Infrequently used

Inhibits P450 enzymes

ADE: Decreased libido, gynecomastia, impotence, decreased testosterone, decreased cortisol, GI issues

Activity: Candida species, Cryptococcus neoformans. Candida krusei is intrinsically resistant.

TOC for susceptible candida, UTIs. Consolidation and maintenance therapy for cryptococcal memingitis.

If CrCl is less than 50, reduce dose by 50% or administer q48h, instead of q24h. ADE: Best tolerated of azoles. Monitor LFTs

Activity: Sporothrix schenckii, histoplasma capsulatum, blastomyces dermatitidis, coccidioides immitis, paracoccidioides brasiliensis. Active against fluconazole-resistant C. krusei and C. glabrata.

Drug of choice for mild-moderate infections caused by endemic dimorphic fungi. Also used in step-down therapy

If CrCl <10, reduce dose by 50%. Drug levels should be monitored after steady-state is reached (2 weeks).

Activity: Transitional therapy for C. krusei. DOC for aspergillus infections. 

If CrCl < 50, IV formulation should not be used.

Drug levels should be monitored due to non-linear PK. 

ADE: Dose-related visual disturbances (color changes, photophobia)

Activity: Broadest spectrum of azoles.

DOC for Zygomycetes

Dosing: Has saturable absorption. Only available in an oral suspension. Highest bioavailablity with a high-fat meal, small, frequent doses, no antacid.

 ADE: GI upset

Only available IV. All three drugs are basically the same.

Cannot be used in UTIs

Activity: Candida species.

DOC for moderate-severe candidemia or in patients with recent azole exposure. DOC for C. Glabrata or C. Krusei.

Dosing: Dose reduction in hepatic impairment.

Interactions: Levels increase with cyclosporins, decrease with rifampin.

Cannot be used in UTIs

Activity: Candida species.

DOC for moderate-severe candidemia or in patients with recent azole exposure. DOC for C. Glabrata or C. Krusei.

Dosing: No loading dose required. 

Interactions: Weak CYP3A4 inhibitor

Cannot be used in UTIs

Activity: Candida species.

DOC for moderate-severe candidemia or in patients with recent azole exposure. DOC for C. Glabrata or C. Krusei.

Cannot be used in UTIs

Activity: Candida species.

DOC for moderate-severe candidemia or in patients with recent azole exposure. DOC for C. Glabrata or C. Krusei.

Only available IV

Activity: Works against most pathogenic fungi. Very broad spectrum. Except: Aspergillus, Scedosporium species, Trichosporon beigelii.

Dosing: Infuse over 4-6 hours to reduce ADE. Give premedication (APAP + benadryl) 30 mins prior to administration. Give NS before and after dose.

ADE: Infusion-related toxicities (N/V/flu-like symptoms), nephrotoxicities. 

Liposomal Amphotericin B

Smaller size, circulates in bloodstream for longer. High concentrations in brain tissue.

Nephrotoxicity, renal infusion ADE are less likely than non-lipid formulation.

Liposomal Amphotericin B

Larger particles, removed from the blood stream quicker than regular amphotericin.

High concentration in liver, spleen, lungs.

Activity: Cryptococcus neoformans, Candida, Aspergillus, Phialophora, Cladosporium.

DOC for cryptococcal meningitis.

Should only be used in combination (w/ amphotericin and fluconazole) due to resistance if used monotherapy.

Only available orally. Penetrates CNS.

Needs dosage adjustment in renal impairment. 

ADE: Dose related. Hematologic effects (check CBC), GI upset, dermatologic effects.