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Flashcards in Antifungals Deck (46):
0

MOA of these drugs is to bind ergosterol in fungal cell membrane leading to cell death

Polyenes

1

Two names of polyenes

Nystatin ( topical)
Amphotericin

2

Which candidia species is not sensitive to amB

C. lusitaniae ( lusitaniae sinks amB like the boat)

3

Other formulations of AmB .. Which one has the least Nephrotoxicity and infusion rxn

Liposomal Amphotericin b ) LAmB

The amp b colloidal dispersion is the worst and worst than the conventional AmB . The lipid complex is ok but lamb is better

6

This Azoles is used for onychomycosis

Itraconazole

7

Amphotericin toxicities and pk and pd

(Bind ergosterols in cell wall)
SE: Nephrotoxicity
Electrolyte wasting
Infusion related reactions

- poorly absorbed that's why given IV , high distribution ( low in CNS) , concentration dependent

8

Inhibit fungal cytochrome p450 decreasing ergosterol formation

Azoles

9

What is the spectrum for amp b

Candidia, cryptococcus neoformans , dimorphic fungi and many molds

10

This Azoles doesn't work against molds

Fluconazole

11

Inhibit beta 1,3-glucan synthase

Echinocandins

12

Azoles effective against ASPERGILLUS

Itraconazole , voriconazole

14

What is flu console ineffective against

C. Glabrata, c. Krusei, ( glide and cruise past fluconazole) aspergillus and molds

16

What is the big issue with Azoles

Drug interactions

17

What Azoles can you use for fungal UTIs

Fluconazole - excreted renally

18

Adverse reactions with Azoles

Hepatoxicity , rash and drug interactions

19

This Azole can be used to treat aspergillus, dematiaceous molds and dimorphic fungi

Itraconazole

20

Name the 5 major Azoles

Fluconazole, itraconazole,voriconazole , posaconazole, ketoconazole

21

Azoles are fungicidal to what and fungi static to

Fungicidal to molds and fungistatic to yeast . They are time dependent

22

This azole is used for invasive aspergillosis, invasive candidiasis, esophageal candidiasis and febrile neutropenia

Voriconazole

23

This drugs SE are visual effects ( purple fringe on stuff, wiggly lines) to hepatotoxicity to visual hallucinations

Voriconazole

24

This drugs main activity is against dermatophytes

Terbinafine

25

Safe for use in pts with renal issues

Echinocandins ( caspofungin, micafungin, anidulafungin)

26

Used in the treatment of candidiasis and prophylaxis but not c. kruseii and c. glabrata

Fluconazole

27

What's the spectrum of the echinocandins

Candida but weak against C. parapsilosis
Active against ASPERGILLUS

Ineffective again CRYPTOCOCCUS and many molds

Fungicidal vs yeasts and pseudo static vs molds ( makes weird balls that don't reproduce but don't die either )

28

This azole was only approved for prophylaxis of fungal infections

Posaconazole

29

Interesting facts about posaconazole

Must be eaten with high fat meal or acidic beverage . ( new IV and oral tablets just approved so won't use the suspension form anymore)

Yeasts including candidia and cryptococcus
Molds including aspergillus and zygomycetes

30

Number 1 treatment for candida if susceptible

Fluconazole

31

This drug inhibits squalene epoxidase preventing synthesis of ergosterol

Terbinafine

33

Pharmokinetics and adverse effects of echinocandins

IV only - poor bioavailability
No CNS distribution
Not really eliminated
Concentration dependent

SE - very well tolerated rxns are rare
Hepatotoxicity , infusion related rxn ( red man syndrome ) and phlebitis if given peripherally so give centrally.

35

Ketoconazole

Poor oral absorption, used topically , occasionally orally. Don't use systemically

36

Name the antimetabolite

5-flucytosine (5-FC)

37

What is C. glabrata susceptible to

Flucytosine, and candins and kinda to AmB

38

What is C. kruseii resistant or kinda resistant to

fluconazole itraconazole , 5-FC and can be resistant to AmB

39

These drugs are used in combo therapy for cryptococcal meningitis

AmB and 5-FC

40

This drug concentrates in the nails ,fat and skin

Terbinafine

41

Where is terbinafine metabolized and excreted

40% bioavailable bc if 1st pass effect .

Metabolized in liver but metabolites are excreted renally . Non linear elimination half life goes from 12 hrs to 200 hours after repeated dosing

42

Terbinafines SE

Hepatotoxicity, neutropenia, Stevens-Johnson syndrome

43

Inhibits fungal mitosis via interaction with microtubules

Griseofulvin

44

All you need to know about griseofulvin

Used for dermatophytes BUT never use because headaches are very common

45

What is c. lusitaniae resistant to

AmB

47

What are the adverse effects of 5-FC

Bone marrow suppression - dose related
GI intolerance, rash, hepatotoxicity

49

Used in onychomycosis

Terbinafine

51

This azole has the worst side effects and Can cause heart failure, qt prolongation and the absorption is so bad you never really know if it was absorbed or not .

Itraconazole

55

This is the number one treatment for aspergillus

Voriconazole

57

Caspofungin , micafungin, anidulafungin

Echinocandins .. All work equally

63

What is the big issue with voriconazole a pk

It's non- linear and there is a disproportional increase in concentration with increase in dose so be careful . It has a high intra and inter patient variability so might need to check the trough levels