MRCEM Notes

Antifungal agents

DrugMechanism of actionAdverse effectsNotes
AzolesInhibits 14α-demethylase which produces ergosterolP450 inhibition
Liver toxicity
Amphotericin BBinds with ergosterol forming a transmembrane channel that leads to monovalent ion (K+, Na+, H+ and Cl) leakageNephrotoxicity, flu-like symptoms, hypokalaemia, hypomagnaseamiaUsed for systemic fungal infections
TerbinafineInhibits squalene epoxidaseCommonly used in oral form to treat fungal nail infections
GriseofulvinInteracts with microtubules to disrupt mitotic spindleInduces P450 system, teratogenic
FlucytosineConverted by cytosine deaminase to 5-fluorouracil, which inhibits thymidylate synthase and disrupts fungal protein synthesisVomiting
CaspofunginInhibits synthesis of beta-glucan, a major fungal cell wall componentFlushing
NystatinBinds with ergosterol forming a transmembrane channel that leads to monovalent ion (K+, Na+, H+ and Cl) leakageAs very toxic can only be used topically (e.g. for oral thrush)
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