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Flashcards in AntiFungals Deck (74)
1

Polyenes

Ampthotercin B, Nystatin

2

Ampho B- MOA

Binds egosterol to disrupt fungal membrane

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Ampho-B role of deoxycholate

Must be compexed to deoxycholate for solubitliy

4

Ampo- B- admin

IV, Intrathecally, bladder wash

5

Ampo B - uses

Systemic fungal infections

6

Ampo-B-AE

Attacks renal cells and RBC's, K, Mg, HCO3 wasting- hydrate and monitor, Infusion related- fever, chills, riggor, hypotenstion, myalgia, arthralgia, HA- premedicate with APAP, NSAIDS and others Thrombophlebitis- prevent with heparin. Amenia- suppresses EPO

7

Ampho-B- newer preps

Better formulations dec nephrotoxicity and allow larger doses BUT don't do anything for rigor and infusion rxnmuch more expensive

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Nystatin- MOA

binds to ergosterol and disrupts membrane

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Nystatin- Uses

oral, vaginal, skin candidiasis

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Nystatin- Admin

topical swish and swallow not orally absorbed

11

Nystatin- AE

not many

12

Pyrimidines

Flucytosine

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Flucytosine- MOA

Flucytosine --> 5- Flurouridylic acid via cytosine deaminase--> inhibits translation, 5- Flurodeoxyuridylic acid --> inhibits thymylate synthase --> inhibits DNA synthesis

14

Flucytosine- Uses

used with Amphoteracin B for cryptococcal meningitis, Never use alone, resistance develops to quickly

15

Flucytosinse- administration

Oral

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Flucytosine- distribution

well absorbed orally

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Flucytosine- 1/2 life

3-6 hrs

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Flucytosine- Excretion

Renal

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Flucytosine- AE

Bone marrow suppression GI- N/V/D. Livertoxicity- reversible

20

Echinocandins

Caspofugin, Micafugin, Andidafugin

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Echinocandins- MOA

inhibit beta 1,3 glucan synthesis- inhibit cell wall production

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Echinocandins- Admin

IV

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Echninocandins- uses

systemic Candida or Apergillus infections

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Echinocandins - drug interactions

Cyclosporine inc blood levels of Caspofugin

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Echinocandins- Protein binding

Highly protein bound

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Echinocandins- CNS penetration

Minimal

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Echinocandins- AE

Histamine related rxns- warmth, swelling, rash, Headache, Hepatotoxicity

28

Griseofluvin- MOA

Inhibits mitotic spindle formation. Binds to human keratin which prevents invasion of fungus. Infected cells slough off eventually non-infected keratinocytes at the basal layer eventually replace

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Griseofluvin- Admin

Oral- best with fatty foods

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Griseofluvin- uses

Fungal infections of: Hair, skin, and nails

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Griseofluvin- 1/2 life

1 day

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Griseofluvin- Excretion

Renal

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Griseofluvin- AE

Headache, Hepatotoxicity, Neuro/leuckopenia, basophilia, photosensitivity, GI, Rash

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Griseofluvin- Effect on enzymes

Inducer

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Griseofluvin- Drug interactions

Inc metabolism of Warfarin and Oral contraceptives

36

Terbinafine- MOA

binds squalene epoxidase --> inhibits ergosterol synthesis

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Terbinafine- Admin

Oral

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Terbinafine- Uses

Mycoses of nails, drug accumulates in the nail beds

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Terbinafine- T 1/2

400 hrs b/c accumulates in hair, skin, and fat and slowly releases

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Terbinafine- Protein binding

High

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Terbinafine- AE

Well tolerated. Uncommon AE- GI, hepatatoxicity, stevents Johnson syndrome

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Terbinafine- drug interactions

Cimetidine- increases levels of Terbinafine

43

Azoles- Types

Imidazoles, Triazoles

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Imidazoles

Ketoconazole, Clotrimazole, Miconazole, Econazole, Butoconazole, Oxiconazole

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Imidazoles- Admin

All topical except Ketoconazole which is for systemic

46

Triazoles

Terconazole, Itraconazole, Fluconazole, Voriconazole, Poscanzole

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Triazoles- Admin

All systemic except for Terconazole which is topical

48

Azoles- MOA

bind 14 alpha demethylase --> inhibit ergosterol synthesis

49

Azoles- CYP450

inhibitors

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Azoles- Uses

Mostly, topical, but some systemic. Superficial infections- ringworm, candidiasis, tinea versicolor/ nigra, fungal keratitis. NOT FOR NAIL/HAIR-THOSE REQ SYSTEMIC

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Ketoconazole- Admin

Oral. Require acidic environment for absorption. Drugs that inhibit acidity in the stomach dec absorption (Histamine2 and PPI)

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Ketoconazole- CYP450

Inhibitor Inc levels of other drugs

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Ketoconazole- AE- hormonal effects

Hormonal due to CYP450 inhib- dec libido, gynecomastia, menstral irregularities. Blocks androgen, cortisol, aldosterone syntehsis and adronergic receptor antagonist

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Ketoconazole- AE- non hormonal

GI- dose dependent rash, hepatotoxicity

55

Itracanazole- Admin

Oral, IV

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Itraconazole- Uses

Candida, Aspergillus

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Itraconazole- absorption

GI absorption- empty stomach and acid

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Iraconazole- AE

GI, Rash, LFTs. hypoTG, Hypokalemia

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Itraconazole- drug interactions

Fatal arrhythmia if given with cisapride or quinidine

60

Intriconazole- Liver enzyme

Potent CYP3A4 inhibitor

61

Fluconazole- Admin

Oral, IV

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Fluconazole- Use

Candida

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Fluconazole- absorption

not affected by food

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Fluconazole- AE

Reversible alopecia, GI, Rash, LFTs

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Fluconazole- Contraindications

Pregnancy- results in fatal skeletal and cardiac muscle deformities

66

Voricaonazole- Admin

Oral, IV

67

Voriconazole- Uses

Candida, Aspergillus

68

Voriconazole- t1/2

variable- dependson drug concentration, non linear kinetics

69

Voriconazole- liver enzymes

Potent CYP3A4 inhibitor--> drug interactions

70

Voriconazole- AE

Visual changes, Cardiovascular, CNS, Rash, LFTs

71

Posconazole- admin

Oral- w/full meals

72

Posconazole- Uses

Candida, Apergillus, Zygomycetes

73

Posconazole- liver enzymes

CYP3A4- moderate inhibitor

74

Posconazole- AE

Cardiovacular- HTN, hpokalemia. CNS- headache, dizziness. GI, LFTs