Term
What antifungal agent binds to ergosterol in fungal cell membranes? |
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Definition
Polyenes:
Amphotericin B
allows leakage of small molecules |
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Term
What are the 2 different formulations of Amphotericin B? |
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Definition
Non-Lipid Based - (Deoxycholate)
Three lipid-based forms - (Abelcet, AmBisome, Amphotec) |
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Term
How is Amphotericin B administered? What is it bound to in the Plasma? |
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Definition
Primarily used IV 90% bound to B-lipoprotein |
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Term
What adverse side effect of Amphotericin B is potentiated by sodium depletion? |
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Definition
Nephrotoxicity Reversible at normal dose Residual damage at high doses |
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Term
What can be done to treat/prevent Fever and chills caused by Amphotericin B? |
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Definition
Premedicate with steroids or antipyretic
Merperidine may help abort if already started |
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Term
What 5 Adverse effects can Amphotericin B cause? |
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Definition
Nephrotoxicity Thrombophlebitis at injection site Fever and Chills Hypersensitivity Reaction Shock-like hypotension |
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Term
What are the therapeutic uses for Amphotericin B? |
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Definition
Candida albicans Histoplasmosis Cryptococcus Aspergillus Blastomyces
Deep Fungal infxns in Pregnant woman |
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Term
What is the preferred treatment for deep fungal infections in Pregnancy? |
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Definition
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Term
What antibiotic inhibits thymidylate synthase and DNA synthesis? |
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Definition
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Term
What drug is 5-Flucytosine almost always used in combination with? |
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Definition
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Term
How is 5-Flucytosine activated in cell? |
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Definition
5-Flucytosine --cytosine deaminase--> 5-FU --UMP pyrophosphorylase--> 5-FUMP --ribonudleotide reductase--> 5-FdUMP --> inhibits thymidylate synthase |
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Term
How does resistance develop to 5-Flucytosine? |
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Definition
Lack of permease
Defective or decreased cytosine deaminase |
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Term
What antifungal agents inhibit synthesis of ergosterol? |
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Definition
Azoles:
Voriconazole
Ketoconazole |
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Term
What organisms are the Azoles active against? |
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Definition
Yeasts (Candida) Dermatophytes (Epidermophyton) Systemic mycoses (Histoplasma) |
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Term
What azole can cause visual disturbances? |
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Definition
Voriconazole (Transient, blurred vision, photophobia, altered perception of color or image) |
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Term
How should Voriconazole be administered in patients with creatinine clearance <50? |
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Definition
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Term
What organisms is Voriconazole used for? |
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Definition
Invasive aspergillosis Scedosporium Fusarium Invasive fluconazole-resistant Candida |
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Term
What Azole has a common side effect of anorexia, nausea, and vomiting? |
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Definition
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Term
What adverse side effects occur with Ketoconazole? |
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Definition
Decrease plasma testosterone conc. Gynecomastia decreased libido and loss of potency in men Menstrual irregularities in women Adrenal steroidogenesis inhibited with high doses |
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Term
What Azoles have hepatic elimination? |
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Definition
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Term
What antifungals should be used to treat Blastomycosis and Histoplasmosis? |
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Definition
Amphotericin B - life threatening infections |
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Term
What antifungals should be used to treat Cryptococcus? |
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Definition
Amphotericin B +/- 5-Flucytocine |
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Term
What antifungals should be used to treat superficial/mucosal Candida Albicans? |
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Definition
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Term
What antifungals should be used to treat disseminated Candida albicans? |
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Definition
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Term
What antifungals should be used to treat Non-albicans candidiasis? (Torulopsis glbrata, Candida krusei) |
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Definition
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Term
What antifungal inhibits squalene epoxidase, necessary for egosterol synthesis? |
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Definition
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Term
What drug concentrates in the hair and nail beds? |
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Definition
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Term
What drug has an adverse side effect of occasional taste disturbance? |
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Definition
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Term
What are the frequent side effects of Terbinafine? |
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Definition
Headache and GI disturbance |
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Term
What is the treatment of Onychomycosal fungal infections? (ringworm of the nails) |
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Definition
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Term
What antifungal disrupts mitotic spindle structures of fungal cells? |
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Definition
Griseofulvin (Fungistatic) |
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Term
Where is Griseofulvin deposited in the body? How is it absorbed? |
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Definition
Keratin precursor cells
well absorbed with ultramicro size form and fatty meal |
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Term
What antifungal is used to treat Dermatophytes? (Epidermophyton, Micosporum, Trichophyton) |
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Definition
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Term
What drugs does Griseofulvin accelerate the metabolism of? |
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Definition
Coumarin Estrogens Oral contraceptives |
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Term
What is the 1st line therapy for M. tuberculosis? |
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Definition
Isoniazid + rifampin + pyrazinamide + ethambutol or streptomycin |
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Term
What is the 1st line therapy for M. Avium complex? |
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Definition
Clarithromycin + ethambutol or clofazimine or ciprofloxacin or amikacin |
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Term
What are the drugs used for Mycobacterum tuberculosis? |
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Definition
Isoniazid Rifampin Ethambutol |
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Term
What TB drug interferes with mycolic acid synthesis? |
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Definition
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Term
What cells is Isoniazid Cidal for? What is it static for? |
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Definition
Cidal - rapidly dividing bacilli (extracellular cavitary lesions)
Static for slow growing (closed caseous lesions and macrophages) |
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Term
What does Isoniazid compete with that can cause Peripheral neuropathy? Who is it more frequent in? How is treated? |
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Definition
pyridoxal phosphate
More frequent in malnourished, diabetics, and alcoholics Corrected with vitamine B6 supplements |
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Term
What causes Hepatotoxicity from Isoniazid use? |
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Definition
Due to toxic metabolite from acetylation of isoniazid |
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Term
What drug interactions does Isoniazid have? |
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Definition
Antacids w/ Al+++ decrease absorption Corticosteriods decrease efficacy Inhibits P450 for phenytoin |
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Term
What is the complex relationship between Isoniazid and Corticosteriods? |
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Definition
Prednisone reduces plasma conc of INH INH inhibits the hepatic metabolism of cortisol |
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Term
What TB drug inhibits RNA synthesis by binding Beta subunit of RNA polymerase? |
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Definition
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Term
What is the absorption of Rifampin imparied by? |
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Definition
Food or para-aminosalicylic acid |
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Term
What TB drug has an adverse side effect of orange-red tears, urine, and saliva? |
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Definition
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Term
What drug interactions does Rifampin have? |
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Definition
P450 inducer (oral anticoagulants and contracepives less effective) Probenecide increases rifampin serum concentrations |
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Term
What is the first line therapy against mycobacterium tuberculosis? |
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Definition
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Term
What else, besides TB, is Rafampin used for? |
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Definition
MRSA and S. epidermidis (w/ vancomycin or gentimicin) Prophylactic against meningitis by meningococci or H. influenzae Eradication of staph in nasal carriers Antileprosy |
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Term
What TB drug has an adverse reaction of Optic Neuritis? |
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Definition
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Term
What TB drugs can cause Hyperuricemia? |
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Definition
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