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Pharma 2nd semester > C.4. Antifungal agents > Flashcards

C.4. Antifungal agents Flashcards

(53 cards)

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1
Q

list 2 Polyenes

A

Amphotericin B and Nystatin

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2
Q

mechanism of action of Amphotericin B and Nystatin

A
  1. interact with ergosterol in fungal membranes to form ‘pores’, which disrupt membrane permeability
  2. Fungicidal effect
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3
Q

what is the basis of Amphotericin and Nystatin resistance?

A

strains that have low ergosterol content in their cell membranes are resistant

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4
Q

spectrum and clinical use of Amphotericin B

A

broadest antifungal spectrum.

systemic infections: Aspergillosis, Blastomyces, candida, Cryptococcus, Histoplasma, Mucor, Sporthrix

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5
Q

clinical use of Nystatin

A

topical for candidiasis

*systemic use is limited due to toxicity

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6
Q

how is Amphotericin given?

A

IV or orally (poor availability)

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7
Q

what is the T1/2 of Amphotericin B?

A

up to 2 weeks

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8
Q

does Amphotericin B have CNS penetration?

A

poor

an intrathecal injection is required against cryptococcal or candida meningitis

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9
Q

clearance of amphotericin

A

hepatic metabolism and renal elimination

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10
Q

adverse effects of Amphotericin infusion-related

A

fever, chills
muscle spasm
injection site phlebitis
hypotension (due to histamine release)

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11
Q

adverse effects of Amphotericin dose-dependent

A
  1. nephrotoxicity (↓ GFR, RTA, K and Mg² wasting, ↓EPO)
  2. CNS toxicity (seizures)
  3. Anemia
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12
Q

what are the means to reduce infusion-related toxicity with Amphotericin administration (4)?

A
  1. anti-histamines
  2. NSAID’s
  3. Meperidine- opioid
  4. Corticosteroids
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13
Q

what are the means to reduce dose-dependent toxicity with Amphotericin administration (4)?

A
  1. liposomal formulation of Amphotericin B
  2. Co-administration with flucytosine
  3. volume expansion with IV saline
  4. K and Mg² supplementation
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14
Q

mechanism of action of azoles

A
  1. interfere with the synthesis of ergosterol

2. Fungicidal effect

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15
Q

resistance mechanism of azoles

A

develops with long term use via ↓ intracellular accumulation and altered sensitivity of target enzymes

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16
Q

what are ketoconazole, clotrimazole and Miconazole?

A

Imidazoles

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17
Q

what is Fluconazole and Itraconazole?

A

1st generation Triazoles

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18
Q

what is Voriconazole?

A

2nd generation Triazole

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19
Q

how are azoles given?

A

oral, parenteral, topical

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20
Q

which azole can penetrate the CSF and cross the BBB?

A

fluconazole

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21
Q

are azoles inhibitors of CYP450 enzymes?

A

yes

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22
Q

what azoles are cleared by hepatic metabolism?

Study These Flashcards
A

ketoconazole
itraconazole
voriconazole

23
Q

which azole is cleared by renal elimination?

24
Q

side effects of azoles

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A

GI symptoms, skin rash
hepatotoxicity (rare)
visual disturbances (voriconazole)
↓ synthesis of steroid hormones cortisol and testosterone –> ↓ libido, gynecomastia (ketoconazole)

25
clinical use of ketoconazole
1. Mucocutaneous candidiasis (topical) 2. Dermatophytosis (topical) 3. Cushing's disease ( ↓ cortisol synthesis) * systemic use is limited cause of side effects
26
clinical use of clotrimazole and Miconazole
topical: dermatophytes, superficial & vaginal candidiasis | OTC drug
27
clinical use of fluconazole
1. esophageal, oropharyngeal, vaginal and invasive candidiasis 2. Coccidiodes infections 3. Cryptococcus meningitis- treatment and prophylaxis
28
clinical use of Itraconazole
1. Dimorphic fungi, Blastomyces and Sporothrix infections | 2. 2nd line agent for Aspergillus, Coccidioides, Cryptococcus, Histoplasma
29
clinical use of Voriconazole
Aspergillus infections | invasive candida infections (including sepsis)
30
what is Flucytosine?
Antimetabolite
31
mechanism of action of Flucytosine (5-FC)?
5-FC is converted to 5-FU by fungal cytosine deamiase ---> 1. tri-phosphorylation, incorporated into fungal RNA 2. 5-FU forms 5-Fd-UMP --> inhibits thymidylate synthase--> thymine ↓ (inhibits DNA synthesis )
32
when does resistance to Flucytosine (5-FC) emerge?
when used alone and not in combination with Amphotericin B
33
Flucytosine is used in combination with....
Amphotericin B or triazole used to treat Cryptococcal meningitis and invasive candidiasis
34
how is Flucytosine given?
orally
35
can Flucytosine enter the CNS?
yes
36
what type of elimination does Flucytosine have?
renal
37
side effects of Flucytosine (5-FU)
1. bone marrow dysfunction (reversible) 2. alopecia 3. liver dysfunction
38
what is Caspofungin and what the mechanism?
an Echinocandin | inhibit the synthesis of β (1-3)-glucan, a critical component of the fungal cell wall.
39
how is Caspofungin given and what is it's T1/2?
IV | T1/2 9-12 h'
40
metabolism of Caspofungin
hepatic
41
clinical uses of Caspofungin
1. candida infections failed to respond to amphotericin B (disseminated and mucocutaneous infections) 2. mucor infection 3. Aspergillus infection
42
side effects of Caspofungin
1. GI distress 2. fever, headaches, flushing, skin rash 3. hepatotoxic (rarely)
43
what are Griseofulvin and Terbinafine?
systemic drugs for superficial fungal infections (cutaneous mycoses- dermatophytosis, onychomycosis)
44
which systemic drug is an inducer of CYP450 enzymes?
Griseofulvin | ↑ warfarin metabolism
45
mechanism of action of Griseofulvin
1. fungistatic effect 2. accumulates in keratin-rich tissues 3. interfere with microtubules function in dermatophytes
46
resistance mechanism of Griseofulvin
↓ drug uptake
47
clinical use of Griseofulvin
Dermatophytosis of the skin and hair *not commonly used!
48
how is Griseofulcin given?
orally
49
how is Terbinafine given?
topically and orally
50
side effects of Griseofulvin
``` GI distress headaches, mental confusion photosensitivity hepatotoxicity Disulfiram-like reaction teratogenic carcinogenic ```
51
mechanism of action of Terbinafine
1. fungicidal effect | 2. inhibits squalene epoxidase--> interfering with ergosterol synthesis
52
clinical use of Terbinafine
1. Onychomycosis | 2. Dermatophytosis of the skin and hair
53
side effects of Terbinafine
GI distress Headache, rash hepatotoxicity taste disturbances

Pharma 2nd semester (49 decks)

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