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Pharmacology- Katzung (Spring 2019) > Antifungal Drugs > Flashcards

Antifungal Drugs Flashcards

1
Q

Polyene antibiotics

A

Amphotericin B
Natamycin
Nystatin

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2
Q

Polyene antibiotics - MoA

A

Binds to ergosterol in cell membrane, increasing membrane permeability and leakage of cell contents

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3
Q

Amphotericin B - Clinical use

A

Systemic and subcutaneous mycoses
Superficial infections

Cryptococcal meningitis
Candidiasis
Coccidioidomycosis
Aspergillosis
Blastomycosis
Histoplasmosis
Mucormycosis 
Protozoa: leishmaniasis and amebic encephalitis
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4
Q

Amphotericin B - Adverse effects

A

Most toxic antibiotic today

Renal toxicity in 80%, it reduces the GFR and contributes to development of hypokalemia and hypomagnesemia

Azotemia (Accumulation of creatinine and urea in blood)

Acute liver failure
Cardiac arrhythmias (Ventricular fibrillation)

Hematopoietic disorders (anemia, leukopenia, thrombocytopenia)

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5
Q

Amphotericin B - Contraindications

A

Contraindicated for patients with renal impairment (should use lipid formulations for these patients)

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6
Q

Amphotericin B - Special considerations

A

Electrolytes should be monitored weekly during treatment

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7
Q

Amphotericin B - Interactions

A

Cyclosporine, antineoplasics, thiazides, corticosteroids: increased hypokalemia

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8
Q

Natamycin - Clinical use

A

Superficial mycoses of skin & mucous membranes

Aspergillus
Candida
Fusarium
Penicillum

Opthalmic suspension for the treatment of fungal blepharitis, conjunctivitis, or keratitis

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9
Q

Nystatin - Clinical use

A

Superficial mycoses of skin & mucous membranes

Candida (mucocutaneous, intestinal, vaginal)

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10
Q

Diazole derivatives

A

Clotrimazole
Econazole
Ketoconazole

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11
Q

Diazole derivatives - MoA

A

Inhibits ergosterol synthesis

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12
Q

Clotrimazole - Clinical use

A

Candidia infection in mouth, throat, vagina, vulva

M. furfur infection in skin (tinea versicolor)

Dermatophyte infections (tinea pedis and tinea cruris) due to epidermophyton, microsporum, trichophyton sp.

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13
Q

Econazole - Clinical use

A

Candidia and dermatophyte infections of skin

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14
Q

Ketoconazole - Clinical use

A

Seborrheic dermatitis

Inoperable cushing syndrome

Once-daily dose for chronic mucocutanous candidiasis

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15
Q

Diazole derivatives - Adverse effects

A 
Systemic administration can cause: 
Skin rash
Elevated liver enzyme levels
Hepatic injury 
Hematopoietic toxicity
GI distress
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16
Q

Azole derivatives - Interactions

A

Inhibits CYP3A4: inhibited metabolism of HMG-CoA reductase inhibitors, benzodiazepines, quinidine, warfarin

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17
Q

Triazole derivatives

A 
Fluconazole
Itraconazole
Posaconazole
Voriconazole
Isavuconazonium
Efinaconazole
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18
Q

Triazole derivative - MoA

A

Inhibition of ergosterol synthesis

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19
Q

Triazole derivates - Adverse effects

A 
Systemic administration can cause: 
Skin rash
Elevated liver enzyme levels
Hepatic injury 
Hematopoietic toxicity
GI distress
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20
Q

Fluconazole - Clinical use

A

Prevention of cryptococcal meninitis in patients with AIDS, and a follow-up therapy in patients successfully treated with amphotericin B to prevent relapse

Coccidioidal meningitis

Mucocutaneous (oropharyngeal and esophageal) and disseminated candidiasis such as endocardial candidiasis

UTIs by Candida

Vaginal candidiasis (single dose)
Inoperable cushing syndrome
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21
Q

Fluconazole - Contraindications

A

Contraindicated during first trimester of pregnancy because of increased risk of birth defects

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22
Q

Fluconazole - Special considerations

A

Only one that penetrates CSF well enough and for this reason, only fluconazole is used in the prophylaxis and treatment of fungal meningitis

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23
Q

Itraconazole - Clinical use

A 
Blastomycosis
Histoplasmosis
Onychomycosis (fungal infections of the nails)
Candidiasis
Coccidioidomycosis
Psuedallesheriasis
Sporotrichosis
24
Q

Which drug is contraindicated for treatment of onychomyscosis in patients with ventricular dysfunction?

A

Itraconazole

25
Q

Posaconazole - Clinical use

A

Enhanced act against Aspergillus and Candidia

Mucormycosis

Fusarium and zygomycetes such as Rhizopus and Mucor species

26
Q

Voriconazole - Clinical use

A

Enhanced act against Aspergillus and Candidia

Esophageal and invasive candidiasis

Cryptococcus, Fusarium, Coccidioides, Pseudallescheria

27
Q

Voriconazole - Adverse effects

A

Visual disturbances such as altered perception of light, abnormally colored vision (chromatopsia), and photophobia

Elevated serum levels of hepatic enzymes (enzymes should be monitored during treatment)

28
Q

Isavuconazonium - Clinical use

A

Enhanced activity against Aspergillus and Candida

Fusarium and zygomycetes such as Rhizopus and Mucor species

29
Q

Efinaconazole - Clinical use

A

Topical treatment of onychomycosis

30
Q

Allylamines

A

Naftifine

Terbinafine

31
Q

Allylamines - MoA

A

Inhibition of ergosterol synthesis

32
Q

Allylamines - Clinical use

A

Superficial dermatophyte infections.

Fungostatic for Candidia

Onychomycosis (Terbinafine)

33
Q

Echinocandin drugs

A

Caspofungin
Micafungin
Anidulafungin

34
Q

Echinocandin drugs - MoA

A

Inhibits fungal cell wall synthesis (noncompetitive inhibition of beta-1-3 glucan synthaze)

35
Q

Caspofungin - Clinical use

A

Candida, Aspergillus

Candida strains resistant to azole compounds

Esophageal, oropharyngeal, and invasive candidiasis

36
Q

Micafungin, Anidulafungin - Clinical use

A

Prophylaxis and treatment of candidiasis and invasive aspergillosis

37
Q

Fluorinated pyrimidine analogue

A

Flucytosine

38
Q

Flucytosine - MoA

A

Is incorporated into fungal RNA, interfering protein synthesis

39
Q

Flucytosine - Clinical use

A

Severe fungal infection in combination with amphotericin B

Candida, Cryptococcus

Endocarditis, pneumonia, meningitis, septicemia

40
Q

Flucytosine - Adverse effects

A

Hematologic toxicity

Cardiac arrest

41
Q

Flucytosine - Special considerations

A

Resistance to flucytosine is quickly developed, administered with amphotericin B

42
Q

Fungistatic antibiotic

A

Griseofluvin

43
Q

Griseofluvin - MoA

A

Disrupts microtubules function and mitosis in dermatophytes

44
Q

Griseofluvin - Clinical use

A

Dermatophytes including Epidermophyton, Microsporum, Trichophyton

Tinea capitis

45
Q

Griseofluvin - Adverse effects

A

Dizziness, headache, insomnia, GI bleeding, hepatitis, skin rash, leukopenia

46
Q

Griseofluvin - Interactions

A

Absorption is increased with high-fat meal

Induces CYP3A4: reducing plasma concentrations of warfarin, oral contraceptives, barbiturates.

47
Q

Pyridine compound

A

Ciclopirox

48
Q

Ciclopirox - Clinical use

A

Skin infections by C. albicans, M. furfur

Tinea versicolor by M. furfur

Onychomycosis

49
Q

Thiocarbamate drug

A

Tolnaftate

50
Q

Tolnaftate - Clinical use

A

Tinea versicolor and mild dermatophyte infections of the skin

51
Q

Polyene antibiotics - Administration

A

Topical: All of them
Oral: Nystatin
IV, intrathecal or intraventricular: Amphotericin B

52
Q

Azole derivatives - Administration

A

Oral: All except Clotrimazole and Econazole
Topical: Clotrimazole, Econazole and Ketoconazole
IV: Fluconazole, Posaconazole, Voriconazole

53
Q

Allylamine drugs - Administration

A

Topical: Both
Oral: Terbinafine

54
Q

Other Antifungal drugs - Administration

A

IV: Caspofungin
Topical: Ciclopirox, Tolnaftate
Oral: Flucytosine, Griseofulvin

55
Q

Which drugs are used for cushing syndrome?

A

Ketoconazole

Fluconazole

56
Q

Which drugs are used for the treatment of onychomycosis?

A

Itraconazole
Terbinafine
Efinaconazole
Ciclopirox

Pharmacology- Katzung (Spring 2019) (52 decks)

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