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Antifungal Drugs
AUA Pharm 4
| Question | Answer |
|---|---|
| Name a Polyene Antifungal | Amphotericin B |
| Use of Amphotericin B | IV for serious life-threatening infections: Aspergillus, Candida, Cryptococcus, Histoplasma |
| Mechanism of Action of Amphotericin B | Binds to ergosterol |
| Side effects of Ampho B (Dose) | Nephrotoxic, Hypokalemia, Normochromic normocytic anemia |
| Side effects of Ampho B (Influsion) | Flu-like symptoms |
| Why do you premedicate patients on Ampho B and for what? | To avoid flu-like symptoms that are infusion dependent. You premedicate with antipyretic, antihistaminic, and antiemetic agents |
| Does Ampho B penetrate the CNS? | Yes, but with extremely low penetration. However, it does not cross blood brain barrier so you have to give it intrathecally |
| Does Ampho B have any drug interactions? | Synergistic with flucytosine |
| Flucystosine is used for? | Resistant Cryptococcus and candidiasis |
| What causes resistant cryptococcus and candidiasis? | decreased ergosterol levels |
| Use of Nystatin | Topically for Candidiasis. CANNOT USE SYSTEMICALLY --> Too toxic. |
| Name -Azole Antifungals | Ketoconazole, fluconazole, itraconazole, clotrimazole, miconazole |
| How do -Azole antifungals work? | block synthesis of ergosterol by inhibiting 14 alpha demethylase in the fungal 450 complex |
| How does resistance to -azole antifungals occur? | decrease intracellular levels of drugs |
| What are -azole antifungals used for? | Candidiasis, coccidiomycosis, paracoccidiomycosis, blastomycosis, and histoplasmosis. |
| Indications of clotrimazole and miconazole and method of administration | given topically for candida and dermatophytic infections |
| side effects of ketoconazole | gynecomastia and decreased libido as well as menstrual irregularities |
| the side effects of ketoconazole mimic the side effects to which other drugs? | spironolactone |
| Does fluconazole penetrate the CSF? | Yes |
| Does itraconazole penetrate the CSF? | No |
| Antifungals with limited indications | Griseofulvin, Terbinafine, and Flucytosine |
| MOA of Griseofulvin | Disruption of mitotic spindle by interfering with microtubules |
| Griseofulvin used for? | tinea cruris (jock itch) |
| a 27 y/o patient noticed increased effects of his griseofulvin. what may have caused this? | alcohol |
| when is griseofulvin contraindicated? | intermittent porphyria |
| MOA of Terbinafine | Inhibits squalene epoxidase |
| Indication of terbinafine? | onychomycosis (nail fungal infection) |
| side effects of terbinafine? | elevated liver function tests |
| MOA of Flucytosine | inhibits thymidylate synthetase to decrease thiamine |
| Flucytosine + Ampho B indicated in? | severe candidiasis in immunocompromised patients |
| Side effects of flucytosine? | decrease bone marrow, leukopenia, thrombocytopenia, severe enterocolitis, and hepatitis. |