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PHARMACOLOGY - Antibiotics and Immunosuppressives > Antifungal Drugs > Flashcards

Antifungal Drugs Flashcards

1
Q

What is the method by which most anti-fungal drugs work?

- what are the two outliers and what do they do?

A
  • They produce alterations in the fungal membrane

Griseofulvin
- Mitotic Spindle Inhibitor

Flucytosine
- Antimetabolite (acts identical to 5 fluorouracile)

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2
Q

Why are antifungal drugs becoming increasingly important (3 reasons) ?

A
  • There are more and more immunocompromised people
  • Prescription of broad spectrum antibiotics also allows them to take over
  • Use of things like catheters that can move fungus from skin into the patients blood
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3
Q

What are the 3 general categories of Antifungals based on what they treat?
- how are they given

A
  1. Systemic Drugs for Systemic Infections (orally or Parenteral)
  2. Oral Drugs for mucocutaneous infections
  3. Topical drugs for mucocutaneous infections
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4
Q

What drugs are prescribed for the majority of fugal infections?
- when is they only time you would use Flucytosine?

A

Majority:

  • Amphotericin B
  • Azoles

Flucytosine is only indicated in Cryptococcal Infections

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5
Q

Why does Amphotericin B cause renal toxicity?

A
  • It acts on Ergosterols, which are similar to human sterols
  • Because it binds some human sterols it can create pores in human cells too
  • Exhibits most toxicity in the Kidney
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6
Q

What is the only administration method for Amphotericin B?

- what form is this drug put into to decrease toxicity

A

IV, putting it into micelles reduces toxicity

  • Other forms (spheres, disks, and ribbons) have been formed but are way more expensive and only allowed for limited improvement
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7
Q

What are patients treated with amphotericin B given prior to treatment to reduce adverse drug effects?

A
  • Antipyretics
  • Antihistamines
  • Meperidine
  • Corticosteroids
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8
Q

Why is anemia a long term side effect of amphotericin use?

A

Anemia is secondary to renal damage. Kidneys produce ERYTHROPOIETIN that is needed to stimulate blood cell formation.

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9
Q

Azole use may result in a pro-arrthmogenic effect. Which have been indicated to produce this effect?

A

Fluconzazole, Posaconazole, and Voriconazole

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10
Q

T or F: no azole should be given during pregnancy if at all possible

A

True, Voriconazole and Fuconazole should especially be avoided

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11
Q

What unique affect sets ketoconazoles apart from the other azoles?

A
  • Potential to cause Adrenal Insufficiency by causing adrenals to decrease corticosteriod production
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12
Q

What are some important Drug-Drug interactions of Voriconazole?

A

Cyclosporine and Tacrolimus

**This is due to its inhibitory effect on CYP3A4

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13
Q

If a patient has fungal meningitis which drugs would you most need to use?

A

Fluconazole
Voriconazole

**Both can access the CSF

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14
Q

What is the best azole drug that has been made thus far, and what are the 3 reasons for this?

A
  1. Penetrates into CSF
  2. Good oral Bioavailability
  3. Large Therapeutic Window
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15
Q

A patient has mucomycosis, what drug to you use to treat it?

A

Posaconazole - its the only drug with activity against this fungus

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16
Q

What are 3 important topical azoles?

A
  1. Clotrimazole
  2. Miconazole
  3. Nystatin
17
Q

T or F: like Flucazole, Flucytosine has a broad therapeutic window.

A

False, Flucytosine has a very narrow therapeutic window

18
Q

Which antifungals are associated with infusion reactions?

A

Amphotericin B

Echinocandins

19
Q

Antifungals associated with Bone Marrow Supression?

A 
5-Flurocytosine 
Amphotericin B (decreased erythropoetin production)
20
Q

Antifungals associated with Cutaneous photosensitivity and malignancy?

A

Voriconazole

21
Q

Antifungals associated with Photopsia?

A

Voriconazole

22
Q

Antifungals associated with CNS issues?

A

Voriconazole

23
Q

Antifungals associated with Renal Toxicity?

A

Amphotericin B

24
Q

Antifungals associated with hepatic dysfunction?

A

All Azoles
Amphotericin B
5-flurocytosine
Echinocandins

25
Q

Antifungals associated with Cardiac problems?

A

Azoles, especially in the presence of other drugs

26
Q

Antifungals associated with GI issues?

A

Itraconazole
Posaconazole
5-flurocytosine

27
Q

What are some side effects that characterize infusion reactions?

A

Chills, Fever, Flushing, Headache

28
Q

Why do azoles cause drug-drug interactions?

A

They are metabolized by CYP3A4 which is a p450 that deals with a lot of different drugs

29
Q

Why does 5-flurocytosine have such unique side effects?

- what is the cause of this?

A

5-flurocytosine is metabolized to 5-flurouricil in Fungi after it is pumped in.

  • Humans don’t have the enzyme that converts 5-flurocytosine to 5-flurouricil, but our bacteria do
  • In GI bacteria convert it so 5-flurouricil (a chemo drug)
  • Because of this we see chemotherapeutic effects of the drug, such as bone marrow suppression, and GI perturbation
30
Q

By what mechanism does resistance to Nystatin and Amphotericin arise?

A

Sterol Modification

31
Q

By what mechanism does resistance to Caspofugin and micafungin arise?

A

Altered Glucan Synthase

32
Q

By what mechanism does Flucytosine resistance arise?

A

Modifying Permease or Thymidine Synthase

33
Q

What mechanism leads to resistance to Ketoconazole, Flutoconazole, and Itraconazole?

A
  • Efflux
  • Demthylase Alteration
  • Bypass
  • overproduction
34
Q

What drug has replaced Griseofulvin in treatment of Dermatophytosis?

A

Terbinafine

35
Q

Why does Amphotericin cause cardiac dysfunction?

A

K+ doesn’t get reabsorbed in the kidney and the heart relies a lot on K+ to contract properly

36
Q

Why are antihistamines and/or hydrocortisone often given before administration of antifungals?
- which antifungals is this usually necessary for?

A

To Reduce the effects of Infusion reactions associated with Amphotericin B and Eichocandins

37
Q

What antimicrobial is notorius for giving people Red Man Syndrome?

A

Vancomycin

PHARMACOLOGY - Antibiotics and Immunosuppressives (12 decks)

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