azole antifungals

Question 1

name some triazoles

Answer 1

fluconazole, itraconazole, voriconazole, posaconazole, isavuconazole.

Question 2

what were clotrimazole and miconazole mostly used for

Answer 2

superficial infections.

Question 3

when was ketaconazole licensed

Answer 3

1981

Question 4

how do azoles work

Answer 4

they inhibit lanosterol 14a demethylase which leads to ergosterol being less produced and toxic methylated sterols building up, results in cell inhibition or death.

Question 5

what are some extra toxicity issues with voriconazole

Answer 5

MHRA, squamous cell carcinoma, hepatotoxicity

Question 6

what do all triazoles have an effect on

Answer 6

electrical cardiac rythm

Question 7

what are azoles metabolised by

Answer 7

cytochrome P450 enzymes. azoles can also inhibit these enzymes.

Question 8

what effect does drug-drug interaction have on patients

Answer 8

affects concentration of triazoles. Use therapeutic drug monitoring for these people.

Question 9

which triazoles need monitoring

Answer 9

itraconazole, voriconazole, posaconazole.

Question 10

what are some mechanisms of antifungal resistance

Answer 10

decrease effective drug concentration, drug target alterations, metabolic bypasses.

Question 11

what are the 2 families of efflux pumps when azoles diffuse passively and efflux pumps actively pump them back out.

Answer 11

ATP binding cassette, major facilitator