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PHARMA > ANTIFUNGAL DRUGS FOR SUBCUTANEOUS > Flashcards

ANTIFUNGAL DRUGS FOR SUBCUTANEOUS Flashcards

1
Q

What is the drug of choice for the treatment of several life-threatening mycoses?

A

Amphotericin B

MOA:
Binds to ergosterol in the plasma membranes of fungal cells which creates pores that leak electrolytes resulting in cell death

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2
Q

Targets of Amphotericin B

A
  • Candida albicans
  • Histoplasma capsulatum
  • Cryptococcus neoformans
  • Coccidioides immitis
  • Blastomyces dermatidis
  • Aspergillus
  • Leishamniasis
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3
Q

Pharmacokinetics of Amphotericin B

A
  • Administered by slow IV
  • Bound to plasma protein
  • Can be found in CSF or synovial fluid
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4
Q

What are the adverse effects of Amphotericin

A

a. Fever (occurs 1 to 3 hr after administration
b. Renal impairment
c. Hypotension
d. Thromboplebitis

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5
Q

what is the antimetabolite antifungals?

A

Flucytosine (5-FC) - synthetic pyrimidine antimetabolites

MOA:
Enters the fungal cells and inhibit conversion of dUMP to dTMP, resulting in disruption of nucleic acid and protein synthesis

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6
Q

what is the enzyme that is only found in fungus, which also serves important function in 5-FC

A

cytosine-specific permase

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7
Q

Antifungal spectrum of Flucytosine

A
  • Fungistatic
  • 5-FC + itraconazole = treating chromoblastomycosis
  • with amphotericin B = meningitis caused by C. neoformans and C. albicans
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8
Q

Pharmacokinetics of Flucytosine

A
  • Oral administration
  • penetrates CSF well
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9
Q

Adverse effect of Flucytosine

A
  • neutropenia and bone marrow related depression
  • hepatic dysfunction = elevation of serum transaminase
  • Nausea, vomitting and dirarrhea
  • Severe enterocolitis
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10
Q

What are the two types of Azole antifungals?

A

imidazole - applied topicallty for cutaneous inf

Triazoles - prophylaxis of cutaneous and systemic mycoses

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11
Q

MOA of Azole antifungal

A

inhibit 14-alpha demethylase (cytochrome P450), thus blocking demethylation of lanosterol to ergosterol, inhibiting fungal cell growth

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12
Q

what are azoles drugs that are metabolized by CYP450-3A4 and isoenzyme?

A

itraconazole and variconazole

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13
Q

what are the inducer and inhibitors drug of CYP450

A

inhibitors - ritonavir
inducers - rifampin and phenytoin

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14
Q

what is the contraindication of azole antifungal

A
  • teratogenic, thus should be avoided in pregnant unless potential benefit outweights the risk of fetus
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15
Q

what is the first triazole antifungal agent?

A

Fluconazole

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16
Q

Spectrum of Fluconazole

A
  • aspergillosis or zygomycosis
  • highly active against = C. neoformans, C. albicans and C. parapsopsilosis
  • effective against most of the forms of mucocutaneous candidiasis
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17
Q

Fluconazole is a drug of choice for?

A

Cryptococcus neoformans

18
Q

Pharmacokinetics of fluconazole

A
  • single dose oral treatment for V. candidiasis
  • ORal and IV dosage
19
Q

Adverse effect of fluconazole

A
  • nausea
  • vomting
  • headache
  • skin rashes
20
Q

Synthetic triazole that has abroad antifungal spectrum compared to fluconazole

A

Itraconazole

21
Q

Spectrum of itrazonazole

A
  • Blastomycosis
  • Sporotrichosis
  • Paracoccidioidomycosis
  • Histoplasmosis
22
Q

Pharmacokinetics of Itraconazole

A

available as
- Capsule
- tablet
- oral solution

23
Q

Adverse effects of itraconazole

A
  • nausea
    -vomiting
  • rashh
  • hypokalemia
  • hypertension
    -edema
  • headache
  • liver toxicity
24
Q

itraconadazole contraindication

A
  • pt with heart failure or ventricular dysfunction
25
synthetic triazole similar to itraconadazole
Posaconazole
26
Spectrum of pocasonazole
- prophylaxis of invasive Candida and Aspergillus infection in immunocompromised pt. - Scedosporium and Zygomycetes
27
Pharmacokinetics of Posaconazole
-oral tablet - IV formulation
28
synthetic triazole related to fluconazole
Voriconazole
29
spectrum of voriconazole
- replaced amphotericin B for aspergillosis - scedosporium and - Fusarium species
30
adverse effect of variconazole
- visual - auditory - hepatotoxicity
31
new extended-spectrum triazole
Isavuconazole
32
spectrum of isavuconazole
- aspergillosis - mucormycosis - Isavuconazonium
33
adverse effect of isavuconazole
-nausea - vomiting - diarrhea - hypokalemia
34
group of semisynthetic, cyclic lipopeptides with an N-linked acyl lipid side chain.
Echinocandins
35
spectrum of Echinocandins
- Aspergillus - Candida species
36
MOA of EChinocandins
- inhibitys the synthesis of Beta(1,3)-D-glucan, leading to lysis and cell death
37
is the only Echinocnadins that does not require a loading dose
Micafungin
38
Adverse effect of Echinocandins
- FEver - Rash -Nausea - and phlebitis at the infusion site
39
1st line option for patient with candidemia
Caspofungin
40
drug for prophylaxis of invasive candidiasis. Also hematopoietic stem cell transplation
Micafungin and Anidulafungin

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