What is mycosis ? And how to treat it - fungal infections and DOC 👇
Infectious diseases caused by fungi called Mycosis….cell wall composed of chitin…Contain Ergosterol
Cutaneous Mycosis/Epidermis= Superficial infection invoving skin …
Drugs for Subcutaneous & Systemic inections
Amphotericin B (Fungicidal/Fungistatic)
From S.nodosus DOC in Systemic mycosis…
MOA
bind to Ergosterol...form pore… Allowing leak of Electrolytes & small molecules…cell death
Antifungal spectrum
activity against Candida albican, Histoplasma capsulatum,Cryptococcus neoforamans, Coccidicoides immitis, Blastomyces dermatitidis, Apergillus
P.K
insoluble in water, Deoxycholate added to form colloidal suspension ↓Nephrotoxicity. …
Liposome formulation AMBISOME, AMPHOTECT, ABELCET…
S.E
fever & chills, Thrombophlebitis, Nephrotoxicity, Hypotension, normocytic anemia exacerbate in HIV pt receiving Zidovudine
Flucytosine (Fungistatic)
Pyrimidine metabolite.
MOA
5-FC enter via Cytosine permease…
5-FC converted 5-Flourodeoxyuridine 5-monophosphate (5-FDUMP)…Ï´ conversion of dUMP into dTMP….Ï´DNA synthesis
Antifungal spectrum:
used with Itraconazole to treat Chromoblastomycosis….with Amphotericin B to treat Candidiasis, Cryptococcosis
S.E:
thrombocytopenia, bone-marrow depression, ↑LFT
Ketoconazole (Fungistatic)
First orally active…
Ï´ C-14α-demethylase…block demethylation of Lanosterol to Ergosterol…
Ï´fungal cell growth
Not selective…also inhibit Human gonadal & steroid synthesis…↓Testosterone, cortisol
Antifungal spectrum
not aspergillus activity,
Itraconazole replaced Ketoconazole…
topical used against Tinea corporis(Trichophyton rubrum), Tinea cruris (T.mentagrophytes), Tinea pedis (E.floccosumm), Tinea versiclor (M.fufur), dandruff
Require Acid for dissolution, Enzyme inhibitor... Teratogenic
S.E:
Frank hepatitis, Gynecomastia, ↓Libido, Impotence, Menstrual irregularity,↑LFT
Fluconazole
Trizole...devoid of Endocrine side effect…mechanism same to Ketoconazole… DOC in S.neoforman for coccidioidomycosis & candidemias…
S.E
Rashes, teratogenic, ↑LFT
Itraconazole
Broad antifungal spectrum…DOC in Blastommycosis,Sporotrichosis,Histoplasmosis, Paracoccidioidomycosis….require acid for dissolution..
S.E
Rash,Hypokalemia, Hypertension, edema…not used in pregnancy,CHF
Voriconazole
Used in Invasive Aspergillosis
Echinocandins
Interfere with fungal cell wall by Ï´ β(1,3)-D-glucan leading to cell death….
1.Capsofungin= first in Echinocandin…S.E; Phlebitis, Flushing due to Histamine release...
2. Micafunngin & Anidulafungin= no dose adjustment in renal impair
Drugs for Cutaneous Mycotic infections
Mold-like fungal infection that cause cutaneous infection are called Dermatophytes/Tinea
Tinea pedis infection of feet, refered as “Ringworm”
Squalene epoxidase inhibitor:
a) Terbinafine=Ï´Squalene epoxidase, ↓Ergosterol synthesis…accumulation of toxic Squalene, cell death
1%Cream & solution used for Tinea pedis, Tinea cruris, Tinea corporis
S.E= Taste & visual disturbancee, Hepatotoxicity, Neutropenia
Griseofulvin (Fungistatic)
Accumulate in Keratin tissue...disruption of Mitotic spindle… inhibition of fungal mitosis….
Abs ↑by fatty meal…
used in nail,skin infection
Nystatin= only topical...oral “Swish & Spit”
Imidazole= Miconazole potent inhibitor of Warfarin
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