Anti-fungals Flashcards

1
Q

How do fungi grow?

A

As single celled (yeasts) or filamentous multicellular aggregates (molds)

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2
Q

How do yeastlike fungi reproduce?

A

Budding

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3
Q

What does dimorphic fungi mean?

A

Fungi can grow as yeasts or as molds

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4
Q

Dimorphic fungi grow as what in host at what in room temp?

A

Yeast in host

Mold at room temp

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5
Q

Fungi that are pathogenic in humans are what?

A

Nonmotile and have a rigid cell well

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6
Q

The cell wall in pathogenic fungi are composed of what?

A

Chitin and polysaccharides

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7
Q

Fungi that are transmissible?

A

Ringworm of the scalp

Thrush in newborns

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8
Q

What are dermatomycoses?

A

Filamentous fungi that live on keratinized tissue

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9
Q

Onychomycoses?

A

Fungal infection of the nail

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10
Q

How does Tolnaftate function?

A

Inhibits fungal squalene epoxidase resulting in decreased ergosterol

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11
Q

What does ergosterol do in fungi?

A

Steroid in fungal cell membranes

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12
Q

Why does Tolnaftate not affect humans?

A

We use cholesterol as steroid in membranes

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13
Q

How does Clotrimazole work?

A

Inhibit CYP450 which catalyzes 14a-demethylation of lanosterol to ergosterol

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14
Q

How do azaleas affect humans?

A

They have a greater affinity for fungal CYP450s but still get humans so they can interfere with drug metabolism

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15
Q

Griseofulvin natural product of whaT?

A

Penicillium griseofulvin

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16
Q

How does Griseofulvin work?

A

Disrupts mitotic spindle by binding to polymerized microtubules to inhibit mitosis

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17
Q

Griseofulvin treats what?

A

Fungal nail infections, treatment can last a year, taken with high fat diet

18
Q

Amphotericin B is amphoteric, what does that mean?

A

Has both acidic and basic groups

19
Q

How do you give Ampho B?

A

IV due to poor GI absorption due to poor water solubility

20
Q

How does Ampho B work?

A

Binding to ergosterol in membranes, pores open, ions and organic molecules leak out

21
Q

How does 5-Fluorocytosine work?

A

Fungi convert 5-Fluorocytosine to 5-fluorouracil which is converted into 5-fluorodeoxyuridine monophosphate which inhibits thymidylate synthase

22
Q

What does inhibiting thymidylate synthase do?

A

Inhibits DNA synthesis

23
Q

In addition to DNA synthesis what else does 5-fluorouracil inhibit?

A

protein synthesis via incorporation into RNA in place of uracil due to van der Waals radius similarity to hydrogen

24
Q

If used in humans by itself what is 5-fluorouracil used as?

A

Anticancer agent

25
Q

Why doesn’t 5-fluorouracil harm humans?

A

Human cells have little or no cytosine deaminase activity

26
Q

5-fluorocytosine used with what can treat systemic Candida and Cryptococcus neoformans meningitis?

A

Ampho B

27
Q

What is 5-fluorocytosine combined with to kill resistant strains

A

Ampho B

28
Q

How does the combo of 5-Fluorocytosine and Ampho B work?

A

Ampho B enhances uptake of 5-fluorocytosine

29
Q

Danger of 5-fluorocytosine?

A

Depresses bone marrow function so don’t give to people with bone marrow depression or bad kidneys due to renal excretion

30
Q

Anti fungal used for systemic infections but weaker than Ampho B?

A

Ketaconazole

31
Q

Distinguishing point about Fluconazole?

A

3 nitrogen in rings

32
Q

Use for Fluconazole?

A

Treatment of meningitis from fungi

33
Q

Biggest danger of Fluconazole

A

Hepatotoxicity

34
Q

Distinguishing feature of Itraconazole?

A

1:1:1:1 racemic mixture of four diastereomers

3 nitrogen rings

35
Q

What do you use Itraconazole for?

A

Histoplasmosis

36
Q

Danger of Itraconazole?

A

Heart failure so don’t give to cardiac patients

Liver failure

37
Q

Itraconazole will interact with what other drugs?

A

Those metabolizes by CYP450

38
Q

How do Echinocandins work?

A

Inhibit 1,3-B glucan synthesis in fungal cell walls via noncompetitive inhibition of 1,3-B-glucan synthase

39
Q

Why do Echinocandins not harm humans?

A

Mammalian cells lack 1,3B-glucan synthase

40
Q

Cross resistance of Echinocandins?

A

None

41
Q

What does Echinocandins synergistic with?

A

Voriconazole and ampho B