FUNGAL INFECTIONS Flashcards
What drugs come under the polyene class?
Amphotericin B
Nystatin
What is amphotericin B?
Polyene macrolide - broad spectrum kills most fungi - fungicidal. Used oral or IV
- IV route very toxic so used for life threatening systemic infections e.g. cryoptococcal meningitis
What is nystatin?
Polyene macrolide - local or topical (oral suspension) for oral infections and cream for skin candida.
Broad spectrum
Mechanism of action of polyenes?
Bind to ergosterol
Form pores in the PM
Leaks K+ / Mg2+ cause . cell cannot maintain ionic balance due to pores
causes cell lysis
Fungicidal depending on conc - note that . high enough concs . will bind to cholesterol too which will affect human cells
What drugs come under the azole class?
- Imidazoles such as miconazole, clotrimazole, ketoconazole
- Triazoles e.g. fluconazole, itraconazole, voriconazole, posaconazole
are triazoles broad spectrum? if so what?
Yes - candida, crytococcusm, aspergillus
Mechanism of action of azoles?
Inhibit lanosterol 14-alpha demethylase CYP450 which interferes with ergosterol synthesis and disrupts PM - fungistatic
are imidazoles broad spectrum
Yes - dermatophytes and candidasis
Brand names for:
miconazole
ketoconazole
clotrimazole
miconazole - daktarin
ketoconazole - nizoral
clotrimazole - canesten
What is flucytosine?
Antifungal (synthetic is fluoropyrimidine) - Converted to 5-FU which disrupts DNA/RNA synthesis (competes with uracil for RNA synthesis)
- Fungistatic
- used in combo with other drugs for severe cryptococcal or candida systemic infections
Is flucytosine used alone?
No - in combo with others for severe cryptotoccal or candida systemic infect
What class is griseofulvin and MoA?
Benzofuran –> binds to polymerised microtubules and inhibits mitosis to stop growth of fungi - thus fungistatic
What is the spectrum of griseofulvin?
Limited . - dermatophytes e.g. tinea capitis
What are the S/E of griseofulvin?
N&V, anorexia, rash, urticaria
What drugs are included in allylamines class and MoA?
Terbinafine (Lamisil) –> mainly on dermatophytes
MoA: inhibits squalene expoxidase to inhibit generation of lanosterol from squalene in ergosterol biosynthesis
- fungistatic / fungicidal
What class of drugs is amorolfine?
Morpholine (amorolfnie is synthetic)