antifungal drugs
DESCRIPTION
Antifungal DRUGSTRANSCRIPT
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OBAT ANTIFUNGI
Dwi Indria AnggrainiUniversitas Lampung
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2Tinea pedis (Buxton et al. ABC of Dermatology 4th ed., 2003)
Tinea cruris (Buxton et al. ABC of Dermatology 4th ed., 2003)
Fungal infection of nail (Buxton et al. ABC of Dermatology 4th ed., 2003)
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ANTIFUNGAL DRUGS
Subcutaneus & systemic Mycoses
- Amfoterisin B - Flucytosine- Ketokonazol- Fluconazole
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Subcutaneous And Systemic Mycoses
Amfoterisin B
Flucytosine
Ketoconazol
Fluconazole
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AMPHOTERICIN B
Obat utama
Toksisitas potensial
Efektif pada: Candida sp, Histoplasma capsulatum,
Cryptococcus neoformans, Coocidiodes immitis, Aspergillus sp,
Blastomyces dermatitidis
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AMPHOTERICIN B
Fungal cell
Ampho-B
PORE
K+ and others
MOA
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AMPHOTERICIN B
PHARMACOLOGICAL PROPERTIES Abs: lemah PO, baik IV Penetrasi lemah ke CNS, menembus plasenta Efek sinergis dengan flucytosine
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THERAPEUTICS USESInfeksi jamur yang berat (khususnya: immunocompromised)Antifungal yang paling efektif (DOC infeksi sistemik utama)
Adverse effects
• Chills & fever (50%) dan impaired renal function (80%)• Rx anaphylaxis, thrombocytopenia, nyeri yang berat, kejang.
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FLUCYTOSINE Antimetabolit sintetik pirimidin Indikasi : mikosis sistemic dengan kombinasi Ampho-B
(tetapi tidak untuk mikosis subcutan) Spektrum Antifungal fungistatic; efektif untuk
mengatasi: candidiasis, cryptococcocis, aspergillosis, chromomycosis
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MOA
transpor aktif ke dalam
sel fungi dan
diubah menjadi 5-FU 5-fluorodeoxyuridylic acid (inhibitor sintesis
pyrimidine dan asam
nukleat)
gangguan sintesis protein
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FLUCYTOSINE
PHARMACOLOGICAL PROPERTIESPO: baik setelah oral adm Penetrates baik pada semua jaringan, dan CNS. Ekskresi : glomerular filtration.Resistensi >> sehingga terbatas penggunaannya
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Adverse effects• Hematological toxicity : neutropenia,
thrombocytopenia, BM depression• Hepatic dysfunction• GI disturbances
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KETOCONAZOLE
Derivat Imidazole MOA :
Blokade c-P450 yang memperantarai demetilasi lanosterol menjadi ergosterol merusak fs membran
Kontraindikasi : digunakan bersama Ampho-B
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PHARMACOLOGICAL PROPERTIESAdm : PO (gastric pH mengganggu Abs)Penetrasi : (-) CSFExcr: primarily through the bile
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FLUCONAZOLE
Inhibisi sintesis fungal membrane sterols ADM : PO, PE Penetrasi ke CSF baik pada meningens yang
normal atau inflamasi
Indikasi: Oropharyngeal, dan systemic candidiasis Acute and maintenance therapy of
cryptococcalmeningitis
ADR : << ketoconazole, (-) endocrinological effect
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Drugs For SuperficialMycotic Infections
Griseofulvin
Nystatin
Miconazole12
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GRISEOFULVIN Antifungal spectrum :
Fungistatic, dermatophytes (Trichopyton, Microsporum, Epidermophyton), pd infeksi tinea berat yang tidak respon dgn antifungal lain.
MOA : berikatan pada mikrotubulus dan mencegah pembentukan spindel dan mitosis pada sel jamur
P-Properties :
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• berikatan pada protein filamen (keratin)• akumulasi pada kulit, rambut, kuku• abs sangat baik PO adm, topikal tidak efektif• dimetabolisme parsial oleh liver; • excresi : feces & urine
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NYSTATIN
Antibiotik polyene yang memiliki sturktur dan mekanisme kerja sama dengan Amphotericin B
Topical treatment, terlalu toksik untuk diberikan secar sistemik
Abs : PO tidak baik, PE adm (-) ADR : jarang karena absorpsi buruk,
terkadang nausea, vomitting
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MICONAZOLE, CLOTRIMAZOLE, ITRACONAZOLE, ECONAZOLE Derivat Imidazole Obat topikal aktif dan tidak diberikan
PE karena severe toxicity (phlebitis, pruritus, nausea, and anemia)
MOA, antifungal spectrum, distribution, type of metabolism = ketoconazole
Dapat digunakan untuk pengobatan :tinea pedis, ringworm, and cutaneous and vulvovaginal candidiasis.
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