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Anti Fungal par Mind Map: Anti Fungal

1. Drugs for systemic infections

1.1. polyene macrolides

1.1.1. Amphotericin B 4 formulas C-AMB L-AMB ABLC ABCD mechanism binds to ergosterol in the cell membrane only binds to fungal sterol, not human cholesterol pharmacokinetics NOT absorbed orally, only IV PPB more than 90% long half life (15 days) does is 5mg/kg does for C-AMB is 0.6mg/kg advantages life saving drug high anti fungal activity broad anti fungal spectrum fungicidal activityh negligible fungal resistance disadvantages nephrotoxicity fever and chills other side effects azotemia (elevation of BUN) in 80% of patients anemia therapeutic uses all life threatening fungal infections patients with severe neutropenia and fever that did not respond to antibacterial agents for 5-7 days

1.2. pyrimidine antimetabolites

1.2.1. flucytosine mechanism impairs DNA synthesis spectrum cryptococcus neoformans some candida pharmacokinetics complete & rapid absorption orally minimal PPB volume of distribution about total body water 1-2 hours to active peak plasma concentration dose is 50-150mg/kg/day (dividid by 4 doses) 80% excreted in urine unchanged half life 3-6 hours dose reduced with renal failure therapeutic uses in combination with AMB in combination with fluconazole adverse effects common bone marrow depression

1.3. azoles

1.3.1. Imidazoles & triazoles mechanism inhibit fungal growth spectrum broad anti fungal spectrum types fluconazole itraconazole posaconazole voriconazole general, common adverse effects nausea vomiting diarrhea headach abdominal pain

1.4. echinocandins

1.4.1. general features active against candidiasis and aspergillus (including the resistant to azoles) act by inhibiting synthesis of beta glucan (important for the cell wall) which causes cell lysis given IV only (not absorbed orally)

1.4.2. types caspofungin metabolism therapeutic use dose micafungin metabolism therapeutic use dose anidulafungin treatment of esophageal candidiasis 100mg followed by 50mg daily

1.5. allylamines

1.5.1. terabinafine inhibits synthesis of ergosterol pharmacokinetics well absorbed orally but goes first pass metabolism (bioavailability 40%) PPB 99% accumulated in skin, nails, and fat initial half life is 12 hours but extends to 200-400 hours in steady state therapeutic uses onychomycosis candidiasis dermatophytosis pityriasis tinea capitis adult oral dose is 250mg daily

2. Drugs for topical infections

2.1. systemic drugs

2.1.1. griseofulvin inhibits mitosis by binding to tubulin effective in topical dermatophytosis trichophytin microsporum epidermophyton dosing (oral) children adults adverse effects nausea vomiting diarrhea dry mouth headache peripheral neuritis vertigo lethargy blurred vision hepatotoxicity neutopenia leucopenia

2.1.2. lodide

2.2. topical drugs

2.2.1. nystatin same action of AMB obtained from streptomyces noursei only topically due to to hight systemic toxicity used for vaginal candidiasis

2.2.2. haloprogin halogenated phenolic ether spectrum epidermophyton trichophyton microsporum pityrosporum candida therapeutic use tinea pedis tinea cruris tinea corporis tinea manuum tinea versicolor twice a day on infected skiing for 2-4 weeks

2.2.3. tolnaftate treatment of most cutaneous mycoses trichophton rubrum t. mentagrophytes t. tonsurans e. floccosum microsporum gypseum m. canis m. audouinii m. furfur 1% preparation

2.2.4. naftifine inhibits biosynthesis of ergosterol broad spectrum 1% cream or gel used for tinea curis tinea corporis cutaneous candidiasis tinea versicolor

2.2.5. imidazoles miconazole 2% and 4% vaginal cream used for or vaginal suppositories at bed time adverse effects econazole deschloro derivative or miconazole penetrates the stratum corneum - found in the mid dermis less than 1% in blood 1% cream used for clotrimazole systemic absorption used for remains in vagina for 3 days after application available as adverse effects butoconazole similar to clotrimazole 2% vaginal cream slower response during pregnancy, so a 6 days course is recommended in 2nd and 3rd trimester tioconazole for vulvovaginal candidiasis single dose of 300mg at bed time