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
Clotrimazole
Imidazole
26
Miconazole
Imidazole
27
Ketoconazole
Imidazole
28
Itraconazole
Triazole
29
Fluconazole
Triazole
30
Voriconazole
Triazole
31
5-flucytosine
Pyrimidine analogue
32
Caspofungin
Echinocandins
33
Terbinafine
Topical preparation
34
Polyenes MOA
Strong affinity for ergosterol | Binding to it causes disruption to fungal cell membrane
35
Amphotercin B ROA
Oral IV Intraarticular
36
Nystatin ROA
Topical (creams ointment suppositories)
37
Amphotercin B SE
Infusion rxn (shake and bake syndrome; fever and chills ) Thrombophlebitis Nephrotoxic Bone marrow suppression
38
Nystatin SE
It is not absorbed to a significant degree from skin, mucous membranes, or the gastrointestinal tract. As a result, nystatin has little toxicity.
39
Amphotercin B DDI
1. aminoglycosides, | 2. vancomycin, 3. NSAIDs, 4. cyclosporine All will increase nephrotoxic potential.
40
Azoles MOA
Inhibit ergosterol synthesis, by inhibiting α- demethylase, which demethylates lanosterol to ergosterol
41
Clotrimazole ROA
Topical | Cream lotion powder pessary
42
Miconazole ROA
Cream powder | Oral gel 2%
43
Ketoconazole ROA
Topical | Shampoo
44
Itraconazole ROA
Oral only | best absorb with food
45
Fluconazole ROA
Oral | IV
46
Voriconazole ROA
Oral (>90% absorb) | IV
47
Amphotercin B clinical application
Invasive aspergillosis Histoplasmosis Systemic candidiasis
48
Nystatin clinical application
Vaginal candidiasis
49
Imidazole are | Useful alternative to ____________
Amphotercin B for treating different systemic fungal infection
50
Clotrimazole clinical application
Clotrimazole - skin and vulvovaginal infections caused by a wide variety of fungi, including Candida.
51
Miconazole clinical application
Miconazole - tineal infections and vulvovaginal candidiasis; oral gel for thrush (alternative to nystatin)
52
Most potent triazole
Itraconazole
53
Itraconazole clinical application
Itraconazole - Trichophyton infections, Histoplasmosis,
54
Fluconazole clinical application
Fluconazole - Cryptococcosis, candidiasis in AIDS patients, vaginal candidiasis
55
Voriconazole clinical application
Voriconazole - Candidaemia; invasive aspergillosis (alternative to amphotericin B)
56
Itraconazole SE
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
Fluconazole SE
GIT disturbance Mild rash May have SJS
58
Voriconazole se
GIT disturbance Mild rash May have SJS 1. hepatitis, 2. visual disturbances: -colour perception defect, -reduced visual acuity, -photophobia.
59
Itraconazole Fluconazole DDI
Warfarin Sulphonylurea Digoxin (Both anole inhibit hepatic CYP450 enzyme) PPI Antacid H2RA (Reduce anole absorption)
60
Voriconazole DDI
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
Flucytosine MOA
Disrupt synthesis of fungal RNA and DNA
62
Caspofungin MOA
Inhibit the synthesis of β(1–3)- glucan =>disruption of the fungal cell wall and cell death.
63
Terbinafine MOA
Squalene accumulates in the cell and Inhibits squalene epoxidase which is involved in the synthesis of ergosterol from squalene.
64
Flucytosine ROA
Oral
65
Caspofungin ROA
IV
66
Terbinafine ROA
Topical - 1% cream: for treatment of dermatophytic infections. Oral – not commonly prescribed.
67
Flucytosine clinical application
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
Caspofungin Clinical application
Mucocutaneous candidiasis and candidaemia, usually in immuno-compromised patients Salvage therapy in patients with invasive aspergillosis (failed response to amphotericin B)
69
Terbinafine clinical application
Against dermatophytic infection of the skin and nails (“keratophilic”).
70
Flucytosine SE
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
Caspofungin SE
1. GIT-related symptoms, fever, histamine-like facial flushing rash, pruritus 2. thrombophlebitis 3. Foetal toxicity (Category C) - Avoid use in pregnancy.
72
Terbinafine SE
Erythema, dry skin. (These can be avoided by not using > 4 weeks).
73
Flucytosine DDI
Quinidine Causes dysthymia
74
Caspofungin DDI
1. rifampicin 2. Carbamazepine 3. cyclosporine (1), (2) are CYP 450 inducers; reduce caspofungin plasma levels Risk of hepatotoxicity