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DD unit 3 > Antifungal review > Flashcards

Antifungal review Flashcards

1
Q

Which conditions facilitate the overgrowth of opportunistic organisms?

A

Alteration of gut flora, immunosuppression, systemic diseases (HIV, diabetes, adrenal suppression).

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2
Q

What are the targets for antifungal drugs? (

A

Ergosterol, B-glucan synthase, inhibit fungal CYP450 and prevent ergosterol synth, inhibit squalene oxidase, interfere with DNA synth

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3
Q

Which drugs target ergosterol?

A

Amphotericin B, nystatin

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4
Q

Which drugs target b-glucan synthase?

A

Echinocandins-micafungin

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5
Q

Which drugs target CYP450?

A

Triazoles - fluconazole, itraconazole; Imidazoles - ketoconazole, clotrimazole, miconazole

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6
Q

Which drugs target squalene oxidase?

A

terbinafine

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7
Q

Which drugs target DNA synthesis?

A

flucytosine

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8
Q

What the the mechanism of action of amphotericin B?

A

binds to ergosterol and opens pores causing leakage of cell components and cell death.

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9
Q

How is ampho B absorbed?

A

Poor oral, so given IV or topically. Can be used in bladder irrigation or injected in to the ventricles

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10
Q

How is ampho B distributed?

A

Rapidly sequestered in tissues and slowly released but little CNS penetration

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11
Q

T or F: Ampho B is the most reliable agent against most fungal pathogens.

A

True. Drug of choice for life-threatening systemic fungal infections.

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12
Q

What are the adverse side effects of ampho B?

A

nephrotoxicity and anemia. Will often see fever, chills, rigor, hypotension (shake and bake). Can give acetaminophen-diphenhydramine or hydrocortisone. Also give merperidine for rigors

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13
Q

What does nystatin do?

A

Similar mechanism of action as ampho B.

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14
Q

How is nystatin given?

A

topical treatment of candida infections

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15
Q

T or F: Nystatin is given systemically by IV.

A

False. toxic so no IV use

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16
Q

What do echinocandins target?

A

b-glucan synthase, a cell wall component

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17
Q

How are echinocandins given?

A

IV

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18
Q

How are echinocandins eliminated?

A

renal, require dosing for renal insufficiency

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19
Q

Which infections are enchinocandins used to treat?

A

aspergilosis that is refractory to ampho or intraconazole

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20
Q

What are the adverse side effects of echinocandins?

A

allerigic type reaction, fever, nausea, headache, phlebitis

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21
Q

T or F: Itracon and Flucon are fungistatic.

A

TRUE

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22
Q

How are itra and flucon given?

A

Orally

23
Q

How are itra and flucon eliminated?

A

Flu - renal; Itra - hepatic

24
Q

T or F: Itracon can enter the CNS.

A

False. Flucon can enter the CNS to treat fungal meningitis.

25
Q

What are the clinical uses of flucon?

A

Vaginal candidiasis if topicals fail. Oropharyng and esophag candidiasis, serious systemic infections. Cryptococcal meningitis in AIDs patients.

26
Q

What are the clinical uses of itracon?

A

dermatophytoses and onchomycosis. Also beneficial for aspergillosis and other system infection over flucon.

27
Q

What are the adverse side effects of flucon?

A

Well tolerated, gi distress, rash, inc liver enzymes. Inhibit cyp450 metabolism so will have drug interactions. Pregnacy cat D

28
Q

What are the adverse side effects of itracon?

A

same as flucon except preg cat C.

29
Q

T or F: Imidazoles are fungicial.

A

True, but only at high concentrations

30
Q

How is ketoconazole given?

A

oral or IV. systemic!

31
Q

How is ketoconazole absorbed?

A

poorly but better at low pH (with food)

32
Q

How is ketoconazole distributed?

A

well, but not in CNS. also crosses the placenta

33
Q

How is ketoconazole eliminated?

A

hepatic, breast milk

34
Q

How is ketoconazole used?

A

chronic mucocutaneous candidiasis

35
Q

How is clotrimazole used?

A

oral and vaginal candidiasis as creams. not used systemically due to toxicity

36
Q

How is ketoconazole toxic?

A

anorexia, nausea, pruritis, rash, dizziness, hepatotox. Can inhibit testosterone synthesis, drug interaction -strong inhibitor of CYP3A4

37
Q

What is the mechanism of action of terbinafine?

A

inhibits squalene oxidase as part of the ergosterol synth pathway.

38
Q

T or F: Terbinafine is fungicidal.

A

True. accumulation of squalene is toxic.

39
Q

How is terbinafine used?

A

orally for onychomycosis - toe and nail infection, topically for athletes foot (tinea cruris and corporis)

40
Q

How is terbinafine toxic?

A

gi upset, rash, headache, inhibition of CYP450 drug metabolism

41
Q

What is the mechanism of action of flucytosine?

A

converted into 5-fluorouracil via fungal cytosine deaminase and interferes with DNA synthesis

42
Q

How is flucytosine administered?

A

oral (qid)

43
Q

How is flucytosine distributed?

A

all over including CNS

44
Q

How is flucytosine eliminated?

A

renal

45
Q

How is flucytosine used?

A

cryptococcus, candidiasis, chromoblastomycosis

46
Q

How is flucytosine toxic?

A

rarely toxic, but can seen nausea, vomiting and rash. High levels have bone marrow depression and abnormal liver function, hair loss.

47
Q

What is the mechanism of action of griseofulvin?

A

Binds microtubules and inhibits mitosis.

48
Q

T or F: Griseofulvin is fungistatic

A

TRUE

49
Q

How is griseo absorbed?

A

oral, but poorly

50
Q

How is griseo distributed?

A

has a high affinity for keratin so it goes to keratin

51
Q

How is griseo eliminated?

A

feces

52
Q

How is griseo used?

A

severe dermatophytosis in skin/hair, nails

53
Q

How is griseo toxic?

A

hypersensitivity reactions, occasionally headache, gi upset, mental confusion

DD unit 3 (5 decks)

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