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Antifungal DRUGS 2
Antifungal DRUGS 2
Antifungal DRUGS 2
Lampung University
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Subcutaneus & Superficial
Systemic Mycoses Mycoses
- Griseofulvin
- Amphoterisin B
- Nystatin
- Flucytosine
- Myconazole
- Ketokonazol
- Clotrimazole
- Fluconazole
- Econazole
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Amphotericin B
Flucytosine
Ketoconazol
Fluconazole
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Has the broadest Potential toxicity,
spectrum of action fungicidal
ADVERSE EFFECTS
• Chills & fever
• Impaired renal function
• Abnormalities of liver function tests and anemia
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A water-soluble pyrimidine analog related to
the chemotherapeutic agent fluorouracil (5-FU).
The spectrum of
activity >>
Cryptococcus Synergy with Synergy with azole
neoformans, candida, amphotericin B drugs
and
chromoblastomycosis
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Taken up by fungal cells
Converted to 5-FU
ADVERSE EFFECTS
• Hematological toxicity: neutropenia, thrombocytopenia, BM
depression
• Hepatic dysfunction
• GI disturbances 14
MOA: inhibition of fungal cytochrome P450 enzymes >> reduction of
ergosterol synthesis
CI: + Ampho-B
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PHARMACOLOGICAL PROPERTIES
Adm: PO (food, antasid, and cimetidine interfere its absorption)
Penetrasi: (-) CSF
Excr: primarily through the bile
ADVERSE EFFECTS
Endocrine effect (eg. gynecomastia)
GI effect
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PO and PE prep
Oral bioavailability is high.
Good CSF penetration
Has the widest therapeutic index of the azoles.
Clinical Uses:
- Mucocutaneous candidiasis
- Cryptococcalmeningitis
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The newest class of antifungal agent
Is a second-line antifungal for those who have
failed or cannot tolerate amphotericin B or an
azole.
MoA: interfere with the synthesis of the
fungal cell wall by inhibiting the synthesis of
β(1,3)-D-glucan >> lysis and cell death.
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PK
A: PE
M: slowly metabolized by hydrolysis and N-
acetylation.
Water-soluble and highly protein bound.
T ½ 9–11 hours
E: urinary and fecal routes
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Clinical Uses
Salvage therapy in patients with invasive
aspergillosis who have failed to respond to
amphotericin B
Mucocutaneous candidiasis and candidal
bloodstream infections
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Griseofulvin
Nystatin
Miconazole
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Antifungal spectrum >> fungistatic, dermatophytes
(trichopyton, microsporum, epidermophyton)
Systemic treatment of dermatophytosis
MOA >> unclear, but it is deposited in newly forming skin
where it binds to keratin
P-Properties
• Absorption is improved when it is given with fatty foods.
• Met: liver
• Excr: feces & urine
• AE: allergic syndrome
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Much like Amphotericin B
Too toxic for PE administration >> only used
topically
Creams, ointments, suppositories, and other
forms
Clinical uses: local candidal infections
ADR: rare >> nausea, vomitting
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Actively topical drugs
MOA, antifungal spectrum, distribution, type
of metabolism = ketoconazole
Clinical Uses: tinea pedis, ringworm, and
cutaneous and vulvovaginal candidiasis.
AE: rare
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Terima Kasih...