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PHARMACOLOGY > 6 Antifungals > Flashcards

6 Antifungals Flashcards

0
Q

what is the main use of amphotericin B

A

synergistically works with flucytosine

it binds to ergosterol and produced a pore allowing flucytosine to get into the fungus

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1
Q

antifungals for systemic mycoses

A
  1. amphotericin B
  2. Flucytosine (5FC) + amphotericin B
  3. ketoconazole
  4. Fluconazole
  5. Caspofungin
  6. Itraconazole
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2
Q

if you hear broad spectrum antifungal for systemic mycoses you would think

A 
amphotericin B
	good vs:
		1. CANDIDA ALBICANS
		2. histoplasma capsulatum
		3. cryptococcus neoformans
		4. coccidioides immitis
		5. blastomyces dermatitidis
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3
Q

if you need a very broad spectrum antifungal for system mycoses you think

A 
itraconazole
	used for:
		1. AIDS ASSOCIATED HISTOPLASMOSIS
		2. DOC FOR BLASTOMYCOSIS
		3. aspergillosis
		4. candidemia
		5. coccidioidomycosis
		6. cryptococcosis
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4
Q

want to treat AIDs patient who develops histoplasmosis, pro would give

A

itraconazole–> bc its used for AIDS related histoplasmosis

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5
Q

MOA of amphotericin B

A

binds to sterol in cell membrane and forms channels/pores K+ and Mg2+ leak out of cell–> cell death

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6
Q

why is amphotericin B not used that much anymore

A

it has a high TI= low doses can be toxic

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7
Q

what is one of the only antifungals for systemic infs that cant get into the CSF

A
  1. amphertericin B
  2. ketoconazole
  3. itraconazole
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8
Q

how would you administer amphitericin B for fungal meningitidis?

A

intra-thecally= in the space between the spinal cord

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9
Q

MOA of Flucytosine

A

5FU–>5FdUMP= false nucleotide

inhibits THYMIDYLATE SYNTHETASE–> no thymidylic acid–> which is an essential DNA product–> w/o this the cell dies

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10
Q

what 2 organisms can flu-cytosine be used against

A
  1. cryptococcus neoformans

2. candida

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11
Q

what is the cause of side effects the flucytosine

A

5-FU is formed from 5-FC

  • 5-FU= formed by intestinal organisms
  • -> CAUSES HEPATOLOGICAL TOXICITY

5FU–> liver problems

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12
Q

which systemic anti-fungal do you have to adjust for in ppl with renal failure

A

flucytosine= 5FC

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13
Q

whats the purpose of conjugating flucytosine with amphotericin B

A

amphotericin B affects cell permeability which opens a poor in the fungi and allows flucytosine to get better penetration

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14
Q

MOA of all -azoles

A

has C-14-demethylase= p450 -

  • it prevents production of ergosterol (blocks the demethylation fo Ianosterol–> ergosterol)
  • which causes the cell to die
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15
Q

ketoconazole is synergistic with…

A

acidic environment/Coca Cola–> improves the absorption of ketoconazole

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16
Q

which 2 drugs would you not use for fungal meningitidis

A
  1. ketoconazole

2. itraconazole

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17
Q

which systemic antifungal would you see used to treat the prostate and what are the side effects?

A

ketoconazole

–> need to give in REALLY HIGH DOSES–>causes decreased testerosterone levels–> IMPOTENCE

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18
Q

why might you use fluconazole

A

it has good CSF penetration–> which means its a good drug for fungal meningitidis
=DOC for fungal meningitidis
DOC–> cryptococcus neoformans= encapsulated fungi

19
Q

why would you use fluconazole during pregnancy

A

it is a p450 - and a potent teratogen

if you dont want mutant babies–> dont give fluconazole

20
Q

what pts would you possible see resistance to fluconazole

A

HIV + patients

21
Q

which drug has anti-androgen properties

A

ketoconazole= decreased testosterone–> IMPOTENCE

22
Q

MOA of caspofungin

A
  • formation of Beta (1,3)-D glucans–> which are found in the fungal cell cell
23
Q

if you have an azole resistant C. albicans you might think of treating with

A

Caspofungin

24
Q

what are the other uses of caspofungins

A
  1. azole resistant C. albicans
  2. aspergillus fumigatus–> opportunist infection of LRT
  3. P carini
  4. H capsulatum
25
Q

caspofungins can cause

A

histamine release

26
Q

how would you administer caspofungin

A

IV infusion over 1 hr

27
Q

when would you give itraconazole over ketoconazole?

A

if you have a male that doesnt want impotence or a case of AIDs associated histoplasmosis, or if pt has kidney disease bc itraconazole is extensively metabolized in the liver

if pt has HTN or edema already present–> wouldnt give itraconazole bc it would exacerbate the pts symptoms

28
Q

what is the broadest spectrum azole

A

posa-con-azole= PUSSY

29
Q

used to treat superficial mycotic infections

A
  1. griseo-fulvin
  2. ter-bin-afine
  3. nystatin
30
Q

MOA of griseofulvin

A

disrupts miotic spindle–> - mitosis

-accumulates in infected newly synthesized keratin containing tissues–. making them unsuitable for growth of fungi

31
Q

which antifungal would you use against the dermatophytes=

  1. tricho-phyton
  2. epidermo-phyton
  3. microsporum
A

griseofulvin

32
Q

if you give griseofulvin what might you want to watch for to make sure it doesnt interfere with the drug?

A

phenobarbital= barbiturate= sleep and anticonvulsant

33
Q

side effect of griseofulvin

A

p450 inducer–> increases the metabolism of other drugs

34
Q

why is griseofulvin not used alot

A

the pt has to take it for months–> yr (multiple times a day)
which results in decreased patient compliance

35
Q

which antifungals are bad for pregnant women?

A
  1. flucytosine

2. griseofulvin

36
Q

how do you administer griseofulvin

A

oral
fine crystalline preps are absorbed from the GI tract

CAN PROMOTE ABSORPTION IF TAKE WITH HIGH FAT MEAL

37
Q

is see acute polyphyria (issue with heme production) and hepatic issues, you might as it the patients on

A

griseofulvin

38
Q

MOA of terbinafine

A
  • fungal enzyme= squalene epoxidase–> accumulation of squalene(sterol), which is toxic to the fungi
39
Q

how can you administer terbinafine?

A
  1. orally

2. topical gel

40
Q

MOA of nystatin

A

similar to amphotericin B–> binds to sterol and produced pore

41
Q

what is the only use of nystatin?

A

topical use of candida

swish and swallow for oral candida

42
Q

what are the topical antifungals

A
  1. keto-conazole
  2. mi-conazole
  3. ter-conazole
  4. clotrim-azole
43
Q

which topical antifungals can be used vaginally

A
  1. miconazole–> monistat
  2. terconazole
  3. clotrimazole
44
Q

which topical antifungal is only used vaginally

A

terconazole

45
Q

what is the use of topical antifungals

A

the tineas

  1. tinea corporis= body
  2. tinea cruris
  3. tinea versicolor
  4. cutaneous candidiasis
46
Q

MOA topical antifungals

A

same as ketochonazole

c-14 alpha demethylase–> which inhibits conversion of Ianosterol to ergosterol
no ergosterol= disrupt membrane function–> increased membrane perm.

PHARMACOLOGY (5 decks)

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