Antifungal Agents Flashcards

1
Q

For many years _____ drug was the only efficacious antifungal drug available for systemic use

A

Amphotericin B

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2
Q

Azole drugs comes with what formations?

A

Oral and parenteral

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3
Q

The only available route of administration of echinocandins

A

Parenteral administration

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4
Q

___ drugs are antifungal antibiotics produced by streptomyces nodosus

A

Amphotericin A and B

Amphotericin A is not in clinical use

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5
Q

___ is an amphoteric polyene macrolide.

A

Amphotericin B

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6
Q

Is effective only on fungi within the lumen of the tract an cannot be used for treatment of systemic disease

A

Oral amphotericin B

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7
Q

___ is a cell membrane sterol, is found in the cell membrane of fungi

A

Ergosterol

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8
Q

The predominant sterol of bacteria and human cell is?

A

Cholesterol

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9
Q

In what sterol does amphoericin B binds to?

A

Ergosterol

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10
Q

MOA of the drug:

Binds to ergosterol and alters the permeability of the cell by forming amphotericin B-associated pores in the cell membrane. The pore allows the leakage of intracellular ions and macromolecules, eventually leading to cell death

A

Amphotericin B

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11
Q

A drug that remains as the anti fungal agent with the broadcast spectrum of action. Has activity against candida albicans, cryptococcus neoformans, pathogenic molds.

A

Amphotericin B

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12
Q

A drug that remains a useful agent for all nearly life-threatening mycotic infections

A

Amphotericin B

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13
Q

Topical drops as well as direct subconjunctival injection of amphotericin B can cure?

A

Mycotic corneal ulcer and keratitis

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14
Q

Two broadcast categories of toxicity in amphotericin B

A

Infusion-related toxicity
- nearly universal and consists of fever, chills, muscle spasms, vomiting, headache
Cumulative toxicity
- renal damage, most significant toxic reaction

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15
Q

A potent antifungal agent that was discovered in 1957 during a search for novel antineoplastc agents. Its spectrum of action is much NARROWER that that of amphotericin B

A

Flucytosine

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16
Q

ROA of flucytosine

A

Only in oral formulation

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17
Q

MOA

Taken up by fungal cells via the enzyme cytosine permease. It is converted intracellularly first to 5-FU and then to 5-fluorodeoxyuridine monophosphate and fluoridine triphosphate, which inhibit DNA and RNA synthesis

A

Flucytosine

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18
Q

Enzyme that takes up flucytosine

A

Fungal cells via enzyme cytosine permease.

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19
Q

Conversion of flucytosine

A
  1. 5-fluroacil
  2. 5-fluorodeoxyuridine monophosphate (FdUMP)
  3. Fluorouridine triphosphate
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20
Q

Spectrum of activity of ____ is restricted to C neoformans and some candida sp

A

Flucytosine

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21
Q

Bone marrow toxicity, with anemia, leukopenia and thrombocytopenia

What drug has this kinds of common adverse effect?

A

Flucytosine

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22
Q

Are systemic compounds that can be classified as either imidazole or triazoles according to the number of nitrogen atoms in the five-membered azole ring

A

Azoles

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23
Q

Examples of imidazole

A

Ketoconazole
Miconazole
Clotrimazole

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24
Q

Examples of triazoles

A

Itraconazole
Fluconazole
Voriconazole
Isavuconazole
Posaconazole

25
Q

The first oral azole introduced into clinical use, is is less selective for fungal P450 than are the newer azoles

A

Ketoconazole

26
Q

Is the azole of choice for treatment of disease due to dimorphic fungi histoplasma, basltomyces and sporothrix

A

Itraconazole

27
Q

An azole that is extensively used in the treatment of dermatophytoses and onychomycosis

A

Intraconazole

28
Q

An azole that has the widest therapeutic index of the azoles , permitting more aggressive dosing in a variety of fungal infections

A

Fluconazole

29
Q

The azole of choice in the treatment and secondary prophylaxis of cryptococcal meningitis

A

Fluconazole

30
Q

An azole agent that is most commonly used for the treatment of mucocutaneous candidiasus

A

Fluconazole

31
Q

Available forms of:

Keto
Itra
Fluco
Vori
Posa
Isavu

A

Keto - PO
Itra - PO, IV
Fluco - PO, IV
Vori - PO, IV
Posa - liquid oral formulation
Isavu - PO, IV

32
Q

Treatment of choice for invasive aspergillosis and some environmental molds

A

Voriconazole

33
Q

A similar spectrum of action in triazoles that has an excellent activity agaist candida sp and dimorphic fungi

A

Voriconazole and itraconzaole

34
Q

An azole that was originally available only in liquid oral formulation.

IV form and sustained acting tabled are now available

A

Posaconazole

35
Q

The broadest spectrum member of the azole family, with activity against most species of candida and aspergillus

A

Posaconazole

36
Q

the first azole with significant activity against the agent of mucormycosis

A

Posaconazole

37
Q

A prodrug o the newest triazole

A

Isavuconazole

38
Q

___ has an antifungal spectrum similar to that of posaconzole

A

Isavuconazole

39
Q

The newest class of antifungal agents to be developed. Theya re large cyclic peptides linked to a long-chain FA

A

Echinocandins

40
Q

The only echinocandins that are only the licensed agents in the category of antifungals

A

Caspofungin, micafungin and anidulafungin

41
Q

The only available form of echinocandins

A

IV formulation

42
Q

Micafungin

Dose of 150mg/d treats?
Dose of 100mg treats?
Dose of 50mg treats?

A

150 - esophageal candidiasis
100 - candidemia
50 - prophylaxis of fungal infections

43
Q

HL of
Caspofungin
Micafungin
Anidulafungin

A

C - 9-11hrs
M - 11-15 hrs
A - 24-48 hrs

44
Q

MOA of echinocandins

A

Inhibits the synthesis of B(1-3) glucan resulting in desruption of the fungal cell wall and cell death.

45
Q

Caspofungin is licensed for use in?

A

Invasive aspergillosis

46
Q

Micafungin is licensed for use in?

A

Mucocutaneous candidiasis, candidemia and prophylaxis of candidal infections

47
Q

Anidulafungin is approved for use in?

A

Esophagel candidiasis, invasive candidiasis, candidemia

48
Q

Very insoluble fungistatic drug derived from species of penicillium

A

Griseofulvin

49
Q

Griseofulvin is only use in the systemic treatment of?

A

Dermatophytosis

50
Q

ROA of griseofulvin

A

Microcrystalline oral form

51
Q

MOA

It is deposited in newly forming skin where it binds to keratin, protecting the sin from new infection

A

Griseofulvin

52
Q

A synthetic allylamine that is used in the treatment of dermatophytoses especially onychomycosis

A

Terbinafine

53
Q

MOA

Inhibits fungal enzyme squalene epoxidase, leads to the accumulation of the sterol squalene, which is toxic to the organism

A

Terbinafine

54
Q

Like griseofulvin, terbinafine is a keratophilic medication, but unlike griseofulvin, it is ____

A

Fungicidal

55
Q

A polyene macrolide much like amphotericin B, too toxic for parental administration and is only used topically

A

Nystatin

56
Q

Nystatin is commonly used for suppression of __ infection

A

Local candidal infection

57
Q

Two azole that are most commonly used topically are?

A

Clotrimazole and miconazole

58
Q

Pleasant-tasting Alternative to nystatin, they are available for treatment of oral thrush.

A

Oral clotrimazole

59
Q

Allymines available as topical creams. Bot are effective for treatment of tinea cruris and tinae corporis

A

Terbinafine and naftifine