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Anti_fungal drugs
- 1. MUTHANNA ALLAMI G.S.M MEDICAL EDUCATION BILAL HUSSEIN DR HARITH ALAWADI LECTURES
- 2. G.S.M MEDICAL LECTURES /MICROBIOLOGY DR HARITH ALAWADI LECTURES 2 G.S.M MEDICAL EDUCATION G.S.M MEDICAL EDUCATION
- 3. G.S.M MEDICAL LECTURES /MICROBIOLOGY DR HARITH ALAWADI LECTURES 3 G.S.M MEDICAL EDUCATION G.S.M MEDICAL EDUCATION There are 5 groups of anti-fungal 1- Lanosterol synthesis inhibitor: terbinafine 2- Cell wall synthesis inhibitor: echinocandins, anidulafungin, capsofungin, micafungin. 3- Cell membrane integrity inhibitors: polyenes (amphotericin B, nystatin) 4- Nucleic acid synthesis inhibitors: flucytosine 5- Ergosterol synthesis inhibitors: Azoles Clotrimazole Fluconazole Itraconazole Isavuconazole Miconazole Ketoconazole Voriconazole
- 4. G.S.M MEDICAL LECTURES /MICROBIOLOGY DR HARITH ALAWADI LECTURES 4 G.S.M MEDICAL EDUCATION G.S.M MEDICAL EDUCATION *ergosterol is the basic unit for the cell membrane integrity in fungi Amphotericin B Mechanism: binds to ergosterol (unique to fungi), forms membrane pores that allows leakage of electrolytes. Clinical use: serious, systemic mycoses. Cryptococcus (amphotericin B with/without flucytosine for cryptococcal meningitis), Blastomyces, coccidioides, histoplasma, Candida, mucor. Intrathecally for fungal meningitis. Supplements K and Mg because of altered renal tubule permeability. Adverse effects: fever/chills (“shake and bake”), hypotension, nephrotoxicity, arrhythmias, anemia, IV
- 5. G.S.M MEDICAL LECTURES /MICROBIOLOGY DR HARITH ALAWADI LECTURES 5 G.S.M MEDICAL EDUCATION G.S.M MEDICAL EDUCATION phelibitis (ampyhoterrible). Hydration decrease nephrotoxicity. Liposomal amphotericin decrease toxicity. ………………………………………………………………………………………………… ………………………………………………………………………………………………… …………………………………………………………………………………………………. ………………………………………………………………………………………………… ………………………………………………………………………………………………… …………………………………………………………………………………………………. ………………………………………………………………………………………………… ………………………………………………………………………………………………… …………………………………………………………………………………………………. ………………………………………………………………………………………………… ………………………………………………………………………………………………… ………………………………………………………………………………………………….
- 6. G.S.M MEDICAL LECTURES /MICROBIOLOGY DR HARITH ALAWADI LECTURES 6 G.S.M MEDICAL EDUCATION G.S.M MEDICAL EDUCATION Nystatin Mechanism: same as amphotericin B. topical use only as too toxic for systemic use. Clinical use: “swish and swallow” for oral candidiasis (thrush), topical for diaper rash or vaginal candidiasis. ………………………………………………………………………………………………… ………………………………………………………………………………………………… …………………………………………………………………………………………………. ………………………………………………………………………………………………… ………………………………………………………………………………………………… …………………………………………………………………………………………………. ………………………………………………………………………………………………… ………………………………………………………………………………………………… ………………………………………………………………………………………………….
- 7. G.S.M MEDICAL LECTURES /MICROBIOLOGY DR HARITH ALAWADI LECTURES 7 G.S.M MEDICAL EDUCATION G.S.M MEDICAL EDUCATION Flucytosine Mechanism: inhibits DNA and RNA biosynthesis by conversion to 5-flurouracil by cytosine deaminase. Clinical use: systemic fungal infections (especially meningitis caused by Cryptococcus) in combination with amphotericin B. Adverse effects: bone marrow suppression. ………………………………………………………………………………………………… ………………………………………………………………………………………………… …………………………………………………………………………………………………. ………………………………………………………………………………………………… ………………………………………………………………………………………………… ………………………………………………………………………………………………….
- 8. G.S.M MEDICAL LECTURES /MICROBIOLOGY DR HARITH ALAWADI LECTURES 8 G.S.M MEDICAL EDUCATION G.S.M MEDICAL EDUCATION ………………………………………………………………………………………………… ………………………………………………………………………………………………… …………………………………………………………………………………………………. ………………………………………………………………………………………………… ………………………………………………………………………………………………… …………………………………………………………………………………………………. ………………………………………………………………………………………………… ………………………………………………………………………………………………… …………………………………………………………………………………………………. ………………………………………………………………………………………………… ………………………………………………………………………………………………… ………………………………………………………………………………………………….
- 9. G.S.M MEDICAL LECTURES /MICROBIOLOGY DR HARITH ALAWADI LECTURES 9 G.S.M MEDICAL EDUCATION G.S.M MEDICAL EDUCATION Azoles Clotrimazole, Fluconazole, Itraconazole, isavuconazole, Miconazole, Ketoconazole, Voriconazole 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. Fluconazole for chronic suppression of cryptococcal meningitis in AIDS patients and candidial infections of all types. Itraconazole for blastomyces, coccidioies, histoplasma. Clotrimazole and micanazole for topical fungal infection. Voriconazole for aspergillus and some
- 10. G.S.M MEDICAL LECTURES /MICROBIOLOGY DR HARITH ALAWADI LECTURES 10 G.S.M MEDICAL EDUCATION G.S.M MEDICAL EDUCATION Candida. Isavuconazole for serious aspergillus and mucor infections. Adverse effects: testosterone synthesis inhibition (gynecomastia, especially with ketoconazole), liver dysfunction (inhibit cytochrome p-450)
- 11. G.S.M MEDICAL LECTURES /MICROBIOLOGY DR HARITH ALAWADI LECTURES 11 G.S.M MEDICAL EDUCATION G.S.M MEDICAL EDUCATION Terbinafine Mechanism: inhibits the fungal enzyme squalene epoxidase Clinical use: dermatophytes (especially onychomycosis; fungal infection of finger or toe nails) Adverse effects: GI upset, headache, hepatotoxicity, taste disturbance. Echinocandins
- 12. G.S.M MEDICAL LECTURES /MICROBIOLOGY DR HARITH ALAWADI LECTURES 12 G.S.M MEDICAL EDUCATION G.S.M MEDICAL EDUCATION Mechanism: inhibit cell wall synthesis by inhibiting synthesis of B-glucan. Clinical use: invasive aspergillosis, Candida. Adverse effects: GI upset, flushing (by histamine release) Griseofulvin Mechanism: interferes with microtubule function, disrupts mitosis. Deposits in keratin-containing tissues (nails).
- 13. G.S.M MEDICAL LECTURES /MICROBIOLOGY DR HARITH ALAWADI LECTURES 13 G.S.M MEDICAL EDUCATION G.S.M MEDICAL EDUCATION Clinical use: oral treatment of superficial infection, inhibits growth of dermatophytes (tinea, ring worm) Adverse effects: teratogenic, carcinogenic, headaches, disulfiram like reaction, increase cytochrome p450 and warfarin metabolism. ………………………………………………………………………………………………… ………………………………………………………………………………………………… …………………………………………………………………………………………………. ………………………………………………………………………………………………… ………………………………………………………………………………………………… …………………………………………………………………………………………………. ………………………………………………………………………………………………… ………………………………………………………………………………………………… ………………………………………………………………………………………………….
- 14. G.S.M MEDICAL LECTURES /MICROBIOLOGY DR HARITH ALAWADI LECTURES 14 G.S.M MEDICAL EDUCATION G.S.M MEDICAL EDUCATION ………………………………………………………………………………………………… ………………………………………………………………………………………………… …………………………………………………………………………………………………. ………………………………………………………………………………………………… ………………………………………………………………………………………………… …………………………………………………………………………………………………. ………………………………………………………………………………………………… ………………………………………………………………………………………………… …………………………………………………………………………………………………. ………………………………………………………………………………………………… ………………………………………………………………………………………………… …………………………………………………………………………………………………. ………………………………………………………………………………………………… ………………………………………………………………………………………………… ………………………………………………………………………………………………….
- 15. G.S.M MEDICAL LECTURES /MICROBIOLOGY DR HARITH ALAWADI LECTURES 15 G.S.M MEDICAL EDUCATION G.S.M MEDICAL EDUCATION ………………………………………………………………………………………………… ………………………………………………………………………………………………… …………………………………………………………………………………………………. ………………………………………………………………………………………………… ………………………………………………………………………………………………… …………………………………………………………………………………………………. ………………………………………………………………………………………………… ………………………………………………………………………………………………… ………………………………………………………………………………………………….