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Pharmacology > Antifungals > Flashcards

Antifungals Flashcards

(49 cards)

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1
Q

Half life of Amphotericin B

A

15 days

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2
Q

Amphotericin B elimination route

A

urine, slowly

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3
Q

Amphotericin is selective for fungi because it targets this molecule

A

Ergosterol, a fungi cell membrane sterol not found in humans

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4
Q

Amphotericin B MOA

A

Creates larger and larger pores that disrupt membrane potential and ion balance

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5
Q

Describe induction therapy for Amphotericin B

A

Pt is started with a does of Amphotericin to aggressively attack fungal infection, and is then switched to a newer azole drug for chronic treatment or prevention

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6
Q

Flucytosine MOA

A

Taken up by fungal enzyme cytosine permease, converted into metabolites that inhibit DNA and RNA synthesis (it’s a pyrimidine analog)

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7
Q

Describe the toxic effects of flucytosine

A

Conversion to anticancer compound 5-FU can cause bone marrow toxicity with anemia

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8
Q

The two kinds of azoles

A

imidazoles and triazoles

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9
Q

The imidazoles

A

Ketoconazole, miconazole

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10
Q

The triazoles

A

Itraconazole, fluconazole, voriconazole, and posaconazole

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11
Q

Imidazoles or triazoles - which have higher specificity for fungal targets?

A

Triazoles (thus fewer adverse effects)

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12
Q

Imidazole and triazole MOA

A

Targets fungal P450s that synthesize ergosterol

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13
Q

Why are azoles at high risk for interacting with other drug types?

A

SInce they target (fungal) P450s, there is some overlap with human P450 interaction as well

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14
Q

This azole has the highest propensity to inhibit mammalian P450 and isn’t used much anymore

A

ketoconazole

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15
Q

Taking these drugs with itraconazole will result in reduced bioavailability

A

Rifamycins (e.g., rifampin)

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16
Q

Itraconazole is the drug of choice to treat these fungi

A

Dimorphic

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17
Q

Azole of choice to treat Aspergillus

A

vorizonacole

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18
Q

Compare the oral bioavailability of fluconazole, ketoconazole, and itraconazole

A

Fluonazole high others low

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19
Q

This azole has the least effect on human P450 enzymes

A

Fluconazole

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20
Q

Drug of choice to treat fungal meningitis

Study These Flashcards
A

Fluconazole (best CSF penetration)

21
Q

Several azoles inhibit this specific liver enzyme

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A

CYP3A4 (does statins, cyclosporine, and tacrolimus)

22
Q

Broadest spectrum of the azoles

23
Q

Echinocandins members

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A

Caspofungin, micafungin, anidulafungin

24
Q

Echinocandins available ROA

25
Compare the tolerance of echinocandins and azoles
Echinocandins are much better tolerated
26
Griseofulvin has significant interaction with these two drugs
Warfarin and phenobarbital
27
Griseofulvin is now only used for this one problem
Systemic treatment of dermatophytosis
28
Griseofulvin - fungistatic or fungicidal?
Fungistatic
29
Terbinafine - fungistatic or fungicidal?
Fungicidal
30
Describe terbinafine MOA
Inhibits ergosterol synthesis by inhibiting fungal enzyme squalene monooxygenase, leading to accumulation of the toxic compound squalene
31
Azoles target this enzyme
14-alpha-demethylase
32
Amphotericin B is in this drug class
Polyenes
33
Allylamines drugs
Terbinafine
34
Terbinafine target
squalene monooxygenase
35
Echinocandins enzyme target
B-1,3-D-glucan synthesis inhibition
36
Flucytosine target
thymidylase synthase
37
Griseofulvin MOA
mitosis inhibition
38
Are echinocandins effective against dimorphic fungi?
No
39
Vorizonacole is a substrate for this P450
CYP2C19
40
All azoles have these significant side effects
Hepatic - CYP450 interactions; cardiac QT prolongation
41
Amphotericin B side effects
Hepatic; renal toxicity; infusion reacitons, anemia from reduced epoetin from BM
42
5-FC side effects
hepatic; GI, bone marrow suppression
43
Echinocandins side effects
Hepatic, infusion reactions
44
Voriconazole side effects
Renal toxicity; CNS toxicity; photopsia; photosensitivity/malignancy
45
Itraconazole side effects
GI; cardiac (CHF contraindication); ED; breast pain, gynecomastia; hot flashes, etc.
46
Posaconazole side effects
GI
47
Almost all antifungals have this side effect
rash
48
Most azoles are hepatically eliminated, except for this one
Fluconazole (renal)
49
These azoles should never be used in a pregnant patient
Fluconazole and Voriconazole (Very Foolish to give!)

Pharmacology (3 decks)

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