Antifungal agents Flashcards Preview

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Flashcards in Antifungal agents Deck (28)
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1
Q

What is a main target for selective therapy against fungus

A

ergosterol, which is used in membranes instead of cholesterol

2
Q

What is the nucleic acid synthesis inhibitors

A

flucytosine

3
Q

Flucytosine MOA

A

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

4
Q

Resistance to Flucytosine

A

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

5
Q

Therapeutic uses of flucytosine

A

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

6
Q

Adverse effects of flucytosine

A

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

7
Q

Mitosis inhibitor antifungal drug

A

Griseofulvin

8
Q

MOA of griseofulvin

A

interupts mitotic spindle, fungistatic. Accumulates in keratin

9
Q

Therapeutic use of griseofulvin

A

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

10
Q

Adverse reactions to griseofulvin

A

headaches, AIP, photosensitivity

11
Q

What is AIP

A

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

12
Q

Squalene epoxidase inhibitors

A

terbinafine (lamisil)

13
Q

MOA of terminafine

A

inhibits squalene epoxidase, squalene acumulation is fungicidal

14
Q

Therapeutic uses of terminafine

A

topical for ringworm, oral use for to and fingernails

15
Q

Adverse reactions to terminafine (4)

A

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

16
Q

Azole prototype

A

fluconazole

17
Q

MOA of fluconazole

A

inhibits ergosterol formation, fungistatic (CYP mediated)

18
Q

What are the two classes of azole

A

imidazoles and triazoles, triazoles more selective

19
Q

Therapeutic use of fluconazole

A

broad spectrum, topicaly or orally

20
Q

Adverse reactions to fluconazole

A

generally well tolerated

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

21
Q

What is the “swish and swallow” treatment for thrush

A

nystatin

22
Q

Inhibitors of fungal membrane stability

A

amphotericin B, nystatin

23
Q

Amphotericin B MOA

A

binds ergosterol and disrupts membrane stability

24
Q

Therapeutic uses of amphotericin B

A

IV, for systemic life threatening fungal infections, including meningitis

25
Q

Adverse reactions to amphotericin B

A

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

26
Q

Inhibitors of fungal cell wall synthesis

A

caspofungin

27
Q

MOA of caspofungin

A

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

28
Q

Adverse effects of caspofungin

A

none, histamine w/ infusion