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Antifungal Agents Flashcards

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1
Q

MOA of Azoles

A

inhibit cytochrome P 450
impaired synthesis of ergosterol
impaired fungal cell membrane formation

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2
Q

MOA of polyenes

A

bind to ergosterol in fungal cell membrane and disrupt membrane integrity

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3
Q

MOA of Flucytosine

A
  • is an anti-metabolite

- inhibits RNA and DNA synthesis

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4
Q

MOA of Echinocandins

A

inhibit synthesis of B(1,3)-D-glucan (cell wall component)

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5
Q

MOA of Griseofulvin

A

anti-mitotic

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6
Q

MOA of Terbinafine

A
  • inhibit squaline epoxidase

- blocks ergosterol synthesis

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7
Q

what are the pharmacokinetics of Triazoles

A
  • metabolized slowly

- less effect on human sterol synthesis

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8
Q

what are the Triaoles drugs

A
  • Itraconazole
  • Voriconazile
  • Fluconazole
  • Posaconazole
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9
Q

what are the Imidazoles

A
  • Clotrimazole
  • Miconazole
  • Ketoconazole
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10
Q

MOA of Azoles

A
  • inhibit cytochrome P 450
  • impaired synthesis of ergosterol
  • impaired fungal cell membrane formation
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11
Q

the selective activity of Azoles is due to what

A

-differences in membrane sterols:
Mammalian: Cholesterol
Fungal: Ergosterol

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12
Q

What are the adverse effects of Ketoconazole

A
  • anorexia, nausea, vomiting, pruritus, rash, dizziness, photophobia
  • reduced plasma testosterone –> gynecomastia, decreased libido and erectile dysfunction in males, menstrual irregularities in females
  • inhibition of adrenal steroidogenesis, decreased cortisol, hepatic toxicity and necrosis
  • teratogenecity
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13
Q

what are the drug interaction of Ketoconazole

A
  • strong inhibitor of CYP3A4 and other enzymes
  • increased serum concentrations of many other drugs
  • Absorption reduced by drugs that decrease gastric acidity (antacids, PPIs, H2-receptor blockers)
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14
Q

Fluconazole is active against what

A

-most Candida species
-Coccidioides and Cryptococcus spp
Histoplasma capsulatum (at higher doses)

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15
Q

Fluconazole is not active against what

A

C. krusei
Many strains of C. glabrata
Most molds

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16
Q

what are the pharmacokinetics of Fluconazole

A
  • lowest affinity for mammalian P450 enzymes

- good water solubility and CSF penetration

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17
Q

what are the adverse effects of Fluconazole

A
  • headache, GI distress, facial edema, rash, pruritus
  • Stevens-Johnson syndrome, anaphylaxis, hepatic toxicity , leukopenia, hypokalemia, QT prolongation, torsades de pointes reported
  • Teratogenic
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18
Q

Fluconazole drug interactions

A
  • strong inhibitor of CYP2C9 and 2C19
  • moderate inhibitor of CYP3A4
  • may increase serum concentrations of drugs metabolized by enzymes especially those metabolized by CYP2C9 and CYP2C19 or CYP3A4 may increase risk of QT prolongation and torsades de pointes
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19
Q

what is the spectrum of activity of Itraconazole

A

broader than fluconazile

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20
Q

Itraconazole is active against what

A 
Cryptococcus neoformans
Aspergillus spp.
Coccidioides spp.
H. capsulatum
Sporothrix spp.
Dermatophytes
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21
Q

Itraconzole is not active against what

A

Scedosporium spp
Scopulariopsis spp.
Flusarium spp
Zygomycetes

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22
Q

what are the adverse effects of Itraconazole

A

-GI distress- nausea, vomiting, rash
-Stevens-Johnson syndrome, hepatic toxicity, edema, hypokalemia, hypertension, negative inotropic effects, congestive heart failure
Peripheral neuropathy, visual disturbances, hearing loss
Teratogenic

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23
Q

Itraconazole is contraindicated in what patients

A

patients with history of heart failure/ventricular dysfunction

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24
Q

drug interactions of Itraconazole

A
  • strong inhibitor of CYP3A4
  • increased serum levels of other drugs metabolized by this system
  • absorption reduced by drugs that decrease gastric acidity (antacids, PPIs, H2 receptor blockers)
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25
spectrum activity of Voriconazole
similar to itraconazole
26
Voriconazole is active against
-most species of Candida -Blastomyces dermatitidis -Cryptococcus neoformans -Paracoccidioides brasiliensis Scedosproium spp -Aspergillus spp -Coccidioides spp. -H. capsulatum -Dermatophytes -Fusarium spp
27
Voriconazole is not active against
Zygomycetes spp | Sporothrix
28
Is Voriconazole or Amphotericin more effective for invasive aspergillosis
Voriconazole
29
what are the pharmacokinetics of Voriconazole
-serum concentrations vary - may required monitoring
30
what are the adverse effects of Voriconazole
Transient visual disturbances- blurred vision, photophobia, altered color or image perception Rash, Stevens-Johnson syndrome, hepatic toxicity, confusion, hallucinations Anaphylaxis Teratogenic
31
drug interactions of Voriconazole
Metabolized by and inhibits, CYP2C19, CYP2C9, and CYP3A4 → serum levels may be influenced by drugs that affect these enzymes and serum levels of other drugs metabolized by these enzymes may be increased
32
what is the spectrum of activity of Posaconazole
- similar to Itraconazole | - activity is twice that of itraconzole
33
Posaconazole has increased activity against
Absidia spp
34
how is Posaconazole administered
oral, taken with meals
35
what are the adverse effects of Posaconazole
Headache, GI distress, rash Hepatic toxicity, QT prolongation Arrythmias, anaphylaxis, angioedema (rare) Teratogenic
36
Prosaconazole drug interactions
Metabolized by UDP glucuronidation Substrate of P-glycoprotein (permeability glycoprotein) Strong inhibitor of CYP3A4 → increased serum levels of other drugs metabolized by this system Used with caution with other drugs known to prolong the QT interval; contraindicated with such drugs that are metabolized by CYP3A4
37
Absorption of Posaconazole is reduced by
drugs that decrease gastric acidity (antacids, PPIs, H2-receptor blockers)
38
what is the solubility of Polyenes: Amohotericin B
- insole in water | - solubility increased by formation of complex with deoxycholate (bile salt)
39
what are the Lipid Amphotericin B products
Ampho B lipid complex - Ribbon- like sheets Ampho B cholesteryl complex - disk-shaped colloidal dispersion Liposomal amphotericin B - Unilamellar vesicle
40
MOA of ampotericin B
binds to ergosterol in fungal cell membrane, disrupts membrane integrity
41
selectivity of Amphotericin B is based on
-differences in membrane sterols: Mammalian: Cholesterol Fungal: Ergosterol
42
Spectrum of Amphotericin B
broad-spectrum fungicidal | *initial therapeutic agent, treatment continued with less toxic antigunal
43
Amphotericin B is the DOC for
life-threatening, fungal infections | -Aspergillus, cryptococcus, histoplasmosis, invasive candidiasis, blastomycosis, mucor, neuropenic fever
44
what are the pharmacokinetics of Amphotericin B
``` No oral bioavailability Metabolism not understood- Hepatic or renal impairment does not affect levels Extensive tissue binding → Long T1/2 (~15 days)\ Concentrates in liver & spleen ```
45
what are the adverse effects of Amphotericin B deoxycholate
- infusion rxns; related to cytokine release; premdedicate with acetaminophen, diphenhydramine, hydrocortisone, and meperidine - nephrotoxicity: dose-limited toxicity; sodium loading with normal saline may provide protection - hypokalemia, hypomagnesemia common due to a mild renal tubular acidosis - anemia, weight loss, thrombocytopenia, mild leukopenia
46
what are the adverse effects of Amphotericin B lipid formuations
Infusion reactions least severe with liposomal amphotericin B Nephrotoxicity less common and less severe than with amphotericin B deoxycholate Hepatotoxicity (rare)
47
what is MOA of Flucytosine
- converted in fungal cytosol to 5-fluoruracil | - 5-fluorouracil inhibits DNA and RNA synthesis
48
Flucytosine seletive activity based on
- cellular uptake by specific enzyme, cytosine pernease | - conversion to 5-fluorouracil by another specific fungal enzyme, cytosine deaminase
49
Flucytosine active against
Cryptococcus neoformans Candida spp Chromoblastomycosis
50
Flucytosine used in combination with
amphotericin B afor cryptococcal meningitis or systemic candidiasis
51
what are the pharmacokinetics of Flucytosine
Good oral bioavailability- administered orally Volume of distribution equals total body water Penetrates the blood brain barrier Renal excretion
52
what are the adverse effects of Flucytosine
dose-related bone marrow toxicity
53
what are the Echinocandins
Caspofungin Anidulafungin Micafungin
54
what is the MAO of Echinocandins
inhibit synthesis of B(1,3)-D-glucan (fungal cell wall component) --> cell wall becomes permeable
55
Echinocandins selective activity based on
absence of cell wall in mammalian cells
56
Echinocandins active against
most species of Candida, Aspergiullus spa
57
what are the Pharmacokinetics of Echinocandins
No oral bioavailability T1/2 ~ 10 hours after IV infusion Extensively bound to albumin Hepatic metabolism, does not significantly involve cytochrome P450 enzymes No clinically significant drug interactions No dose adjustment required in renal dysfunction
58
what are the adverse effects of Echinocandins
Generally well tolerated Occasional rash, fever, nausea, vomiting, headache, hypokalemia and mild hepatic toxicity Stevens-Johnson syndrome, exfoliative dermatitis, anaphylaxis - rare Teratogenic
59
hat is Griseofulvin used for
- mucocutaneous infections | - fungal skin, nail, hair infections
60
what is the MAO of Griseofulvin
antimitotic-interacts with polymerized microtubules leading to disruption of the mitotic spindle
61
what is the activity of Griseofulvin
Fungistatic for various species of the dermatophytes | Microsporum, Epidermophyton, and Trichophyton
62
what are the pharmacokinetics of Griseofulvin
Blood levels quite variable Best absorption when taken with a fatty meal T1/2 = 24 hours Keratophilic- binds to keratin, protects skin and nails from further infection
63
what are the adverse effects of Griseofulvin
Generally well tolerated- incidence of adverse effects is very low Headache, nausea, vomiting Teratogenic
64
Griseofulvin interactions
induces hepatic cytochrome P450 isoforms
65
what is Terbinafine used for
mucococutaneous infections
66
what is the MAO of Terbinafine
inhibit squaline epoxidase -blocks ergosterol synthesis -impaired fungal cell membrane synthesis FUNGICIDAL
67
selective activity of Terbinafine is due to
1000 to 10,000 times higher binding affinity for the fungal enzyme
68
what are the pharmacokinetics of Terbinafine
``` Well absorbed but significant first pass metabolism to inactive metabolites Highly lipophilic Accumulates in skin and nails T1/2 = 200 to 400 hours at steady state Keratophilic ```
69
what are the adverse effects of Terbinafine
Well tolerated- incidence of adverse effects is very low Nausea, diarrhea, headache, rash Hepatotoxicity, neutropenia, Stevens-Johnson syndrome (rare) Teratogenic
70
Drug Interactions of Terbinafine
none | does not affect cytochrome P450 isoforms

Pharmacology (23 decks)

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