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CMOD > Antifungals > Flashcards

Antifungals Flashcards

1
Q
  • MOA: fungicidal, causes loss of cell membrane integrity by forming pores in the membrane, allowing leakage
  • Very toxic to the kidneys
  • Amphipathic molecule, but poorly soluble
  • Must be administered by IV
  • Given with other lipid drugs to improve solubility and decrease renal toxicity
  • MOR: Sterol modification
A

Amphotericin B

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2
Q
  • MOA: Inhibitor of Beta-1-2 glucan, an important structural component of the cell wall
  • Must be given parentally
  • Well tolerated
  • Used against APERGILLUS and CANDIDA SP
  • MOR: Altered synthetase
A

Caspofungin (Echinocandins)

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3
Q
  • MOA: Block synthesis of ergosterol, a major fungal sterol component of the cell membrane
  • Prevent conversion of lanosterol to ergosterol
  • Works through Cytochrome P450 Inhibition
  • Eliminated in the urine
  • Cannot give during pregnancy
  • Can reach CSF
  • Overall best profile w/ widest therapeutic index
  • MOR: Efflux, Demthylase alteration, Bypass, Overproduction
A

Fluconazole

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4
Q
  • MOA: Block synthesis of ergosterol, a major fungal sterol component of the cell membrane
  • Prevent conversion of lanosterol to ergosterol
  • Works through Cytochrome P450 Inhibition
  • Very poor ability to penetrate into CSF
  • One of the highest incident of side-effects
  • Poor oral bio-availability
  • MOR: Efflux, Demthylase alteration, Bypass, Overproduction
A

Itraconazole

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5
Q
  • MOA: Block synthesis of ergosterol, a major fungal sterol component of the cell membrane
  • Blocks conversion of squalene to squalene epoxide, leading to a toxic buildup of squalene
  • No effects upon CYP activity
  • Well tolerated, except with transient lymphopenia and neutropenia
  • Avoid giving to immunosuppressed patients
  • MOR: Efflux
A

Terbinafine

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6
Q
  • MOA: Block synthesis of ergosterol, a major fungal sterol component of the cell membrane
  • Prevent conversion of lanosterol to ergosterol
  • Works through Cytochrome P450 Inhibition
  • Cannot give during pregnancy
  • Can reach CSF
  • Highest problem with cytochrome-mediated drug-drug interactions
  • Associated with photosensitive dermatitis and hallucinations
A

Voriconazole

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7
Q
  • MOA: nucleic acid synthesis inhibitor that prevents cell replication
  • Pyrimidine analog with narrow therapeutic window
  • Enters fungal cell via enzyme cytosine permease
  • Converted to 5-FU and mediated in intestinal microflora
  • Associated with hematologic toxicities like anemia, leukopenia, and thrombocytopenia
  • MOR: Permease or modifying enzymes mutation
A

Flucytosine

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8
Q
  • MOA: Block synthesis of ergosterol, a major fungal sterol component of the cell membrane
  • Prevent conversion of lanosterol to ergosterol
  • Works through Cytochrome P450 Inhibition
  • Very poor ability to penetrate into CSF
  • Can cause irreversible hepatic damage and adrenal insufficiency
  • At high [conc], can inhibit aldosterone, cortisol, and testosterone, useful in treating prostate cancer
  • MOR: Efflux, Demthylase alteration, Bypass, Overproduction
A

Ketoconazole

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9
Q
  • MOA: Inhibitor of Beta-1-2 glucan, an important structural component of the cell wall
  • Must be given parentally
  • Well tolerated
  • Used against APERGILLUS and CANDIDA SP
  • MOR: Altered synthetase
A

Micafungin

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10
Q
  • MOA: Block synthesis of ergosterol, a major fungal sterol component of the cell membrane
  • Prevent conversion of lanosterol to ergosterol
  • Works through Cytochrome P450 Inhibition
  • One of the highest incident of side-effects
  • Only azole with activity against MUCORMYCOSIS
  • Oral administration w/ CYP-mediated drug-drug interactions
A

Posaconazole

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11
Q
  • MOA: Mitotic Spindle Inhibitor in cell nucleus, which also makes it a cell-cycle inhibitor
  • Systemic treatment of dermatophytosis
  • CYP3A4 inducer
  • Drug interactions: warfairin, oral contraceptives, cyclosporine, and aprepitant
A

Griseofulvin

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12
Q
  • MOA: Topical form of Amphotericin B
  • Topical drug used to treat CANDIDIASIS
  • MOR: Sterol modification
A

Nystatin

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13
Q

What drug(s) do you use for ASPERGILLOSIS?

A

Voriconazole IV

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14
Q

What drug(s) do you use for BLASTOMYCOSIS (mild)

A

Itraconazole PO

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15
Q

What drug(s) do you use for BLASTOMYCOSIS (severe)

A

Amphotericin B IV then Itraconazole PO

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16
Q

What drug(s) do you use for CANDIDIASIS

A

Fluconazole PO

17
Q

What drug(s) do you use for CRYPTOCOCCUS

A

Amphotericin B IV + Flucytosine PO, then Fluconazole PO

18
Q

What drug(s) do you use for HISTOPLASMOSIS

A

Amphotericin B IV + Itraconazole PO

19
Q

What drug(s) do you use for MUCORMYCOSIS

A

Amphotericin B

20
Q

What drug(s) do you use for Sporotrichosis

A

Amphotericin B IV and/or Itraconazole PO

21
Q

What is a drug comparable to Amphotericin B?

A

Nystatin

22
Q

Topical drugs used to treat CANDIDIASIS infection

A

Clotrimazole and Miconazole

CMOD (8 decks)

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