufloxib; Roxin; Austria: Floxacin; Norflostad; Urobacid†; Zoroxin; Belg.: Chibroxol; Zoroxin; Braz.: Androfloxin; Chibroxin†; Flox†; Floxacin; Floxanor; Floxatom†; Floxatrat†; Floxilin†; Floxinol; Genitoflox; Neofloxin; Norf; Norflamin†; Norflox; Norfloxasan; Norfloxil; Norfloxmed; Norxacin†; Norxin; Quinoform; Respexil; Uritrat; Uroflox†; Uroplex†; Uroseptal; Uroxazol-N; Canad.: Apo-Norflox; Noroxin†; Chile: Chibroxin†; Fulgram; Noroxin†; Urekolin†; Cz.: Gyrablock; Nolicin; Denm.: Zoroxin†; Fin.: Lexinor†; Noroxin†; Fr.: Chibroxine; Noroxine; Ger.: Bactracid; Barazan; Chibroxin; Firin; Norflohexal; Norflosal; Norflox; Norflox-Azu†; Norflox-Puren†; Norfloxbeta; Norfluxx; Gr.: Alenbit; Constilax; Dirunez†; Fluseminal; Grenis; Lemorcan; Lorcamin; Norocin; Ovinol; Pistofil; Setanol; Sinobid; Sofasin; Steinaclox; Urobacid; Urospes-N; Vetamol; Hong Kong: Floxen; Janacin; Lexiflox; Lexinor†; Mitatonin; Rexacin†; Uroctal; Hung.: Nolicin; India: Bacigyl; Biofloxin; Norbactin; Norflox; Normax; Indon.: Pyrflox; Israel: Apirol; Chibroxin†; Ital.: Diperflox; Flossac; Fulgram†; Norflox; Noroxin; Renoxacin; Sebercim; Theanorf; Uticina; Utinor; Jpn: Baccidal; Malaysia: Chibroxin†; Floxen†; Janacin; Lexinor†; Norbactin†; Norfloxin; Norfloxinor†; Rexacin; Trizolin; Urinox; Urobacid; Mex.: Baxamed; Difoxacil; Floxacin; Microxin; Noflorox; Noroxin; Norquinol; Oranor; Neth.: Chibroxol; Noroxin; NZ: Noroxin; Philipp.: Euroflox; Lexinor; Norbactin; Nortram; Septinor; Uritracin; Urobacid; Utiflox; Utinor; Winaflox; Pol.: Chibroxin; Nolicin; Port.: Besflox; Chibroxol; Noroxin; Quinoflex†; Taflox†; Uroflox; Rus.: Gyrablock (Гираблок); Negaflox (Негафлокс); Nolicin (Нолицин); Norbactin (Норбактин); Norfacin (Норфацин); Norilet (Норилет); Normax (Нормакс); S.Afr.: Floxin; Noroxin; Utin; Singapore: Bexinor; Chibroxin†; Effectsal; Foxgoria; Gyrablock; Norbactin; Sefnor†; Trizolin†; Urobacid†; Spain: Amicrobin; Baccidal; Chibroxin; Esclebin; Espeden; Nalion; Norflok; Noroxin; Senro; Uroctal; Xasmun; Swed.: Lexinor; Switz.: Chibroxol†; Norflocine; Noroxin; Norsol; Noxufen; Thai.: BGB Norflox†; Foxin; Foxinon; Gonorcin; Janacin; Lexfor†; Lexinor; Loxone; MFlox; Manoflox; Myfloxin; Noracin; Norbactin; Norcin; Norfcin; Norflo†; Norflocin; Norfloxin; Norfloxyl; Norsa†; Norxacin; Norxia; Noxine; Noxinor; Proxinor; Rexacin; Sefnor; Snoffocin; Trizolin†; Urinox; Uritracin; Vesxacin; Xacin; Turk.: Noroxin; UAE: Uroxin; UK: Utinor; USA: Noroxin; Venez.: Chibroxin†; Danilon; Norflosan†; Norfloval†; Norilet†; Noroxin. Multi-ingredient: Arg.: Nor 2; Urotem Dol; India: Bacigyl-N†; BiofloxTZ; NM Powder; Nor T; Norflox TZ; Normax TZ; Parabact; Powergyl; Tinvista-NF; Mex.: Mictasol.
Published May 08, 2019.