MICRO - Antifungals Flashcards

1
Q

Amphotericin B (Mechanism, Clinical use, Toxicity)

A

Forms Membrane Pores

Mechanism:

  • Binds ergotsterol in fungal cell membrane
  • Creates pores –> cell leakage of electrolytes

Clinical use:

  • Severe fungal infections
    • Cryptococcus, Histoplasma, Coccidiodies, Mucor, Blastomyces, Candida
  • Intrathecal for meningitis

Toxicity:

  • Nephrotoxicity
    • Low K+ –> Arrythmias
    • Low Mg2+
    • Hypotension
    • Supresison of EPO –> anemia
  • IV phlebitis
  • Fevers / chills

Tox. treat: Hydration

** Can give alternative (Liposomal Amphotericin) with less toxicity

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2
Q

Amphotericin B (Mechanism, Clinical use, Toxicity)

A

Forms Membrane Pores

Mechanism:

  • Binds ergotsterol in fungal cell membrane
  • Creates pores –> cell leakage of electrolytes

Clinical use:

  • Severe fungal infections
    • Cryptococcus, Histoplasma, Coccidiodies, Mucor, Blastomyces, Candida
  • Intrathecal for meningitis

Toxicity:

  • Nephrotoxicity
    • Low K+ –> Arrythmias
    • Low Mg2+
    • Hypotension
    • Supresison of EPO –> anemia
  • IV phlebitis
  • Fevers / chills

Tox. treat: Hydration

** Can give alternative (Liposomal Amphotericin) with less toxicity

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3
Q

Amphotericin B (Mechanism, Clinical use, Toxicity)

A

Forms Membrane Pores

Mechanism:

  • Binds ergotsterol in fungal cell membrane
  • Creates pores –> cell leakage of electrolytes

Clinical use:

  • Severe fungal infections
    • Cryptococcus, Histoplasma, Coccidiodies, Mucor, Blastomyces, Candida
  • Intrathecal for meningitis

Toxicity:

  • Nephrotoxicity
    • Low K+ –> Arrythmias
    • Low Mg2+
    • Hypotension
    • Supresison of EPO –> anemia
  • IV phlebitis
  • Fevers / chills

Tox. treat: Hydration

** Can give alternative (Liposomal Amphotericin) with less toxicity

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4
Q

Nystatin (MOA, Use)

A

Forms Membrane Pores

MOA:

  • Binds ergosterol in cell membrane
  • Creates pores –> electrolyte leakage

USE:

  • Topical use:
    • Diaper rash
    • Vaginal candidiasis
  • Oral candidiasis (swish and swallow)
    • not absorbed from GI tract
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5
Q

Nystatin (MOA, Use)

A

Forms Membrane Pores

MOA:

  • Binds ergosterol in cell membrane
  • Creates pores –> electrolyte leakage

USE:

  • Topical use:
    • Diaper rash
    • Vaginal candidiasis
  • Oral candidiasis (swish and swallow)
    • not absorbed from GI tract
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6
Q

Flucytosine (MOA, USE, TOX)

A

Nucleic acid synthesis

MOA:

  • –>[Cytosine Deaminase] –> 5-FU –| DNA/RNA synthesis

USE:

  • Systemic mycosis with Amphotericin B
    • (especially cryptococcal meningitis)

TOX:

  • Bone marrow suppression
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7
Q

Flucytosine (MOA, USE, TOX)

A

Nucleic acid synthesis

MOA:

  • –>[Cytosine Deaminase] –> 5-FU –| DNA/RNA synthesis

USE:

  • Systemic mycosis with Amphotericin B
    • (especially cryptococcal meningitis)

TOX:

  • Bone marrow suppression
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8
Q

Flucytosine (MOA, USE, TOX)

A

Nucleic acid synthesis

MOA:

  • –>[Cytosine Deaminase] –> 5-FU –| DNA/RNA synthesis

USE:

  • Systemic mycosis with Amphotericin B
    • (especially cryptococcal meningitis)

TOX:

  • Bone marrow suppression
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9
Q

Azoles (MOA, USE, TOX)

A

Ergosterol Synthesis

MOA:

  • Inhibits CYP450
    • Lanosterol –> [CYP450] –> Ergosterol

USE:

  • Local and less serious systemic
  • Fluconazole:
    • AIDS + Cryptococcal Meningitis
    • Candida (any kind)
  • Itraconazole:
    • Blastomyces
    • Coccidiodes
    • Histoplasma
  • Cotrimazole and Miconazole:
    • Topical

TOX:

  • Inhibition of testosterone synth
    • Gynecomastia (especially ketoconazole)
  • Liver dysfunction (CYP450 inhibition)

[Clotrimazole, fluconazole, itraconazole, ketoconazole, miconazole, voriconazole]

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10
Q

Azoles (MOA, USE, TOX)

A

Ergosterol Synthesis

MOA:

  • Inhibits CYP450
    • Lanosterol –> [CYP450] –> Ergosterol

USE:

  • Local and less serious systemic
  • Fluconazole:
    • AIDS + Cryptococcal Meningitis
    • Candida (any kind)
  • Itraconazole:
    • Blastomyces
    • Coccidiodes
    • Histoplasma
  • Cotrimazole and Miconazole:
    • Topical

TOX:

  • Inhibition of testosterone synth
    • Gynecomastia (especially ketoconazole)
  • Liver dysfunction (CYP450 inhibition)

[Clotrimazole, fluconazole, itraconazole, ketoconazole, miconazole, voriconazole]

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11
Q

Azoles (MOA, USE, TOX)

A

Ergosterol Synthesis

MOA:

  • Inhibits CYP450
    • Lanosterol –> [CYP450] –> Ergosterol

USE:

  • Local and less serious systemic
  • Fluconazole:
    • AIDS + Cryptococcal Meningitis
    • Candida (any kind)
  • Itraconazole:
    • Blastomyces
    • Coccidiodes
    • Histoplasma
  • Cotrimazole and Miconazole:
    • Topical

TOX:

  • Inhibition of testosterone synth
    • Gynecomastia (especially ketoconazole)
  • Liver dysfunction (CYP450 inhibition)

[Clotrimazole, fluconazole, itraconazole, ketoconazole, miconazole, voriconazole]

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12
Q

Terbinafine (MOA, USE, TOX)

A

Lanosterol synthesis

MOA:

  • –| Squalene Epoxidase
    • Squalene –> [SE] –> –> Lanosterol

USE:

  • Dermatophytes (especially onchomycosis)

TOX:

  • GI upset
  • Headaches
  • Taste disturbance
  • Hepatotoxicity
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13
Q

Terbinafine (MOA, USE, TOX)

A

Lanosterol synthesis

MOA:

  • –| Squalene Epoxidase
    • Squalene –> [SE] –> –> Lanosterol

USE:

  • Dermatophytes (especially onchomycosis)

TOX:

  • GI upset
  • Headaches
  • Taste disturbance
  • Hepatotoxicity
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14
Q

Terbinafine (MOA, USE, TOX)

A

Lanosterol synthesis

MOA:

  • –| Squalene Epoxidase
    • Squalene –> [SE] –> –> Lanosterol

USE:

  • Dermatophytes (especially onchomycosis)

TOX:

  • GI upset
  • Headaches
  • Taste disturbance
  • Hepatotoxicity
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15
Q

Echinocandins (MOA, USE, TOX)

A

Cell wall synthesis

MOA:

  • –| Beta-glucan synthesis

USE:

  • Invasive Aspergillosis
  • Candida

TOX:

  • GI upset
  • Histamine release –> flushing

[Anidulafungin, caspofungin, micafungin]

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16
Q

Echinocandins (MOA, USE, TOX)

A

Cell wall synthesis

MOA:

  • –| Beta-glucan synthesis

USE:

  • Invasive Aspergillosis
  • Candida

TOX:

  • GI upset
  • Histamine release –> flushing

[Anidulafungin, caspofungin, micafungin]

17
Q

Echinocandins (MOA, USE, TOX)

A

Cell wall synthesis

MOA:

  • –| Beta-glucan synthesis

USE:

  • Invasive Aspergillosis
  • Candida

TOX:

  • GI upset
  • Histamine release –> flushing

[Anidulafungin, caspofungin, micafungin]

18
Q

Griseofulvin (MOA, USE, TOX)

A

Microtubles

MOA:

  • –| Microtubules –> disrupted mitosis

USE:

  • Dermatophytes
    • Oral drug concentrated in keratin containing tissues

TOX:

  • –>+ CYP450 (and wafarin metabolism)
  • Teratogenic, carcinogenic
  • Confusion
  • Headaches
19
Q

Griseofulvin (MOA, USE, TOX)

A

Microtubles

MOA:

  • –| Microtubules –> disrupted mitosis

USE:

  • Dermatophytes
    • Oral drug concentrated in keratin containing tissues

TOX:

  • –>+ CYP450 (and wafarin metabolism)
  • Teratogenic, carcinogenic
  • Confusion
  • Headaches
20
Q

Griseofulvin (MOA, USE, TOX)

A

Microtubles

MOA:

  • –| Microtubules –> disrupted mitosis

USE:

  • Dermatophytes
    • Oral drug concentrated in keratin containing tissues

TOX:

  • –>+ CYP450 (and wafarin metabolism)
  • Teratogenic, carcinogenic
  • Confusion
  • Headaches