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Antifungals Flashcards

(55 cards)

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1
Q

Types of Fungal infections

A
  1. Superficial mycoses- Affects skin, mucous membranes, hair & nails
  2. Subcutaneous mycoses- Affects dermis, subcutaneous tissues & adjacent bone
  3. Systemic mycoses- Affects internal organs
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2
Q

MC Systemic fungal infections

A
  1. Candidiasis
  2. Cryptococcosis
  3. Aspergillosis
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3
Q

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A
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4
Q
A

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5
Q

Classification of Antifungals by MOA

A
  1. Alter cell membrane permeability
    - Polyenes
    - Azoles
    - Allylamines
  2. Block Nucleic acid synthesis
    - Flucytosine
  3. Disrupt microtubule function
    - Griseofulvin
  4. Disrupt fungal cell wall
    - Echinocandins
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6
Q

Classification of Antifungals by Clinical use

A
  1. Drugs for Subcutaneous & Systemic mycoses
    - Systemic drugs = Amphotericin B, Flucytosine, Azoles & Echinocandins
  2. Drugs for superficial mycoses
    - Systemic drugs
    - Topical drugs
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7
Q

Amphotericin B MOA

A

Binds to Ergosterol –> Forms pores in cell membrane –> Leakage of intracellular ions & macromolecules –> Cell death

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8
Q

Amphotericin Activity

A
  • Broadest spectrum

- Activity against Clinical significant yeasts, Organisms causing endemic mycoses & Pathogenic molds

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9
Q

Pharmacokinetics of Amphotericin B

A
  • Highly insoluble
  • Poor GI absorption = MUST be IV
  • Low CSF Penetration = Intrathecal therapy necessary for meningitis
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10
Q

Uses of Amphotericin B

A
  • Nearly all life-threatening fungal infections

- Used as initial induction to rapidly reduce fungal burden –> Pts, then continue w/ an azole

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11
Q

Infusion- related AEs of Amphotericin B

A
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12
Q

Other/ Slow toxicity AEs of Amphotericin B

A
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13
Q

Lipid formulations of Amphotericin B

A

Developed to reduce Nephrotoxicity

  1. Liposomal Amphotericin B (L-AMB)
  2. Amphotericin B Lipid Complex (ABLC)
  3. Amphotericin B colloidal Dispersion (ABCD)
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14
Q

MOA of Flucytosine

A

Taken up by fungal cells via Cytosine Permease –> Converted intracellularly to 5-flurouracil (5-FU) –> Converted to 5-fluorodeoxyuridine monophosphate (5-FdUMP)
- Also forms Fluorouridine Triphosphate (5-FUTP)

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15
Q

Actions of %- Fluorodeoxyuridine Monophosphate (5-FdUMP)

A

Inhibits Thymidylate Synthetase –> Blocks dTMP synthesis/ Inhibits DNA synthesis

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16
Q

Actions of Fluorouridine Triphosphate (5-FUTP)

A

Inhibits protein synthesis

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17
Q

Why is Flucytosine & Amphotericin B combined

A

Mammalian cells are unable to convert the parent drug to its active metabolite

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18
Q

Specrum of Flucytosine

A
  • Fungistatic
  • Narrow spectrum
  • NEVER used as single agent - Avoid resistence
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19
Q

Uses of Flucytosine

A
  • Serious infections caused by susceptible strains of Candida &/or Cryptococcus

USED w/ Amphotericin B to avoid resistance

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20
Q

AEs o Flucytosine

A
  • Bone marrow toxicity

Results from metabolism to 5-fluorouracil

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21
Q

Classification & names of Azoles

A
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22
Q

MOA of Azoles

A

Inhibits 14-a-sterol demethylase –> Dec Ergosterol synthesis –> Disrupt membrane function –> Inc permeability

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23
Q

Ergosterol synthesis

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A

Conversion of Lanosterol to Ergosterol by the fungal Cytochrome P450 enzyme 14-a-sterol Demethylase

24
Q

AEs of Azoles

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A
  • Relatively non-toxic

- Minor GI upset

25
MOA of Ketoconazole
26
Uses of Ketoconazole
27
Pharmocokinetics of Fluconazole
28
Uses of Fluconazole
29
Pharmacokinetics of Itraconazole
- Metabolized by CYP3A4 - Strong CYP3A4 Inhibitor - Poor bioavailability - Poor CSF penetration - Absorption dec. by Antacids, H2 blockers, & PPI
30
Uses of Itraconazole
31
AEs of Itraconazole
Fatal arrhythmias when given w/ Cisapride or Quinidine
32
Spectrum of Voriconazole
Similar to Itraconazole
33
Uses of Voriconazole
DOC for Invasive aspergillosis
34
AEs of Voriconazole
- Transient visual disturbances
35
Spectrum of Posaconazole
Similar to Itraconazole + Activity against Zygomycetes (eg. Mucor)
36
Pharmacokinetics of Posaconazole
Inhibits CYP3A4
37
Properties of Systemic Azoles
38
Names of Echinocandins
Caspofungin
39
MOA of Caspofungin
Inhibits 1-3-D-glucans synthesis in fungal cell wall --> Cell death
40
Spectrum of Caspofungin
- Active against CANDIDA & ASPERGILLUS | - NO activity against Cryptococcus neoformans
41
Pharmacokinetics of Caspofungin
- IV only | - Large cyclic peptides linked to long-chain fatty acids
42
Names of Systemic Drugs used for Superficial mycoses
1. Griseofulvin 2. Terbinafine 3. Ketoconazole 4. Fluconazole 5. Itraconazole
43
MOA of Griseofulvin
Disrupts mitotic spindle --> Inhibits Mitosis
44
Uses of Griseofulvin
1. Dermatophytosis only (Severe cases of skin, hair & nails) | - Replaced largely by Itraconazole & Terbinafine
45
Pharmacokinetics of Griseofulvin
- Absorption improved when given w/ fatty foods | - P450 Inducer - Inc metabolism of other drugs like warfarin
46
MOA of Terbinafine
Inhibits Squalene Epoxidase --> Inhibits Ergosterol synthesis & Cause toxic level accumulation of squalene in fungal cells
47
Uses of Terbinafine
- Onychomycosis
48
AEs of Terbinafine
- GI upset - Rash - Headache - Taste disturbance - Inc serum liver transaminases
49
Pharmacokinetics of Terninafine
- Inhibits CYP2D6 - Causes Inc liver transaminases - Allylamine - ORAL
50
Names of Topical drugs used for Superficial Mycoses
1. Nystatin 2. Amphotericin B 3. Clotrimazole 4. Miconazole 5. Ketoconazole 6. Terbinafine
51
Pharmacokinetics of Nystatin
- Oral/ Vaginal or Cutaneous (too toxic for IV) - NO GI, skin or vagina absorption --> Little toxicity - Similar to Amphotericin B MOA & structure - Polyene macrolide
52
Uses of Nystatin
Candidiasis ONLY
53
Topical use of Terbinafine
Tinea cruris & Tinea corporis | - Topical cream
54
Topical Azoles
Clotrimazole & Miconazole (MC used) | - OTC
55
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Pharmacology (16 decks)

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