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Antifungals
Antifungals
13
Pharmacology
Professional
03/25/2012

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Term
Amphotericin B
Definition
Antifungal polyene, binds to ergosterol and forms pores in cell membrane. Fungocidal or fungostatic depending on the fungus. Given by IV only.
Used in life threatening mycoses, immunocomp, cryptococcal meningitis, deep/disseminated infections.
Most severe side effect is nephrotoxicity, also anemia, hypokalemia, and hypomagnesemia
Term
Nystatin
Definition
Antifungal polyene, binds to ergosterol and forms pores in the cell mem. Used for candida infections (oropharyngeal thrush, vaginal candidiasis, and intertrigenous candida infections)
Term
Fluconazole
Definition
Antifungal azole, inhibits fungal lanosterol 14-a-demethylase (last enzyme in making ergosterol)
Treats menengial coccidiodes or cryptococcus, cutaneous and deep Candidiasis.
Adv effects: Nausea and vomiting (may require anti-emetic), potent teratogen (fetal endocrine toxicity)
Term
Itraconazole
Definition
Antifungal azole, inhibits fungal lanosterol 14-a-demethylase (last enzyme in making ergosterol). Effective in treating Dermatophytoses, invasive aspergillosis, sporotrichosis, and blastomycosis, onychomycosis.
Adv effects: Nausea and vomiting (may require anti-emetic), hypokalemia, hypotension
Term
Ketoconazole
Definition
Antifungal azole, inhibits fungal lanosterol 14-a-demethylase (last enzyme in making ergosterol)
Useful in chronic mucocutaneous Candidiasis and Seborrheic dermatitis (shampoo form, M. furfur)
Adv effects: can inhibits some human CYP enzymes and reduce androgen and corticosteroid synthesis. Nausea and vomiting (may require anti-emetic)
Term
Miconazole
Definition
Antifungal azole, inhibits fungal lanosterol 14-a-demethylase (last enzyme in making ergosterol)
Adv effects: Nausea and vomiting (may require anti-emetic)
Term
Anidulafungin
Definition
Echinocandin, inhibits beta-glucan synthase (makes part of the cell wall), Fungostatic.
Works against Aspergillus and Candida species.
Very long half life (24-48 hours).
Term
Caspofungin
Definition
Echinocandin, inhibits beta-glucan synthase (makes part of the cell wall), Fungostatic.
Works against Aspergillus and Candida species.
Adv effects: given with Cyclosporine can cause elevated hepatic enzymes.
Term
Micafungin
Definition
Echinocandin, inhibits beta-glucan synthase (makes part of the cell wall), Fungostatic.
Works against Aspergillus and Candida species. Useful as prophylaxis for Candida infection during BM transplant.
Term
Flucytosine
Definition
Water soluble pyrimidine analog. Converted to 5-FU then either to 5-dUMP (inhibits thymidylate synthase and DNA synthesis) or 5-FUMP (blocks RNA synthesis).
Used to treat deep Candida infections, Cryptococcal meningitis (with Amphotericin B), and Chromoblastomycosis (with Itraconazole).
Adv effects due to conversion to 5-FU: reversible myelosuppression, liver dysfxn, toxic enterocolitis.
Term
Terbinafine
Definition
Blocks squalene epoxidase (part of ergosterol synth) leading to increased squalene which is toxic to the fungus (fungicidal).
Treats infection by dermatophytes and Candida and M. furfur. Takes a long time to work.
Adv effects: inhibits CYP2D6
Term
Tolnaftate
Definition
MOA unknown, thought to be the same as Terbinafine. Treats dermatophyte, Candida, and M. furfur infections.
Term
Griseofulvin
Definition
Oral admin --> disseminated in keratinized tissues. Disrupts fungal mitosis by binding microtubules (fungistatic). Effective against dermatophytes but takes a long time to work.
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