Antifungals

Question 1

Antifungals that don’t work on the cell wall?

Answer 1

Griseofulvin and flucytosine

Question 2

Systemic fungal infection DOC

Answer 2

amphotericin B

Question 3

Amphotericin B (Fungizone) MOA

Answer 3

Interacts with ergosterol within the membrane to create a pore that leads increased permeability and to depolarization. Fungicidal.

Question 4

Amphotericin B Toxicity

Answer 4

NEPHROTOXIC (slow renal excretion).

Question 5

Amphotericin B infusion toxicity

Answer 5

immediate during infusion. Chills, fever, muscle spasm, vomiting, HA.

Question 6

Flucytosine (ancobon) MOA

Answer 6

Enters the cell. Is converted into 5-fluorouracil and interrupts DNA and RNA synthesis. Conversion happens in fungal and bacterial cells.

Question 7

Flucytosine kinetics

Answer 7

Oral. Enters the CSF.

Question 8

Amphotericin B kinetics

Answer 8

Broad spectrum. IV. Poor CNS penetration.

Question 9

Cryptococcus infections DOC

Answer 9

Flucytosine with amphotericin B

Question 10

Flucytosine toxicity

Answer 10

renal, bone marrow depression (anemia, leukopenia, thrombocytopenia),hepatotoxicity.

Question 11

Azoles (4)

Answer 11

ketoconazole, fluconazole, voriconazole, itraconazole

Question 12

Azoles MOA

Answer 12

inhibit the production of ergosterol. Causes an accumulation of toxic intermediates and increases membrane permeability which inhibits fungal growth. Fungistatic.

Question 13

Ketoconazole toxicity

Answer 13

Inhibits P450s (drug interactions), gynecomastia.

Question 14

Fluconazole kinetics

Answer 14

oral/IV. Renal elimination. Penetrates the CSF.

Question 15

Antifungals that penetrate the CSF?

Answer 15

Fluconazole and flucytosine.

Question 16

Fluconazole toxicity

Answer 16

Less drug interactions than the others

Question 17

Aspergillus DOC

Answer 17

Voriconazole with amphotericin B

Question 18

Voriconazole toxicity

Answer 18

Metabolized by and inhibits P450s mainly CYP2C19 (A LOT of drug interactions), Visual impariment.

Question 19

Itraconazole toxicity

Answer 19

potent inhibitor or CYP3A4

Question 20

Echinocandins (3)

Answer 20

Caspofungin, Micafungin, Anidulafungin

Question 21

Echinocandins MOA

Answer 21

inhibits sythesis of cell wall component called beta (1,3)-D-glucan which is not present in mammalian cells. “penicillin of antifungals” Fungicidal.

Question 22

Caspofungin uses

Answer 22

treatment of invasive aspergillosis in refractory patients. Also for esophageal candidiasis.

Question 23

Caspofungin toxicity

Answer 23

Less drug interactions!

Question 24

Griseofulvin (fulvicin U/F) MOA

Answer 24

enters the cell and binds to the microtubules to destroy the mitotic spindle. Fungistatic. Binds to keratin to prevent new skin infections.

Question 25

Onychomycosis DOC

Answer 25

Griseofulvin

Question 26

Griseofulvin kinetics

Answer 26

used for dermatophytes. Oral only.

Question 27

Griseofulvin toxicity

Answer 27

headache

Question 28

Griseofulvin contraindications

Answer 28

acute intermittent porphyria, hepatocellular failure.

Question 29

Terbinafine (lamisil) MOA

Answer 29

interferes with sterol sythesis. oral or topical.

Question 30

Terbinafine use

Answer 30

effective against onychomycosis but not the DOC

Question 31

Nystatin (myostatin) MOA

Answer 31

polyene antibiotic. Creates pores in the membrane similar to amphotericin B.

Question 32

Nystatin Uses

Answer 32

oral or topical for candida infections.

Question 33

Naftifine (Naftin)

Answer 33

OTC for athletes foot/jock itch

Question 34

Tolnaftate (tinactin)

Answer 34

OTC for athletes foot/jock itch

Question 35

Tioconazole (vagistat)

Answer 35

OTC azole

Question 36

Miconazole (monistat)

Answer 36

OTC azole

Question 37

Clotrimazole (Lotrimin)

Answer 37

OTC azole. Lozenge for candidal infections.