Antifungals: Azoles

Question 1

MOA azoles

Answer 1

decreased ergosterol synthesis by inhibition of fungal cyp450 with higher affinity for fungal than human

Question 2

when to use ketoconazole

Answer 2

less selective but used topically for tinea corporis, cruris, pedis, versicolor; cutaneous candidiasis, seborrheic dermatitis and dandruff

Question 3

when to use systemic ketoconazole and why

Answer 3

is a corticosteroid suppressor, so systemic for prostate cancer to decrease testosterone and for hyperadrenal states to reduce adrenal steroids.

Question 4

SE of systemic ketoconazole?

Answer 4

gynecomastia

Question 5

what is itraconazole used for

Answer 5

dimorphic fungi like histoplasma, blastomyces, sporothrix, aspergillus

Question 6

boxed warning of itraconazole

Answer 6

negative ionotropic effects may exacerbate CHF

Question 7

benefit of fluconazole

Answer 7

least effect on hepatic microsomal enzymes

and have high water solubility, good CSF penetration, and high bioavailability

Question 8

when to use fluconazole

Answer 8

cryptococcal meningitis, mucocutaneous candidiasis, orally for tx and prevention of vaginal candidiasis

Question 9

what does fluconazole NOT have activity against?

Answer 9

aspergillus or other filamentous fungi

Question 10

spectrum of voriconazole

Answer 10

aspergillus, candida, dimorphic fungi

Question 11

kinetics of voriconazole

Answer 11

hepatically metabolized

INHIBITOR OF CYP3A4

Question 12

what are the topical azoles

Answer 12

clotrimazole, miconazole