azole antifungals Flashcards

1
Q

name some triazoles

A

fluconazole, itraconazole, voriconazole, posaconazole, isavuconazole.

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2
Q

what were clotrimazole and miconazole mostly used for

A

superficial infections.

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3
Q

when was ketaconazole licensed

A

1981

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4
Q

how do azoles work

A

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

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5
Q

what are some extra toxicity issues with voriconazole

A

MHRA, squamous cell carcinoma, hepatotoxicity

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6
Q

what do all triazoles have an effect on

A

electrical cardiac rythm

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7
Q

what are azoles metabolised by

A

cytochrome P450 enzymes. azoles can also inhibit these enzymes.

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8
Q

what effect does drug-drug interaction have on patients

A

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

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9
Q

which triazoles need monitoring

A

itraconazole, voriconazole, posaconazole.

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10
Q

what are some mechanisms of antifungal resistance

A

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

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11
Q

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

A

ATP binding cassette, major facilitator

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12
Q
A
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