Antifungals Flashcards
Which groups of antifungals have an action that inhibits membrane synthesis?
Azoles
Echinocandins (Caspofungin)
Which groups of antifungals have an action that inhibits membrane function?
Polyenes
Allylamines
Which groups of antifungals have an action that inhibit nucleic acid synthesis and mitosis?
Others - Flucytosine, Griseofulvin
What is the mechianism of action of Azoles?
Inhibit 14-alpha-demethylase (cytochrome p-450 enzyme) which is responsible for producing ergosterol
=> ergosterol deplete => inhibit membrane formation
Th. fungi is killed by:
- inhibition of growth (inhibition of membrane formation)
- increased permeability of membrane
- accumulation of toxic sterol intermediates in cell
Describe the interactions of Azoles with other drugs
Many drug interactions due to varying effects on human p450 enzymes
What are the two classes of Azoles?
Imidazoles
Triazoles
When are imidazoles used?
Only in topical treatment because of its toxicity
- treatment of candida
- treatment of tinea
Give examples of Imidazoles
Ketoconazole
Miconazole
Clotrimazole (an active ingredient in Canesten)
Give examples of Triazoles
Fluconazole
itraconazole
Voriconazole
What can Fluconazole be used against?
Candida, Cryptococcus, Dermatophytes
- Candida krusei often resistant
Fluconazole can be administered in which ways?
Topical
Oral - well absorbed from GIT
Rarely IV
Why does fluconazole give good systemic availability?
Penetrates CSF
Excreted unchanged by kidney
What can Voriconazole be used against?
Life-threatening Candida
Aspergillus infection
Voriconazole can be administered in which ways?
Oral
IV - avoid in renal impairment
What can Itraconazole be used against?
Candida
Aspergillus
Cryptococcus