Antifungal Flashcards
Unique targets for anti fungal therapy
Fungal cell membrane
Fungal cell wall
What drugs can be used for systemic fungal infections?
Amphotericin B, most azoles, fucystosine, and echinocandins
Amphotericin B MOA
Binds to egosterol in fungal cell membrane, and forms amp B containing pores=>alter membrane permeability=>fungicidal
Amphotericin B recommended use
Systemic Candidiasis
Cryptococcal Meningitis
Systemic disease caused by molds, including dimorphics
Amp B resistance
Reduced concentration of erogsterol in the membrane
Amp B Pharm properties
Nearly insoluble in water, widely distributed except for CNS
Amp B Adverse
Infusion reaction in almost all patients=> fever, chills, muscle spasms, vomiting, headache, HTN
Nephortoxicity=>decreased renal perfusion
Azoles MOA
Inhibit enzyme responsible for ergosterol synthesis=>make membrane leaky and damaged
Azole spectrum of activity
Pathogenic yeast=>candida and cryptococcus
Systemic mycoses
Dermatophytes
Azole resistance
Efflux pumps, mutation in target genes, and decreased ergosterol content in membrane
Azoles Adverse
Relatively non-toxic
Some GI problems
Interaction with P450=>varies from drug to drug
Fluconazole distinguishing characteristics, first line treatment for?
First line drug for many fungal infections=>highest therapeutic index
Widely distributed including CNS
Lowest interaction w/ P450 enzymes
Agent of choice for: candida, cryptococcis, coccidiomycosis
Itraconazole compared to fluconazole
Lipophilic
Broader spectrum of activity
Lower therapeutic index
More drug-drug interactions
Voriconazole Spectrum of activity. What is voriconazole the tx of choice for?
Very broad=> candida, endemic dimorphics
**due to low toxicity, has replaced amp B as tx of choice for aspergillosis
Voriconazole adverse rxns
Transient visual disturbances and hallucinations