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PHARMACOLOGY (2nd year) > ANTIFUNGAL DRUGS > Flashcards

ANTIFUNGAL DRUGS Flashcards

1
Q

• Produced by Streptomyces nodosus
• Highly effective, a mainstay, in serious invasive & deep-
seated infections
• Toxicto kidneys - many side effects or adverse drug reactions

A

AMPHOTERICIN B

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2
Q

• Amphoteric polyene (many double bonds) macrolide (containing a large lactone ring of ≥ 12 atoms)
• Nearly insoluble in water
• Conventionally, the first preparation is as a colloidal
suspension of AmB + Na deoxycholate for IV injection

A

AMPHOTERICIN B

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3
Q

Advantages:
• ↑ daily dose of parent drug
• ↑ tissue conc. in the RE organs
• ↓ infusion related side effects
• Marked ↓ in nephrotoxicity

A

• Amphotericin B Liposomal (L-AmB)
• Amphotericin B Cholesteryl Sulfate
• Amphotericin B Lipid Complex (ABLC)

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4
Q

• Poorly absorbed from GIT
• Oral AmB
- Only used for luminal fungi
- Not for systemic disease

A

AMPHOTERICIN B

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5
Q

• Wide tissue distribution
• Unfortunately, only 2-3% penetrates CSF
- Need intrathecal

A

AMPHOTERICIN B

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6
Q

• Mode of Action:
- Affinity for ergosterol found in fungi cell membrane →→
pore formation → leakage of IC ions & macromolecules →
cell death

A

AMPHOTERICIN B

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7
Q

• Broadest spectrum of action. Fungicidal.

A

AmB ANTIFUNGAL ACTIVITY & CLINICAL USES

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8
Q

• Often used as induction therapy to rapidly reduce fungal burden (then replaced by newer azole drugs for chronic Tx or relapse prevention)

A

AmB ANTIFUNGAL ACTIVITY & CLINICAL USES

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9
Q

Adverse effects of AmB

A

Infusion Related Toxicity – immediate

Cumulative Toxicity – slow occurring

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10
Q

● Immediate/Rapid
● Nearly universal
○ Fever, chills, muscle spasms, vomiting, headache, low BP might manifest while infusing AmB
● Ameliorated by slowing down or low infusion rate or low daily dose
● Premedication with antipyretics, antihistamines, Meperidine, corticosteroids
● Test dose of 1 mg IV to gauge severity of reaction

A

INFUSION RELATED TOXICITY

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11
Q

Slow occurring
● More serious AE
● Renal damage or nephrotoxicity most significant and in almost all patients
○ Variable azotemia
- Azotemia: increase in BUN and
creatinine
- can be stabilized or will need renal
replacement therapy like dialysis
● Reversible: low renal perfusion (prerenal)
● Irreversible component:
○ AmB is very notorious for Tubular
injury associated with prolonged Tx (>4 grams cumulative dose)

A

CUMULATIVE TOXICITY

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12
Q

increase in BUN and creatinine

A

AZOTEMIA

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13
Q

Water soluble pyrimidine analog related to
5-Fluorouracil (5-FU) used for treating cancer.

A

FLU(ORO)CYTOSINE

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14
Q

Exhibit synergism with AmB and Itraconazole for
CNS Fungal Infection.

A

FLU(ORO)CYTOSINE

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15
Q
  1. Mainly used for CNS Infections
    2.Cryptococcal meningitis Cryptococcus
    neoformans(COMBINED WITH AMP B)
  2. UTI (IF RESISTANT TO FLUCONAZOLE)
A

FLU(ORO)CYTOSINE

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16
Q

FLU(ORO)CYTOSINE
ADVERSE EFFECTS

A
  1. Bone marrow depression
    - Anemia
    - Leukopenia
    - Thrombocytopenia
  2. Liver enzyme derangement
  3. GIT disturbances
    - Toxic enterocolitis
    NARROW THERAPEUTIC WINDOW
17
Q
  1. Broadest spectrum of action among antifungals
    a. Amphotericin B
    b. Fluorocytosine
    c. Fluorouracil
    d. None of the above
18
Q

T/F. Fluorocytosine is poorly absorbed in the GIT, hence it is given via injection.

19
Q

Can cause tubular injury as its adverse effect
a. Amphotericin B
b. Fluorocytosine
c. Fluorouracil
d. Itraconazole

20
Q

T/F. Fluorocytosine is widely distributed in the body fluid compartments including the CSF

21
Q

Fluorocytosine has a synergistic effect with this drug in the treatment of Chromoblastomycosis
a. AmB
b. 5FU
c. Fluconazole
d. Itraconazole

22
Q

Based on chemical structure, which among the drugs is not classified as triazole?
a. Voriconazole
b. Fluconazole
c. Posaconazole
d. Sulconazole

23
Q

What is the microbial source of Amphotericin B?
a. Streptomyces natalenis
b. Streptomyces nodosus
c. Streptomyces noursei
d. Streptomyces niveus

A

b. Streptomyces nodosus

24
Q

Which is not an advantage of lipid formula AmB
a. Increase daily dose of parent drug
b. Increase tissue concentration in
reticuloendothelial (RE) organs
c. Decrease infusion-related side effects
d. Marked increase in nephrotoxicity

A

d. Marked increase in nephrotoxicity

25
Q

T/F. Even now with the advent of newer antifungal agents, amphotericin B is still highly effective, and a mainstay in serious invasive & deep-seated infections.

26
Q

T/F. Cryptococcus is the most common cause of fungal infections in HIV and immunocompromised patients.

27
Q

Ketoconazole
Econazole
Clotrimazole
Butoconazole
Miconazole
Sulconazole

A

KEC-BMS

IMIDAZOLE
(AZOLE)

28
Q

I-V-F-P
Itraconazole
Voriconazole
Fluconazole
Posaconazole

A

*TRIAZOLE (AZOLE)

29
Q

POLYENE ANTIBIOTIC (oldest AmB)

A

Amphotericin B Nystatin

30
Q

ECHINOCANDIN
(most recent AmB)

A

Caspofungin
Micafungin
Anidulafungin

PHARMACOLOGY (2nd year) (16 decks)

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