Antifungal agents Flashcards Preview

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Flashcards in Antifungal agents Deck (28):
1

What is a main target for selective therapy against fungus

ergosterol, which is used in membranes instead of cholesterol

2

What is the nucleic acid synthesis inhibitors

flucytosine

3

Flucytosine MOA

selective active transport (cytosine permease), converted to 5-FU then 5FdUMP, fungistatic

4

Resistance to Flucytosine

must be used in combination due to development of resistance in individual patient

5

Therapeutic uses of flucytosine

1) yeast infections
2) fungal meningitis
3) Aspergillus
w/ amphotericin B

6

Adverse effects of flucytosine

hematologic, hepatotoxic, w/ amphotericine B can cause kidney damage, CYP3A4 inhibitor

7

Mitosis inhibitor antifungal drug

Griseofulvin

8

MOA of griseofulvin

interupts mitotic spindle, fungistatic. Accumulates in keratin

9

Therapeutic use of griseofulvin

Oral, hair, skin, and nail fungal infections may take 2-6 weeks, commonly used for scalp ringworm. Replaced by faster acting drugs

10

Adverse reactions to griseofulvin

headaches, AIP, photosensitivity

11

What is AIP

acute intermittent porpyria, due to induction of CYPs that increase demand for heme.

12

Squalene epoxidase inhibitors

terbinafine (lamisil)

13

MOA of terminafine

inhibits squalene epoxidase, squalene acumulation is fungicidal

14

Therapeutic uses of terminafine

topical for ringworm, oral use for to and fingernails

15

Adverse reactions to terminafine (4)

inhibits CYP 2D6, induces 3A4
skin reactions
disturbance of taste
hepatotoxicity

16

Azole prototype

fluconazole

17

MOA of fluconazole

inhibits ergosterol formation, fungistatic (CYP mediated)

18

What are the two classes of azole

imidazoles and triazoles, triazoles more selective

19

Therapeutic use of fluconazole

broad spectrum, topicaly or orally

20

Adverse reactions to fluconazole

generally well tolerated
1) GI upset
2) inhibition of CYPs
3) hepatotoxicity
4) avoid during pregnancy

21

What is the "swish and swallow" treatment for thrush

nystatin

22

Inhibitors of fungal membrane stability

amphotericin B, nystatin

23

Amphotericin B MOA

binds ergosterol and disrupts membrane stability

24

Therapeutic uses of amphotericin B

IV, for systemic life threatening fungal infections, including meningitis

25

Adverse reactions to amphotericin B

Well-tolerated topically and orally
IV infusion can cause cytokine storm, renal toxicity, hematologic toxicity
lipid formulation less toxic, more expensive

26

Inhibitors of fungal cell wall synthesis

caspofungin

27

MOA of caspofungin

disrupts cell wall integrity resulting in osmotic stress and lysis, fungicidal

28

Adverse effects of caspofungin

none, histamine w/ infusion