Antifungals

Itraconazole
(Sporonox)

Blocks ergosterol synthesis by inhibiting 14α-demethylase

Fungistatic, lipophilic, needs acidic milieu for absorption

SE: ↑ LFTs, ↓ WBC, ↑ TG, nephrotoxicity, CHF worsening

Tx: dimorphic fungi, aspergillosis, candidiasis, superficial dermatophytes, onychomycosis, sporotrichosis

Inhibits cyt p450
(↑ levels of digoxin, cyclosporine, etc.)
Category C

SE: visual disturbances

Inhibits cyt p450
(↑ levels of digoxin, cyclosporine, etc.)
Category C

Fungistatic, crosses blood–brain barrier

Tx: candidiasis, pityriasis versicolor (PV), cryptococcosis, histoplasmosis, superficial dermatophytes, coccidioidomycosis

Inhibits 14α-demethylase Category C

Fungistatic, lipophilic, needs acidic milieu for absorption, ↑ absorption with food, inhibits cytochrome p450

SE: fulminant hepatitis (rare), ↑ LFTs (15%), gynecomastia

Tx: dermatophytes, candidiasis, dimorphic fungi, PV

Terbinafine
(Lamisil)

Inhibits squalene epoxidase (first step of ergosterol synthesis)

Category B

Fungicidal, biotransformed in liver, does NOT inhibit cyt p450

SE: nausea, metallic taste, liver damage, drug-induced LE

Tx: onychomycosis, tinea corporis, tinea pedis

Binds ergosterol and forms membrane pores

Category B

SE: acute reaction after infusion (fever, chills, nausea, tachypnea), nephrotoxicity, agranulocytosis, seizures, arrhythmias

Inhibits synthesis of glucan (fungal cell wall)

Category C

IV administration

Tx: candidiasis and aspergillosis

Disrupts microtubule function
(metaphase arrest)
Category C

Fungistatic, ↑ absorption w/ fatty meal, induces cytochrome p450 (may ↓ warfarin level), resistance seen in T. rubrum

SE: headache, paresthesias, photosensitivity, drug-induced LE, worsens acute intermittent porphyria

Tx: dermatophytes (NOT yeast or bacteria)