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Foundations 7 > Antifungal Drugs > Flashcards

Antifungal Drugs Flashcards

1
Q

Most antifungals inhibit

A

Ergosterol

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2
Q

Rates of fungal infections in females

A

Lower pre puberty and post menopausal because ergosteorl looks like progesterone and estrogen

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3
Q

3 ways we attack fungi

A

Bind to ergosterol
Inhibit lanosterol demethylase
Inhibit Squalene epoxidase

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4
Q

Azole drugs mech, side effects, resistance

A

Drugs inhibit lanosterol demethylase (a p450 enzyme) (bind to heme)

Human and fungal have same enzyme…also a p450 enzyme and inhibit its expression…inhibit human sterol synthesis and drug metabolism

Mutations in lanosterol demethylase

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5
Q

Active site of P450 protein

A

Heme uses an iron to oxidize drugs and metabolites

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6
Q

What happens to P450 drugs with azoles

A

Increased concentrations

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7
Q

Fluconzaole use

A

Choice for candidiasis and both cryptococcal and coccidioidal meningitis

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8
Q

Dosage of fluconzaoler

A

Effective orally and also given IV…minimally metabolized and crosses BBB

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9
Q

Fluconazole side effcts

A

Fewer than ketoconazole…significant interactions (think statins, PIs, and cyclosporine)

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10
Q

Miconazole use

A

Topically and used for tinea corporis, tinea pedis, and vaginal candidosis

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11
Q

Side effects of miconazole

A

Side effects include local burning, itching, irritation

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12
Q

Jublia is more effective than

A

Terbinafine…jublia actually penetrates he toenail

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13
Q

Candida albicans tx

A

Azoles or polyenes

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14
Q

Histoplasma capsulatum tx

A

Azoles and polyenes especially itraconazole and amphotericin B

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15
Q

Blastomyces dermatidis tx

A

Itraconazole…amphotericin B is 2nd choice

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16
Q

Cryptococcus neoformans tx

A

Amphotericin B…if meningitis combine with fluconazole

17
Q

Candida glabrata tx

A

Reistant to azoles and polyenes…treat with topical flucytosine and boric acid

18
Q

Microsporum canis.audouni tx

A

infections of hair, nail, and toes…treat with griseofulvin

19
Q

Amphotericin B mech

A

Disrupts cell membrane and binds ergosterol

20
Q

Amphotericin B use and side effects

A

Broad spectrum

Fever and chills and allergic reactions (tx with tylenol)…principal, dose limiting toxicity is renal dysfunction…hypotension, hypokalemia, and others

21
Q

Nystatin use, admin, and side effects

A

Similar to amphotericin but only topical tx for oral candidosis
Minimal absorption orally
Minial side effects topically

22
Q

Flucytosine mechanism

A

Enters via cytosine-specific permease enzyme and converted to 5-FU by cytosine deaminase…eventually blocks DNA and protein synthesis by disrupting thymidylate sunthase

Mammalian cells do NOT convert flucytosine to fluorouracil

23
Q

Resistance to flucytosine

A

Through decreased uptake of the drug by permease or decreased cytosine deaminase activity

24
Q

Flucytosine admin and side effects

A

Well absorbed and penetrates orally…always used with amphotericin B to slow development of resistance

Leucopenia and thrombocytopenia…nausea, vomiting and diarrhea

25
Q

Girseofulvin mech

A

Binds to MTs to disrupt the mitotic spindle and block replication in mitosis…specific to fungi

26
Q

Griseofulvin administration

A

Orally…concentrates in skin at sites of newly synthesized keratin containing tissues…induces P450 enzymes

27
Q

Griseofulvin side effects

A

Rare but could be allergic response, heachache, nausea, and liver toxocity

28
Q

Terbinafine mech

A

Inhibits squalene epoxidase in ergosterol synthesis

Non-azole inhibitor of sterol synthesis

29
Q

Terbinafine admin

A

Topically…administered orally, concentrates in skin and nail beds

30
Q

Caspofungin mech

A

Inhibits 1,3-B-D-Glucan synthesis blocking cell wall synthesis

Good against candida and aspergillus…good for CNS as well…not absorbed in GI and must be injected

Limited side effects

Foundations 7 (19 decks)

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