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CPR Exam 1 > Anti-Fungal/TB/Influenza Drugs > Flashcards

Anti-Fungal/TB/Influenza Drugs Flashcards

1
Q

What is Amphotericin B’s MOA?

A

Binds to Ergosterol on Fungal cells but not human cells, forms pore in fungal plasma membrane causing intracellular leakage

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2
Q

What Anti-Fungal has the broadest spectrum of action, but also the most adverse effects?

A

Amphotericin B

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3
Q

What are the mechanisms of Resistance to Amphotericin B?

A

Anything that could disrupt Amphotericin B’s binding to ergosterol

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4
Q

How is Amphotericin B administered?

A

Amphotericin B is administered IV as it has poor GI absorption and oral administration is only effective if the fungal infection is in the gut

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5
Q

How does Amphotericin B cause side effects?

What are some of its side effects?

A

Amphotericin B may cause side effects by binding to human membrane sterols instead of ergosterol.

Side effects may include, fever, myalgias, chills, HA, vomiting, Hypotension, Muscle spasms, and Renal Damage. Chronically may lead to anemia, seizures

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6
Q

What is Flucytosine’s MOA?

A

Flucytosine is taken up by fungal cells, converted into 5-FU intracellularly and then subsequently to FdUMP and FUTP.

FdUMP inhibits DNA synthesis
FUTP inhibits RNA Synthesis

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7
Q

What is the spectrum of action of Flucytosine?

A

Flucytosine is effective against:
C. Neoformans
Candida spp.

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8
Q

What is the mechanism of resistance against Flucytosine?

A

Altered metabolism is thee means of gaining resistance against Flucytosine

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9
Q

How is Flucytosine administered?

A

Flucytosine is administered orally

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10
Q

How may Flucytosine cause side effects?

What are some of the side effects Flucytosine may cause?

A

Flucytosine may be accidentally converted to the chemotherapeutic agent 5-FU outside of fungal cells.

Side effects may include:
Bone marrow toxicity with anemia, leukopenia, thrombocytopenia
Less commonly, liver enzyme issues

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11
Q

What are the two classes of Azoles?

A

Imidazoles

Triazoles

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12
Q

What is the one Imidazole we discussed?

A

Ketoconazole

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13
Q

What are the 4 Triazoles we discussed?

A

Itraconazole
Fluconazole
Voriconazole
Posaconazole

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14
Q

What class of Anti-Fungal Drugs are the most well-tolerate of all Anti-Fungal Drugs?

A

The Azoles are the most well-tolerated Anti-Fungals

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15
Q

What is the most well-tolerated Azole?

A

Fluconazole is the most well-tolerated Azole.

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16
Q

What is the MOA of the Azoles?

A

Azoles Inhibit Fungal Cytochrome P450 enzymes, leading to decreased ergosterol production

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17
Q

What is the mechanism of gaining resistance against Azoles?

A

Upregulation of Fungal Cytochrome P450 Enzymes will lead to resistance against Azoles

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18
Q

What is unique about the adverse effects of Azoles?

What side effects may you get?

A

Azoles are generally well tolerated, non-toxic, and have few side effects.

Side effects may include:
Minor GI Upsets, Liver Enzyme abnormalities, Drug interactions possible due to interactions with Human CYP450

19
Q

Which Azole is least specific for Fungal CYP450 and may have greater effect on human CYP450’s?

A

Ketoconazole

20
Q

Which Azole is the drug of choice for treating Aspergillus spp.?

A

Voriconazole is the drug of choice fro treating Aspergillus spp.

21
Q

What spectrum of problems is Fluconazole most commonly used for?

A

Fluconazole is the drug of choice for treatment and prophylaxis for Cryptococcal Meningitis, and is most commonly used for the treatment of Mucocutaneous candidiasis

NO ACTIVITY ON ASPERGILLUS

22
Q

Which human CYP does Voriconazole often inhibit?

A

CYP3A4 (Statins)

23
Q

What are some of the side effects you might see with Voriconazole specifically?

A 
Side effects of Voriconazole may include:
Rash
Elevated Hepatic Enzymes
Visual Disturbances 
photosensitivity dermatitis
24
Q

What is the spectrum of action for Voriconazole?

A

Drug of choice for Aspergillus spp.
Candida krusei
Dimorphic fungi

25
Q

What is the only Azole with significant activity against Mucormycosis?

A

Posaconazole

26
Q

What is the newest Azole?

What are its uses?

A

Posaconazole

Mucormycosis
Prophylaxis for bone marrow transplants, induction of chemotherapy
Salvage therapy for invasive Aspergillus

27
Q

What is the MOA of Echinocandins?

A

Echinocandins work by destabilizing the fungal cell wall via inhibition of Glucan Synthase, causing decreased beta1-3 glucan synthesis

28
Q

What are the 3 Echinocandins we discussed?

A

Caspofungin
Micafungin
Anidulafungin

29
Q

What are the side effects of Echinocandins? How are they tolerated?

A

Echinocandins are well tolerated

Side effects may include:

  • Minor GI Symptoms
  • Flushing
30
Q

How is resistance to Echinocandins gained?

A

Resistant to Echinocandins is gained by the gain of a point mutation in Glucan Synthase

31
Q

How are Echinocandins Administered?

A

IV

32
Q

Oseltamivir

A

Oral Administration
Prodrug activated by hepatic Esterase
Side effects include N/V, HA, Diarrhea, Fatigue

33
Q

Zanamivir

A

Administered directly to respiratory tract via inhalation. Not recommended for patients with underlying airways disease

Side Effects - cough, bronchospasm, nasal and throat discomfort, reversible decrease in pulmonary function.

34
Q

Peramivir

A

Administered as a single dose IV treatment for Acute, Uncomplicated Influenza in adults

Side Effects - Diarrhea, Skin or HSN Rxn’s

35
Q

What are the 2 Adamantanes we discussed?

A

Amantadine

Rimantadine

36
Q

What is the MOA of Adamantanes?

A

Adamantanes function by blocking the M2 Proton Ion channel of the virus particle, leading to an Inhibition in the uncoating of Viral RNA, and induces conformational changes in Hemagglutinin

37
Q

What types of Influenza do Neuraminidase Inhibitors work on?

A

They function w/ both Influenza A and B strains

38
Q

What strains of Influenza do Adamantanes work on?

A

Adamantanes work against Influenza A

39
Q

What resistance is there to Neuraminidase Inhibitors?

A

Resistance to Neuraminidase Inhibitors is rare

40
Q

What is the Resistances to Adamantanes?

A

There are high rates of Adamantanes Resistance in H1N1 and H3N2

41
Q

How are Adamantanes administered?

How commonly are they used?

A

Adamantanes are administered orally, they are not commonly used in the treatment or prevention of Influenza

42
Q

What are the Adverse effects of Adamantanes?

A

Adamantanes Side effects include:
- nausea, anorexia, nervousness, difficulty in concentrating, insomnia, light-headedness, and birth defects have been noted following exposure during pregnancy

43
Q

What are the most active, first-line drugs used to treat TB?

A

Rifampin

Isoniazid

CPR Exam 1 (9 decks)

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