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PR3124 CA1 > Lecture 4- antifungal agents > Flashcards

Lecture 4- antifungal agents Flashcards

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1
Q

what does fungal cell membrane contain?

A

ergosterol instead of cholesterol

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2
Q

2 broad categories of antifungal drug

A
  1. drug for subcutaneous and systemic mycotic infections

2. drugs for cutaneous mycotic infection

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3
Q

what are the classes of antifungal drugs (3)

A
  1. polyenes
  2. azoles
  3. achinocandins
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4
Q

how do polyenes work?

A

bind to ergosterol and cause pores to develop in cell membrane

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5
Q

how do azoles work

A

inhibits lanosterol 14 alphs demethylase and inhibits ergosterol synthesis

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6
Q

echinocandins MOA

A

inhibits beta 1,3- glucan synthase

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7
Q

types of polyenes? (2)

A
  1. amphotericin B

2. nystatin

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8
Q

amphotericin B MOA

A

bind to ergosterol in plasma membrane –> form pores–> pores disrupt membrane func–> allow electrolytes to leak out–> cell death

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9
Q

amphotericin B spectrum

A

fungicidal

wide coverage

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10
Q

amphotericin B indication

A

against oral candidiasis

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11
Q

amphotericin B ROA

A

topical, slow IV

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12
Q

amphotericin B absorption

A

poor csf penetration

extensively bound to plasma protein

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13
Q

amphotericin B excretion

A

urine, bilé

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14
Q

amphotericin B adverse

A

fever and chills, nephrotoxicity

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15
Q

amphotericin B CI

A

renal impairment

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16
Q

amphotericin B preg

A

cat B

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17
Q

5-flucytosine MOA

A
  • convert 5FU to 5-fluorouridine triphosphate (FUTP) FUTP then inhibits protein synthesis
  • 5FU metabolised into FdUMP– inhibits DNA synthesis
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18
Q

5-flucytosine spectrum

A

fungistatic

used in combi with other drugs eg. ampho B to treat candidiasis

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19
Q

5-flucytosine absorption and ROA

A

absorbed well by oral route
penetrates well into CSF
dose adjusted inrenal impari

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20
Q

5-flucytosine adverse

A

GI, bone marrow suppression- need to monitor leucocytes and platelets, hepatotox

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21
Q

5-flucytosine resistance

A

can be due to decreased level of any eznyesm inthe conversion of 5FC to its metabolites
very susceptible to resisitance– usually dont use alone

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22
Q

types of echinocandins (3)

A
  1. caspofungin
  2. micofungin
  3. anidulafungin
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23
Q

echinocandins MOA

A

inhibit activity of glucan synthase complex–> loss of structural integrity of cell wall

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24
Q

echinocandins properties

A
  • lack oral bioavail
  • extensive protein binding
  • cannot penetrate CSF
  • broad specturm activity
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25
caspofungin ROA
IV
26
caspofungin use
first line for invasive candidiasis | second line for invasive aspergillosis
27
caspofungin elim
in urine and faces no need dose adjustment not met by cyp450 enzymes
28
caspofungin adverse
GIT, fever, chills, rashes
29
classes of azole antifungals (2)
1. imidazole | 2. triazoles
30
azole MOA
inihibit c14 alpha demethylase (CYP450) enzymes--> block demethylation --> disrupts membrane structure and func--> inhibit fungal cell growth
31
triazoles ROA and use
systemically | treat cutaneous and systemic fungal infection
32
types of triazoles (3)
1. fluconazole 2. itraconazole 3. voriconazole
33
fluconazole ROA
oral, iv
34
fluconazole uses
- treat candidemia, cryptococcal meningitis, vulvovaginal candidiasis single dose oral tx
35
itraconazole roa
oral apsules taken after full meal oral soln on empty stomach poor csf penetration due to larger size
36
itroconazole indications
braod antifungal spectrum | treat blastomycosis and aspergillosis
37
itraconazole excretion
met by live, excreted in urine and faeces
38
voriconazole ora
oral, iv
39
voriconazole indicationa
braod spectrum antifungal agent | treat invasive aspergillosis and candida infections
40
voriconazole distri
high oral bioavail | good csf penetration
41
itraconazole adverse
cardiotoxicity
42
voriconazole adverse
neurotoxicity
43
triazoles adverse
QT prolongation, rash, nausea, hepatotoxicity
44
triazoles resistnace
mutation in c14 alpha demethylase gene--> decrease azole binding
45
triazoles pregnancy
avoided fluco and itra cat C vori cat d
46
classes of antifungals used to treat SUBCUTANEOUS AND SYSTEMIC infection
1. ampho B 2. 5-flucytosine 3. echonicandins 4. triazoles
47
types of imidazoles (2)
- clotrimazole | - . miconazole
48
imidazoles roa
topical
49
imidazoles uses
tinea corposis, tinea cruris, tinea pedis...
50
imidazoles adverse
contact dermititis, edema
51
clotrimazole uses
- dermatophyte infections | - vulvovaginal candidiasis
52
miconazole uses
treat tinea pedis, tinea cruris, vulvovaginal candidiasis
53
miconazole abdosprtion
penetrates skin well but does not get absorbed into blood
54
miconazole adverse
contact dermititis, vulvar irritation, edema | gi disturbances
55
what class is nystatin?
polyene antifungal
56
nystatin roa
oral, cream , pessary | NOT used parentareally due to systemic tox
57
nystatin use
broad spec treat oral or GI fungal infections and vulvovaginal candidiasis for cutaneous and oral candida infections
58
terbinafine moa
inhibit squalene epoxidase increase membrane permeability death of fungal cell
59
terbinafine roa
oral, topical
60
terbinafine uses
oral: treat dermatophyte onychomycoses (nail) and tinea capitis (scalp) topical: ringworm
61
terbinafine ci
avoid in pt with renal impari or hepatic dysfunc | - oral avoided during breastfeeding
62
terbinafine in preg
cat A- vaginal | cat b- oral
63
cutaneous antifungals (3)
1. imidazoles (clot and mico) 2. nystatin 3. terbinafine

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