Anti-fungal Drugs Flashcards

1
Q

Which fungi cause superficial mycoses (dandruff, tinea vesicolor)

A

malessezia globosa, malessezia furfur

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2
Q

what fungi cause cutaneous mycoses? (dermathphytosis)

A

microsporum, trichophyton, epidermophyton

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3
Q

what is a cutaneous mycosis called that isn’t caused by microsporum, trichophyton, or epidermophyton?

A

dermatomycosis

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4
Q

microsporum, tricophyton, and epidermophyton infect what to cause dermathphytosis

A

infect skin, hair, nails

metabolize and live off of keratin

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5
Q

cutaneous mycoses are often associated with areas of the body that are:

A

poorly aerated
excessive moisture/sweatuing
tight clothing
high humidity

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6
Q

what are some examples of cutaneous mycoses

A
skin mycoses aka ringworm
tinea corporis
tinea pedis (athletes foot)
tinea cruris (jock itch)
tinea capitis (mycosis of scalp)
tinea barbae (mycosis of beard)
tinea unguium (mycosis of nail, aka onychomycosis)
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7
Q

what are the characteristics of subcutaneous mycoses?

A

chronic, localized
following traumatic implatation with soil fungi
may appear as a small nodule that grows and may drain or ulcerate
can become systemic, especially in immunocompromised

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8
Q

what are some examples of subcutaneous mycoses?

A

sporotrichosis (rose handlers disease)
chromoblastomycosis
mycetona

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9
Q

what fungi causes sporotrichosis

A

sporothrix schenckii

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10
Q

what fungi causes chromoblastomycosis

A

many agents, all dematiacious fungi

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11
Q

systemic infections can be either:

A

dimorphic

opportunistic

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12
Q

what are some examples of infections that are considered systemic?

A
soft tissue
UTI
pneumonia
meningitis
septicemia (in blood)
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13
Q

what are the characteristics of systemic mycoses?

A

entry into host by inhalation of airborne spores
spores germinate in lung
asymptomatic primary pulmonary infection is common
acute pulmonary disease less common
chronic pulmonary or dissemination infection is rare
-can infect immunocompetent or immunocompromised patients
-fungus endemic to a particular region

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14
Q

what are the different systemic mycoses that can occur

A

histoplasmosis
blastomycosis
coccidiomycosis
paracoccidiomycosis

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15
Q

blastomyces dermatitidis is endemic to:

A

mississippi river, ohio river, great lakes

characterized by broad based budding with thick walls that appears double contoured

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16
Q

coccidioides immitis is endemic to:

A

southwest USA
valley fever

appears with arthrospores when grown in lab
-dont want to expose lab workers so often sent away for molecular testing

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17
Q

paracoccidiodes brasiliensis is endemic to:

A

central and south america

90% of symptomatic disease found in males
mariners wheel morphology

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18
Q

histoplasma capsulatum is endemic to:

A

eastern and central USA

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19
Q

the opportunistic mycoses are:

A
candidiasis
cryptococcosis
aspergillosis
mucomycosis
pneumocystis jiroveci
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20
Q

what populations have the tendency to be immmunocompromised?

A
debilitated patients
indwelling catheters
prosthesis
HIV 
diabetes or chronic renal, hepatic, cardiac disease
alcoholism
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21
Q

describe candidiasis

A

candida albicans - most common species
overgrowth –> yeast infection
-normally kept under control by normal bacterial flora (almost all infections are endogenous)
lab ID by culture - gram positive, yeast with “feet”
usually occurs in moist areas
-can involve GI tract, kidnesy, liver, spleen, bloodstream, UT, respiratory tract, heart, eye

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22
Q

describe mucosal candidiasis

A

thrush

can be oral, vulvovaginal, esophogeal

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23
Q

describe cryptococcus

A

cryptococcus neoformans

site of infection = lung, meninges, CSF, blood, skin, mucous membranes, systemic
capsules stain pik with mucicarmine
diagnosis with india ink or antigen test* capsule***

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24
Q

describe aspergillosis

A

caused by aspergillus, several species
found in dust, soil, decomising organic matter (environmental)
- spores inhaled and can have a variety of symptoms

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25
Q

what does aspergillosis look like in tissue?

A

septated hypae
branching occurs at 45 degree angles
appears in radial facial, hypae nearly parallel
in cavitary lesions, conidial heads may be observed

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26
Q

describe mucomycosis

A

infection with zygomycete, rhizopus most comon
infection begins in nasal mucosa or sinuses and progresses to the orbit, palate, and brain
-aggressive and rapidly fatal

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27
Q

what do zygomycetes look like in tussue

A

large, nonseptated hypae
ribbon like
branch at 90 degrees

28
Q

Name the antifungal drugs

A
ampotericin B, nystatin
5-fluorocytosine
ketoconazole, miconazole, clotrimazole
fluconazonle, itraconazole, voriconazole, posaconazole 
caspofungin, micafungin, anidulafungin
griesofulvin
terbinafine, butenafine, naftifine
cicliprox, tolnaftate, selenium sulfide
29
Q

what are the seven antifungal drug classes

A
polyenes
azoles (imidazoles, triazoles)
allylamines
echinocandidins
grisans
pyrimadine
miscellaneous
30
Q

what is the target for polyenes?

A

ergosterol

31
Q

what is the target for azoles and allylamines

A

ergosterol biosynthesis

32
Q

what is the target for echinocandidins

A

cell wall biosynthesis (beta-1,3-glucan synthesis)

33
Q

what is the target for griesans

A

microtubules

34
Q

what is the target of pyrimidine analogs

A

DNA synthesis

permease critical

35
Q

amphotericin B and nystatin are:

A

polyenes

36
Q

5FC is:

A

pyrimidine analog

37
Q

ketoconazole, micronazole, clotrimazole are:

A

imidazoles

38
Q

fluconazole, itraconazole, voriconazole, posaconazole are:

A

triazoles

39
Q

caspofungin, micafungin, anidulafungin are:

A

echinocandidins

40
Q

griesofulvin is:

A

griesan

41
Q

terbinafine, butenafine, naftifine are:

A

allylamines

42
Q

cicliprox, tolnaftate, and selenium sulfide are:

A

miscellaneous antifungals

43
Q

what are the uses for ampho B

A

drug of choice for must systemic life threatening fungal infections
very broad spectrum
usually given IV

no CNS penetration

44
Q

what are the uses for nystatin

A

candida, especially thrush (cutaneous mycoses

minimal GI absorption so when taken orally, it only treats GI problems

45
Q

what are the uses for 5FC

A

used in combination with ampho B to treat candida, cryptococcus, aspergillus (opportunisitic infections)

46
Q

what are the uses for imidazoles

- ketoconazole, micronazole, clotrimazole

A
broad spectrum against fungi
no CNS penetration
oral and topical 
absorption requires an acidic gastric environment (decreased with antacids)
mostly replaced by the triazoles
47
Q

what are the uses for triazoles

-fluconazole, itraconazole, voriconazole, posaconazole

A

broad spectrum against fungi
better Gi tolerance
inhibits P450
all but itraconazole penetrate the CNS

48
Q

which triazole cannot penetrate CNS

A

itraconazole

49
Q

what are the uses over echinocandins

-caspofungin, micafungin, anidulafungin

A

used as a second line after ampho B
newer, expensive
effective against aspergillus, candida

50
Q

what are grisans (griesofulvin) used for

A

tinea infections

effective against dermatophytes (fungi that metabolize keratin)

51
Q

what are allylamines used for
terbinafine
butenafine
naftifine

A

treat tinea
topical application
-terbinafine is oral

52
Q

what antifungals have mechanisms that are not well characterized?

A

cicliprox
tolnaftate
selenium sulfate

53
Q

what is the mechanism of polyenes

A

amphotericin B
nystatin

forms pores in the membrane by binding to ergosterol causing loss of K and other small molecules

54
Q

what is the mechanism of 5FC

A

enters fungus using permease (not found in mammals)

converted to 5FU and then incorporated into nucleic acid (pyrimidine analog)

55
Q

what is the mechanism of imidazoles

A

ketoconazole, microconazole, clotrimazole

inhibits production of ergosterol from lanosterol

56
Q

what is the mechanism of triazoles?

A

fluconazole, itraconazole, voriconazole, posaconazole

inhibits production of ergosterol from lanosterol

57
Q

what is the mechanism of echinocandins

A

caspofungin, micafungin, anidulafungin

inhibits cell wall biosynthesis by inhibiting beta-gucan production

58
Q

what is the mechainsm of griesofulvin

A

inhibits microtubule function, preventing mitosis

binds to keratin in skin and hair making them more resistant to fungal infection

59
Q

what is the mechanism of allylamines

A

terbinafine, butenafine, naftifine

inhibits ergosterol production via squalene epoxide

60
Q

what are the side effects of amphoB

A

nephrotoxicity

can make pores in human cells because it also can bind cholesterol to a certain extent

61
Q

what are the side effects of nystatin

A

makes pores in human cells by binding to cholesterol

highly insoluble, toxic if given IV - topical and oral but minimal GI absorption)

62
Q

what are the side effects of 5FC

A

bone marrow suppression

GI upset

63
Q

what are the side effects of ketoconazole

A

inhibits with CYP450, interferes with testosterone and cortisol production
GI upset
hepatic dysfunction

64
Q

what are the side effects of micronazole and clotrimazole

A

too toxic to give IV but also poorly absorbed as a topical

65
Q

what are the side effect of the triazoles

A

CYP450 interactions
hepatic dysfunctions
-safer than imidazoles

66
Q

which antifungals have few untoward effects?

A

echinocandidins
allylamines (headaches and gi upset minor)
driesofulvin has rare but serious adverse effects

67
Q

what rare side effects does griesofulvin have?

A

hepatotoxicity, GI irritation
bone marrow suppression
headaches