antifungals/antiprotozans/antihelminths

Question 1

lanosterol synthesis inhibition

Answer 1

terbinafine

Question 2

cell wall synthesis inhibition

Answer 2

echinocandins (anidulafungin, caspofungin, micafungin)

Question 3

cell membrane integrity inhibition

Answer 3

polyenes (Amphotericin B, Nystatin)

Question 4

nucleic acid synthesis inhibition

Answer 4

flucytosine

Question 5

ergosterol synthesis inhibition

Answer 5

-conazoles

Question 6

Amphotericin B MOA

Answer 6

binds ergosterol (unique to fungi); forms membrane pores that allow leakage of electrolytes

Question 7

Amphotericin B use

Answer 7

serious, systemic mycoses

intrathecally for fungal meningitis

Question 8

Amphotericin B coadmin

Answer 8

Supplemental K and Mg bc of altered renal tubule permeability

Hydration: dec nephrotoxicity

Question 9

Amphotericin B ADR

Answer 9

Fever/chills, hypotension, nephrotoxicity, arrhythmias, anemia, IV phlebitis,

Question 10

which type of Amphotericin B decreases toxicity?

Answer 10

liposomal amphotericin

Question 11

Nystatin MOA

Answer 11

same as Amphotericin B; ONLY topical due to extreme systemic toxicity

Question 12

Nystatin use

Answer 12

swish and swallow for oral candidiasis

topical for diaper rash/vaginal

Question 13

Flucytosine MOA

Answer 13

inhibits RNA and DNA biosynthesis by conversion to 5-FU by cytosine deaminase

Question 14

Flucytosine use

Answer 14

systemic fungal infections (esp. meningitis by Cryptococcus) in combo with Amphotericin B

Question 15

Flucytosine ADR

Answer 15

bone marrow suppression

Question 16

Conazoles MOA

Answer 16

inhibit fungal sterol synthesis by inhibiting p450 enzyme that converts lanosterol to ergosterol

Question 17

conazoles use

Answer 17

local and less serious systemic mycoses

Question 18

fluconazole use

Answer 18

chronic suppression of cryptococcol AIDS pt and candida infections of all types

Question 19

itraconazole use

Answer 19

blastomyces, coccidioides, histoplasma

Question 20

clotrimazole, miconazole use

Answer 20

tropical fungal infections

Question 21

conazole ADR

Answer 21

testosterone synthesis inhibition (gynecomastia w/ ketoconazole); liver dysfunction (inhibits p450)

Question 22

terbinafine MOA

Answer 22

inhibits the fungal enzyme squalene epoxidase

Question 23

terbinafine use

Answer 23

dermatophytoses (esp. onchomycosis)

Question 24

terbinafine ADR

Answer 24

GI upset, HA, hepatotoxicity, taste disturbance

Question 25

Echinocandins MOA

Answer 25

inhibit cell wall synthesis by inhibiting synthesis of B-glucan

Question 26

Echinocandin use

Answer 26

invasive aspergillosis, Candida

Question 27

Echinocandin ADR

Answer 27

GI upset, flushing (induces histamine)

Question 28

Griseofulvin MOA

Answer 28

interferes w/ microtubule function, disrupts mitosis.

deposits in keratin-containing tissues (i.e. nails)

Question 29

Griseofulvin use

Answer 29

oral tx of superficial infections; inhibits growth of dermatophytes

Question 30

Griseofulvin ADR

Answer 30

teratogenic, carcinogenic, confusion, HA, p450 inducer –> inc warfarin metabolism

Question 31

Antiprotozoan therapy

Answer 31

pyrimethamine (toxo); suramin and melarsoprol (Trypanosoma brucei); nifurtimox (T cruzi); sodium stibogluconate (leishmaniasis)

Question 32

Anti-mite/louse therapy

Answer 32

Permethrin, malathion, lindane

Question 33

Permethrin MOA

Answer 33

blocks Na channels –> neurotoxicity

Question 34

Malathion MOA

Answer 34

AChE inhibitor

Question 35

Lindane MOA

Answer 35

blocks GABA channels –> neurotoxicity

Question 36

Chloroquine MOA

Answer 36

blocks detox of heme into hemozoin. heme accumulates and is toxic to plasmodia

Question 37

Chloroquine use

Answer 37

Tx of plasmodium species other than P. falciparum

Question 38

Chloroquine ADR

Answer 38

retinopathy, pruritus (in dark skinned individuals)

Question 39

Chloroquine resistance

Answer 39

due to membrane pump dec. intracellular concentration of drug

Question 40

P. falciparum treatment

Answer 40

artemether/lumefantrine OR atovaquone/proguanil

Question 41

life-threatening malaria tx

Answer 41

Quinidine (US), quinine (outside US), or artesunate

Question 42

antihelminthic therapy

Answer 42

mebendazole (microtubule inhibitor), pyrantel pamoate, ivermectin, diethylcarbamazine, praziquantel