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MOHD4: Exam 3 Drugs > Antifungal Agents > Flashcards

Antifungal Agents Flashcards

1
Q

Name the drug:

Binds ergosterol –> forms pores –> alter membrane permeability –> Leak Na+, K+, H+ –> cell death

A

Polyene antibotics: amphotericin B, nystatin

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2
Q

Name the drug:

Polymerized microtubules –>disrupt fungal mitosis

A

Griseofulvin

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3
Q

Name the drug:

Pyrimidine analog –> inhibits fungal DNA and RNA synthesis

A

Antimetabolites: flucytosine

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4
Q

Name the drug:
Blocks ergosterol synthesis by binding to and inhibiting fungal
cytochrome P450 enzyme lanosterol 14-alpha-demmthylase

A

Azoles: imidazoles, triazoles

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5
Q

Name the drug:

Block ergosterol synthesis at a step other than inhibited by azoles

A

Allylamines: terbinafine

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6
Q

Name the drug:

Inhibit synthesis of glucan

A

Caspofungin

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7
Q

Drug of choice for most life threatening systemic fungal infections (Candida, Aspergillus, Cryptococcus)

A

Amphotericin B

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8
Q

Amphotericin B

Fungicidal or fungistatic?

A

Fungicidal

Fungistatic depending on low pH, concentration, fungal organism

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9
Q

T/F: Amphotericin B is poorly absorbed in GI tract

A

True

Oral admin only for infections within GI lumen (topical)

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10
Q

Which of the follow is true about Amphotericin B?
A. It is highly soluble
B. It is excreted by the liver over a short amount of time
C. Resistance rarely develops
D. It is well absorbed from skin and mucous membranes

A

C

A. It is insoluable. Must be dissolved in bile salt detergent solution.
B. Excreted by kidney over prolonged amount of time
D. Poorly absorbed. Topical for superficial Candida infections

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11
Q

Lipid formulation of Amphotericin B is used to target ___
High concentrations found in:
Low concentration found in:

A

reticuloendothelial system
High concentration in liver, spleen, lung
Low concentration in kidney

Useful for pts w/ renal dysfunction requiring long term amph B

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12
Q

What adverse effect is nearly always associated w/ Amphotericin B?

A

Nephrotoxicity

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13
Q 
Which of the following is NOT a drug interaction of Amphotericin B?
A. Digitalis
B. Griseofulvin
C. Azoles
D. Aminoglycosides
E. Cyclosporine
A

B.

All others are drug interactions of Amphotericin B

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14
Q

Which of the following is TRUE?
A. Nystatin has a wider spectrum than amph B
B. Nystatin is administered parenterally, orally and topically
C. Amphotericin B has a bitter, unpleasant taste
D. Nystatin is drug of choice for candida infection of oral cavity.
E. It is well absorbed from skin, mucous membranes and GI tract

A

D

A. Narrower
B. Orally and topically. Too TOXIC to be used parenterally
C. Nystatin has a bitter, unpleasant taste
E. It is NOT well absorbed from skin, mucous membranes and GI tract

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15
Q

Griseofulvin

Fungicidal or fungistatic?

A

Fungistatic

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16
Q

Griseofulvin administration

A

Oral

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17
Q

Uses of Griseofulvin

A

Dermatophytosis (hair, nails, skin)

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18
Q

Name the drug:

Contraindicated for men who want children

A

Griseofulvin

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19
Q

Flucytosine

Fungicidal or fungistatic?

A

Fungistatic

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20
Q

Flucytosine administration

A

Oral

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21
Q

Flucytosine treats ___

A

systemic fungal infections, Severe Candida infections and Cryptococcus meningitis

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22
Q

T/F Flucytosine rarely develops resistance.

A

False. Resistance is common

Should be used in combination w/ amph B

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23
Q

Flucytosine is used in combination w/ ___

A

Amph B

24
Q 
Which of the following is FALSE about Flucytosine?
A. Good oral bioavailability
B. Poor CNS penetration
C. Renal excretion
D. GI intolerance is an adverse effect
A

B. GOOD CNS penetration: meningitis

25
Q

T/F: Azoles bind to ergosterol to inhibit ergosterol synthesis.

A

False. Azoles do NOT bind to ergosterol.

It inhibits ergosterol synthesis by blocking fungal CYP enzyme activity

26
Q

T/F: Azoles have a lot of drug interactions

A

True

27
Q

Name 3 Imidazoles

A

Ketoconazole
Micronazole
Clotrimazole

28
Q

Which azole?

Greater propensity to inhibit mammalian CYPs

A

Ketoconazole

Interfere w/ metabolism of other drugs –> enhance toxicity
Limited use

29
Q

Which azole?

Effective topically against cutaneous candidiasis

A

Miconazole

Uses: Jock itch, ringworm, athlete’s foot, vaginal infections, oral thrush

Limited use due to toxicity

30
Q

Which of the following is FALSE about Clotrimazole?
A. Liver metabolized
B. Highly effective alternative to fluconazole
C. May cause minor GI upset
D. Oral/topical administration

A

B. good alternative for nystatin

31
Q

Drug of choice for oropharyngeal candidiasis in AIDS patients

A

Clotrimazole

32
Q 
Which of the following is NOT a triazole?
A. Fluconazole
B. Itraconazole
C. Voriconazole
D. Ketoconazole
E. Efinaconazole
A

D. Ketoconazole is an imidazole

Posaconazole is also a triazole

33
Q

Which of the follow is TRUE about Itraconazol?
A. It has a narrower spectrum than fluconazole
B. It has poor GI tract absorption
C. Oral and topical administration
D. Treatment of Aspergillus, fluconazole-resistant Candida infections

A

D

A. Broader
B. Good GI absorption
C. Oral, IV

34
Q

Name the drug:

Better CNS penetration than other azoles

A

Fluconazole

35
Q

Fluconazole resistance in: (3)

A

C. krusei
C. glabrata
NOT active against molds

36
Q

Fluconazole administration

A

Oral, IV

37
Q

First line agent for invasive infections by Candida and refractory mucocutaneous candidiasis

A

Fluconazole

38
Q

Voriconazole is more potent in vitro against ___ (2)

A

Yeast

Mold

39
Q

Voriconazole administration

A

Oral, IV

40
Q

T/F: Voriconazole has low toxicity

A

True

41
Q

Only azole w/ significant activity against zygomycoses

A

Posaconazole

42
Q

T/F: Voriconazole has very little drug interactions

A

False. Inhibits CYP3A4

43
Q

First line therapy for aspergillosis

A

Voriconazole

44
Q

Name the drug:

A side effect that causes dose related, transient vision side effects

A

Voriconazole

45
Q

T/F: Posaconazole is poor oral bioavailability

A

False

Better when diet contains high fat

46
Q

Posaconazole uses

A

Prophylaxis of invasive fungal infection in BMT w/ GVHD and hematologic maligancy and prolonged neutropenia

47
Q

Topical treatment of onychomycosis

A

Efinaconazole

48
Q

Allylamines

Fungicidal or fungistatic?

A

Fungicidal

49
Q 
Which of the following is FALSE about allylamines?
A. Good GI absorption
B. Metabolized by liver
C. Oral, IV administration
D. Limited drug interaction
A

C. Topical, oral

D. True but co-admin w/ rifampicin and cimetidine affects clearance of terbinafine

50
Q

Caspofungin, micafungin, anidulafungin are ___

A

glucan synthesis inhibitors

51
Q

Used for invasive candidiasis resistant to other antifungals

A

Caspofungin: glucan synthesis inhibitors

52
Q

Only azole w/ significant activity against zygomycoses

A

Posaconazole

53
Q

Use for invasive aspergillosis/mold infections

A

Caspofungin: glucan synthesis inhibitors

54
Q

Azole of choice for crytococcal meningitis

A

Fluconazole

55
Q

Terbinafine is a ___

A

Allylamine

56
Q

Mechanism of action of terbinafine

A

Inhibit cell membrane synthesis

MOHD4: Exam 3 Drugs (5 decks)

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