Lecture 4: Anti-Fungal Agents Flashcards

1
Q

____ is used to treat superficial infections
A. Ketoconazole
B. Miconazole
C. Fluconazole
D. Griseofulvin

A

D. Griseofulvin

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2
Q

Which four anti-fungal drugs are used to treat systemic, subcutaneous fungal infections?

A

Keto/Mico/Fulco/Itra-conazole

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3
Q

What type of therapy is indicated for patients who are febrile, neutropenic and do NOT responds to broad spectrum antibacterial treatment? Which broad-spectrum anti-fungal drugs should be used?

A

Empiric Anti-Fungal Therapy
1. Miconazole
2. Amphotericin B

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4
Q

Prophylactic Antifungal therapy is commonly used in which patient populations?
A. Immunocompromised
B. Immunocompetent

A

A. Immunocompromised

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5
Q

What are the two major groups of -azoles?

A

Imidazole
Triazoles

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6
Q

Which three drugs can be used to treat mild to moderate Tinea infections?

A

Clotrimazole
Miconazole
Tolnaftate

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7
Q

Which five drugs are used to treat moderate-severe Tinea infections?

A

Ketoconazole
Miconazole
Fluconazole
Itraconazole

Terbinafine

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8
Q

Which two drugs can be used to treat severe Tinea infections?

A

Griseofulvin and Ketoconazole

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9
Q

True or False: Drugs that end in -azole can be used to treat Tinea Versicolor

A

True

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10
Q

The -azoles, Nystatin, Terbinafine and Amphotericin B are used to treat:
A. Candidiasis
B. Tinea Versicolor
C. Dermatitis

A

A. Candidiasis

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11
Q

Amphotericin B and Nystatin affects:
A. Ergosterol Synthesis
B. Cell wall Synthesis
C. Nuclear Division
D. Membrane Function

A

D. Membrane Function

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12
Q

Azoles affects:
A. Ergosterol Synthesis
B. Cell wall Synthesis
C. Nuclear Division
D. Membrane Function

A

A. Ergosterol Synthesis

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13
Q

Griseofulvin affects:
A. Ergosterol Synthesis
B. Cell wall Synthesis
C. Nuclear Division
D. Membrane Function

A

C. Nuclear Division

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14
Q

Echinocandins affect:
A. Ergosterol Synthesis
B. Cell wall Synthesis
C. Nuclear Division
D. Membrane Function

A

B. Cell wall Synthesis

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15
Q

Squalene, a precursor sterol, is converted to lanosterol via:

A

Squalene monooxygenase

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16
Q

Which two molecules inhibit Squalene Monooxygenase?

A

Terbinafine and Tolnaftate
- Accumulation of squalene

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17
Q

The -azoles inhibit this enzyme:
A. Squalene monooxygenase
B. 14-a demethylase (P450)

A

B. 14-a demethylase (P450)
- Accumulation of lanosterol

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18
Q

Which enzyme converts lanosterol to ergosterol?
A. Squalene monooxygenase
B. 14-a demethylase (P450)

A

B. 14-a demethylase (P450)

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19
Q

Amphotericin B binds to ____ in the fungal cell membrane
A. phospholipids
B. cholesterol
C. sterols (ergosterol)
D. mycolic acid

A

C. sterols (ergosterol)

20
Q

As a result of Amphotericin B binding to sterols, ___ is formed in cell membrane, ____ increase and ___ are lose

A

pores/channels; permeability increases; K

21
Q

Ergosterol can also bind to which mammalian cells?

A

Kidney cells
Erythrocytes

22
Q

How must ergosterol be given?
A. Orally
B. Anally
C. Parenterally
D. IV
E. IM

A

C. Parenteral

23
Q

What are the two AE associated with ergosterol?

A

Nephrotoxicity and reversible Anemia (hypochromic, normocytic)

24
Q

True or False: ergosterol is used to treat localized infections

A

False - systemic

25
Q

True or False: Systemic triazoles are more quickly metabolizes and have more of an effect on human sterol synthesis than imidazoles

A

False - systemic triazoles are more SLOWLY metabolized and have LESS of an effect on human sterol synthesis than imidazoles

26
Q

All -azoles have a triazole nucleus. It contains two Nitrogens. If the third molecule is a carbon it is a ____ and if it is a N it is a _____

A

C = imidazole
N = triazole

27
Q

Both imidazole and triazoles inhibit which enzyme?

A

sterol-14-a-demethylase (P450 enzyme)
- leads to demethylation of lanosterol

28
Q

Clotrimazole, Miconazole, and Ketoconazole are ______
A. Triazoles
B. Imidazoles

A

B. Imidazoles

29
Q

True or False: Itraconazole and Fluconazole are Triazoles

A

True

30
Q

Why do endocrine abnormalities can result from Ketoconazole use? Examples?

A

Ketoconazole inhibits steroid biosynthesis

Females: menstrual abnormalities
Males: gyecomastia

31
Q

Why can Ketoconazole result in DDI?

A

Inhibits P450

32
Q

True or False: Miconazole has low toxicity and is used for systemic fungal infections

A

True

33
Q

True or False: Fluconazole is used for systemic infections and has low toxicity

A

True

34
Q

Which drug disrupts cell’s mitotic spindle structure, therefore arresting metaphase of cell division, as well as is deposited in keratin precurosor cells (hair, skin nails)?
A. Griseofulvin
B. Ketoconazole
C. Fluconazole

A

A. Griseofulvin
- Use is 2-4 wks to 6 mths

35
Q

Which drug mainly treats skin infections (dermatophytoses)?
A. Griseofulvin
B. Ketoconazole
C. Fluconazole

A

A. Griseofulvin

36
Q

Like Amphotericin B, Nystatin binds to sterols in the fungal ___ ____
A. Cell Membrane
B. Cell Wall
C. Cytoplasm

A

A. Cell Membrane

37
Q

True or False: Nystatin is absorbed via: skin, mucous membranes, and GI tract

A

False - it is NOT

38
Q

True or False:
Nystatin can be used via parentral use but Amphotericin B cannot

A

False - Nystatin CANNOT (too toxic) be used parentrally but Amphotericin B CAN!

39
Q

Which of the following conditions does Nystatin typically treat?
A. Dermititis infections
B. Candidal infections
C. Chicken Pox

A

B. Candidal infections

40
Q

___ interferes with sterol biosynthesis by inhibiting squalene monooxygenase, which result in decreased ergosterol and accumulation of squalene
A. Amphotericin B
B. Nystatin
C. Tolnaftate

A

C. Tolnaftate

41
Q

True or False: Nystatin and Tolnaftate have low toxicity

A

True

42
Q

Terbinafine hydrochloride has the same mechanism as Tolnaftate, meaning it inhibits _____ enzyme, which results in decreased ergosterols and accumulation of squalene

A

squalene monooxygenase

43
Q

_____ is the first antifungal to belong to the echinocandins class of antifungal agents

A

Caspofungin

44
Q

_____ inhibit synthesis of B1,3-D-glucan, an essential polysaccharide component of the CELL WALL of filamentous fungi

A

Echinocandins

45
Q

What are the main uses of Echinocandins?

A

Esophageal candidiasis and invasive aspergillosis (for patients who are REFRACTORY or INTOLERANT to other antifungals!!)