Nystatin is a polyene macrolide much like amphotericin B. It is too toxic for parenteral administration and is only used topically. Nystatin is currently available in creams, ointments, suppositories, and other forms for application to skin and mucous membranes. It is not absorbed to a significant degree from skin, mucous membranes, or the gastrointestinal tract. As a result, nystatin has little toxicity, although oral use is often limited by the unpleasant taste.
Nystatin is active against most Candida sp and is most commonly used for suppression of local candidal infections. Some common indications include oropharyngeal thrush, vaginal candidiasis, and intertriginous candidal infections.
The two azoles most commonly used topically are clotrimazole and miconazole; several others are available (see Preparations Available). Both are available over the counter and are often used for vulvovaginal candidiasis. Oral clotrimazole troches are available for treatment of oral thrush and are a pleasant-tasting alternative to nystatin. In cream form, both agents are useful for dermatophytic infections, including tinea corporis, tinea pedis, and tinea cruris. Absorption is negligible, and adverse effects are rare.
Topical and shampoo forms of ketoconazole are also available and useful in the treatment of seborrheic dermatitis and pityriasis versicolor. Several other azoles are available for topical use (see Preparations Available).
Terbinafine and naftifine are allylamines available as topical creams (see Chapter 61). Both are effective for treatment of tinea cruris and tinea corporis. These are prescription drugs in the USA.
Lipid formulations: Lower toxicity, higher doses can be used
Fluconazole, voriconazole, posaconazole, isavuconazole: Fluconazole has excellent CNS penetration, used in fungal meningitis •FlucytosineInterferes with DNA and RNA synthesis selectively in fungi Synergistic with amphotericin•systemictoxicity in host due to DNA and RNA effects Cryptococcus and chromoblastomycosis infections Oral•duration,hours•renalexcretion•Toxicity: Myelosuppression PYRIMIDINE ANALOG • Micafungin, anidulafungin: Micafungin increases levels of nifedipine, cyclosporine, sirolimus; anidulafungin is relatively free of this interaction •TerbinafineInhibits epoxidation of squaleneinfungi•increasedlevels are toxic to fungi Reduces ergosterol •preventssynthesisoffungal cell membrane Mucocutaneous fungal infections Oral•duration,days•Toxicity: Gastrointestinal upset, headache, hepatotoxicity•Interactions: None reported ALLYLAMINE
Lipid formulations Abelcet, AmBisome
Clotrimazole Generic, Lotrimin, Mycelex, others
Econazole Generic, Ecoza
Fluconazole Generic, Diflucan
Flucytosine Generic, Ancobon
Griseofulvin Grifulvin, Gris-Peg
Itraconazole Generic, Sporanox, Onmel
Ketoconazole Generic, Nizoral, others
Miconazole Generic, Oravig, Micatin
Oxiconazole Generic, Oxistat, others
Terbinafine Generic, Lamisil
Terconazole Generic, Terazol 3, Terazol 7
Tioconazole Vagistat-1, Monistat 1
Tolnaftate Generic, Aftate, Tinactin, others
Ashbee HR et al: Therapeutic drug monitoring (TDM) of antifungal agents: Guidelines from the British Society for Medical Mycology. J Antimicrob Chemother 2014;69:1162.