Term
| What are two categories of superficial mycoses? |
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Definition
| Dermatophytes and Candidiasis (Candida albicans) |
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Term
| What are three dermatophyte infections? |
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Definition
| 1. tinea infections. 2. ringworm. 3. onychomycosis (Trichophyton rubrum). |
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Term
| What are five types of systemic mycoses? |
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Definition
| 1. Candidiasis. 2. Aspergilliosis. 3. Blastomycosis. 4. Histoplasmosis. 5. Coccidiomycosis. |
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Term
| What is the difference between human and fungal cell membranes? |
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Definition
| human cell membranes have cholesterol, fungal cell membranes have ergosterol |
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Term
| How do most antifungal drugs work? |
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Definition
| either bind selectively to ergosterol or inhibit P450-mediated ergosterol synthesis. *organ toxicities and drug interactions directly related to cross-over effect on human cells* |
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Term
| What are the 4 main categories of antifungals and which is the most common? |
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Definition
1. Azoles. (most common) 2. Allylamines. 3. Polyenes. 4. Echinocandins. |
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Term
| What kind of antifungal are Clotrimazole and Miconazole? |
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Definition
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Term
| What kind of antifungal are Ketoconazole (Nizoral), *Fluconazole (Diflucan), Itraconazole, and Voraconazole (Vfend)? |
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Definition
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Term
| What kind of antifungal is Terbinafine (Lamisil)? |
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Definition
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Term
| What kind of antifungal are Amphotericin B and Nystatin? |
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Definition
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Term
| What kind of antifungal are Caspofungin, Micafungin, and Anidulafungin? |
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Definition
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Term
| What are two miscellaneous antifungals? |
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Definition
| Griseofulvin and Flucytosine |
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Term
| What are 6 considerations when choosing an antifungal? |
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Definition
1. site of infection. 2. spectrum of activity. 3. immunocompetence. 4. adverse reaction profile. 5. drug interactions. 6. cost. |
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Term
| What is the MOA of azoles? |
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Definition
| block ergosterol biosynthesis and inhibit cytochrome P450 dependent lanosterol C14-demethylase |
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Term
| What is the dose limiting toxicity of azoles? |
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Definition
| liver failure - monitor LFTs |
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Term
| What is the pregnancy category for azoles? |
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Definition
| Category C - except Voraconazole which is Category D, avoid during pregnancy |
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Term
| What are 3 concerns with azoles? |
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Definition
| drug interactions, cholesterol synthesis, cell toxicity |
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Term
| How do you treat tinea infections? |
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Definition
1st - Clotrimazole (Lotrimin AF) OTC. 2nd - Miconazole (Desenex) OTC. 3rd - Econazole (Spectazole), oxiconazole (Oxistat), sertaconazole (Ertaczo) Rx |
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Term
| How do you treat vulvovaginal candidiasis? |
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Definition
| *specially formulated creams, tablets, suppositories* OTC - clotrimazole, miconazole. Rx - econazole, terconazole, fluconazole (Diflucan) |
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Term
| Which drug was the first azole antifungal, has less specific affinity for fungal P450 enzyme, is only for superficial dermatophytes, and relies on gastric acidity for absorption? |
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Definition
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Term
| What are 4 adverse reactions of Ketoconazole (Nizoral)? |
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Definition
| GI upset (20-50%), rash, inhibition of adrenal steroid synthesis, hepatotoxic potential |
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Term
| What drug interaction is Ketoconazole (Nizoral) involved with? |
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Definition
| potent inhibitor of CYP3A4 |
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Term
| Which drug is the most common prescription azole for Candida infections, has a large volume of distribution (even to CSF, eye, urine), is renally eliminated, and is the best tolerated azole? |
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Definition
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Term
| How do you treat vulvovaginal candidiasis using Fluconazole (Diflucan)? |
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Definition
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Term
| What are 4 adverse reactions of fluconazole (Diflucan)? |
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Definition
| GI (5-10%), rash, h/a, alopecia |
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Term
| What drug interactions are fluconazole (Diflucan) involved in? |
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Definition
| potent inhibitor of CYP2C9 and moderate inhibitor of CYP3A4 |
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Term
| Which drug has a greater spectrum than fluconazole, including activity against Aspergillus, and has 60% greater absorption with solution than capsules? |
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Definition
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Term
| What are 4 adverse rxns of Itraconazole (Sporanox)? |
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Definition
| GI (20%), taste disturbances, elevated liver enzymes, rare heart failure with long tx |
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Term
| What drug interaction is Itraconazole (Sporanox) involved with? |
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Definition
| potent inhibitor of CYP3A4 |
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Term
| Which drug has similar spectrum of activity as itraconazole but better against Aspergillus, has oral and IV forms, and is indicated for invasive candidiasis and aspergillus? |
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Definition
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Term
| What are 4 adverse rxns of Voriconazole (Vfend)? |
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Definition
| transsient vision disturbances (30%), rash, photosensitivity, hallucinations |
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Term
| What drug interactions are voriconazole (Vfend) involved with? |
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Definition
| inhibits CYP2C9, 2C19, and 3A4 |
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Term
| What is the relationship between Voriconazole and Phenytoin? |
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Definition
| Vfend is metabolized by and inhibits CYP2C19 and Phenytoin is metabolized by and induces CYP2C19. SO phenytoin toxicity and/or antifungal failure are your consequences |
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Term
| Which drug has similar spectrum of activity to itraconazole but better against zygomycetes such as Mucor, is available as oral suspension that must be taken with high fat meals, and is reserved for moderate fungal infections resistant to oral itraconazole? |
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Definition
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Term
| What drug interaction is Posaconazole (Noxafil) involved with? |
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Definition
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Term
| What type of antifungals disrupt synthesis of glucan polymers in cell wall, are given IV qd, and are alternatives to azole antifungals for Candida and Apergillus? |
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Definition
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Term
| What are the adverse rxns of echinocandins? |
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Definition
| fever, phlebitis at infusion site, and elevated LFTs |
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Term
| How do you treat onychomycosis with Itraconazole (Sporanox)? |
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Definition
| pulse therapy: 400mg/day for 7 days/month for 2 (fingernails) to 4 (toenails) months |
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Term
| Which drug blocks ergosterol synthesis, is indicated for onychomycosis, is pregnancy category B and inhibits CYP2D6? |
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Definition
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Term
| What are the adverse rxns of Terbinafine (Lamisil)? |
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Definition
| Common: GI upset, h/a, rash. Less common: hepatotoxicity, Stevens-Johnson syndrome, blood dyscrasias, taste disturbance |
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Term
| How do you treat onychomycosis with Terbinafine (Lamisil)? |
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Definition
| 250mg/day for at least 6 (fingers) to 12 (toenails) weeks. Drug levels can persist in nails for 30 weeks. Usually more effective than intraconazole. |
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Term
| Which drug binds directly to ergosterol, is drug of choice for many systemic fungal infections (usually Candida), is given as slow IV infusion or bladder irrigation, and is the preferred drug for deep fungal infections in pregnancy? |
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Definition
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Term
| What are the adverse rxns of Amphotericin B? |
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Definition
| Infusion related: fever, chills, n/v, h/a, myalgias. Nephrotoxicity secondary to afferent arteriole constriction. Hypokalemia secondary to renal tubule toxicity. |
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Term
| How can you reduce acute adverse rxns of Ampotericin B? |
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Definition
| use lipid formulations. (ABLC, AmBisome, Amphotec) |
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Term
| How can you prevent infusion related rxns and nephrotoxicity from AmpB? |
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Definition
| Infusion related: prophylaxis with NSAIDs, hydrocortisone, diphenhydramine. Nephrotoxicity: prophylaxis with 250ml NS IV infusion |
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Term
| What is an older polyene antifungal used in OTC topical creams and ointments and is sometimes given as oral suspension for oral thrush? |
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Definition
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Term
| What is an older antifungal for dermatophyte inf, and is better absorbed with high fat meals but has poor tolerance d/t allergic rxns, photosensitivity, GI distress and neuro effects? |
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Definition
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Term
| Which drug is used in IV form for severe systemic infections with AmpB, is converted to 5-flurouracil intracellularly and is very toxic? |
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Definition
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