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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 and 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 and 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 and Triazole 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

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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20
Q

Fluconazole - Contraindications

A

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

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21
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

22
Q

Itraconazole - Clinical use

A 
Blastomycosis
Histoplasmosis
Onychomycosis (fungal infections of the nails)
Candidiasis
Coccidioidomycosis
Psuedallesheriasis
Sporotrichosis
23
Q

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

A

Itraconazole

24
Q

Posaconazole - Clinical use

A

Enhanced act against Aspergillus and Candidia

Mucormycosis

Fusarium and zygomycetes such as Rhizopus and Mucor species

25
Voriconazole - Clinical use
Enhanced act against Aspergillus and Candidia Esophageal and invasive candidiasis Cryptococcus, Fusarium, Coccidioides, Pseudallescheria
26
Voriconazole - Adverse effects and Interactions
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) Caspofungin: additive activity for invasive aspergillosis
27
Isavuconazonium - Clinical use
Enhanced activity against Aspergillus and Candida Fusarium and zygomycetes such as Rhizopus and Mucor species
28
Efinaconazole - Clinical use
Topical treatment of onychomycosis
29
Allylamines
Naftifine | Terbinafine
30
Allylamines - MoA
Inhibition of ergosterol synthesis
31
Allylamines - Clinical use
Superficial dermatophyte infections. Fungostatic for Candidia Onychomycosis (Terbinafine)
32
Echinocandin drugs
Caspofungin Micafungin Anidulafungin
33
Echinocandin drugs - MoA
Inhibits fungal cell wall synthesis (noncompetitive inhibition of beta-1-3 glucan synthaze)
34
Caspofungin - Clinical use
Candida, Aspergillus Candida strains resistant to azole compounds Esophageal, oropharyngeal, and invasive candidiasis
35
Micafungin, Anidulafungin - Clinical use
Prophylaxis and treatment of candidiasis and invasive aspergillosis
36
Fluorinated pyrimidine analogue
Flucytosine
37
Flucytosine - MoA
Is incorporated into fungal RNA, interfering protein synthesis
38
Flucytosine - Clinical use
Severe fungal infection in combination with amphotericin B Candida, Cryptococcus Endocarditis, pneumonia, meningitis, septicemia
39
Flucytosine - Adverse effects
Hematologic toxicity | Cardiac arrest
40
Flucytosine - Special considerations
Resistance to flucytosine is quickly developed, administered with amphotericin B
41
Fungistatic antibiotic
Griseofluvin
42
Griseofluvin - MoA
Disrupts microtubules function and mitosis in dermatophytes
43
Griseofulvin - Clinical use
Dermatophytes including Epidermophyton, Microsporum, Trichophyton Tinea capitis
44
Griseofulvin - Adverse effects
Dizziness, headache, insomnia, GI bleeding, hepatitis, skin rash, leukopenia
45
Griseofulvin - Interactions
Absorption is increased with high-fat meal Induces CYP3A4: reducing plasma concentrations of warfarin, oral contraceptives, barbiturates.
46
Pyridine compound
Ciclopirox
47
Ciclopirox - Clinical use
Skin infections by C. albicans, M. furfur Tinea versicolor by M. furfur Onychomycosis
48
Thiocarbamate drug
Tolnaftate
49
Tolnaftate - Clinical use
Tinea versicolor and mild dermatophyte infections of the skin
50
Which drugs are used for cushing syndrome?
Ketoconazole | Fluconazole
51
Which drugs are used for the treatment of onychomycosis?
Itraconazole Terbinafine Efinaconazole Ciclopirox

Pharmacology (55 decks)

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