Antifungals Flashcards

1
Q

What are 3 echinocandins?

A

Capsofungin
Andulafungin
Micafungin

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2
Q

What is the MOA of echinocandins? Is the target located in the cell membrane or the cell wall?

A

Cell wall inhibition by inhibition B-1-3 glucan synthase located in the cell membrane

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3
Q

What two organisms are targeted by echinocandins? Is it fungicidal?

A

Candida (yeast)
Aspergillus (mold)
Yes

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4
Q

What is the preferred route for capsofungin? Effective or ineffective? When is it given?

A

IV
Very effective
Given when not responding to Azol

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5
Q

Where is capsofungin metabolized? What are 2 relatively mild AE? Contraindications and drug interactions?

A

Liver
Headache/chills
DI: Cyclosporine
Contraindications: Hepatic impaired patients

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6
Q

What is a pharmokinetic advantage of andulafungin?

A

48 hour half like

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7
Q

What is micafungin regularly prescribed for? What is its main AE?

A

Prophylactic for candida treatment in neutropenic patients (transplant pts)
Histamine release with cyclospoins and sirolimus

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8
Q

What organism has been reported to have resistance to capsofungin?

A

Candida albicans

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9
Q

What is the MOA of Polyenes?

A

Targets cell membrane, punches hole in egosterol

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10
Q

What are two polyenes?

A

Amphotericin B

Nystatin

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11
Q

How does the route differ for each of the two polyenes?

A

Amphotericin - oral/slow IV

Nystatin - topical use/oral

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12
Q

Is amphotericin B narrow or broad spectrum? What types of fungal infections is it mainly used for?

A

Extremely broad

Life-threatening fungal infections

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13
Q

What is a major AE of amphotericin B? What are two subsequent conditions this causes? What two problems does it cause in the kidney?

A

Nephrotoxicity - Azotermia (high N2) and Anemia - reduction of erythropoetin synthesis
Clogs renal artery
Necrosis of Distal tubual

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14
Q

What other forms of Amphotericin are available?

A

Less toxic forms

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15
Q

When is the only time when Amphotericin B can penetrate the CNS?

A

When CNS is inflammed

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16
Q

What is Nystatin the drug of choice to treat? What two other conditions does it topically treat?

A

Oroesophageal thrush

Diaper rash and Vaginal Candidiasis

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17
Q

Why can’t nystatin be given IV?

A

Too toxic for systemic

18
Q

What is the one mild AE of oral Nystatin?

A

GI disturbance

19
Q

What is the MOA of Azoles? What essential enzyme does it target?

A

Inhibits membrane by inhibiting formation of ergosteral from lanosterol
Targets Cytochrome P450 mediated 14-alpha demethylase

20
Q

What route is ketoconazole typically given? Due to being a CYP inhibitor, what AE can it cause? It is more harmful or safer than amphotericin B? Is it used in the US for nail and skin infections?

A

Topically (was first oral drug)
Hepatotoxic
Safer
Not used in US for nail and skin infections

21
Q

What subset of fungi does itraconazole target? Is it recommended for systemic infections?

A

Dimorphic

No

22
Q

What is the most commonly given azole? Is it good for systemic infections?

A

Fluconazole

Yes

23
Q

Which azole is good at penetrating the CSF and strictly eliminated int he urine, thus safe in hepatic dysfunction patients?

A

Fluconazole

24
Q

Which fungal infection is fluconazole most commonly used for? Prophylaxis for which? Used in most stable patients for?

A

Mucocutaneous Candidiasis
Crytococcal meningitis
Candida Albicans

25
Q

Which fungus does fluconazole have no activity against?

A

Aspergillus

26
Q

Which azole can be given when a fungus is resistant to fluconazole and which is also active against aspergillus?

A

Voriconazole

27
Q

What does voriconazole inhibit, therefore requiring a dose reduction if a person is on cyclosporine or tacrolimus?

A

CYP3A4

28
Q

Which three AE reactions are unique to the azole voriconazole?

A

Neurotoxicity
Visual changes
Photosensitivity

29
Q

Which azole is the only one active against mucorales? It is also a step-down therapy from amphotericin B.

A

Posaconazole

30
Q

What is the major AE of all azoles besides fluconazole?

A

Hepatotoxicity

31
Q

What are miconazole and clotrimazole used for?

A

Superficial mycoses

32
Q

What do allylamines target? What are two main allylamines?

A

Fungal cell membrane inhibition
Naftifine
Terbinafine

33
Q

What is the route of naftifine? What does it subsequently treat? It is trip action against what?

A

Topical
Dermatophyte (athlete’s foot, ring worm of groin/body)
Anti-bacterial, fungal, and inflammatory

34
Q

What does terbinafine target to reduce ergosterol production?

A

Squalene epozide synthase

35
Q

What route is terbinafine typically given? What drug is it superior to?

A

Onychomycosis

Superior to itraconazole

36
Q

What mild AE does terbinafine cause?

A

Mild GI

37
Q

What is the only agent to act on nucleic acids/DNA synthesis? What is its unquie MOA? What does the active form inhibit

A

Flucytosine
Pro-drug, active form 5-FU
Inhibits thymydylate synthase (thymine production)

38
Q

Since it can develop resistance easily, what can flucytosine be used synergistically with?

A

Amphotericin B

39
Q

What is the fairly severe AE of flucytosine?

A

Myelosuppression

40
Q

What is the only drug to act on mitosis? What is this drug only used for?

A

Griseofulvin

Systemic dermatophytosis

41
Q

What are the two MOA of Griseofulvin, human and fungi respectively?

A

Human - binds to keratin in new formed keratinocytes, protecting skin from new infections
Fungi - irreversibly binds to microtubule, preventing spindle formation