Antifungals Flashcards Preview

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Flashcards in Antifungals Deck (17):
1

amphotericin B and nystatin

polyene antifungals

2

binds to ergosterol in fungal cell membrane; allows leakage of small molecules; hydrophilic and hydrophobic sides; form pores in cell membrane through which K+ and Mg++ can leak out

polyene antifungals

3

amphotericin B: fungicidal, fungistatic or both

fungicidal

4

nystatin: fungicidal, fungistatic or both

both

5

polyene antifungal: primarily IV, greater than 90% bound to B-lipoprotein; nephrotoxicity (dose limiting)--> less severe with lipid based forms; sodium loading may ameliorate toxicity; fever and chills; preferred treatment for deep fungal infections

amphotericin B

6

polyene antifungal: topical or oral administration only; candidal infections of oral cavity

nystatin

7

why doesnt 5-flucytosine (ancobon) block thymidylate synthase in humans?

mammalian cells do not have cytosine deaminase

8

antimetabolite; inhibits thymidylate synthase and DNA synthesis; fungicidal or static; almost always used in combo with amphotericin B--> penetrates CSF and treats meningitis; reduce dose with renal deficiency

5-flucytosine

9

inhibit synthesis of ergosterol--> necessary sterol for fungal cell membrane; broad spectrum antifungal

imidazole antifungal agents

10

azole: inhibits P450 enzyme causing potential increase in serum levels of concurrent drugs

fluconazole

11

azole: not significant to CSF; mostly bile excretion; potent inhibitor of CYP3A4; broader spectrum than fluconazole

itraconazole

12

azole: exhibits genetic polymorphism (CYCP2C19 deficiency =increased conc); contraindicated with drugs that induce P450 including rifampin, rifabufin, carbamazapine, long acting barbiturates

voriconazole

13

which azole? easily crosses to CSF

fluconazole

14

which azoles? hepatic elimination

itra- and voriconazole

15

which azole? renal elimination

fluconazole

16

azole: if swallowed can increase hepatic enzymes in the plasma and rarely lead to hepatitis

clotrimazole

17

inhibits alpha (1,3)D-glucan synthesis-- integral components of fungal cell WALL

caspofungin