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Pharm Block 3 > Antifungal drugs > Flashcards

Antifungal drugs Flashcards

1
Q

What anti fungal drug is effective for most serious systemic mycoses?

A

Amphotericin B*

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2
Q

MOA of Amphotericin B*

A

lipophilic; binds ergosterol in fungal membranes, producing membrane instability/leakage

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3
Q

Is Amphotericin B* absorbed in the GI tract?

A

NO; oral administration only effective on fungi in GI lumen

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4
Q

What is important for renal toxicity

A

Daily dose, total cumulative dose

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5
Q

Explain the toxicity of Amphotericin B*

A
  • Fever, nausea, vomiting, headache, chills
  • Hypotension, hypokalemia, tachypnea
  • 90% will show nonpermanent nephrotoxicity; permanent renal damage can occur, which is related to total drug dose
  • Reversible hyopochromic, normocytic anemia
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6
Q

What is used for serious infections due to Candida, Cryptococcus?

A

Flucytosine*

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7
Q

What is Flucytosine* use with

A

amphotericin* (synergistic)

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8
Q

MOA of Flucytosine*

A

contain a cytosine deaminase that converts 5-FC to 5-FU, and 5-FU then block nucleic acid synthesis(???)

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9
Q

Toxicity of Flucytosine*

A
  • Nausea, vomiting, diarrhea, enterocolitis
  • Leukopenia, thrombocytopenia
  • Reversible elevated hepatic enzymes
  • Extreme caution w/ patients w/ renal insufficiency or bone marrow depression
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10
Q

What are the imidazole and triazoles used for serious fungal infections

A

fluconazole*
itraconazole*
voriconazole*

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11
Q

MOA of imidazoles and triazoles

A

inhibit sterol 14alpha-sterol demethylase (a fungal cytochrome P450); this blocks the conversion of lanosterol to ergosterol, which deprives the membranes of ergosterol

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12
Q

What is fluconazole* used for

A

Cryptococcus meningitis, some Candida

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13
Q

What is itraconazole* used for

A

Blastomyces, Histoplasma, Candida (esophogeal and oropharyngeal)

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14
Q

What is Voriconazole* used for

A

invasive Aspergillus, Fusarium, Scedosproium

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15
Q

Level of CNS penetration of the imidazoles and triazoles

A
  • fluconazole* – excelent
  • itraconazole* – none
  • voriconazole – thought to be some
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16
Q

Elimination of imidazoles and triazoles

A
  • fluconazole* – excreted unchanged in urine

- itraconazole, vorivonazole – metabolized by liver

17
Q

General side effect of imidazoles and triazoles

A
  • Nausea, vomiting, rash, diarrhea, headache
  • hepatotoxicity (fluconazole* – lowest incidence)
  • discontinue if signs of liver dysfunction appear
  • inhibits metabolism of several drugs
18
Q

Specific side effect of itraconazole*

A

contraindicated w/ several drugs that inhibit CYP3A4

19
Q

Specific side effect of voriconazole*

A

visual disturbances

20
Q

What is Caspofungin* used for

A

Treatment of invasive Aspergillus in patients intolerant of/refractory to other drugs and also Candida

21
Q

MOA of Caspofungin*

A

inhibits fungal cell wall synthesis by non-competitively blocking synthesis of beta(1,3)-D-glucan

22
Q

Toxicity of Caspofungin*

A
  1. fever, nausea/vomiting

2. phlebitis at injection site

23
Q

What drugs are used for the treatment of superficial candida infections

A

Fluconazole, Miconazole, Clotrimazole, Itraconazole, Nystatin*, Amphotericin B

24
Q

Toxicity of Clotrimazole*

A

In oral form, may cause abnormal liver function tests

25
Q

Which drug is used exclusively for Candida

A

Nystatin*

26
Q

Opthalmic treatment of fungal infection

A

Natamycin*

27
Q

Toxicity of Natamycin*

A

conjunctival chemises and hyperemia

28
Q

Topical preparations for treatment of dermatophytic infections

A

Miconazole, Clotrimazole, Tolnaftate, Terbinafine, Ciclopirox*

29
Q

What drug is the only topic Rx for fungal nail infections

A

Ciclopirox*

30
Q

Oral preparations for treatment of dermatophytic infections

A

Terbinafine, Griseofulvin, Itraconazole

31
Q

MOA of terbinafine*

A

inhibits fungal squalene epoxidase; non-competitive; accumulation of squalene damages fungal cell membranes

Pharm Block 3 (10 decks)

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