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Anit-fungal pharm
pharmacology of antifungals
| Question | Answer |
|---|---|
| Terbinafine | used in the treatment of dermatophytoses, is keratophilic and fungicidal |
| Terbinafine | interferes with ergosterol biosnynthesis |
| Terbinafine | adverse effects are rare and consitst of GI upset and headache |
| Voriconazole | well abosrbed orally, metabollized in the liver |
| Voriconazole | toxicities--> rash, elevated liver enzymes and transient visual disturbances |
| Itraconazole | absorption is increased by food, bioavailability is reduced when taken with rifamycins, poor CNS penetration |
| Itraconazole | used extensively in the treatment of dermatophytoses and onychomycosis |
| Flucytosine | inhibits thymidylate synthetase and thus pyrimidine and nucleic acid synthesis |
| Flucytosine | well absorbed orally, penetrates CNS, excreted by glomerular filtration, will accumulate in renal failure |
| Flucytosine | resistance develops rapidly, must be used in combination with other drugs |
| Flucytosine | depresses bone marrow function |
| Griseofulvin | binds to microtubules and prevents spindle formation and mitosis is in fungi |
| Griseofulvin | accumulates in skin, hair, and nails |
| Griseofulvin | adequately absorbed after oral administration, partially metabolized in liver, excreted in feces and urine |
| Griseofulvin | oral therapy for dermatophyte infection, used long term for hair and nail infection |
| Griseofulvin | well tolerated, rare CNS effects and hepatotoxicity |
| Nystatin | similar in structure and mechanism to amphotericin B |
| Nystatin | too toxic for systemic administration |
| Nystatin | used primarily for Candida infection of the skin, mucous membranes, and intestinal tract |
| Fluconazole | IV or Oral |
| Fluconazole | useful for oropharyngeal, isopharyngeal, and systemic candidiasis |
| Fluconazole | Penetrates CSF- drug of choice for cryptococcal meningitis |
| Ketoconazole | can be administered orally or topically; elevation of gastric pH impairs absorption |
| Ketoconazole | used systemically for certian mycoses, does not penetrate CSF, metabolized liver |
| Ketoconazole | no resistance, causes gastric upset, itching, rashes, and headache |
| Azoles | inhibits cytochrome P-450 mediated sterol demythelation of lanosterol to ergosterol |
| Azoles | broad spectrum antifungals, also inhibit many gram positive bacteria and some protozoa |
| Amphotericin B | adverse effects- Chills and fever (50%), impaired renal function (80%) |
| Amphotericin B | may also produce anaphylaxis, thrombocytopenia, severe pain, and seizures |
| Amphotericin B | used to treat the most severfungal infections including; candida albicans, histoplasma capsulatum, crytpococcus neoformins, coccidiodes unnutus, Asperigillis |
| Amphotericin B | resistance results from decreased membrane ergosterol or reduced Amphotericin binding, may be used in combined therapy with flucytosine |
| Amphotericin B | poorly absorbed from GI, given orally only for GI infection, 90% portien bound, eliminated through biliary, has poor CNS penetration, can be given intrathecally |
| Amphotericin B | binds to ergosterol, alters membrane permeability, may bind with mammel cholesterol and cause/ explain some adverse effects |
| MOA of nystatin | Bind ergosterol in fungal cell membrane |
| Toxicity of amphotericin | Nephrotoxicity |
| gynecomastia | SE seen only in men with administration of ketoconazole |
Created by:
swohlers
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