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Antifungal agents
board prep
11
Medical
Graduate
04/06/2008

Additional Medical Flashcards

 


 

Cards

Term

 

 

 

Amphotericin B

Definition

MOA: interact w/ ergosterol (fungal component) to form "artificial pores" which disrupt the membrane permeability of the fungus

 

Spectrum: DOC for Aspergillus, Candida, Cryptococcus, Histoplasma, Mucor & Sporothrix 

 

Synergistic w/ Flucytosine in Candida & Cryptococcus infxns

 

SE: fever, chills, muscle rigor, hypotension (d/t histamine release so pretreat w/ antihistamine)

Dose-dependent nephrotoxicity (dec. GFR, tubular acidosis, dec. K+, Mg2+)

Term

 

 

 

Nystatin

Definition

topical antifungal, too toxic for systemic use

 

 

Term

 

 

 

-Azoles

Definition

ketoconazole, fluconazole, itraconazole

 

MOA: interfere w/ synthesis of ergosterol by inhibiting a fungal P450 enzyme (14-a-demethylase) that converts lanosterol to ergosterol

 

 

 

Term

 

 

 

Ketoconazole

Definition

Co-DOC: for Paracoccidiodes, back up for Blastomyces & Histoplasma

Oral use in mucocutaneous candidiasis or dermatophytoses

 

Absorption is dec. w/ antacids

 

Metabolized by liver enzymes can get inhibition of P450s

 

SE: dec. synthesis of steroids, including cortisol & testosterone --> dec. libido, gynecomastia, menstrual irregularities

Term

 

 

 

Fluconazole

Definition

DOC for esophageal/invassive candidiasis & coccidioidomycoses

Prophylazis and suppression in cryptococcal meningitis

 

Only one that penetrates into the CSF, eliminated via urine largely unchanged

 

SE: dec synthesis of steroids, including cortisol and testosterone --> dec. libido, gynecomastic, menstrual irregularities

Term

 

 

 

Itraconazole

Definition

DOC in blastomycoses and sporotrichoses

 

Absorption is increased w/ food intake

 

Metabolized by liver enzymes so can inhibit P450

 

SE: dec. synthesis of steroids including cortisol and testosterone --> dec. libido, gynecomastia, menstrual irregularities

Term

 

 

 

Clotrimazole & Miconazole

Definition
Topical antifungals for candidal and dermatophytic infxns
Term

 

 

 

Flucytosine

Definition

MOA: Activated by fungal cytosine deaminase to 5-fluorouracil which is incorporated into fungal RNA

5-FU also forms another cmpd that inhibits thymidylate synthase --> dec. thymine

 

Used in combo w/ amphotericin B in severe candidal and cryptococcal infxns that enter CSF

 

SE: toxic to bone marrow

Term

 

 

 

Griseofulvin

Definition

Active orally against dermatophytes by disrupting microtubule structure in newly formed keratin

 

SE: HA, thrush, peripheral neuritis, phototoxicity, potentiates EtOH

Term

 

 

 

Microtubule inhibitors

Definition

1. Griseofulvin

2. Colchicine

3. Vincristine

4. Vinblastine

5. Paclitaxel

Term

 

 

 

Terbinafine

Definition

Active only against dermatophytes by inhibiting squalene epoxidase --> dec. ergosterol

May be superior to griseofulvin in onychomycoses (toe/fingernail infxn)

 

SE: GI distress, rash, HA, inc. liver function tests

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