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Pharmacology > Antifungals > Flashcards

Antifungals Flashcards

0
Q

Two names of polyenes

A

Nystatin ( topical)

Amphotericin

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1
Q

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

A

Polyenes

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2
Q

Which candidia species is not sensitive to amB

A

C. lusitaniae ( lusitaniae sinks amB like the boat)

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3
Q

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

A

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

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6
Q

This Azoles is used for onychomycosis

A

Itraconazole

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7
Q

Amphotericin toxicities and pk and pd

A

(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
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8
Q

Inhibit fungal cytochrome p450 decreasing ergosterol formation

A

Azoles

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9
Q

What is the spectrum for amp b

A

Candidia, cryptococcus neoformans , dimorphic fungi and many molds

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10
Q

This Azoles doesn’t work against molds

A

Fluconazole

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11
Q

Inhibit beta 1,3-glucan synthase

A

Echinocandins

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12
Q

Azoles effective against ASPERGILLUS

A

Itraconazole , voriconazole

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14
Q

What is flu console ineffective against

A

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

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16
Q

What is the big issue with Azoles

A

Drug interactions

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17
Q

What Azoles can you use for fungal UTIs

A

Fluconazole - excreted renally

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18
Q

Adverse reactions with Azoles

A

Hepatoxicity , rash and drug interactions

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19
Q

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

A

Itraconazole

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20
Q

Name the 5 major Azoles

A

Fluconazole, itraconazole,voriconazole , posaconazole, ketoconazole

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21
Q

Azoles are fungicidal to what and fungi static to

A

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

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22
Q

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

A

Voriconazole

23
Q

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

A

Voriconazole

24
Q

This drugs main activity is against dermatophytes

A

Terbinafine

25
Q

Safe for use in pts with renal issues

A

Echinocandins ( caspofungin, micafungin, anidulafungin)

26
Q

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

A

Fluconazole

27
Q

What’s the spectrum of the echinocandins

A

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
Q

This azole was only approved for prophylaxis of fungal infections

A

Posaconazole

29
Q

Interesting facts about posaconazole

A

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
Q

Number 1 treatment for candida if susceptible

A

Fluconazole

31
Q

This drug inhibits squalene epoxidase preventing synthesis of ergosterol

A

Terbinafine

33
Q

Pharmokinetics and adverse effects of echinocandins

A

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
Q

Ketoconazole

A

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

36
Q

Name the antimetabolite

A

5-flucytosine (5-FC)

37
Q

What is C. glabrata susceptible to

A

Flucytosine, and candins and kinda to AmB

38
Q

What is C. kruseii resistant or kinda resistant to

A

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

39
Q

These drugs are used in combo therapy for cryptococcal meningitis

A

AmB and 5-FC

40
Q

This drug concentrates in the nails ,fat and skin

A

Terbinafine

41
Q

Where is terbinafine metabolized and excreted

A

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
Q

Terbinafines SE

A

Hepatotoxicity, neutropenia, Stevens-Johnson syndrome

43
Q

Inhibits fungal mitosis via interaction with microtubules

A

Griseofulvin

44
Q

All you need to know about griseofulvin

A

Used for dermatophytes BUT never use because headaches are very common

45
Q

What is c. lusitaniae resistant to

A

AmB

47
Q

What are the adverse effects of 5-FC

A

Bone marrow suppression - dose related

GI intolerance, rash, hepatotoxicity

49
Q

Used in onychomycosis

A

Terbinafine

51
Q

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 .

A

Itraconazole

55
Q

This is the number one treatment for aspergillus

A

Voriconazole

57
Q

Caspofungin , micafungin, anidulafungin

A

Echinocandins .. All work equally

63
Q

What is the big issue with voriconazole a pk

A

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

Pharmacology (28 decks)

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