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37 Cards in this Set

  • Front
  • Back

General Azole




MOA

Inhibit the production of ergosterol, a key component of the fungal cell membrane




Inhibition via blocking a fungal CYP450 enzyme

General Azole




Spectrum of Activity

Candida spp:


-Excellent for albicans


-Variable for glabrata




Cryptococcus neoformans




Endemic fungi




Some dermatophytes




Aspergillus




Mucormycoses

General Azole




PK

Highly bioavailable (IV=PO)

General Azole




Adverse Effects

Hepatotoxicity

General Azole




DDI/ Other

Notable DDIs:


-HIV medications


-Calcineurin inhibitors (cyclosporine, tacrolimus)-Anticonvulsants-Rifampin

Fluconazole




Class

Azole

Fluconazole




Clinical Use

Empiric antifungal treatment




Candida infections UTI

Fluconazole




PK

Only one that needs to be renally dosed

Itraconazole




Class

Azole

Itraconazole




Clinical Use

non-life threatening cases of endemic mycoses

Worst DDI

DDIs worst with itraconizole (and voriconazole)

Voriconazole




Class

Azole

Voriconazole




Clinical Use

-DOC for aspergillus

Posaconazole




Class

Azole

Posaconazole

Clinical Use

Mucormycoses




Some prophylaxis regimens

Posaconazole




PK

Requires a high fatty meal for absorption

Amphotericin B




MOA

Binds to ergosterol and forms pores that allow molecules to leak in/out of the cell




Results in cell death

Amphotericin B




Spectrum of Activity

Candida spp: broadest

Amphotericin B




Clinical Use

-DOC for Cryptococcus neoformans-


DOC for life threatening endemic mycoses-


DOC for mucormycoses




-Aspergillus (second line to Variconozol)




-Broad Spectum Candida




-oddball fungus

Amphotericin B




Adverse Effects

Nephrotoxicity


-Causes electrolyte abnormalities




Infusion Reactions


-fever, and chills




Hepatotoxicity

Amphotericin B




DDI/ Other

Now use lipid formulation that is believed to be less toxic: Premidicate before use

Capsofungin, Micafungin, Anidulafungin




Class

Echinocandins

Capsofungin,Micafungin,Anidulafungin




MOA

Inhibits the production of 1-3-B-D-glucan, a key component of fungal cell walls by inhibiting 1-3-B-D glucan synthase enzyme

Capsofungin,Micafungin,Anidulafungin




Spectrum of Activity

Candida spp:


-Includes glabrata


-NO C.parapsilosis




Aspergillus

Capsofungin,Micafungin,Anidulafungin




Clinical Use

DOC for C.glabrata




Aspergillus:


-Combination or prophylaxis


-Monotherapy only when patient can’t tolerate voriconazole or amphotericin

Capsofungin,Micafungin,Anidulafungin




PK

IV only




Not renally eliminated

Capsofungin,Micafungin,Anidulafungin




Adverse Effects

VERY WELL TOLERATED

Flucytosine




MOA

Converted by fungal cells to 5-FU, and then to other products to inhibit DNA/RNA synthesis

Flucytosine




Spectrum of Activity

Candida




Aspergillus




Cryptococcus

Flucytosine




Clinical use

Never as monotherapy!




Synergy with amphotericin B in severe infections

Flucytosine




Adverse Effects

Bone marrow suppression:




Hepatotoxicity

Terbinafine




Class

Antifungals for dermatophytes

Terbinafine




MOA

Blocks ergosterol production by inhibiting squalene epoxidase production

Terbinafine



Adverse Effects

Hepatotoxicity

Griseofulvin




Class

Antifungals for dermatophytes

Griseofulvin




MOA

Prevents infections of new skin structuresEventually the infected ones die and get replaced

Griseofulvin




Adverse Effects

Allergic reactions




Hepatotoxicity