Antifungal Medications

Question 1

Amphotericin B: MOA

Answer 1

• Binds ergosterol

- Alters membrane permeability

Question 2

Amphotericin B and CNS activity

Answer 2

Poor penetration

Question 3

Main adverse reaction with Amphotericin B use (1)

Answer 3

Nephrotoxicity, caused by vasoconstriction of afferent renal arterioles

Question 4

T/F Amphotericin B has an infusion related side effect

Answer 4

True, if given rapidly patients may report shaking, chills, fever
*Pre-medicate with NSAIDS, Aspirin

Question 5

Amphotericin B: Spectrum of Activity

Answer 5

All fungal infections (except rare instances)

Question 6

Amphotericin B Lipid Complex

Answer 6

New Amphotericin is given as a lipid complex, which some studies show DECREASED NEPHROTOXICITY

Question 7

5-Fluocytosine: MOA

Answer 7

• Penetrates fungal cell wall
• Altered by cytosine deaminase
• Inhibits pyrimidine metabolism

Question 8

5-Fluocytosine and CNS

Answer 8

Good CNS penetration

Question 9

Main adverse reaction associated with 5-Fluocytosine (1)

Answer 9

Bone marrow hypoplasia

Question 10

When should 5-Fluocytosine be used?

Answer 10

Serious infections:

• Candida
• Cryptococcus

Question 11

T/F 5-Fluocytosine is often administered with Amphotericin B

Answer 11

True, resistance is problematic when used alone

Question 12

2 broad categories of Azoles

Answer 12

1. Imidazole

2. Triazole

Question 13

1 drug in the Imidazole category

Answer 13

Ketoconazole

Question 14

4 drugs in the Triazole category

Answer 14

Fluconazole
Itraconazole
Voriconazole
Posaconazole

Question 15

Azole: MOA

Answer 15

• Interfere with fungal cytochrome P450 enzymes

- Conversion of Lanosterol to Ergosterol cannot occur

Question 16

Which Azole broad category is used the most. Why?

Answer 16

Traizoles have increased affinity for fungal p450 enzymes

Question 17

Ketoconazole causes decrease in what 2 serum levels

Answer 17

• Testosterone

- Adrenocorticotropic hormone

Question 18

Drug interactions with Azole use (3)

Answer 18

1. Antacids
2. Cycolsporin (increased serum)
3. Warfarin (increased anticoagulation)

Question 19

Which Azole drug is not commonly used in the United states?

Answer 19

Ketoconazole

Question 20

Which Azole is the primary treatment for CNS fungal infections

Answer 20

Fluconazole

Question 21

T/F Fluconazole is altered by gastric pH/Food in stomach

Answer 21

False

Question 22

What Azole drug is commonly used to treat systemic fungal infections

Answer 22

Itraconazole

Question 23

Which Azole is used to treat invasive aspergillosis

Answer 23

Voriconazole

Question 24

T/F Voriconazole serum levels are decreased in patients who have recently had a high fat meal

Answer 24

True

Question 25

What are 2 adverse reactions with Voriconazole use

Answer 25

1. p450 Interactions | 2. Visual disturbances

Question 26

What Azole is used in severely immunocompromised patients in treatment of Candida and Aspergillus infections?

Answer 26

Posaconazole

Question 27

T/F Posaconazole inhibits CYP34A

Answer 27

True

Question 28

Caspofungin acetate: MOA

Answer 28

Inhibition of gluten synthesis

Question 29

Why is caspofungin generally used as a second line drug?

Answer 29

Phlebitis, elevated Serum creatinine

Question 30

What is the indicated use of caspofungin acetate (2)

Answer 30

1. Invasive aspergillosis | 2. Candidiasis

Question 31

Griseofulvin: MOA

Answer 31

Disrupts mitotic spindle structure

Question 32

T/F Griseofulvin is a p450 suppressor

Answer 32

False. It is an inducer, meaning increased metabolism

Question 33

Main use of griseofulvin

Answer 33

Dermatophytosis

Question 34

Terbinafine: MOA

Answer 34

- Squalene epoxidase inhibitor | - Inhibits sterol synthesis

Question 35

T/F Terbinafine interacts with p450

Answer 35

True

Question 36

Main use of Terbinafine

Answer 36

Onychomycosis (fungus under nail) after topical therapy has failed

Question 37

T/F Terbinafine is safe to give to pregnant patients

Answer 37

False

Question 38

3 main drugs to treat oral candidiasis (thrush)

Answer 38

1. Nystatin (rinse) 2. Clotrimazole troches (tablet) 3. Amphotericin B suspension (rinse)