azole antifungals Flashcards
name some triazoles
fluconazole, itraconazole, voriconazole, posaconazole, isavuconazole.
what were clotrimazole and miconazole mostly used for
superficial infections.
when was ketaconazole licensed
1981
how do azoles work
they inhibit lanosterol 14a demethylase which leads to ergosterol being less produced and toxic methylated sterols building up, results in cell inhibition or death.
what are some extra toxicity issues with voriconazole
MHRA, squamous cell carcinoma, hepatotoxicity
what do all triazoles have an effect on
electrical cardiac rythm
what are azoles metabolised by
cytochrome P450 enzymes. azoles can also inhibit these enzymes.
what effect does drug-drug interaction have on patients
affects concentration of triazoles. Use therapeutic drug monitoring for these people.
which triazoles need monitoring
itraconazole, voriconazole, posaconazole.
what are some mechanisms of antifungal resistance
decrease effective drug concentration, drug target alterations, metabolic bypasses.
what are the 2 families of efflux pumps when azoles diffuse passively and efflux pumps actively pump them back out.
ATP binding cassette, major facilitator