LEC 2 - Antifungals Flashcards

(66 cards)

1
Q

What are the three categories of a fungal disease?

A

Superficial
Subcutaneous
Systemic

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2
Q

What is involved in a systemic fungal infection?

A

Normally start in the lungs

Then spreads to other organs

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3
Q

What is involved in a subcutaneous fungal infection?

A

Dermis
Subcutaneous tissues
Occasionally adjacent

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4
Q

What is involved in a superficial fungal infection?

A

Skin
Other keratinized structures
Mucous membranes

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5
Q

Are most antifungals -cidal or -static?

A

Fungistatic

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6
Q

What is clearance of a fungus in a host most dependent?

A

Host’s response to the presence of the fungus

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7
Q

When is clearance in a host unlikely in regards to a fungus?

A

Immunosuppressed animals

Primary/Secondary immunodeficiency disease

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8
Q

What are the three major reasons that treating a fungal infection takes so much longer than a bacterial infection?

A

Grow more slowly
Most medications are -static so immune system has to work
Fungus can cause inflammatory response making worse

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9
Q

What are the four major classes of antifungals?

A

Allylamines
Azoles
Echinocandins
Polyenes

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10
Q

Spectrum: Allyamines

A

Broad

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11
Q

Major drugs: Allyamines

A

Naftitine
– and –
Terbinafine

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12
Q

Administration route: Naftitine

A

Topical

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13
Q

Administration route: Terbinafine

A

Topical + Systemic table

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14
Q

Action: Allyamines

A

Inhibit activity of squalene epoxidase

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15
Q

What happens when the activity of squalene epoxidase is inhibited?

A

Lack of ergoseterol + Increased squalene

= Toxic effect

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16
Q

Where does terbinafine concentrate in the body?

A

Dermis
Epidermis
Adipose tissue
Nails

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17
Q

What can terbinafine be used for?

A

Dermatophytes
Aspergillus spp.
Dimorphic fungi
Yeast

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18
Q

Spectrum: Azoles

A

Fungistatic + Broad

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19
Q

Activity: Azoles

A

Inhibition of sterol 14-a demethylase

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20
Q

Groups: Azoles (not specific medications)

A

Imidazoles
— and –
Triazoles

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21
Q

What does the inhibition of sterol 14-a demethylase cause?

A

Depletion of ergosterol and increase in 14-a methylsterols

Disrupts fungal membrane + growth

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22
Q

What is important to remember when giving an azole to an animal?

A

Cytochrome P450 dependent - can cause serious drug interactions

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23
Q

What animal is the use of Azoles contraindicated in? Why?

A

Pregnant animals

due to Teratogenicity

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24
Q

Medications: Imidazoles

A

Ketoconazole
Clotrimazole
Miconazole
Econazole

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25
Medications: Triazoles
Fluconazole Itraconazole Voriconazole Posaconazole
26
Which, Imadazoles or Triazoles, has greater affinity for fungus?
Triazoles
27
What is the drug of choice for aspergillus?
Voriconazole
28
Why was Voriconazole produced?
To overcome resistance that was occurring to fluconazole + itraconazole
29
What is posaconazole good for?
Deep mycoses
30
Spectrum: Echinocandins
Narrow
31
Activity: Echinocandins
1,3 B-glucan synthesis inhibition
32
What happens when 1,3 B glucan is inhibited by Echinocandins?
Component of cell wall is destroyed
33
Forms: Echinocandins
Caspofungin Micafungin Anidulafungin
34
What is caspofungin not effective against?
Cryptococcus neoformans -- or -- Zygomycetes
35
Spectrum: Polyenes
Broad
36
Medication: Polyenes
Amphotericin B
37
Activity: Amphotericin B
Binds to sterols W/ somewhat of an affinity to ergosterol changes cell permeability
38
Administration: Polyenes
IV
39
What is the problem with giving Amphotericin B via IV?
Nephrotoxic | -- binds to sterol rich cell membranes in renal tubules
40
What are the 3 formulations of polyenes?
Lipid complex Liposomal Colloid suspension
41
What fungus have some resistance to polyenes?
Canidia -- and -- Aspergillus
42
What are the five other antifungal compounds?
``` Griseofulvin Flucyctosine Isodides Morpholines Nucleoside-peptides ```
43
Use: Griseofulvin
Dermatophyte infections
44
Action: Griseofulvin
Interferes with microtubule formation | Inhibits division
45
What is a side effect of Griseofulvin?
Teratogenic effects
46
Medicine: Fluorinated Pyrimidine
5-Flucytosine
47
Action: Fluorinated Pyrimidine
``` Cell entry Competes with uracil in RNA synthesis = RNA miscoding + Inhibition of protein synthesis Inhibition of thymidylate synthesis = Inhibition of DNA synthesis ```
48
Spectrum: 5 - Flucytosine
Narrow - mostly yeasts
49
What should 5-Flucytosine be used with? Why?
Quick to build resistance | Use with = Amphotericin B + Fluconazole
50
What are the two types of Iodides?
Sodium -- and -- Potassium
51
What type of iodide should be used in animals?
Sodium
52
Action: Sodium iodide
Interferes with cell metabolic enzymes
53
Use: Sodium iodide
Treatment of sporotrichosis
54
What three major things can happen with Iodide use?
Iodism Host defense defense system impairs Infertility
55
Define: Iodism
``` Lacrimation Increased respiratory secretion Inappetence Tachycardia Cardiomyopathy in CATS ```
56
What causes the host defense system to be impaired with sodium iodide use?
Decreased immunoglobulin production -- and -- Reduced phagocytosis in leukocytes
57
Medicines: Morpholines
Amorolfine
58
Action: Amorolfine
Inhibits ergosterol synthesis
59
Administration: Amorolfine
Topically
60
Medication: Nucleoside Peptides
Nikkomycin Z
61
Action: Nikkomycin Z
Inhibits chitin synthase - no fungal wall development
62
What does Nikkomycin Z help increase the effects of?
Flucytosine Azoles Echinocandins
63
Medication: Substituted Pyridone
Ciclopirox olamine
64
Action: ciclopirox olamine
Alters membrane transport Damages fungal cell membrane Interferes with metabolism
65
Spectrum: Subsituted pyridone
Broad
66
What is Subsituted pyridone fungicidal for?
CA Malassezia Dermatophytes