Exam III Anti-fungal Drug Names Flashcards by Brian Fisher

Yeast

Candida SP.**

Pneumocystis jyrovecii

Cryptococcus neoformans

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Mold

Aspergillus SP.**

Mucor

Dermatophytes

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Dimorphic

Blastomyces

Coccidiomycosis

Histoplasma

Sporotrichosis

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Allylamines

4 Fines

Terbinafine

Butenafine

Naftifine

AmorolFine

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Allylamine MOA

Inhibit Squalene -> no ergosterol synthesis (reducing fungal cell membrane)

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Allylamine Coverage

Tinea (Cosporis/Pedis/Cruris)

Onychomycosis (Terbinafine)

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Allylamine MISC facts

Terbinafine is the only one you can use for Onychomycosis

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Polyenes

Nystatin (PO/Topical/Susp)

Amphotericin B Deoxycholate (AmB-d) (IV)

Amphotericin B Lipid complex (ABLC)

Liposomal Amphotericin B (L-AmB)

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Polyenes MoA

Binds Ergosterol. Cell Leaks

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Nystatin Coverage

Candida only

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Amphotericin B (and Derivs) Coverage

Most Candida spp. and Aspergillus spp.

Most Fungi except no Fusarium spp. and A. Terreus

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Amphotericin B ADRs/DDIs

Extremely nephrotoxic. Dose-Dependent decrease in GFR (monitor).

K, Mg, HCO3 wasting (electrolyte derangement)

Decreased EPO production. Avoid W/other nephrotoxic drugs

Acute Infusion RXN. _{(pre-medicate with APAP, or IBU, diphenhydramine +/- steroids, Rigors: meperidine)}

Support with Fluids (Hydrate)

Thrombophlebitis (heparin), cardiac arrhythmias, and Rash

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Amphotericin B DDIs worst to least.

AmB-d (base)

ABLC

_{(Less Nephrotoxic & Less infusion RXN)}

L-AmB

_{(Less nephrotoxic & Less infusion RXN & better CNS penetration)}

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Imidiazoles

Clotrimazole

Ketoconazole

Miconazole

Econazole

Mebendazole

Oxiconazole

Sertaconazole

Sulconazole

Thiabendazole

CloK ME MOST azole

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Ketoconazole (and other Imidazoles) MoA

Inhibit 14a-demethylase. No conversion of lanosterol to ergosterol. No CM synthesis.

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Ketoconazole Coverage

Andida spp., blastomycosis, histoplasmosis (high failure)

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Ketoconazole DDIs

CYP450/3A4 substrate ->CYP inhibition

Needs acidic gastric pH -> H2RA, PPI, antacid interactions

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Ketoconazole MISC

Poor distribution into CSF and eye

Contraindicated in patients w/ hepatic impairment

Excreted in Feces

Available in many forms

Half-life 8 Hrs

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Triazoles

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Fluconazole (PO/IV/S)

Voriconazole (PO/IV/Drops)

Isavuconazole (PO/IV)

Itraconazole (PO/IV/S)

Posaconazole (PO/IV/S)

F VIIP

Triazole MoA

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Inhibit 14-a demethylase. No conversion of lanosterol to ergosterol. No CM synthesis.

Fluconazole& Itraconazole coverage

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C. Glabrata

C. Krusei

Aspergillus (Fluconazole only)

Fusarium

Scedosporium

Zygomycetes

Fluconazole ADR/DDI

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Minor CYP3A4 / Moderate CYP2C9 inhibitor

If CrCL <50 half the dose.

Fluconazole MISC

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Wide distribution

CNS Penetration

Halflife 30 hrs 98-125 in renal impairment

Voriconazole coverage

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Scedosporim

Zygomycetes

Voriconazole ADR/DDI

NVD Liver dysfunction Visual abnormalities HA Substrate and inhibitor of CYP3A4/2C9/2C19 Reduced Bioavailability w/ high fat meals

Voriconazole Misc

Good CNS **_Monitor_** SCr Electrolytes LFTs (Nephrotoxic) Ophthalmic exam if \> 4 weeks therapy QTc for prolongation

Isavuconazole coverage

Invasive Aspergillosis Mucormycosis

Isavuconazole ADR/DDI

Loading Dose QT shortening Nephrotoxic GI Hypotension Hypo K/Mg Inhibition: CYP3A4, P-glycoprotein, OCT-2

Isavuconazole Misc

Best bioavailability Half life 130 Hrs No Renal/Hepatic dosing Administered as Prodrug Isavuconium Monitor LFTs

Fluconazole & Itraconazole coverage

**_NO_** C. Glabrata C. Krusei Aspergillus (Fluconazole only) Fusarium Scedosporium Zygomycetes

Itraconazole ADR/DDI

99% protein bound Capsule or solution, no change Renal adjustment

Itraconazole MISC

Capsules with food Suspension without food

Posaconazole Coverage

**_NO_** Scedosporium

Posaconazole ADR/DDI

Potent 3A4 Inhibitor Inhibitor & substrate P-glycoprotein GI HA Hepatotoxic (rare) QT Prolongation Hemolytic Uremic Syndrome

Posaconazole MISC

Higher oral bioavailability w/food DEC absorption w/ PPIs, H2RA Oral Slow-Onset No renal adjust Monitor: SCr, electrolytes, LFTs

Echinocandins

Caspofungin Anidulafungin Micafungin CAM Fungin

Echinocandin MoA

Inhibit glucan synthesis in Cell wall -\> cell Wall ruptures Good distribution, poor CNS penetration

Echinocandin coverage

Invasive Candidiasis Empiric coverage in netropenic fever (immunocompromised fever) _{Fungicidal against most Candidiasis spp} _{Fungistatic vs Aspergillus}

Caspofungin ADR/DDI

CYP inducers reduce dose -\> increase dose Cyclosporin may increase AUC by 35% Reduces tacrolimus (immunosuppressant) levels by 20%

Micafungin ADR/DDI

Increases concentration of Sirolimus (anti-transplant rejection drug) Increases AUC and Cmax of nifedipine

Anidulafungin ADR/DDI

None

Echinocandin MISC

Well tolerated No renal adjust Extensive half-life, once daily dosing 97-99% protein bound

Flucytosine Coverage

ALL Candida **EXCEPT** C. Krusei Cryptococcus neoformans Aspergillus sp.

Flucytosine MoA

Anti-metabolite (decreases DNA synthesis) Has synergy, usually Co-administered

Flucytosine ADR/DDI

Never use alone (resistance develops quickly) Synergy w/ Amphotericin B. NVD Bone Marrow Suppression (dose-dependent avoid other suppressors) Enterocolitis Hepatotoxicity (avoid other nephrotoxic agents)

Flucytosine MISC

Admin over 15 min w/food to limit N/V Monitor: CBC/SCr/LFTs and serum levels (especially in pts w/poor renal)

Exam III Anti-fungal Drug Names Flashcards

(46 cards)