PHARM A56c: Antifungal Therapy Flashcards

1
Q

What are the major 3 components of the fungal cell wall?

A

Mannoproteins, B-(1,3)- and B-(1,6)-glucans, and chitin

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2
Q

What is the main component of the fungal cell membrane?

A

Ergosterol

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3
Q

What class of anti-fungal drugs are membrane-disrupting agents?

A

Polyenes

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4
Q

What is the mechanism of action of polyenes? What is the prototype of this class?

A

Binds sterols (preferentially ergosterol), forming a pore that disrupts osmotic integrity of cell membrane- FUNGICIDAL

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5
Q

True or False: Polyenes penetrate into CSF, vitreous humor, and amniotic fluid.

A

False: they do NOT penetrate

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6
Q

What is Amphotericin B used for?

A

Serious systemic infections and fungal meningitis

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7
Q

What are the major complications of polyene/ amphotericin B?

A

Nephrotoxicity

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8
Q

What classes of antifungal drugs inhibit the synthesis of ergosterol?

A

Azoles and allylamines

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9
Q

What enzymatic step is inhibited by Allylamines (terbinafine)?

A

The conversion of squalene to squalene epoxide by qualene epoxidase

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10
Q

What enzymatic step is inhibited by azoles?

A

The conversion of lanosterol to ergosterol by 14-alpha-sterol demethylase

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11
Q

What are the two major classes of azoles and what is the prototype of each?

A

Imidazoles (ketoconazole) and triazoles (fluconazole)

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12
Q

What enzymes are especially important in drug-drug interactions with azoles?

A

Cytochrome P450

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13
Q

What are the adverse effects associated with azoles?

A

Hepatotoxicity, hypertension, visual impairment, and inhibition of testosterone synthesis

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14
Q

Which antifungal is contraindicated for cardiac patients?

A

Itraconazole

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15
Q

What adverse effects are associated with terbinafine?

A

Taste disturbances; hepatotoxicity

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16
Q

What class of antifungals are glucan synthesis inhibitors? What is the prototype?

A

Echinocandins; Micafungin

17
Q

What is the mechanism of action of micafungin?

A

Inhibit beta-1,3 glucan synthesis- Fungicidal

18
Q

What is the mechanism of action of flucytosine?

A

Block fungal, DNA, RNA, and Protein synthesis— fungistatic

19
Q

What is the mechanism of griseofulvin?

A

Fungal spindle disrupter (mitosis inhibitor)– Fungistatic

20
Q

Where does griseofulvin accumulate in the body?

A

Keratin precursor cells

21
Q

What are the adverse affects of griseofulvin?

A

Severe teratogenic effects and confusion