Antfungals Flashcards

1
Q

Name the Triazole antifungals…

A

Fluconazole
Itraconazole
Posaconazole
Voriconazole

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2
Q

What is the mechanism of action of the -azoles?

A

Impeded ergosterol synthesis through direct inhibition of the cytochrome P450 dependent enzyme 14-alpha-sterol-demethylase
–> enzyme necessary for the biosynthetic pathway of ergosterol, which is an essential molecule of the fungal cell membrane

Inhibition of lanosterol demethylase

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3
Q

What are the major uses of fluconazole?

A

Some Candida spp
Cryptococcus
Endemic mycoses

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4
Q

What are the major uses of Voriconazole and itraconazole?

A

Everything covered by fluconazole and aspergillus and broader Candida app. coverage

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5
Q

What are the major uses of Posaconazole?

A

Everything covered by fluconazole, Voriconazole, and itraconazole and

  • Fusarium
  • Mucorales
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6
Q

What are the major side effects seen with the -azoles?

A

Hepatotoxicity

Inhibits CYP450

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7
Q

What is the side effect seen with Voriconazole?

A

Visual disturbances–Bluish hue

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8
Q

Used for thrush/esophageal candidiasis?

A

Fluconazole

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9
Q

Used for prophylaxis of systemic histoplasmosis?

A

Itrazonazole

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10
Q

Used for invasive aspergillosis?

A

Voriconazole

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11
Q

Used for prophylaxis of aspergillosis/candidiasis in immunocompromised pts?

A

Posaconazole

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12
Q

What is the mechanism of action of amphotericin B?

A

Inhibition of ergosterol–generates pores in the fungal cell membrane–allowing leakage of K and Mg

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13
Q

What are the major uses of amphotericin B?

A

Life-threatening invasive fungal infections
Broad anti fungal spectrum

Occasionally used with flu cytosine in immunocompromised hosts

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14
Q

What are the side effects seen with amphotericin B?

A

Nephrotoxicity!! –Pretty much expected with chronic use

Acute infusion related reactions

  • Fever, chills, rigors
  • Pre-medicating with diphenhydramine, APAP, meperidine

Electrolyte abnormalities

  • HypoMg
  • HypoK
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15
Q

What is used for better tolerability of amphotericin B?

A

Lipid formulations

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16
Q

Name the Echinocandins…

A

Caspofungin
Micafungin
Anidulafungin

17
Q

What is the mechanism of action of the echinocandins?

A

Inhibit synthesis of Beta (1,3)-D-glucan–an essential component of the fungal cell wall

18
Q

What are the uses for the echinocandins?

A

Life-threatening fungal infections unresponsive to older agents

  • Candida
  • Aspergillus
19
Q

What is the mechanism of action of Flucytosine?

A

Pyrimidine analogue that inhibits DNA and RNA synthesis

20
Q

What are the uses for flucytosine?

A

Used in combo with amphotericin B in life threatening fungal infections in immunocompromised pts

  • Cryptococcus
  • Some Candida spp

Develops resistance quickly if used as mono therapy

21
Q

What are the side effects of Flucytosine?

A

Bone marrow toxicity

  • Leukopenia
  • Anemia
  • Thrombocytopenia

Liver dysfunction possible

22
Q

What is the mechanism of action of nystatin?

A

Pores are formed in the fungal cell membrane–allowing leakage of K and Mg

23
Q

What are the uses of nystatin?

A

Topically against superficial fungal infections–candidiasis only

24
Q

What is the mechanism of action of efinazonazole?

A

Inhibit ergosterol synthesis by inhibiting lanosterol demethylase

25
Q

What are the uses of efinazonazole?

A

Candida and tinea

26
Q

What are the side effects of efinazonazole?

A

Application site dermatitis

Pain

27
Q

What is the mechanism of action of tolnaftate and terbinafine?

A

Inhibit ergosterol synthesis by inhibiting squalene epoxidase

28
Q

What are the uses of tolnaftate and terbinafine?

A

Topical dermatophytes

29
Q

What are the side effects of tolnaftate and terbinafine?

A

Hepatotoxicity