Anti-Fungal Agents Flashcards

1
Q

Bacterial derivative of Amphotericin B

A

Streptomyces nodosus

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2
Q

MOA of Amphotericin B

A

Binding to ergosterol to create pores leading to increased cell permeability and lysis

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3
Q

Therapeutic uses of amphotericin B

A

Used as induction regime and treatment of all life-threatening mycotic infections; immunosuppressed individuals

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4
Q

Adverse effects of amphotericin B

A

Nephrotoxicity (decreased EPO) causing anemia; infusion related toxicity

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5
Q

New AMB Formulations

A

AMB Lipid Complex (ABLC)
AMB colloidal dispersion (ABCD)
Liposomal AMB

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6
Q

Drug of choice for nearly all life-threatening mycotic infections

A

New AMB formulations

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7
Q

New AMB formulation that deliver AMB to reticuloendothelial cells in the liver and spleen

A

Liposomal AMB

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8
Q

These drugs produce lower AMB levels

A

ABLC and ABCD

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9
Q

Polyene macrolide active against Candida spp.

A

Nystatin

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10
Q

Therapeutic usage of nystatin

A

Oropharyngeal thrush, vaginal candidiasis and intertriginous candidal infections

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11
Q

Pharmacokinetics of nystatin

A

use only as topical agent “swish and spit or swish and swallow”

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12
Q

MOA of azoles

A

inhibit lanosterol 14-demethylase leading to decreased ergosterol synthesis

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13
Q

Azole type with lesser degree of specificity causing higher drug interactions and side effects

A

Imidazole

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14
Q

Azole type with lower toxicity and less propensity to inhibit mammalian sterol synthesis

A

Triazole

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15
Q

Common effect of azole groups

A

Both groups affect CYP450 causing a drug-drug interaction

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16
Q

Azole with 3 nitrogen atoms with good oral absorption and high propensity to inhibit mammalian CYP450

A

Ketoconazole

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17
Q

Adverse effects of Ketoconazole

A

Reduction in testosterone synthesis and suppression of estradiol synthesis

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18
Q

Drugs that decrease absorption of ketoconazole

A

H2 blockers, PPI, and antacids

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19
Q

Drugs that decrease efficacy and induce metabolism of ketoconazole

A

Rifampicin
Phenobarbital
Carbamazepine
Phenytoin

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20
Q

Drugs that cause torsades des pointes with Ketoconazole

A

Terfenadine
Astemizole
Cisapride

21
Q

Fluorinated bistriazole that does not require an acidic environment

A

Fluconazole

22
Q

Only renal triazole

A

Fluconazole

23
Q

Therapeutic use of Fluconazole

A

Treatment and secondary prophylaxis of cryptococcal meningitis

24
Q

Adverse effects of fluconazole

A

reversible alopecia

25
Q

Synthetic triazole with 2 enantiomeric pairs each possessing 3 chiral centers

A

Itraconazole

26
Q

Therapeutic use for Itraconazole

A

For aspergillus; most systemic mycosis not associated with meningitis

27
Q

Drug of choice for paracoccidioidomycosis and chromomycosis

A

Itraconazole

28
Q

MOA of flucytosine

A

Inhibits thymidylate synthesis which is an important component of DNA

29
Q

Therapeutic use of flucytosine

A

Used as part of combination regimen with:
Amphotericin B for cryptococcal meningitis
Itraconazole for chromoblastomycosis

30
Q

Adverse effect of flucytosine

A

Bone marrow toxicity

31
Q

This anti-fungal drug is derived from Penicillium and is active against dermatophytes

A

Griseofulvin

32
Q

MOA of griseofulvin

A

Binds to microtubules leading to defective cell wall formation and binds to keratin protecting the skin from new infection

33
Q

Therapeutic use of griseofulvin

A

Oral fungistatic agent used in systemic treatment of dermatophytosis

34
Q

Water-soluble, semisynthetic lipopeptide synthesized from the fermentation product of Glurea lozonensis

A

Terbinafine

35
Q

MOA of terbinafine

A

noncompetitive inhibition of squalene monooxygenase to prevent ergosterol synthesis; squalene accumulation

36
Q

Adverse effect of terbenafine

A

Steven-Johnson Syndrome

37
Q

Topical used for ringworm, tinea versicolor, and mucocutaneous candidiasis

A

Triazoles

38
Q

Ketal triazole similar to ketoconazole and clotrimazole

A

Terconazole and Butoconazole

39
Q

Topical anti-fungal used for Candida vulvovaginitis

A

Tioconazole

40
Q

Topical anti-fungal used for common pathogenic dermatophytes

A

Oxiconazole, Sulconazole, Sertaconazole

41
Q

Topical anti-fungal that penetrates the stratum corneum and is found in effective concentration down to the mid-dermis

A

Econazole

42
Q

Topical anti-fungal where fungicidal concentration remains in the vagina for as long as 3 days

A

Clotrimazole

43
Q

Close chemical congener of econazaole that penetrates stratum corneum for more than 4 days

A

Miconazole

44
Q

Drug used to treat seborrheic dermatitis of the scalp

A

Ciclopirox olamine

45
Q

Halogenated phenolic ether used to treat tinea pedis, cruris, manuum, and versicolor

A

Haloprogin

46
Q

Thiocarbamate fungicidal ineffective against Candida and is associated with pruritus

A

Tolnaftate

47
Q

An allylamine that inhibits squalene 2,3-epoxidase that inhibits synthesis of ergosterol

A

Naftifine

48
Q

Drug used for treatment of tinea cruris and tinea corporis

A

Naftifine