Antifungals

Question 1

In cancer pts, 1st and 2nd most common cause of fungal deaths

Answer 1

1. Candida

2. Aspergillosis

Question 2

Cell wall synthesis inhibitors

- Echinocandins (3)

Answer 2

Anidulafungin
Caspofungin
Micafungin

Question 3

Antifungals that forms membrane pores

- Polyenes

Answer 3

Amphotericin B

Nystatin

Question 4

Antifungals that inhibit nucleic acid synthesis

Answer 4

Flucytosine

Pentamidine

Question 5

Antifungals that inhibit Ergosterol synthesis by inhibiting cytP450

Answer 5

Azoles

• fluconazole
• itraconazole
• keto
• vori
• ter

Question 6

Polyenes

• Ampho B
• Nystatin

Targets?

Answer 6

Bind Ergosterol on fungal membrane + forms membrane pores

*as resistance builds, fungi can downregulate ergosterol or have thicker membranes

Question 7

Toxicity of amphoB

Answer 7

1. Fever/chills 
"shake and bake"
2. Nephrotoxicity
3. IV phlebitis
"amphoterrible"
4. Hypotension, arrythmia, anemia

Question 8

Why do you supplement AMphoB with K+ and Mg+?

Answer 8

bc of altered renal tubule permeability

Question 9

MOA of Azoles

Answer 9

Inhibit fungal sterol (ergosterol) syntheiss by inhibiting Cyt P450 that converts lanosterol to ergosterol.

Question 10

Drug of choice for cryptococcal meningitis (AIDS

Answer 10

Fluconazole

Question 11

Only antifungal that is renally eliminated

Answer 11

Fluconazole

Question 12

MOA of echinocandins

Answer 12

Inhibit cell wall synthesis by inhibiting synthesis of B-glucan

Question 13

Clinical use of Echinocandins

Answer 13

Invasive aspergillosis

Candida

Question 14

Flucytosine MOA

Answer 14

Inhibits NA synthesis by conversion of Flucytosine to to 5-fluorouracil by cytosine deaminase

*mammals do not have cytosine deaminase

Question 15

Toxicity of flucytosine

Answer 15

Bone marrow suppression

Question 16

MOA of griseofulvin

Answer 16

interferes w/ microtubule fxn;
disrupts mitosis
- accumulates in keratin containing cells

Question 17

Toxicity of griseofulvin

Answer 17

Teratogenic
Carcinogenic
Increase CYTP450 and warfarin metabolism

Question 18

Which antifungals accumulate in nails

Answer 18

Terbinafine

Griseofulvin

*both are great to treat dermatophytes! (tinea, ringworm)

Question 19

MOA of terbinafine

Answer 19

Interferes with fungal enzyme, squalene epxide

(prev squalene –> squalene epoxide) and eventually ergosterol cannot be formed