Antifungal medications Flashcards

1
Q

What is the MoA of Amphotericin B?

A

Binds to ergosterol of fungal PM and alters membrane permeability, causing cell lysis

Can be fungistatic or fungicidal

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2
Q

How is Amphotericin B distributed?

A

Has poor CSF penetration

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3
Q

What are the ADRs of amphotericin B?

A

Nephrotoxicity

Anemia

Systemic: shaking, chills, fever, myalgias

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4
Q

What is the potential benefit of Amphotericin Lipid formulations?

A

Lower incidence of nephrotoxicity

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5
Q

What is the MoA of 5-Fluocytosine?

A

Penetrates fungal cell where it is deaminated by a fungus specifi enzyme

Inhibits pyrimidine metabolism an ultimately RNA and protein synthesis

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6
Q

How does FLuorocytosine distribute?

A

60-100% CSF penetration

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7
Q

What are the ADRs of 5-Fluocytosine?

A

Bone marrow hypoplasia

More common in prolonged therapy

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8
Q

What is the MoA of Azole products?

A

Interfere with fungal cytochrome P450 enzymes responsible for ergosterol production

Fungistatic or fungicidal

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9
Q

What are the ADRs of azole antifungals?

A

N/V

Hepatitis

Increases aminotransferases

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10
Q

What ADR is specific to Ketoconazole?

A

Dose dependent depression of serum testosterone and ACH

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11
Q

What are the drug interactions for azole antifungals?

A

Antacids, PPIs and H2 antagonists

Cyclosporin

Warfarin

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12
Q

Describe the absorption of Ketoconazole.

A

Rapidly absorbed from GI tract

pH dependent bioavailability (increased pH, decreased absorption)

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13
Q

Describe the absorption and distribution of Fluconazole.

A

Rapidly absorbed from GI tract

Widely distributed, readily into CSF

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14
Q

How is Fluconazole eliminated?

A

Renal, 60-80% unchanged in urine

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15
Q

How is Itraconazole distributed?

A

Widely distributed

Poorly into CSF

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16
Q

How is Itraconazole used in therapy?

A

Effective for oral therapy of histo/blasto

Useful for aspergillosis

17
Q

How is Voriconazole absorbed and distributed?

A

GI, decreased by high fat meals

40-70% in CSF

18
Q

How is voriconazole eliminated?

A

Metabolized in liver

Interacts with CYP3A4

19
Q

How is voriconazole used in therapy?

A

Invasive aspergillosis and Fusarium spp.

Candidiasis

20
Q

What is the use of Posaconazole?

A

Candida and Aspergillus infection in immunocompromised patients

Inhibits CYP3A4

21
Q

What is the MoA of Caspofungin acetate?

A

Echinocandin - blockes fungal cell wall synthesis

Glucan synthesis inhibitor

22
Q

What is Caspofungin acetate used for?

A

Candidiasis

Invasive aspergillosis

23
Q

What are the ADRs of Caspofungin acetate?

A

Phlebitis, headache, fever

Increased LFTs, SrCr

24
Q

What is the MoA of Griseofulvin?

A

Disrupts the cells mitotic spindle structure

25
Q

What is the use of Griseofulvin?

A

Dermatophytosis

26
Q

What are the ADRs of Griseofulvin?

A

NVD

Hypersensitivity

Hepato/Nephrotoxicity

Headace

CYP3A4 inducer

27
Q

What is the MoA of Terbinafine?

A

Synthetic allylamine derivative

Inhibits squalene epoxidase

28
Q

What are the ADRs of Terbinafine?

A

Hypersensitivity/Rash - erythema multiforme, toxic epidermal necrolysis

Liver enzyme abnormalities

Headache

29
Q

What are the drug interactions with Terbinafine?

A

Cimetidine - T clearance decreased

Rifampin - T clearance increased

Cyclosporin - increased clearance

Warfarin

30
Q

What is Terbinafine used for?

A

Onychomycosis

Consider ADRs

31
Q

What are the treatments of oral candidiasis?

A

Nystatin - oral suspension

Clotrimazole troches

Amphotericin B