Antifungal Drugs

Question 1

What is the fungal equivalent of cholesterol?

Answer 1

Ergosterol

Question 2

Which class of antifungal medication is fungicidal?

Answer 2

Polyenes. Ex. Nystatin, pimaricin, amphotericin B

Question 3

What is the target of polyene drugs?

Answer 3

Ergosterol. Binds to it forming holes in the cell membrane

Question 4

What is the difference between superficial and systemic mycoses?

Answer 4

Superficial- limited to the epidermal region
Systemic- invade the skin, lungs and lymphatic tissue

Question 5

Which fungus structure is critical for cell viability and pathogenicity?

Answer 5

Cell wall

Question 6

Allylamine examples

Answer 6

Naftifine, terbinafine, butenafine

Question 7

Allylamine MOA

Answer 7

Inhibit ergosterol biosynthesis at the level of squalene epoxidase

Question 8

Azole/triazole examples

Answer 8

Fluconazole, itraconazole, ketoconazole

Question 9

Azole/triazole MOA

Answer 9

Inhibit cytochrome P450 dependent enzymes (C14-alpha-demthylase) involved in the biosynthesis of ergosterol

Question 10

Polyene example

Answer 10

Nystatin, pimaricin, amphotericin B

Question 11

Polyene MOA

Answer 11

Interact with sterols in the cell membrane to form channels through which small molecules leak from the out of the fungal cell

Question 12

Echinocandin examples

Answer 12

Caspofungin, micafungin, anidulafungin

Question 13

Echinocandin MOA

Answer 13

Concentration-dependent, noncompetitive inhibitors of β-1,3 glucan synthase, an essential component of the fungal cell wall

Question 14

5-fluorocytosine MOA

Answer 14

Inhibitor of both DNA and RNA synthesis via the intracytoplasmic conversion of 5-fluorocytosine to 5-fluorouracil.

Question 15

Polyene structure

Answer 15

Alternating conjugated double bonds that constitute a part of their macrolide ring structure

Question 16

Polyenes have ____ times binding affinity for ergosterol over cholesterol

Answer 16

500 times

Question 17

First broad spectrum antifungal

Answer 17

Nystatin

Question 18

True or false: Natamycin is absorbed systemically

Answer 18

False

Question 19

Which polyene is available in IV formulation?

Answer 19

Amphotericin B

Question 20

Difference between conventional and liposomal formulation of amphotericin B?

Answer 20

Liposomal formulation less nephrotoxic

Question 21

Amphotericin B adverse effects

Answer 21

Nephrotoxicity, hypokalemia, hypomagnesemia, bone marrow suppression

Question 22

Which antifungal was synthesized as a potential serotonin reuptake inhibitor?

Answer 22

Naftifine

Question 23

Where does terbinafine accumulate?

Answer 23

Nails

Question 24

Azole structure

Answer 24

5-membered nitrogen heterocyclic ring compound containing at least one other non-carbon atom (nitrogen, sulfur, or oxygen)

Question 25

Which agent may be used for neonatal thrush?

Answer 25

Miconazole

Question 26

Which agent is considered the treatment of choice for aspergillus?

Answer 26

Voriconazole

Question 26

Difference between isoconazole and miconazole?

Answer 26

Chlorine substitution pattern

Question 26

Which CYP enzymes does fluconazole inhibit?

Answer 26

CYP2C9 and CYP3A4

Question 27

Voriconazole adverse effects

Answer 27

Hepatotoxicity, visual disturbances (common), hallucinations, QTC prolongation and dermatologic reactions

Question 28

True or false: Caspofungin is not viable as an oral drug and must be administered intravenously

Answer 28

True