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Spring Exam #3 - Antifungals
n/a
19
Pharmacology
Graduate
05/08/2010

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Term
amphotericin B (Amphotec)
Definition
Polyene macrolide;
MoA: binds to sterols in fungi, can also bind to kidney & erythrocytes;
Toxicities:
- fever & chills, renal, anemia;
Indications:
- sytemic: broad range;
- superficial: candidiasis;
- protozoal infections;
Term
ketoconazole (Nizoral)
Definition
imidazole;
MoA:
- inhibition of sterol 14-a-demethylase affects ergosterol biosynthesis & membrane function;
- Half-life: 7-8 hrs;
Toxicities:
- GI: N/V;
- endocrinologic abnormalities;
Indications:
- systemic: broad range EXCEPT Aspergillosis & Mucormycosis;
- superficial: Candidiasis and Ringworm;
Term
miconazole (Monistat)
Definition
imidazole;
MoA:
- inhibition of sterol 14-a-demethylase affects ergosterol biosynthesis & membrane function;
- Half-life: 12 hrs;
Toxicities:
- low toxicity;
Indications:
- Systemic: Coccidiomycosis, Cryptococcosis, Pseudo Elescheriasis;
- Superficial: Candidiasis;
Term
fluconazole (Diflucan)
Definition
triazole;
MoA:
- inhibition of sterol 14-a-demethylase affects ergosterol biosynthesis and membrane function;
- Half-life: 25-30 hrs;
Toxicities:
- low toxicity;
Indication:
- Systemic: broad range EXCEPT Aspergillosis & Mucormycosis;
- Superficial: Candidiasis;
Term
itraconazole (Sporanox)
Definition
triazole;
MoA:
- inhibition of sterol 14-a-demethylase affects ergosterol biosynthesis & membrane function;
- Half-life: 30 hrs;
Toxicity:
- low toxicity;
Indications:
- Systemic: broad range except Mucormycosis;
- Superficial: Candidiasis;
Term
griseofulvin (Fulvicin)
Definition
antibiotic produced by Penicillum grisofulvum;
MoA:
- disrupts cell mitotic apparatus, arrests cells in metaphase;
- deposited in Keratin precursor cells;
Toxicity:
- CNS: HA;
- GI: N/V;
- Hypersensitivity (rare);
Indications:
- dermatophytoses
Term
nystatin (Mycostatin)
Definition
polyene antibiotic;
MoA:
- binds to sterols of fungal cell membrane, cell leak;
Toxicity:
- low toxicity;
- hypersensitivity (rare);
Indications:
- Candidiasis;
Term
tolnaftate (Aftate, Dr. Scholl's, Tinactin, NP-27)
Definition
synthetic thiocarbamate;
MoA:
- inhibition of squalene monooxygenase affects ergosterol biosynthesis & membrane function;
Toxicities:
- low toxicity;
Indications:
- Dermatophytoses;
Term
terbinafine HCl (Lamisil)
Definition
synthetic allylamine;
MoA:
- inhibition of squalene monooxygenase affects ergosterol biosynthesis & membrane function;
Toxicity:
- low toxicity;
Indication:
- Dermatophytoses;
- Candidiasis;
Term
caspofungin (Cancidas)
Definition
semisynthetic lipopeptide;
MoA:
- blocks synthesis of (1,3)-d-glucan, a polysaccharaide of fungal cell wall;
Toxicity:
- fever, rash, N/V;
Indications:
- Systemic: Aspergillosis;
- Candidiasis (esophageal)
Term
Empiric Antifungal Therapy
Definition
Drugs of Choice: amphotericin B, miconazole;
Routinely used for:
- neutropenic pts, seriously ill pts;
Term
Prophylactic Antifungal Therapy
Definition
General Measures:
- maintenance of personal hygiene, hand washing, adhere to restricted diet of cooked foods, avoid invasive procedures;
Chemoprophylaxis:
- administer polyenes (Nystatin), amphotericin B, imidazoles (miconazole, ketoconazole), and triazoles (fluconazole, itraconazole);
Term
Drug Selection for Mild to Moderate Tinea infections
Definition
clotrimazole (Lotrimin);
miconazole (Fungold);
tolnaftate (Aftate, Tinactin);
Term
Drug Selection for Moderate-Severe Tinea infections
Definition
ketoconazole (oral, Nizoral);
miconazole (Monistat-Derm);
fluconazole (oral, Diflucan);
itraconazole (SporanoxR);
terbinafine (oral, Lamisil);
Term
Drug Selection for Severe Tinea Infections
Definition
griseofulvin (oral, Fulvicin);
ketoconazole (oral, Nizoral);
Term
Drug Selection for Tinea Versicolor
Definition
ketoconazole (oral Nizoral);
ketoconazole cream (Nizoral);
ketoconazole antidandruff shampoo;
miconazole (Monistat);
fluconazole (oral, Diflucan);
itraconazole (oral, Sporanox);
clotrimazole (Lotrimin);
Term
Drug Treatment for Cutaneous Candidiasis
Definition
amphotericin B (Amphotec);
ketoconazole cream 2% (Nizoral);
ketoconazole (oral, Nizoral);
miconazole (Micatin);
fluconazole (oral, Diflucan);
itraconazole (oral, Sporanox);
clotrimazole (Lotrimin);
nystatin (Mycostatin, Nilstat);
terbinafine (oral, Lamisil);
Term
Drug Therapy for Vulvovaginal Candidiasis
Definition
ketoconazole (oral, Nizoral);
miconazole (Monistat 3);
fluconazole (oral, Diflucan);
itraconazole (oral, Sporanox);
clotrimazole (Lotrimin);
nystatin (Mycostatin, Nilstat);
Term
Drug Therapy for Oropharyngeal Candidiasis
Definition
ketoconazole (oral, Nizoral);
fluconazole (oral, Diflucan);
itraconazole (oral, Sporanox);
clotrimazole (oral, Lotrimin);
nystatin (Mycostatin, Nilstat);
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