Antifungfal Drugs

Question 1

amphotericin B: use, mechanism, side effect

Answer 1

• broad spectrum for most systemic mycoses
• binds ergosterol in fungal membranes producing membrane instability/leakage
• side effect: nephrotoxicity

Question 2

flucytosine: use, mechanism, side effect

Answer 2

• serious infections due to Candida and Cryptococcus
• converted by fungal enzyme to 5-FU, whose metabolites then bock nucleic acid synthesis
• side effect: nephrotoxicity

Question 3

imidazoles/triazoles: mechanism, drug names

Answer 3

• inhibit enzyme that converts lanosterol to ergosterol, depriving membranes of ergosterol
• FIV: fluconazole, itraconazole, voriconazole

Question 4

fluconazole: mechanism, candida spectrum (sites, species), use other than Candida

Answer 4

• inhibits enzyme that converts lanosterol to ergosterol, depriving membranes of ergosterol
• sites: CNS and urinary
• least: some albicans and glabrata, no krusei
• Cryptococcus meningitis

Question 5

itraconazole: mechanism, candida spectrum (sites, species), uses other than Candida

Answer 5

• inhibits enzyme that converts lanosterol to ergosterol, depriving membranes of ergosterol
• sites: esophageal and oropharyngeal
• intermediate: albicans, glabrata, some krusei
• Blastomyces, Histoplasma

Question 6

voriconazole: mechanism, candida spectrum (sites, species), use other than Candida

Answer 6

• inhibits enzyme that converts lanosterol to ergosterol, depriving membranes of ergosterol
• sites: not urinary
• broad: covers many species
• invasive Aspergillus

Question 7

list imidazoles/triazoles from broadest to least broad candida spectrum

Answer 7

voriconazole, itraconazole, fluconazole

Question 8

imidazole/triazole with CNS penetration

Answer 8

fluconazole

Question 9

which antifungals can cause nephrotoxicity?

Answer 9

amphotericin B and flucytosine

Question 10

imidazole/triazole used against crpytococccus meningitidis

Answer 10

fluconazole

Question 11

imidazole/triazole used against blastomyces and histoplasma

Answer 11

itraconazole

Question 12

antifungals used to treat invasive Aspergillus

Answer 12

voriconazole, caspofungin

Question 13

imidazole/triazole that has risk of serious cardiovascular events/death?

Answer 13

itraconazole

Question 14

side effects of imidazole/triazoles?

Answer 14

• mild hepatotoxicity

- potent inhibitors of many CYP enzymes

Question 15

caspofungin: uses, mechanism

Answer 15

• invasive Aspergillus, Candida (esophageal and systemic)

- inhibits fungal cell wall synthesis by blocking synthesis of beta(1,3)-D-glucan

Question 16

drugs used to treat superficial Candida infections

Answer 16

FACIN: fluconazole, clotrimazole, itraconazole, nystatin, amphotericin B

Question 17

nystatin: use, mechanism

Answer 17

• superficial Candida infections

- mechanism similar to amphotericin B: binds ergosterol in fungal membranes producing membrane instability/leakage

Question 18

treatment of ophthalmic fungal infections

Answer 18

natamycin

Question 19

natamycin: use, mechanism

Answer 19

• treatment of ophthalmic fungal infections

- mechanism similar to amphotericin B: binds ergosterol in fungal membranes producing membrane instability/leakage

Question 20

only FDA-approved topical Rx for fungal nail infections

Answer 20

ciclopirox

Question 21

terbinafine: use, mechanism

Answer 21

• oral preparation for severe dermatophyte infections refractory to topical therapy
• inhibits fungal squalene epoxidase; fungicidal

Question 22

inhibits fungal squalene epoxidase

Answer 22

terbinafine

Question 23

inhibit enzyme that converts lanosterol to ergosterol, depriving membranes of ergosterol

Answer 23

imidazole/triazoles: fluconazole, itraconazole, voriconazole

Question 24

griseofulvin: use, mechanism

Answer 24

• for recalcitrant dermatophytic infections of skin, hair, nails
• children with tinea capitis
• interferes with microtubule function/mitotic spindle/mitosis