Antifungal Agents

Question 1

DNA and RNA synthesis inhibitor (converted to 5-FU -> f-FdUMP and FUTP); fungistatic

Answer 1

flucytosine

Question 2

resistance due to mutations of perm ease and deaminase

Answer 2

flucytosine

Question 3

narrow spectrum agent used to treat systemic candidiasis, cryptococcal meningitis, and aspergillus

Answer 3

flucytosine

Question 4

synergistic effect due to enhanced uptake due to fungal cell membrane damage

Answer 4

flucytosine and amphotericin B

Question 5

Adverse reactions: bone marrow suppression, reversible hepatotoxicity

Answer 5

flucytosine

Question 6

binds to tubulin, thereby disrupting assembly of the mitotic spindles; fungistatic

Answer 6

griseofulvin

Question 7

drug accumulates in keratin precursor and binds tightly to keratin; allow new growth of skin, hair, and nails to be fungal free

Answer 7

griseofulvin

Question 8

commonly used in children for treatment of tinea capitus

Answer 8

griseofulvin

Question 9

prevents conversion of squalene to lanosterol, a precursor of ergosterol; causes accumulation of squalene (cytotoxic)

Answer 9

terbinafine

Question 10

topical use for ringworm; oral use on onychomycosis of toe- and fingernails

Answer 10

terbinafine

Question 11

Adverse reactions (oral route only): cutaneous lupus, SJS, disturbances of taste; liver failure

Answer 11

terbinafine

Question 12

inhibit 14a-sterol demethylase - causes destabilization of cell membrane and associated enzymes; fungistatic

Answer 12

itraconazole

Question 13

need to check susceptibility of organism to choose appropriate member of this class

Answer 13

azoles

Question 14

broad spectrum agent used topically or orally against many pathogenic fungi

Answer 14

itraconazole (azoles)

Question 15

Adverse reactions: HTN, hypokalemia and edema, cardiac suppression

Answer 15

itraconazole

Question 16

Drug interaction - numerous drug interactions due to inhibition of human CYPs

Answer 16

azoles

Question 17

binds to ergosterol and disrupts membrane stability; forms pores in membrane and allows leakage of cellular contents

Answer 17

amphotericin B, nystatin

Question 18

broad spectrum agent useful for nearly all life-threatening systemic mycoses including cryptococcal meningitis

Answer 18

amphotericin B

Question 19

“swish and swallow” treatment of oral thrust

Answer 19

nystatin

Question 20

Adverse reactions: cytokine storm (infusion-related), renal toxicity/ischemia, myelosupression resulting in anemia

Answer 20

amphotericin B

Question 21

non-competitive inhibitors of beta-(1,3)-D-glucan synthesis; disrupts cell wall integrity resulting in osmotic stress and cell lysis

Answer 21

caspofungin

Question 22

therapy of deeply invasive aspergillosis in patients unresponsive to traditional agents; systemic candidiasis

Answer 22

caspofungin