Antifungal Drugs

Front 1

What do Polyenes and Azoles target?

Back 1

Polyenes and Azoles target fungal cell membrane

Front 2

Most common cause of mucocutaneous fungal infections

Back 2

Candida albicans is the most common cause of mucocutaneous fungal infections

Front 3

Opportunistic mycoses

Back 3

Aspergillus, Candida, Cryptococcus, Phycomycetes

Front 4

2 primary classes of anti-fungals

Back 4

Polyenes and Azoles are the two major classes of anti-fungals

Front 5

Major drugs classified as Polyene Anti-Fungals

Back 5

Nystatin and Amphotericin B are the two drugs classified as Polyene Anti-Fungals

Front 6

Mechanism of action of Polyene Anti-Fungals (Nystatin and Amphotericin B)

Back 6

Nystatin and Amphotericin B act like detergents and remove ergosterol from fungal membranes--> leakage of cellular contents and death

Front 7

Clinical use of Nystatin

Back 7

Nystatin is very effective for topical and oral Candida infections

Front 8

Mode of administration of Nystatin

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Nystatin is NEVER given IV, given as an oral suspension of pastille form

Front 9

Clinical use of Amphotericin B

Back 9

Amphotericin B only used for progressive, potentially life-threatening fungal infections

Front 10

Serious adverse side effects of Amphotericin B

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Amphotericin B causes *nephrotoxicity*, hypotension, electrolyte imbalances, fever, allergic reactions

Front 11

Drug considered most toxic IV anti-infective on the market, way to reduce toxicity

Back 11

Amphotericin B is the most toxic IV anti-infective on the market (esp. for the kidney); sodium loading with normal saline to reduce toxicity

Front 12

Chief sterol in fungal membranes

Back 12

Ergosterol is the chief sterol in fungal membranes

Front 13

Mechanism of action of Azole drugs (anti-fungal)

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Azole drugs inhibit lanosterol 14-alpha-demethylase (blocks egosterol synthesis)

Front 14

Adverse side effects of Azole anti-fungal drugs, what needs to be monitored

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Azole anti-fungal drugs have the potential to cause serious liver damage because they inhibit fungal and some human forms of CYP450

Monitor liver function during long-term therapy and be aware of other drugs patient is taking that may be affected

Front 15

Which anti-fungal Azole drug has the lowest incidence of side effects?

Back 15

Fluconazole (Azole anti-fungal) has the lowest incidence of side effects

Front 16

Clinical uses of Fluconazole

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Cryptococcal meningitis in AIDS patients, Oropharyngeal and Esophageal Candidiasis, Prophylaxis in HIV patients for Mucosal Candidiasis

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Azole anti-fungal that has a broader spectrum of activity

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Itraconazole has a broader anti-fungal spectrum than Fluconazole

Front 18

Adverse side effect of Itraconazole (Azole anti-fungal)

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Itraconazole has side effect of serious hepatotoxicity

Front 19

Patient population for whom Itraconazole use is contraindicated

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Itraconazole is contraindicated for patients taking Cisapride, Dofetilide, Ergot Alkyloids, Lovastatin, Simvastatin

Front 20

Spectrum of Voriconazole (Azole anti-fungal)

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Voriconazole has a similar spectrum of activity to Itraconazole but has activity against Fusarium

Front 21

Adverse side effects of Voriconazole (Azole anti-fungal)

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Side effect of Voriconazole is visual disturbances (blurred vision, altered perception of color)

Front 22

Patient population for whom Voriconazole use is contraindicated

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Voriconazole should NOT be given to pregnant women

Front 23

Clinical uses of Ketoconazole (Azole anti-fungal)

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Ketaconazole has limited use because of its high incidence of side effects:
*Gynecomastia and menstrual irregularities (can inhibit testosterone and estradiol synthesis)*, severe liver toxicity

Front 24

Drug used to treat oral Candidiasis in AIDS patients

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Clotrimazole used to treat oral candidiasis in AIDS patients

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Clinical use of Posaconazole

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1. Posaconazole used as prophylaxis of invasive Aspergillus and disseminated Candidiasis in severely immunocompromised hosts
2. Posaconazole active against Candida species that are resistant to other azoles
3. Posaconazole active against Zygomycetes

Front 26

Clinical use of Griseofulvin

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Griseofulvin used for nail and scalp infection that do not respond to topical therapies

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Adverse side effects of Flucytosine

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Flucytosine is very toxic to bone marrow and kidneys

Front 28

Clinical application of Flucytosine and why

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Flucytosine used only in combination with Amphotericin B to treat severe candida or cryptococcal infections (allows Amphotericin B dose to be reduced)

Front 29

Mechanism of action of Echinocandins (anti-fungal)

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Echinocandins inhibit fungal enzyme 1,3-beta-D-glucan synthesis

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Benefit of Echinocandins (anti-fungal)

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Echinocandins are safe to use in renally-impaired patients

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Clinical use of Caspofungin

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Caspofungin is excellent for life-threatening systemic fungal infections in patients that cannot tolerate Ampotericin B

Front 32

Benefit of Micafungin

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Micafungin does not have major effects on CYP450 system or drugs metabolized by it

Front 33

Drug used to treat pregnant patients with life-threatening fungal infections

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Amphotericin B used to treat pregnant patients with life-threatening fungal infections

Front 34

Drugs classified at Echinocandins

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Caspofungin, Micafungin, Anidulafungin are Echinocandins (inhibit fungal enzyme 1,3-beta-D-glucan synthesis)