Antifungals Flashcards

(46 cards)

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

23
Q

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

24
Q

This drugs main activity is against dermatophytes

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

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
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