Antifungals

Question 1

Echinocandins are…

Answer 1

Inhibitors of fungal cell wall

Question 2

e. g. Caspofungin
- Inhibit enzyme B1,3 glucan synthase
- Drugs are fungicidal
- Severe allergic reactions, blood in urine, fainting, fatigue, fever

Answer 2

Echinocandins (inhibitors of fungal cell wall)

Question 3

Ergosterol is…

Answer 3

An essential component of fungal plasma membrane

Question 4

Polyenes, Azoles and Allymines are examples of…

Answer 4

Inhibitors of Ergosterol

Question 5

e. g. Amphotericin B, Nystatin
- Bind to ergosterol and form pores making plasma membrane leaky
- Prolonged use associated with kidney faliure

Answer 5

Polyenes

Question 6

e. g. Imidazoles, Triazoles
- Inhibit C-14 demethylase which inhibits ergosteol synthesis
- Increased build up of toxic intermediates
- Potent
- Constipation, Diarrhea, dizziness, fatigue, headache, n+v

Answer 6

Azoles

Question 7

e. g. Terbinafine, Amorolfine
- Behave as typical amines
- Prevent one of the 1st steps i ergosterol synthesis
- Work as epoxide inhibitors
- Upset stomach, gas, diarrhea, nausea, pain, headaches, dizziness, rash

Answer 7

Allymines

Question 8

Flurocytocine is an…

Answer 8

Inhibitor of fungal RNA and DNA synthesis

Question 9

• Metabolised to 5-flurouracil which is a toxic metabolite
• Reduced DNA and RNA synthesis
• Combine with azoles
• High levels of resistance

Answer 9

Flurocytocine