577

lor; Aknecolor; Canestene; Corisa!; Fungotox; Gromazol; Gyno­ Nitrate (BANM. USAN, r/NNM) Canestene; Imazol; Undex au ; Thai.: Caginal; CAS - 130- 16-5. Canasone; Canazol; Candazole; Candex; Candid; Candinox; BPF36H!G6S. (..Q4707 .Ec_qnaiol, hltf to pitrat� d'; UNII - a tc61'l.-?Z6f€;, . . Canesten; Cenecon; Chingazol; Clomaz; Clotri; Clotricin; Clo­ Ecor'!a.iqll _Nrtras; Econazo.• lrl \leri: Ekonats olilitttaa�tt:. E�<:ma· trimed; Comatt; Comazol; Cotren; CSTt; Defungo; Dermaten; Profile zo lnitrat; Ek<:�mzbl-rrltrat;: Ekonazofl1.r,i o.- Mtfrato de Dermizole; Fadaet; Fango Cream; Fungi; Fungicon; Fungiderm; . · nltraa tas;rp Gynebo; Gynestin 200; Gyno-Clotrin; Gynosten; Hofra B; Cloxiquine has been included in preparations used topically eco�a40!; R7 148c27; 3k9Ha3PJJ fi•r a+. Hofra; Kanezint; Kenet; Klamacin; Lamazone; Lyma; Manoma­ for the treatment of fungal and bacterial skin infections. It is (±)-I-{2A:Dkhloro.-f:lc\4'chSQ- !3050;lorob€ rqifoxy)phefjeth;.rl)ln11d· a component of halquinol. p. 309.1. ato!e> nitrate: . · · · zole; Mycoda; Mycoderm-C; Mycoril; Mycotopic; Mycozole; .\ . . . Myda; Nestic; P-Gyzole; RanoTroct; Taraten; Vagizole; Vama­ CiaH15CisN,0,HN0-;""444· .7 zole; Vanesten; Zema; Turk.: Canesten; Clozol; Fungostent; . - J4 169-Q2-6 (ec onozofe, . Gyno-Canesten; UK: Canesten Combi; Canesten; Fungederm; CAS ProprietaryPreparations (details are given in Volume B) . Ukr.: Candibene (Kmwr6eHe); Candid (KaHAH!1): Imazol Aeconazql�TC-.- 001AC nitrate).03: . . (llMa3on); USA: Fungi Cure Intensive; Gyne�Lotrimin; Lotrimin Decoderm trivalentt; . . Multi-ingredient Preparations. Austria: 000iA.GOIACb3,' F0-5: AF; Lotrimin; Mycelex-7; Mycelex; Venez.: Canesten; Clortilen; Indon.: Decoderm 3. Clotrizol; Fugolin; Ginolotricomb; Gyno Canesten; Imazol; Ipa­ ATC Vet ....,. QGIJ IA}:(Js. UN/I H43/JWVIIJ iVE. lat; Micozol; Palik. Pharmacopoeias. In Chin., Eur. (see p. and US. Multi-ingredient Preparations. Arg. : Becortin; Calmurid; Cortis­ Hydrochloride fr!NNMJ Ph. Eur. 8: (Econazole Nitrate). A whitevii), or almost white pec; Dicasone Complex; Empecid Cort; Gentacort Plus; Hongal; Claconazole Hydi chlorlde; Crcieonozol. Chlorhydrate e; crystalline powder. Very slightly soluble in water; slightly Lotricomb; Micomazol B; Quadriderm; Quiacort G Plus; Vagi­ () d Crocoriazol; hidrocloruro de; CroconilZoli Hydtochlciriduin; soluble in alcohol; sparingly soluble in dichloromethane; san Compuesto; Vitacortil; Austral.: Canesoral Duo; Femazole soluble in methyl alcohol. Protect from light. Duo; Hydrozole; VagiClear Duo; Austria: Imazol Duo; Myko Hidrocloruro . de . croconazol; . (crownazole); Cordest; Belg.: Lotriderm; Braz.: Baycuten; Canad.: Canesoral f\pol

The symbol t denotes a preparation no longer actively marketed 578 Antifun als

Ecomi; Econitet; Ecosonet; Ecozol; Heads Shampoot; Hung. : and at least 14 days after resolution of symptoms for Gyno-Pevaryl; Pevaryl; India: Ecanol; Irl.: Ecostatint; Gyno­ AdverseEffects and Precautions oesophageal infections; doses of up to 400 mg daily may be Pevaryl; Israel: Gyno-Pevaryl; Pevarylt; Ita!. : Dermazolt; Eco­ Burning and itching have been reported after the used for oesophageal candidiasis if necessary. dergin; Ecomesol; Ecomi; Ecorex; Ecosteril; Ganazolo; Ifenec; application of nitrate. Fluconazole 150 mg as a single oral dose may be used for Micos; Pevaryl; Polinazolo; Malaysia: Gyno-Pevaryl; Mex.: Are­ Intravaginal preparations of fenticonazole may damage genital candidiasis (vaginal candidiasis or candida! colex; Micostyl; Pevaryl; Neth.: Pevaryl; Norw.: Pevaryl; NZ: latex contraceptives and additional contraceptive measures balanitis). Ecremet; Pevaryl; Philipp.: Pevaryl; Pol.: Gyno-Pevaryl; are therefore necessary during local application. Dermatophytosis, pityriasis versicolor, and Candida Pevaryl; Pevazol; Port.: Gyno-Pevaryl; Pevaryl; Rus.: Ecalin For a discussion of the caution needed when using azole infections of the skin may be treated with fluconazole (3KliJ1HH)t; Ecodax (3KOAa.Kc); Gyno-Pevaryl (fmm-IleBapHJI); antifungals during pregnancy, see under Pregnancy in lienee (HijleHex); S.Afr.: Ecodermt; Econal-Ct; Gyno-Pevaryl; 50 mg orally once daily for up to 6 weeks. Precautions of Fluconazole, p. 579.3. Pevaryl; Singapore: Gyno-Pevaryl; Pevaryl; Spain: Ecotam; Systemic candidiasis, cryptococcal meningitis, and Micoespect; Swed.: Pevaryl; Switz.: Gyno-Pevaryl; Pevaryl; other cryptococcal infections may be treated with Thai.: Econ; UK: Ecostatint; Gyno-Pevaryl; Pevaryl; Ukr.: Eco· Antimicrobial Action fluconazole orally or by intravenous infusion; the initial dax (EKOAa.Kc); USA: Ecoza; Spectazole; Venez.: Gyno-Pevaryl; dose is 400 mg followed by a maintenance dose of 200 to Fenticonazole is an imidazole antifungal active against a Miconax; Pevaryl. 400 mg once daily. Duration of therapy is based on clinical range of organisms including dermatophyte pathogens, and mycological response, but is usually at least 6 to 8 weeks Malassezia furfur, Candida a/bicans. Multi-ingredient Preparations. Arg.: Diflunazol; Filoderma Plus; and in cryptococcal meningitis; in the USA, treatment for I 0 to Griseocrem; Griseoplus; Austria: Pevisone; Belg.: Pevisonet; 12 weeks after the CSF cultures become negative is (t\:!"''T); (erffi�); China: Fu Yan Ning Ji Bai Fu Pevisone r i recommended. Fluconazole may also be used in daily doses YiFuQing Zhaohuile Pevison; P.r.�P.?. ?_! ()_n,�...... Denm.: (l!iR of I 00 to 200 mg orally or intravenously to prevent relapse Pevisonet; Fin.: Pevisone; Fr. : Pevisone; Ger.: Epipevisone; PraprielaryPreparations (details ate given in Volume B) .fil!¥tf); (:fitmil\\' ); (li!l111i'Jf); after a primary course of antifungal treatment for acute Gr.: Pevison; Hong Kong: Ecocort; Pevisone; Triamecon; Trico­ Single-ingredient Preparations. Austria: Lomexin; Belg.: Gynox­ cryptococcal meningitis in patients with AIDS. nazole; India: Bestopic; Cobederm-Ht; Ecodax-G; Halog-E; in; Braz. : Fentizol; Lomexin; Cz. : Lomexin; Fr. : Lomexin; Ter­ In immunocompromisedpatients at risk of fungal infections, Mediron; Israel: Pevisonet; Ital.: Pevisone; Malaysia: Aecoras; lomexin; Ger.: Fenizolan; Lomexint; Gr.: Lomexin; Hung.: fluconazole may be given prophylactically in a dose of 50 Ecocort; Econazine; Endix; Kifugan; Norw.: Pevisone; Philipp. : Gynoxin; Lomexin; Irl.: Gynoxin; Lomexin; Ital.: Falvin; to 400 mg daily orally or by intravenous infusion, although Nizolex; Pevaryl HPt; Pevisone; Pol. : Pevisone; Port.: Pevisone; Lomexin; Lore nil; Mex.: Lomexin; Neth.: Gynoxin; Pol.: S.Afr.: Pevisone; Singapore: Ecocort; Econazine; Epiderm; Pevi­ Gynoxin; Port.: Lomexin; Rus.: Lomexin (JloMeKCHH); S.Afr.: long-term prophylaxis has been associated with the sone; Swed.: Pevisone; Switz.: Pevisone; Thai.: Ecocort; Eco­ Lomexin; Spain: Laurimic; Lomexin; Turk.: Gyno-Lomexin; emergence of resistant organisms (see under Intermittent derm; Econazine; Tricozole; UK: Econacortt. (JloMeKcHH); Doses, below). UK: Gynoxin; Ukr.: Lomexin Venez.: Mycofentin. For details of doses used in children and in those with Pharmacopoeial Preparatians renal impairment, see p. 579.!. BP 2014: Econazole Cream; Econazole Pessaries. Fluconazole raAN, usAN. riNN! Reviews. 1. Grant SM, Clissold SP. Fluconazole: a review of its pharmacodynamic and pharmacok:inetic properties, and therapeutic potential in superficial and systemic mycoses. Drugs 1990; 39: 877-916. Correction. ibid. 40: 862. 2. Kowalsky SF, Dixon DM. Fluconazole: a new antifungal agent. Clin Pharm 1991; 10: 179-94. 3. Goa KL, Barradell LB . Fluconazole: an update of its pharmacodynamic and pharmacokinetic properties and therapeutic use in major superficial and systemic mycoses in immunocompromised patients. Drugs 1995; 50: 658-90. 4. Charlier C, et al. Fluconazole for the management of invasive candidiasis: where do we stand after 15 years? J Antimicrob Chemother 2006; 57: 384-410. Pharmacopoeias. In Chin., Bur. (see p. vii), and US. Pharmacopooias. In Bur. (see p. vii) for veterinary use only. Administration. HIGH DOSES. Doses higher than those in Ph. Eur. 8: (Enilconazole for Veterinary Use; Enilconazole Ph. Eur. 8: (Fluconazole). A white or almost white, licensed product information for fluconazole have been BP(Vet) 2014). A clear, yellowish, oily liquid or solid mass. hygroscopic, crystalline powder. It exhibits polymorphism. tried, and in some cases are routinely recommended, for Very slightly soluble in water; freely soluble in alcohol, in Slightly soluble in water; freely soluble in methyl alcohol; patients with some life-threatening fungal infections. For methyl alcohol, and in toluene. Store in airtight containers. soluble in acetone. Store in airtight containers. cryptococcal meningitis in HIV-infected patients, oral flu­ Protect from light. USP 36: (Fluconazole). A white or almost white, crystalline conazole doses of 800 mg to 2 g daily have been used in powder. Slightly soluble in water; soluble in alcohol and in some second-line induction regimens. In the USA. some acetone; sparingly soluble in chloroform and in isopropyl experts1 have suggested: Profile alcohol; freely soluble in methyl alcohol; very slightly • 800 mg daily when used with soluble in toluene. Store in airtight containers at a Enilconazole is an imidazole antifungal used topically in • at least 800 mg, and preferably !.2 g daily when used veterinary medicine for the treatment of fungal skin temperature below 30 degrees. with infections in cattle, horses, and dogs. It is also used by • 800 mg to 2 g daily, preferably 1.2 g daily or more, when inhalation for the treatment of aspergillosis in ostriches. Incompatibilityand stability.References. fluconazole is used alone l. Lor E, et al. Visual compatibility of fluconazole with commonly used Daily oral doses of up to 800 mg have also been used in injectable drugs during simulated Y-site administration. Am J Hosp Pharm 1991; 48: 744-6. consolidation treatment of non-HIV infected patients with 2. Couch P, et al. Stability of fluconazole and amino adds in parenteral cryptococcal meningitis, 1 and 800 mg daily has been Fenticonazole Nitrate nutrient solutiorn. Am J Hosp Pharm 1992; 49: 1459-62. suggested for CNS blastomycosis.2 For the treatment of (BANM, USAN, rfNNM) 3. Hunt-Fugate AK, et al. Stability of fluconazole in injectable solutions. Am CNS coccidioidomycosis, some experts' suggest initial J Hosp Pharm 1993; SO: 1186-7. 4. Ishisaka DY. Visual compatibility of fluconazole with drugs given by oral doses of 800 mg to I g fluconazole daily; for continuous infusion. Am J Hosp Pharm 1994; 51: 22�0 and 2292. disseminated disease, up to 2 g daily has been used. 5. Dotson B, Churchwell MD. Physical compatibility of 4% sodium citrate Intravenous doses of 10 mg/kg daily have been tried in with 23.4% sodium chloride, fluconazole, and . Am J Health­ disseminated candidiasis, 4 and US guidelines' suggest up Syst Pharm 201 1; 68: 377-8. to 12 mg/kg daily if fluconazole is to be used for CNS infection. When used for treatment of disseminated Uses and Administration neonatal candidiasis, a dose of 12 mg/kg daily has also Fluconazole is a triazole antifungal used for superficial been suggested.' mucosal (oropharyngeal. oesophageal. or vaginal) candi­ l. Perfect JR, et al. Clinical practice guidelines for the management of diasis and for fungal skin infections. It is also given for cryptococcal disease: 2010 update by the Infectious Diseases Society of America. Clin Infect Dis 2010; 50: 291-322. Also available at: http://www. systemic infections including systemic candidiasis, cocci­ journals.uchicago.edu/doi/pdf/ 10.1086/649858 (accessed 16/08/10) dioidomycosis, and cryptococcosis, and has been tried in 2. Chapman SW, et al. Clinical practice guidelines for the management of blastomycosis, histoplasmosis, and sporotrichosis. The place blastomycosis: 2008 update by the Infectious Diseases Society of America. Clin Infect Dis 2008; 46: 1801-12. Also available at: http://www. of fluconazole in the treatment of fungal infections is journals.uchicago.edu/doi!pdf/ 10.1086/588300 (accessed 16/08/10) discussed in the various sections under Choice of Pharmacopoeias. In Bur. (see p. vil). 3. Galgiani JN, et al. Infectious Diseases Society of America. Coccidioido­ Antifungal, p. 563.!. Fluconazole has also been used for mycosis. Clin Infect Dis 2005; 41: 1217-23. Also available at: http://www. Ph. Eur. 8: (Fenticonazole Nitrate). A white or almost the treatment of cutaneous leishmaniasis, for details see joumals.uchicago.edu/doi/pdf/ 10.1086/496991 (accessed 16/08/10) white, crystalline powder. Practically insoluble in water; 4. Graninger W, et al. Treatment of Candida albicans fungaemia with p. 579.2. 26: sparingly soluble in dehydrated alcohol; freely soluble in fluconazole. J Infect 1993; 133-46. Fluconazole is given orally or by intravenous infusion in 5. Pappas PG, et al. Clinical practice guidelines for the management of dimethylformamide and in methyl alcohol. Protect from similar doses. For intravenous infusion it is given as a candidiasis: 2009 update by the Infectious Diseases Society of America. light. solution containing 2mg/mL at a rate of 5 to IOmL/minute Clin Infect Dis 2009; 48: 503-3 5. Also available at: http://www.journals. (300 to 600 mL/hour). In the USA. a maximum infusion uchicago.edu/doi/pdf/1 0.1086/596757 {accessed 16/08/1 0) Uses and Administration rate of 100 mL/hour is recommended. INTERMITTENT DOSES. Concern has been expressed about the For superficial mucosal candidiasis (other than increasingly widespread use of fluconazole1 and, in parti­ Fenticonazole is an imidazole antifungal used locally as the genital candidiasis), the usual oral dose of fluconazole in the cular, about the impact of continuous fluconazole therapy nitrate in the treatment of vulvovaginal candidiasis UK is 50 mg dally, although 100 mg daily may be given if in immunocompromised patients on the development of (p. 564.1). A 200-mg pessary is inserted into the vagina at necessary. Treatment usually continues for 7 to 14 days in resistance (see under Antimicrobial Action, p. 580.2). bedtime for 3 nights or a 600-mg pessary is inserted once oropharyngeal candidiasis (except in severely immunocom­ Nevertheless, fluconazole remains popular for primary and only at bedtime. It is also available as a 2% vaginal cream; promised patients), for 14 days in atrophic oral candidiasis secondary prophylaxis. Some investigators have suggested 5 g is inserted into the vagina twice daily for 3 days. associated with dentures, and for 14 to 30 days in other the use of intermittent doses2•3 although this could further Fenticonazole nitrate is also applied topically as a 2% cream mucosal candida! infections including oesophagitis. increase the risk of infections with resistant organisms. or solution for the treatment of fungal skin infections. Higher doses are recommended in the USA where an Once-weekly treatment with. fluconazole has been tried Reviews. initial dose of fluconazole 200 mg is followed by 100 mg in onychomycosis4 and tinea capitis.' In HIV-infected l. Veraldi S, Milani R. Topical fenticonazole in dermatology and once daily and where the minimum treatment period is 14 patients with oropharyngeal candidiasis, a single 750-mg gynaecology: current role in therapy. Drugs 2008; 68: 2183-94. days for oropharyngeal infection, or a minimum of 21 days oral dose of fluconazole has been reported to be as effective

All cross-references refer to entries in Volume A