Antifungals

Question 1

Flucytosine

Answer 1

Inhibits protein and nuclei acid synthesis
Uptake by cytosine permease
Flucytosine > 5FU > 5FUMP into RNA
Inhibits protein synthesis no proper folding
IRREVERSIBLE
SYSTEMIC

Question 2

Griseofulvin - DERMATOPHYTE

Answer 2

Disrupts Microtubules and inhibits mitosis
Interacts with tubulin to interfere with Microtubule/spindle formation
Cells arrested in metaphase

Question 3

Echinocandins eg caspofungin

Answer 3

Disruption of cell wall
Non comp inhibition of beta-1,3-glucan synthase (FKS1p subunit)
Fungistatic and cidal
Fatty acid tail - anchoring
Tyrosine - binding/ interaction
Modified side chains for solubility

Question 4

Nikkomycin z - DERMETOPHYTE

Answer 4

UDP-GlcNAc similar structure
Comp inhibition of chitin synthesis
Vet settings not human

Question 5

Triterpenoids eg ivrexafungerp

Answer 5

Disruption of cell wall
Beta-1,3-glucan synthase inhibitor by binding to different site
Treats Candida & c.auris

Question 6

Polyenes eg Amphotericin B

Answer 6

Target ergosterol in convo with flucytosine
Increase cell permeability
Increased efflux of k causing lysis
Lipid formulations (decrease side effects)

Question 7

Allyamines - DERMOTOPHYTE

Answer 7

Disruption of cell membrane
Non comp inhibition of squalene
Decreased ergosterol increased squalene = toxic
Non selective

Question 8

Azoles eg isavucanazole

Answer 8

Disruption of cell memebrane
Comp inhibitor of alpha 14 demethylase
Basic imidazole or 1,2,3 triazole to bind iron via nitrogen ring
Remainder bind rest of protein
P450 interactions

Question 9

Morphalines - DERMETOPHYTE

Answer 9

Inhibits 14 reductase and 8 isomerase in ergosterol synthase pathway
Synergetic

Question 10

Compound AR12

Answer 10

Blocks fungal acetyl co A synthetase 1
Needed for metabolism
Increased host response - decreased chaperone proteins
Target species Candida albicans
Completed phase 1