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
Posaconazole - Clinical use
Enhanced act against Aspergillus and Candidia Mucormycosis Fusarium and zygomycetes such as Rhizopus and Mucor species
26
Voriconazole - Clinical use
Enhanced act against Aspergillus and Candidia Esophageal and invasive candidiasis Cryptococcus, Fusarium, Coccidioides, Pseudallescheria
27
Voriconazole - Adverse effects
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
Isavuconazonium - Clinical use
Enhanced activity against Aspergillus and Candida Fusarium and zygomycetes such as Rhizopus and Mucor species
29
Efinaconazole - Clinical use
Topical treatment of onychomycosis
30
Allylamines
Naftifine | Terbinafine
31
Allylamines - MoA
Inhibition of ergosterol synthesis
32
Allylamines - Clinical use
Superficial dermatophyte infections. Fungostatic for Candidia Onychomycosis (Terbinafine)
33
Echinocandin drugs
Caspofungin Micafungin Anidulafungin
34
Echinocandin drugs - MoA
Inhibits fungal cell wall synthesis (noncompetitive inhibition of beta-1-3 glucan synthaze)
35
Caspofungin - Clinical use
Candida, Aspergillus Candida strains resistant to azole compounds Esophageal, oropharyngeal, and invasive candidiasis
36
Micafungin, Anidulafungin - Clinical use
Prophylaxis and treatment of candidiasis and invasive aspergillosis
37
Fluorinated pyrimidine analogue
Flucytosine
38
Flucytosine - MoA
Is incorporated into fungal RNA, interfering protein synthesis
39
Flucytosine - Clinical use
Severe fungal infection in combination with amphotericin B Candida, Cryptococcus Endocarditis, pneumonia, meningitis, septicemia
40
Flucytosine - Adverse effects
Hematologic toxicity | Cardiac arrest
41
Flucytosine - Special considerations
Resistance to flucytosine is quickly developed, administered with amphotericin B
42
Fungistatic antibiotic
Griseofluvin
43
Griseofluvin - MoA
Disrupts microtubules function and mitosis in dermatophytes
44
Griseofluvin - Clinical use
Dermatophytes including Epidermophyton, Microsporum, Trichophyton Tinea capitis
45
Griseofluvin - Adverse effects
Dizziness, headache, insomnia, GI bleeding, hepatitis, skin rash, leukopenia
46
Griseofluvin - Interactions
Absorption is increased with high-fat meal Induces CYP3A4: reducing plasma concentrations of warfarin, oral contraceptives, barbiturates.
47
Pyridine compound
Ciclopirox
48
Ciclopirox - Clinical use
Skin infections by C. albicans, M. furfur Tinea versicolor by M. furfur Onychomycosis
49
Thiocarbamate drug
Tolnaftate
50
Tolnaftate - Clinical use
Tinea versicolor and mild dermatophyte infections of the skin
51
Polyene antibiotics - Administration
Topical: All of them Oral: Nystatin IV, intrathecal or intraventricular: Amphotericin B
52
Azole derivatives - Administration
Oral: All except Clotrimazole and Econazole Topical: Clotrimazole, Econazole and Ketoconazole IV: Fluconazole, Posaconazole, Voriconazole
53
Allylamine drugs - Administration
Topical: Both Oral: Terbinafine
54
Other Antifungal drugs - Administration
IV: Caspofungin Topical: Ciclopirox, Tolnaftate Oral: Flucytosine, Griseofulvin
55
Which drugs are used for cushing syndrome?
Ketoconazole | Fluconazole
56
Which drugs are used for the treatment of onychomycosis?
Itraconazole Terbinafine Efinaconazole Ciclopirox