Antifungals Flashcards Preview

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Flashcards in Antifungals Deck (23):
1

clotrimazole

topical OTC for tinea and candida

2

miconazole

topical OTC for tinea and candida

3

ketoconazole

for systemic infection; relies on gastric acidity for absorption
used for superficial dermatophytes, Cushing's syndrome (dec cort synth), prostate cancer (dec test synth), hypercalcemia in sarcoidosis (inh form active vit D)

4

ADR ketoconazole

less specific affinity for fungal P450 -> GI, rash, inhibits adrenal steroid synthesis (gynecomastira, dec libido), hepatotoxic potential
potent CYP 3A4 inhibitor

5

MOA azoles

inhibit lanosterol -> ergosterol by inhibiting P450-dependent lanosterol C14-demethylase

6

ADR of azoles

drugs intx, cholesterol synthesis, cell toxicity
pregnancy cat C (vori is D)
liver failure (monitor LFTs)

7

fluconazole

oral and IV for candida prophylaxis and tx
*renal elimination
best tolerated of all azoles
ADR: GI, rash, HA, alopecia (high dose); strong CYP 2C9 and 2C19 inhibitor, 3A4 in high doses

8

itraconazole

greater spectrum than flu, includes Aspergillus
used for onychomycosis
ADR: GI, diarrhea, taste disturbances, elevated LFTs, rare HF with long therapy (neg inotrope)
strong CYP 3A4 and P-glycoprotein inhibitor

9

voriconazole

better against Aspergillus than itra
for invasive candidiasis and aspergillosis, penetrates CNS but not urine
ADR: transient visual disturbances, rash, photosensitivity, hallucinations, prolonged QT
inhibits CYP 2C9, 2C19, 3A4; preg cat D

10

posaconazole

better for mucor than vori
oral suspension taken with high-fat meal or liquid supplement, reserved for mod fungal infxn res to itra
poor penetration to CSF and urine
ADR: like flu, strong CYP 3A4 inhibitor

11

terbinafine MOA

inhibits squalene -> squalene epoxide = toxic, suicidal mechanism

12

uses and ADR terbinafine

onychomycosis (> itra)
ADR: GI complaints, HA, rash; less common: hepatotoxicity, SJS, blood dycrasias, taste disturbances
strong CYP 2D6 inhibitor, preg cat B

13

polyenes MOA

bind ergosterol in cell membrane

14

uses amphotericin B

slow IV infusion for systemic infections and in pregnancy

15

lipid formulation of ampho B

fewer acute reactions but more expensive

16

ADR ampho B

infusion-related (fever, chills, n/v, HA, myalgias - prophy with NSAID, hydrocortisone, diphenhydramine), nephrotoxicity d/t aff arteriole constriction (prophy with saline), hypokalemia d/t renal tubule toxicity

17

nystatin

polyene; topical cream or ointment, sometimes oral suspension for oral thrush
can be used for recurrent gut infections in AIDS patients

18

echinocandin MOA

inhibits B-glucan synthase, disrupting glucan polymers in cell wall

19

caspofungin, micafungin, anidulafungin

echinocandin antifungals

20

uses of echinocandins

DOC for invasive candidiasis (minimal CSF or urine penetration), alternative to azole antifungals for candida and aspergillus infections

21

echinocandin ADRs

fever, phlebitis at IV site, elevated LFTs, minimal drug interactions

22

griseofulvin

for dermatophyte infections
poor tolerance d/t allergic reactions, photosensitivity, GI distress, neurologic effects
take with high-fat meal for best absorption
enzyme inducer

23

flucytosine

anti-cancer drug not used anymore d/t BM toxicity
inhibits DNA/RNA synthesis when converted to 5-FU intracellularly (toxic antimetabolite)
was used for severe systemic infections with ampho B