Antifungals

Question 1

what are the antifungal targets?

Answer 1

ergosterol synthesis (membrane)
beta-glucan synthesis (cell wall)
pore formation (cell wall)
DNA synthesis

Question 2

what is a yeast?

Answer 2

single cells, multiply by budding or fission

Question 3

what is an example of a yeast?

Answer 3

candida, cryp

Question 4

what is a mould?

Answer 4

multiply by spores

Question 5

what is an example of a mould?

Answer 5

mucor, aspergillus

Question 6

what are the polyenes?

Answer 6

nystatin, amphotericin B, natamycin

Question 7

what is the polyene moa?

Answer 7

binds to ergosterol in cell membrane, forming a pore

Question 8

polyene PKPD

Answer 8

poorly stable
toxic
not bioavailable

Question 9

what are the triazoles?

Answer 9

fluconazole, itraconazole, oral miconazole

Question 10

what is the triazole moa?

Answer 10

inhibits CYP450 in fungi that converts lanosterol to ergosterol

Question 11

fluconazole

Answer 11

active against yeasts

high bioavailability

Question 12

itraconazole

Answer 12

broad spectrum

bioavailability increases with acidic environment

Question 13

what are the echinocandins?

Answer 13

caspofungin, micafungin, anidulafungin

Question 14

what is the echinocandin moa?

Answer 14

inhibits beta glucan synthesis, increases permeability of cell wall

Question 15

what is the allylamine?

Answer 15

terbinafine

Question 16

what is the terbinafine moa?

Answer 16

inhibits squalene epoxidase which is involved in the ergosterol synthesis pathway

Question 17

triazole pkpd

Answer 17

AUC:MIC 25-100

Question 18

terbinafine pkpd

Answer 18

good bioavailability

Question 19

what does terbinafine target?

Answer 19

moulds and dermatophytes

Question 20

what is the flucytosine moa?

Answer 20

taken up by fungal cells then converted to 5-fu, which is incorporated into fungal RNA which blocks DNA synthesis

Question 21

flucotosine pkpd

Answer 21

high bioavailability

pkpd T > MIC