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Antifungal Flashcards

1
Q

Amphotercin B

Oral absorption

A

Poor oral absorption

Use only if fungi with the lumen of GI tract

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2
Q

Itraconazole oral absorption

A

Best with food

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3
Q

Flucornazole oral absorption

A

Nearly complete

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4
Q

Voriconazole oral absorption

A

90%

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5
Q

Flucytosine oral absorption

A

Absorb rapidly and well in git

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6
Q

Caspofungin oral absorption

A

ONLY IV

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7
Q

Antifungal good CSF

A

Fluconazole
Voriconazole
Flucytosine

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8
Q

Amphotercin B protein binding

A

90%

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9
Q

Itraconazole BP

A

99%

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10
Q

Caspofungin BP

A

Highly

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11
Q

Flucytosine BP

A

Minimal

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12
Q

Antifungal Liver metabolism

A

Itraconazole

Voriconazole

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13
Q

Antifungal minimal metabolism

A

Flucytosine

Caspofungin

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14
Q

Eliminated in the urine antifungal

A

Amphotercin B
Fluconazole
Flucytosine
Caspofungin

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15
Q

Eliminated in GIT antifungal

A

Caspofungin

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16
Q

Eliminated in the liver antifungal

A

Itraconazole

Voriconazole

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17
Q

Amphotercin B half life

A

15days

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18
Q

Itraconazole t1/2

A

24-42hr

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19
Q

Fluconazole half life

A

25-30hr

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20
Q

Voriconazole half life

A

6hr

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21
Q

Caspofungin half life

A

25-30hr

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22
Q

Flucytosine half life

A

3-6h Normal

Renal failure
As long as 200h

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23
Q

Amphotercin B

A

Polyene

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24
Q

Nystatin

A

Polymenes

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25
Q

Clotrimazole

A

Imidazole

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26
Q

Miconazole

A

Imidazole

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27
Q

Ketoconazole

A

Imidazole

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28
Q

Itraconazole

A

Triazole

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29
Q

Fluconazole

A

Triazole

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30
Q

Voriconazole

31
Q

5-flucytosine

A

Pyrimidine analogue

32
Q

Caspofungin

A

Echinocandins

33
Q

Terbinafine

A

Topical preparation

34
Q

Polyenes MOA

A

Strong affinity for ergosterol

Binding to it causes disruption to fungal cell membrane

35
Q

Amphotercin B ROA

A

Oral
IV
Intraarticular

36
Q

Nystatin ROA

A

Topical (creams ointment suppositories)

37
Q

Amphotercin B SE

A

Infusion rxn (shake and bake syndrome; fever and chills )

Thrombophlebitis
Nephrotoxic
Bone marrow suppression

38
Q

Nystatin SE

A

It is not absorbed to a significant degree from skin, mucous membranes, or the gastrointestinal tract. As a result, nystatin has little toxicity.

39
Q

Amphotercin B DDI

A
  1. aminoglycosides,

2. vancomycin,
3. NSAIDs,
4. cyclosporine
All will increase nephrotoxic potential.

40
Q

Azoles MOA

A

Inhibit ergosterol synthesis, by inhibiting α- demethylase, which demethylates lanosterol to ergosterol

41
Q

Clotrimazole ROA

A

Topical

Cream lotion powder pessary

42
Q

Miconazole ROA

A

Cream powder

Oral gel 2%

43
Q

Ketoconazole ROA

A

Topical

Shampoo

44
Q

Itraconazole ROA

A

Oral only

best absorb with food

45
Q

Fluconazole ROA

46
Q

Voriconazole ROA

A

Oral (>90% absorb)

IV

47
Q

Amphotercin B clinical application

A

Invasive aspergillosis
Histoplasmosis
Systemic candidiasis

48
Q

Nystatin clinical application

A

Vaginal candidiasis

49
Q

Imidazole are

Useful alternative to ____________

A

Amphotercin B for treating different systemic fungal infection

50
Q

Clotrimazole clinical application

A

Clotrimazole - skin and vulvovaginal infections caused by a wide variety of fungi, including Candida.

51
Q

Miconazole clinical application

A

Miconazole - tineal infections and vulvovaginal candidiasis; oral gel for thrush (alternative to nystatin)

52
Q

Most potent triazole

A

Itraconazole

53
Q

Itraconazole clinical application

A

Itraconazole - Trichophyton infections, Histoplasmosis,

54
Q

Fluconazole clinical application

A

Fluconazole - Cryptococcosis, candidiasis in AIDS patients, vaginal candidiasis

55
Q

Voriconazole clinical application

A

Voriconazole - Candidaemia; invasive aspergillosis (alternative to amphotericin B)

56
Q

Itraconazole SE

A

GIT disturbance
Mild rash

May have SJS

  1. Headache Serious side effects:
  2. cardiac suppression (due to negative inotropic action on cardiac muscle)
  3. hepatotoxicity
57
Q

Fluconazole SE

A

GIT disturbance
Mild rash

May have SJS

58
Q

Voriconazole se

A

GIT disturbance
Mild rash

May have SJS

  1. hepatitis,
  2. visual disturbances: -colour perception defect,
    -reduced visual acuity,
    -photophobia.
59
Q

Itraconazole
Fluconazole

DDI

A

Warfarin
Sulphonylurea
Digoxin

(Both anole inhibit hepatic CYP450 enzyme)

PPI
Antacid
H2RA
(Reduce anole absorption)

60
Q

Voriconazole DDI

A

Carbamazepine
Erythromycin

Voriconazole is both a substrate and inhibitor of CYP450 enzymes.
Avoid concomitant use of
potent CYP450 inducers, like carbamazepine, and
inhibitors, like erythromycin.

61
Q

Flucytosine MOA

A

Disrupt synthesis of fungal RNA and DNA

62
Q

Caspofungin MOA

A

Inhibit the synthesis of β(1–3)- glucan =>disruption of the fungal cell wall and cell death.

63
Q

Terbinafine MOA

A

Squalene accumulates in the cell and Inhibits squalene epoxidase which is
involved in the synthesis of ergosterol from squalene.

64
Q

Flucytosine ROA

65
Q

Caspofungin ROA

66
Q

Terbinafine ROA

A

Topical - 1% cream: for treatment of dermatophytic infections.

Oral – not commonly prescribed.

67
Q

Flucytosine clinical application

A

Effective against systemic yeast infections if given orally.
Systemic Candidiasis and Cryptococcal meningitis (combined with amphotericin B).
Combination allows use of amphotericin B at a lower dose, thus reducing the risk of nephrotoxicity.

Combine with itraconazole for chromoblastomycosis

68
Q

Caspofungin Clinical application

A

Mucocutaneous candidiasis and candidaemia, usually in immuno-compromised patients

Salvage therapy in patients with invasive aspergillosis (failed response to amphotericin B)

69
Q

Terbinafine clinical application

A

Against dermatophytic infection of the skin and nails (“keratophilic”).

70
Q

Flucytosine SE

A
  1. Bone marrow suppression is most serious. Monitor leucocytes and platelets weekly.
  2. Hepatotoxicity - mild and reversible damage is common; monitor liver enzymes (ALT and AST weekly.
71
Q

Caspofungin SE

A
  1. GIT-related symptoms, fever, histamine-like facial flushing rash, pruritus
  2. thrombophlebitis
  3. Foetal toxicity (Category C) - Avoid use in pregnancy.
72
Q

Terbinafine SE

A

Erythema, dry skin.
(These can be avoided by not using > 4 weeks).

73
Q

Flucytosine DDI

A

Quinidine

Causes dysthymia

74
Q

Caspofungin DDI

A
  1. rifampicin
  2. Carbamazepine
  3. cyclosporine

(1), (2) are CYP 450 inducers; reduce caspofungin plasma levels

Risk of hepatotoxicity

Antibiotic (21 decks)

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