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Pharmacology - Midterm 2 > Antifungals > Flashcards

Antifungals Flashcards

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1
Q

Polyene antibiotic that binds to Ergosterol and forms pores in the cell wall, leading to ion leakage and cell death

A

Amphotericin B

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2
Q

Antifungal agent with the broadest spectrum of activity, including fungicidal

A

Amphotericin B; used against yeasts, endemic mycoses, and pathogenic molds

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3
Q

Highly insoluble and formulated as deoxycholate colloidal suspension

A

Amphotericin B

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4
Q

PK of Amphotericin B

A

Slow IV infusion (poor oral absorption); Low penetration into CSF; Intrathecal for Meningeal disease

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5
Q

Often used as initial induction regimen to reduce fungal burden, then followed by an Azole

A

Amphotericin B

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6
Q

Preferred treatment for deep fungal infections during prenancy

A

Amphotericin B

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7
Q

AE of Amphotericin B

A

Infusion-related: fever and chills, muscle spasms, vomiting, headache, hypotension

Anemia due to decreased Erythropoietin

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8
Q

Premedication with which drugs may alleviate AE of Amphotericin B?

A

Antihistamines, Glucocorticoids, Antipyretics, or Meperidine

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9
Q

How does Amphotericin B cause renal toxicity?

A

Slow toxicity by binding Cholesterol and forming pores in the mammalian cell membranes

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10
Q

How can renal damage by Amphotericin B be attenuated?

A

Administration of Saline infusion with Amphotericin B

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11
Q

What should be monitored during Amphotericin treatment?

A

Liver and Kidney function, serum electrolytes (Mg and K), blood counts, and hemoglobin

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12
Q

How does Amphotericin B affect the CNS?

A

Slow toxicity: Intrathecal administration can cause seizures and neurological damage

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13
Q

3 Lipid formulations of Amphotericin B

A

Liposomal Amphotericin B (L-AMB)
Amphotericin B Lipid Complex (ABLC)
Amphotericin B Colloidal Dispersion (ABCD)

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14
Q

Why are Lipid formulations of Amphotericin B used?

A

Packaging Amphotericin B in lipid carriers reduces exposure to nephron –> reduces nephrotoxicity

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15
Q

Synthetic Pyrimidine antimetabolite that uses Cytosine permease to enter fungal cells

A

Flucytosine

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16
Q

MOA of Flucytosine

A

Fungistatic; Enters fungal cell via Cytosine permease –> converted to 5-Fluorouracil (5-FU) —> converted to 5-fluorodeoxyuridine monophosphate –> inhibits thymidylate synthase –> no synthesis of dTMP.

Fluorouridine triphosphate (5-FUTP) is also formed –> inhibits protein synthesis

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17
Q

PK of Flucytosine

A

Mammalian cells cannot convert it into its active metabolites

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18
Q

Combination of Flucytosine and which drug gives a synergistic effect?

A

Amphotericin B

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19
Q

Nicknamed the “suicide inhibitor”

A

Flucytosine

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20
Q

Description of Flucytosine

A

Narrow spectrum; used in combination with other drugs for synergism and to avoid resistance

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21
Q

Which drug is combined with Amphotericin B to treat systemic candidiasis and cryptococcosis?

A

Flucytosine

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22
Q

Indications of Flucytosine

A

Candida and/or Cryptococcal infections

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23
Q

AE of Flucytosine

A

Bone marrow toxicity; due to metabolism by intestinal flora to 5-Fluorouracil

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24
Q

Triazoles

A

Itraconazole, Fluconazole, Voriconazole, Posaconazole

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25
Imidazoles
Ketoconazole, Miconazole, Clotrimazole
26
Are Azoles used for Systemic or Superficial mycoses?
Systemic mycoses
27
Classifications of Azoles
Imidazoles and Triazoles
28
MOA of Azoles
Azoles inhibit CYP450 enzyme 14-alpha-sterol demethylase, which usually converts Lanosterol to Ergosterol --> disrupts membrane function and increases permeability
29
Specificity of Azoles is due to a greater affinity for fungal CYP450 enzymes than for human CYP450 enzymes. Which Azoles have greater specificity?
Triazoles
30
AE of Azoles
GI upset; relatively non-toxic
31
PK of Ketoconazole
Strong inhibitor of CYP3A4; can potentiate Warfarin and Cyclosporine toxicities Poor CSF penetration
32
How do Antacids, H2-blocker, and PPIs affect Ketaconazole absorption?
Ketaconazole is best absorbed at low gastric pH; these drugs interfere with absorption
33
Indications of Ketaconazole
Superficial mycoses; narrow spectrum
34
AE of Ketaconazole
Decreased testosterone levels, gynecomastia, decreased libido in men, menstrual irregularities High doses may inhibit adrenal steroid synthesis --> decrease plasma cortisol concentrations
35
PK of Fluconazole
High oral bioavailability, good CSF penetration, Oral and IV
36
Drug interactions of Fluconazole
Moderate inhibitor of CYP3A4 but strong inhibitor of CYP2C9 --> increased plasma levels of Zidovudine, Phenytoin, and Warfarin
37
Fluconazole has no activity against which type of fungi?
Aspergillus and filamentous fungi
38
DOC for Asperigillosis
Voriconazole
39
Contraindications of Itraconazole
Potentially fatal arrhythmias when given with Cisapride or Quinidine
40
PK of Itraconazole
Metabolism by CYP3A4 and strong inhibitor of CYP3A4 Poor CSF penetration Absorption reduced by antacids, H2-blockers, and PPIs
41
Indications for Itraconazole
Dimorphic fungi (Blastomyces, Sporothrix, and Histoplasma), Dermatophytoses, Onchomycosis, and Aspergillus (but replaced by Voriconazole for this)
42
AE of Voriconazole
Transient visual disturbances and numerous drug interactions
43
PK of Voriconazole
Metabolized by and inhibits CYP2C19, CYP2C9, and CYP3A4
44
Antifungal activity of Posaconazole
Zygomycetes such as Mucor
45
Which two Imidazoles have similar spectrum of activity to Itraconazole?
Posaconazole and Voriconazole
46
PK of Posaconazole
Inhibits CYP3A4
47
Only Systemic Azole with renal elimination (all others are hepatic)
Fluconazole
48
Which Systemic Azole has the highest CSF:serum ratio i.e. best CSF absorption?
Fluconazole
49
Antifungal activity of Capsofungin
Candida and Aspergillus
50
PK of Capsofungin
IV
51
MOA of Capsofungin
Inhibits synthesis of beta 1-3-D-glucans in the fungal cell wall --> disruption of cell wall and death
52
An Echinocandin
Capsofungin
53
MOA of Griseofulvin
Disrupts mitotic spindle --> inhibits mitosis
54
Indications of Griseofulvin
Treatment of dermatophytosis; replaced by Itraconazole and Terbinafine
55
PK of Griseofulvin
Absorption enhanced by fatty meals
56
Drug Interactions of Griseofulvin
Induces CYP450 enzymes: increases metabolism of Warfarin, etc.
57
Antifungal Allylamine
Terbinafine
58
MOA of Terbinafine
Inhibits Squalene epoxidase --> decreased Ergosterol synthesis and toxic accumulation of squalenes in fungal cell
59
Indications of Terbinafine
Most effective against Onychomycosis; also used for Tinea cruris and Tinea corporis
60
AE of Terbinafine
GI effects, rash, etc.
61
Drug interactions of Terbinafine
Doesn't affect CYP450 --> NO DRUG INTERACTIONS
62
Polyene macrolide Antifungal with similar structure and MOA as Amphotericin B
Nystatin
63
Only used for Candidiasis in cutaneous, vaginal, oral administration
Nystatin
64
PK of Nystatin
Too toxic for IV administration and not absorbed from GI, skin, or vagina --> little toxicity
65
Indication of topical Amphotericin B
Cutaneous candidiasis
66
2 Azoles most commonly used topically
Miconazole and Clotrimazole; both OTC
67
PK of Terbinafine
Accumulates in keratin; available orally or as topical cream
68
Treatment of esophageal candidiasis
IV/Oral Fluconazole
69
Treatment of urinary candidiasis
IV/Oral Fluconazole
70
Treatment of oropharyngeal candidiasis
Mild: topical Clotrimazole or Nystatin Moderate to severe: Oral Fluconazole AIDS patient: Oral Fluconazole
71
Treatment of vulvovaginal candidiasis
Topical Azoles or Oral Fluconazole
72
Treatment of recurrent vulvovaginal candidiasis
Oral Fluconazole
73
Treatment of Candidemia
IV Fluconazole or an IV Echinocandin
74
Treatment of cutaneous candidiasis
Topical Amphotericin B, topical Azole, or topical Nystatin
75
Treatment of Cryptococcosis
Amphotericin B + Oral Flucytosine then Oral Fluconazole
76
Treatment of invasive Aspergillosis
IV and then Oral Voriconazole
77
Treatment of Mucormycosis
Amphotericin B
78
Treatment of Fusariosis
Amphotericin B
79
Treatment of Onychomycosis
Oral Terbinafine or Oral Itraconazole or Oral Fluconazole
80
DOC for Pneumocystis jiroveci pneumonia treatment and prophylaxis in immunocompromised
Co-trimoxazole
81
Alternative therapies for Pneumocystic jiroveci
``` Clindamycin + Primaquine Atovaquone Dapsone + Trimethoprim Pentamidine Moderate to severe: also give Prednisone ```

Pharmacology - Midterm 2 (16 decks)

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