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5 Cards in this Set

  • Front
  • Back

Fluconazole

Class: azole antifungal



Mechanism: antagonist of CYP450 ergosterol synthesis required for cell wall function



Spectrum: Candida albicans, cryptococcus, blastomycosis, coccidiomycosis



Metabolism: 80% excreted unchanged



Interactions: CYP2C19 strong inhibition, CYP2C9 3A4 moderate inhibition



Side effects: long Qtc, hepatotoxicity, seizures, toxic epidermal necrolysis

Caspofungin

Class: echinocandin antifungal



Mechanism: antagonist of b(1-3) D glucan synthesis required for fungal cell wall synthesis



Spectrum: invasive aspergillosis, invasive candidiasis



Metabolism: hydrolysis and acetylation, mainly hepatic. <1% excreted unchanged



Interactions: levels increased by calcineurin inhibitors/decrease levels of CNIs



Side effects: cytopaenias, rash, hypertension, transaminitis, pleural effusion

Amphotericin B

Class: polyene antifungal



Mechanism: Binds to cell wall ergosterol causing leak of cell contents and cell death



Spectrum: invasive aspergillosis, invasive candidiasis, cryptococcus, leishmaniasis



Metabolism: long half life, non linear kinetics, no dose adjustment



Interactions: antihypertensives, nephrotoxins



Side effects: nephrotoxicity, proximal tubular defect, hypotension, bradycardia, heart failure, infusion reactions

Voriconazole

Class: azole antifungal



Mechanism: inhibits CYP450 ergosterol synthesis causing failure of cell wall synthesis



Spectrum: invasive aspergillosis, Candida albicans, Candida glabrata, Candida krusei, prophylaxis in HSCT and haematological malignancy



Metabolism: hepatic through CYP450, 2% FU



Interactions: substrate for CYP2C19, 2C9, 3A4. Strong inhibitor of 3A4, moderate inhibitor of 2C19, 2C9. Saturable Metabolism



Side effects: visual disturbance/hallucinations, photosensitivity, nephrotoxicity, transaminitis, pancreatitis, Qtc prolongation, rash

Itraconazole

Class: azole antifungal



Mechanism: inhibits ergosterol synthesis causing failure of cell wall synthesis



Spectrum: invasive aspergillosis, oral/oesophageal candidiasis, histoplasmosis, coccidiomycosis, tinea



Metabolism: hepatic through CYP450, <0.02% FU



Interactions: substrate for 3A4, strong 3A4 inhibition, p-glycoprotein inhibition



Side effects: drowsiness, heart failure, hepatotoxicity, hearing loss, neuropathy