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Lung Pharm > Stauginger Fungal > Flashcards

Stauginger Fungal Flashcards

1
Q

What drug contains 50 mg of amphotericin B intercalated into a liposomal
membrane consisting of:

  1. 213 mg hydrogenated soy phosphatidylcholine
  2. 2 mg cholesterol
  3. 84 mg distearoylphosphatidylglycerol
  4. 0.64 mg alpha tocopherol
  5. 900 mg sucrose
  6. 27 mg disodium succinate hexahydrate
A

AmBisome

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2
Q

A macrocyclic-polyenes-antifungal antibiotic drug produced from a strain of Streptomyces nodosus

A

Amphotericin B

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3
Q

This drug acts by binding to the sterol component of a cell membrane leading to alterations in cell permeability and cell death and has a high affinity for the ergosterol component of fungal cell membrane

A

Amphotericin B

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4
Q

This drug can bind to the cholesterol component of the mammalian cell and can leads to cytotoxicity

In particular, this drug can be very nephrotoxic!!!

A

Amphotericin B

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5
Q

What can be used to treat Cryptococcus neoformans and Blastomyces dermatitidis?

(also Aspergillus and Candida)

A

Amphotericin B

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6
Q

Amphotericin B is indicated in ..?

A
  1. Cryptococcus neoformans
  2. Blastomyces dermatitidis

(also aspergillum and candida)

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7
Q

What type of drug is amphotericin B?

A

polyene

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8
Q

What can Amphotericin B overdose cause?

A

fatal cardiac arrest

fatal cardiopulmonary arrest

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9
Q

What adverse reaction has been reported with Amphoceterin B?

A

Anaphylaxis… closely monitor initial dosing

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10
Q

Amphoceterin B can have nephrotoxic effects with which drugs?

A
  1. Aminoglycosides
  2. Cyclosporine
  3. Antineoplastic agents (cisplatin, nitrogen mustard compounds)

ACA

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11
Q

Which is more nephrotoxic, amphotericin B deoxycholate or Ambisome?

A

amphotericin B deoxycholate

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12
Q

Should Amphotericin B be used primarily for treating patients with life threatening fungal infections or non-invasive forms of fungal infections such as oral thrush, esophageal or vaginal candidiasis in patients with normal neutrophil counts?

A
  • used primarily for treating patients with life threatening fungal infections
  • NOT for non-invasive forms of fungal infections
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13
Q

What happens if amphoceterin B is mixed with skeletal muscle relaxants and digitalis glycosides?

A

hypokalemia may be exaggerated

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14
Q

Amphotericin B may increase the toxicity of what drug?

A

flucytosine

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15
Q

Fluconazole, itraconazole, econazole, terconazole, butoconazole, and tioconazole are what class of drug?

A

Azole

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16
Q

What drug is active against fluconazole-resistant strains of Candida?

A

Newer triazoles such as Vorivonazole, posaconazole, ravuconazole

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17
Q

What is Vorivonazole?

A

Newer triazole Active against fluconazole-resistant strains of Candida

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18
Q

What drug mechanism of action, involves interruption of the conversion of lanosterol to ergosterol via binding to fungal cytochrome P-450 and subsequent disruption of fungal membranes?

A

Fluconazole - this is MOA of other Azoles too

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19
Q

What azole drug is indicated in the tx of
-Candida UTI/Peritonitis

-Vaginal candidiasis

-Oropharyngeal and
esophageal candidiasis (thrush),
  • Cryptococcal meningitis
  • Prophylaxis of candidiasis with bone marrow transplant
A

Fluconazole

20
Q 
If someone is taking a drug that is known to prolong the QT interval and is metabolized via the enzyme CYP3A4 such as:
pimozide,
astemizole, 
cisapride
erythromycin
quinidine
(PACE Q)
What anti fungal should NOT be given?
A

Fluconazole

21
Q

What drug is contraindicated for co-administration with fluconazole based on multple dose interaction study?

A

terfenadine

  • patients on multiple doses of 400 mg/day or higher of fluconazole should not take terfenadine at the same time
22
Q

Your patient is pregnant with a fungal infection, can she take fluconazole?

A
  • FDA says no- can cause serious and specific birth defects

- no adequate controlled trials though

23
Q

How does Fluconazole cause QT prolongation?

A

inhibition of Rectifier Potassium Channel current

24
Q

What can amplify QT prolongation in patients on fluconazole?

A
  • The QT prolongation (torsade de pointes) caused by other medicinal products (such as amiodarone) may be amplified via the inhibition of cytochrome P450 (CYP) 3A4
  • Erythromycin +fluconazole can amplify torsades (sudden heart death can occur
  • Hypokalemia and cardiac failure patients are at increased risk for life threatening ventricular arrhythmias and torsades
25
Q

What do azole antifungals inhibit?

A

Azole antifungals also are both substrates and inhibitors of the cytochrome P450 family CYP3A4

26
Q

Use of azoles with what drugs can increase serum concentration of those drug?

A

Concomitant use of azoles increases the concentration of…

  1. serum concentrations of calcium channel blockers
  2. immunosuppressants, chemotherapeutic drugs
  3. benzodiazepines
  4. tricyclic antidepressants
  5. macrolides
  6. SSRIs

leads to potentially serious and lethal drug-drug interactions

27
Q

What is MOA of itraconazole?

A

interrupts conversion of lanosterol to ergosterol via binding to fungal cytochrome P-450 and subsequent disruption of fungal membranes

28
Q

How can you increase the absorption of itraconazole?

A

take it with food and a high acidic beverage. -> acid increases its absorption

29
Q

What drug has a black box warning for pts with heart failure due to its inotropic effects?

A

Itraconazole

30
Q

What metabolizes itraconazole?

A

cytochrome P450 3A4 isoenzyme system (CYP3A4),

31
Q

What azole has activity against

  1. Aspergillus,
  2. Dematiaceous mold
  3. Sporothrix Schenckii
A

Itraconazole

32
Q

What is the MOA of Voriconazole?

A

interruption of the demethylation of 14-a-lanosterol in the conversion to ergosterol via binding to fungal cytochrome P-450 and subsequent disruption of fungal membranes

33
Q

A patient has

  • non stop N/V
  • loss of appetite
  • stomach/abdominal pain
  • yellowing eyes/skin
  • dark urine

What antifungal could they be taking?

A

Itraconazole can cause fatal liver disease

34
Q

Patients with Hereditary Galactose Intolerance, Lapp Lactase Deficiency or Glucose- Galactose Malabsorption should not take what drug? Why?

A

Voriconazole, it contains lactose

35
Q

What enzyme does oral voriconazole have the greatest affinity for? does it affect kidneys?

A

CYP2C19

  • oral voriconazole is not affected by renal failure
36
Q

What should you consider with parenteral voriconazole?

A

the parenteral preparation is solubilized in a compound that is secreted by the kidneys

use dose adaptation in cases of renal impairment

37
Q

Caspofungin, micagugin, and anidulafugin are what drug class?

A

Echinocandins

38
Q

What are Echinocandins used for?

A
  • The drugs in this class include caspofungin, micafungin and anidulafungin
  • Approved for IV use in systemic Candida infections
39
Q

What drug class is semisynthetic, cyclic lipopeptides with an N-linked acyl lipid?

A

Echinocandins (caspofungin, micafungin and anidulafungin)

40
Q

What echinocandin is indicated in tx of candidemia, acute disseminated candidiasis, candida peritonitis, and absess?

A

Micafungin (echinocandin class)

41
Q

What is used for prophylaxis of candida infections in patients undergoing hematopoietic stem cell transplant?

A

Micafungin (echinocandin class)

42
Q

What drug class can cause red man syndrome from histamine?

A

Echinocandins

43
Q

Who has a black box warning against micafungin? why?

A

European medical agency has BBW for micafugin

  • caused foci of altered hepatocyte after tx period > 3 months in rats
44
Q

What drug is a pyramidine analogue against fungal species that interferes with purine and pyrimidine metabolism?

A

Flucytosine

45
Q

What drug has a black box warning for extreme caution in bone marrow depression, hepatic impairment, renal impairment and is contraindicated in pregnancy and breast feeding

A

Flucytosine

46
Q

What drug class inhibits glucan synthase for fungal cell wall?

A

Echinocandins

47
Q

What drug is used with liposomal amphoceterin B for cryptococcal meningitis tx?

A

flucytosine

Lung Pharm (5 decks)

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