Pharm- antifungal therapy Flashcards
Amphotericin B
MECHANISM: Binds ergosterol (unique to fungi); forms membrane pores that allow leakage of electrolytes
CLINICAL USE: Serious systemic mycoses. Intrathecally for fungal menigngitis. Supplement K and Mg because fo altered renal tubule permeability
TOXICITY: Fever/chills, hypotension, nephrotoxicity, arrhythmias, anemia, IV phlebitis. Hydration decreases nephrotoxicity
Nystatin
MECHANISM: Binds ergosterol- forms membrane proes that allow leakage of electrolytes
CLINICAL USE: “Swish and swallow” for oral canidiasis (thrush); topical for diaper rash or vaginal canidiases
Flucytosine
MECHANISM: Inhibits DNA and RNA biosynthesis by conversion to 5-fluoruracil by cytosine deaminase
CLINICAL USE: Systemic fungal infections (especially Cryptococcus meningitis) in combo with amp B
TOXICITY: Bone marrow suppression
Clotrimazole, fluconazole, intraconazole, ketoconazole, miconazole, voriconazole
CLASS: Azoles
MECHANISM: Inhibit fungal sterol( ergosterol) synthesis by inhibiting the cytochrome P-450 enzyme that converts lanosterol to ergosterol
CLINICAL USE: Local and less serious systemic mycoses.
TOXICITY: Testosterone synthesis inhibition ( gynecomastia, especially with ketoconazole) liver dysfunction ( inhibits cytochrome P-450)
Chronic suppression of cryptococcal meningitis in AIDS pateints and candial infections of all types
Fluconazole
Blastomyces, Coccidioides, Histoplasma
Intraconazole
Azoles for topical fungal infections
Clotrimazole and miconazole
Terbinafine
MECHANISM: Inhibits the fungal enzyme squalene epoxidase
CLINICAL USE: Dermatophytoses (especially onychomycosis- funal infection of giner or toe nails)
TOXICITY: GI upset, headaches, hepatotoxicity, taste disturbance
Anidulafungin, caspofungin, micafungin
CLASS: Echinocandins
MECHANISM: Inhibit cell wall synthesis by inhibiting synthesis of B-glucan
CLINICAL USE: Invasive aspergillosis, Canidia
TOXICITY: GI upset, flushing ( by histamine release)
Griseofulvin
MECHANISM: Interferes with microtubule function; disrupts mitosis. Deposits in keratin-containing tissues ( nails)
CLINICAL USE: Oral treatment of superficial infections; inhibits growth of dermatophytes ( tinea, rightworm)
TOXICITY: Teratogenic, carinogenic, confusion, headaches, ^ cytochrome P-450 and warfarin metabolism
Pyrimethamine
antiprotozoan therapy that treats TOXOPLASMOSIS
Suramin and melarsoprol
antiprotozoan therapy that treats Trypansoma brucei
Nifurtimox
antiprotozoan therapy that treats T. cruzi
Sodium stibogluconate
Antiprotozoan therapy that treats leishmaniasis
Permethrin, malathion, lindane
used to treat scabies (Sarcoptes scabiei) and lice (pediculus and Pthirus)
Permethrin (blocks Na channels leading to neurotoxicity)
lindane ( blocks GABA channals leading to neurotoxicity)
malathion (acetylcholinesterase inhibitor)
