Brainscape's Knowledge GenomeTM


Top Flashcards (Certified)
All Flashcards

Pharmacology > Exam 3: Antifungals > Flashcards

Exam 3: Antifungals Flashcards

(46 cards)

Start Studying
1
Q

What is the MOA of antifungals and what are the two exceptions to this?

A

They target the cell membrane or cell wall, except for Griseofulvin and Flucytosine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

What is Amphotericin B produced by?

A

Streptomyces Nodosus

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

What is the MOA of amphotericin B?

A

Interaction with sterol of fungal membrane, ergosterol, that results in the loss of intracellular components through depolarization and pore formation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

What is the spectrum of Amphotericin B. Is it fungicidal or static?

A

Broad spectrum.

Fungicidal

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

What is the DOC for most systemic fungal infections?

A

Amphotericin B

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

What is the likely cause of the toxicities of amphotericin?

A

It binds to human membrane sterols as well as fungal sterols.
Due to either
1) Infusion of drug
2) Reactions occurring over time

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

What are the infusion related toxicities of Amphotericin B?

A

Immediate.

Chills, fever, muscle spasms, headache, vomiting. May occur with each injection and can be lessened by slowing the infusion rate or decreasing daily dose

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

What are the toxicities that occur from reactions over time with Amphotericin B?

A
  • Powerful nephrotoxicity agent (dose dependent and can cause irreversible kidney damage)
  • Azotemia (BUN and creatinine elevated)
  • Hepatic failure
  • Hypersensitivity
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

What is the MOA of Flucytosine?

A

Flucytosine is converted to 5- fluorouracil which interferes with fungal DNA and RNA synthesis

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

What is the spectrum of Flucytosine?

A

Lower than amphotericin B, used for cryptococcus neoformans, some strains of candida, aspergillosis fumigatus, etc.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

What is the DOC for crytococcus infections?

A

Flucytosine plus amphotericin B (significant synergistic effect)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Does Amphotericin B or Flucytosine have better CSF penetration?

A

Flucytosine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

What are the toxicities of Flucytosine?

A

Depression of bone marrow, GI disturbace, elevated ALT/AST

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

What is the MOA of the “-azoles”?

Static or cidal?

A

Inhibits synthesis of ergosterol, leads to depletion of ergosterol and accumulation of toxic sterols causing increased permeability and inhibition of fungal growth.

Fungistatic

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

What is the spectrum of ketoconazole?

A

Broad spectrum antifungals

Poor CNS penetration

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

What are the toxicities associated with ketoconazole?

A
  • Potent inhibitor of P450s, drug interactions
  • Gynecomastia and impotence due to inhibition of adrenal and testicular function
  • Prolonged QT
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

What are the contraindications of Ketoconazole?

A

Hepatic disease

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

Why is fluconazole used in Fungal meningitis?

A

It penetrates well into body fluids, particularly CSF where drug concentration reaches 50-90%

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

What are the toxicities associated with Fluconazole?

Study These Flashcards
A
  • Less toxic than amphotericin B or Flucytosine and better tolerated than Ketoconazole
  • Less drug interactions, but potent inhibitor of CYP2C9
  • Headache
20
Q

What is used for suppressive therapy and/or prophylactic therapy in HIV+ patients?

21
Q

How is fluconazole administered?

22
Q

How is Ketoconazole administered?

Study These Flashcards
A

Oral, or available in shampoos and creams

23
Q

How is Voriconazole administed?

24
Q

What is the DOC for Aspergillus?

Study These Flashcards
A

Voriconazole and amphotericin B

25
What are the toxicities associated with Voriconazole?
-Drug interactions (potent inhibitor of P450s) -Genetic polymorphism of CYP2C19 Extensive metabolizer results in low drug concentration Poor metabolizer results in high drug concentration -Reversible visual impairment
26
What is the spectrum of Itraconazole?
Active against many of the same fungi as ketoconazole and fluconazole, but has greater activity against Apergillus (but not DOC!)
27
What are the toxicities associated with Itraconazole?
- Drug interactions (potent inhibitor of CYP34A) | - GI effects
28
How is itraconazole administered?
Oral or IM
29
How does Itraconazole bioavailability change when taken via capsule and oral solution?
- Capsules: 40-50% if administered on empty stomach, 90-100 when administered with meal - Oral solution: 55% under fed conditions, increases to 72% under fasting
30
What is the spectrum for Isavuconazonium?
Indicated for the treatment of Mucormycosis and invasive aspergillosis
31
What are the toxicities associated with Isavuconazonium?
- Drug interactions (moderate inhibitor of CYP3A4) - Nephrotoxicity - Decrease in the QT interval
32
What are the contraindications of Isavuconazonium?
Patients with familial short QT syndrome
33
What is the spectrum for Posaconazole?
Indicated for the treatment of Apergillus and candida
34
What are the toxicites associated with Posaconazole?
- Drug interactions (potent inhibitor of CYP3A4) | - GI upset, stomatitis, vaginal bleeding, hypokalemia, and thrombocytopenia
35
What are the 3 drugs in the Echinocandins class?
Caspofungin, Micafungin, and Andulafungin
36
What makes Caspofungin a good treatment option for Apergillosis?
Lack of nephrotoxicity and few drug interactions
37
How is caspofungin administered?
IV slow infusion
38
What is the MOA of Griseofulvin? Is it cidal or static?
Binds to the microtubules of certain fungi. It binds specifically to keratin and prevents infection in new skin. Fungistatic
39
What is the DOC for onychomycosis?
Griseofulvin
40
What are the contraindications for griseofulvin?
- Acute intermittent porphyria - Hepatocellular failure - Pregnancy and men 6 months prior to fathering a child
41
What are the toxicites associated with griseofulvin?
GI upset, headache*, disulfiram like effects, hematological disturbances, rashes, photosensitivity, etc
42
What is the MOA of Terbinafine? Is it cidal or static?
Interferes with sterol biosynthesis, inhibits squalene monooxygenase, build up of squalene is toxic to fungi. Fungicidal
43
What is terbinafine used to treat?
Less active against candida, but effective for onychomycosis (not DOC).
44
What is nystatin used for?
Potent antibiotic used for candidal infections.
45
How is nystatin administered?
Orally for GI candida infections and topically for other candida infections
46
What is efinaconazole used for? How it it administered?
Onychomycosis of the toenail caused by trichophyton rubrum and trichophyton mentagrophytes Topical

Pharmacology (25 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2025 Bold Learning Solutions. Terms and Conditions