Antifungals Flashcards

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1
Q

Itraconazole = Treatment of choice for

A

candida, endemic (dimorphic) fungi

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2
Q

Nystatin treats

A

treat oral candidiasis

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3
Q

Nystatin is active against

A

most Candida sp and is most commonly used for suppression of local candidal infections

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4
Q

Allylamine subclass?

A

terbinafine

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5
Q

Allylamine

Terbinafine spectrum?

A

Activity against fungi that cause tinea: trichophyton, epidermophyton, and microsporum

Tera been fine at the MET

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6
Q

Allylamine

terbinafine, MOA

A
  • Inhibits squalene epoxidase enzyme
  • Causes accumulation of squalene which is toxic to cell
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7
Q

Allylamine

terbinafine ( fungicial or fungistatic?)

A

fungicidal

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8
Q

Allylamine

terbinafine, adverse effect?

A

hepatotoxicity

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9
Q

Allylamine

terbinafine, contraindications

A

Can’t take if you have liver issues

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10
Q

Long treatment time with no alcohol use (6-12 wks)

what antibiotic?

A

terbinafine

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11
Q

Inhibits some ____ enzymes for terbinafine

A

liver

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12
Q

Azoles

imidazoles, names

A

clotrimazole, miconazole, ketoconazole

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13
Q

Azoles

imidazoles have __ nitrogens

A

2 nitrogens

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14
Q

Miconazole is used to treat

A

cutaneous Candida infections

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15
Q

Azoles

triazoles have __ nitrogen rings

A

3

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16
Q

Azoles

triazoles, names

A

fluconazole, itraconazole, voriconazole

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17
Q

Azoles

Clotrimazole and miconazole used topically for

A

vulvovaginal candidiasis

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18
Q

Azoles

Oral clotrimazole treat

A

oral thrush

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19
Q

Azoles

Imidazoles treat

A
  • Dermatophytes (tinea) and candida
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20
Q

Ketoconazole was used topically for

imdiazole

A

hair and scalp issues (tinea)

not anymore

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21
Q

Fluconazole used for

Triazoles

A

candida (especially albicans) and cryptococcus

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22
Q

Oral fluconazole is the preferred treatment for

triazoles

A

Candida esophagitis

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23
Q

“diflucan”

fluconazole

Triazoles

A

vaginal yeast infections and thrush

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24
Q

reduced bioavailability of itraconazole when taken with

A

rifamycins (rifampin, rifabutin, rifapentine)

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25
Q

Voriconazole treats

triazoles

A

candida, and more so for aspergillus (less for endemic)
- Treatment of choice for aspergilloses

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26
Q

Azoles, -cidial or -static?

A

fungistatic

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27
Q

what antifungal

Work on last step in ergosterol formation. lanosterol to ergostreol

A

azoles

28
Q

what antifgunal?

  • Prevents conversion of lanosterol to ergosterol by inhibiting enzyme
A

azoles

29
Q

Azoles resistance

A

Resistance:
* efflux pumps
* target site alteration (mutate enzyme to prevent drug from binding)
* bypass pathways
* upregulations of lanosterol

30
Q

drug interaction for azoles

A
  • Interfere with liver enzymes that metabolize medications (cP450)
  • Increased concertation of other medications
  • Higher risk of toxicity
31
Q

adverse effects

Fluconazole and voriconazole can cause

triazoles

azoles

A
  • QT elongation
32
Q

adverse effects

  • vision changes
    and photosensitivy

medication?

A

Voriconazole

azoles

triazoles

33
Q

is the broadest-spectrum member of the azole family, with activity against most species of Candida and Aspergillus

A

Posaconazole

triazoles

34
Q

adverse effects

Edema
Exacerbate heart failure

A

Itraconazole

azoles

triazoles

35
Q

adverse effects

Cross blood brain barrier to treat meningitis

A

Fluconazole and Voriconazole

azoles

triazoles

36
Q

Polyenes subclass?

A

(amphotericin B)

37
Q

amphotericin B, spectrum

A

Very broad and kill lots of different fungi

38
Q
  • Used for severe fungal infection initially and then switched to another medication due to side effects

what antifungal?

A

Polyenes (amphotericin B)

39
Q

Amphotericin B is used to treat

A

systemic Candida infections

40
Q

amphotercin b, -cidial or -static?

A

fungicidal

41
Q

resistance for Polyenes (amphotericin B)

A
  • Uses ergosterol to kill fungal cells
    • Binds to ergosterol and make a membrane pore
  • Not much resistance
42
Q
  • Given only IV
    • Poorly bioavailable
    • Has a formulation with a liposome that makes it less toxic (nephrotoxic)

what antifungal

A

Polyenes (amphotericin B)

43
Q

adverse effect

Immediate onset: muscle spasms, headache, fever & chills (rigors), hypotension, electrolyte imbalance, nausea and vomiting

what antifungal?

A

Polyenes (amphotericin B)

44
Q

Delayed adverse effects for Polyenes (amphotericin B)

A

severe nephrotoxicity
long term

45
Q

drug interactions for amphotericin b?

A

Vancomycin and aminoglycosides (antibiotics)

- Nephrotoxic drugs

46
Q
  • Not great to use for pregnant women
    contraindications

3 drugs

A
  • Polyenes (amphotericin B)
  • Flucytosine
  • Echinocandins (micafungin, caspofungin, anidulafungin)
47
Q

Flucytosine is effective against

A
  • Only effective against cryptococcus and some candida
48
Q

converted by cytosine deaminase to 5-flurouracil (active form) which inhibits DNA/RNA synthesis, what drug and why?

A

Flucytosine, Humans don’t have cytosine deaminase

49
Q

Amphotericin B make pore for flucytosine to

A

get into the fungi cell

50
Q

Flucytosine Resistance:

A

alteration of metabolic pathway to avoid activation step

51
Q

what antifungal?

Synergy: Always used with another drug (never used as monotherapy due to quick resistance)

A

Flucytosine

52
Q

adverse effect of

  • Non-selective activation causes Bone marrow toxicity (decreases in blood cells) from amphotercin b
A

Flucytosine

53
Q

Flucytosine

Nephrotoxicity (bad when used with ___

A

amphotericin B

54
Q

Flucytosine is given

A

Orally bioavailable

55
Q

Flucytosine

Contraindication:

A

pregnancy especially in first trimester

56
Q

Echinocandins, 3 drugs

A

(micafungin, caspofungin, anidulafungin)

57
Q

Echinocandins treats?

(micafungin, caspofungin, anidulafungin)

A
  • Candida and Aspergillus
58
Q

Echinocandins is used to treat

(micafungin, caspofungin, anidulafungin)

A

systemic candida infections

59
Q

Echinocandins is used as salvage therapy for

(micafungin, caspofungin, anidulafungin)

A

aspergillosis after voriconazole

60
Q

Echinocandins, -cidal or -static?

(micafungin, caspofungin, anidulafungin)

A

fungicidal

61
Q

Inhibits enzyme beta-1,3 glucan synthase

what antifungal?

A

Echinocandins

(micafungin, caspofungin, anidulafungin)

62
Q

Echinocandins they work on cell wall
by

(micafungin, caspofungin, anidulafungin)

A

preventing the synthesis of Beta-1,3-glucans

63
Q

Echinocandins Resistance:

(micafungin, caspofungin, anidulafungin)

A

mutation of the glucan synthase so it cannot bind to echinocandin

64
Q

Echinocandins is not orally bioavailable so must be given

(micafungin, caspofungin, anidulafungin)

A

must be given IV

65
Q

is the agent most commonly used for the treatment of mucocutaneous candidiasis

A

Fluconazole