antifungal therapy for mycoses
DESCRIPTION
pharmacologyTRANSCRIPT
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ANTI-FUNGAL DRUGS
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MECHANISMS OF ACTION OF SOME
ANTI-FUNGAL DRUGS
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DRUGS/CHEMOTHERAPY
A. Drugs acting on the cell membrane1. Disrupts the integrity of the cell membrane by binding to ergosterol
• Amphotericin B/AMB (fungicidal)- most commonly used
• Nystatin (fungicidal)
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DRUGS/CHEMOTHERAPY
2. Interacts with C-14, demethylase to block demethylation of lanosterol to ergosterol
• Imidazole – (Clotrimazole, Ketoconazole, miconazole)
• Triazole (Fluconazole, itraconazole))
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DRUGS/CHEMOTHERAPY
B.Nuclear division blocker – Griseofulvin (fungistatic)
C. DNA synthesis blocker – 5 flurocytosine/ 5FC (fungistatic)
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SUPERFICIAL MYCOSES: TREATMENT
SUPERFICIAL MYCOSES
TREATMENT
1. Pityriasis Versicolor
2.5% selenium sulfide for 10 min daily for 7 days topical miconazole, itraconazole and ketoconazole
2. Tinea Nigra (Tinea nigra palmaris)
topical keratolytic solutions of sulfur, salicylic acid, or tincture of iodine
3. Black piedra shave or cut the hairs short
4. White piedra shave or cut the hairs short
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CUTANEOUS MYCOSES: TREATMENT
body infection – therapy consist of thorough removal of infected and dead epithelial
structures and application of a typical antifungal
chemical (Miconazole, Clotrimazole, Econazole, Ciclopirox) scalp infection – require Griseofulvin nail infection – requires months of griseofulvin treatment and
sometimes surgical removal of the nailFoot Infections
1. Acute phase = soak in potassium permanganate 1: 5,000 until acute inflammation subsides
2. Chronic phase = apply antifungal drug
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NYSTATIN Isolated from Streptomyces; first antimycotic antibiotic. Polyene antibiotic with broad spectrum of activity. MOA: Binds to sterols in fungal cell membranes, thereby
increasing membrane permeability and making the cell more susceptible to destruction.
Pharmacokinetic profile: Given by oral or topical route.
ADR: Local burning and itching (topical).GI upset (NAV, diarrhea), renal toxicity (PO).
Therapeutic Uses: Prevention and topical treatment of superficial candidal infections of
the skin and mucous membranes (gums, GIT, rectum, vagina).
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MOA OF NYSTATIN
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GRISEOFULVIN Fungistatic in activity. MOA: Inhibits fungal cell mitosis by being accumulated in
the newly-synthesized keratin-containing tissue, thus producing multinucleated defective cells that bind to the microtubules, thereby disrupting mitotic spindle.
Pharmacokinetic profile: Orally administered; t1/2: 24 hours. Distributes to growing nails and skin, binding to keratin and
making the cells resistant to fungal infection. Biotransformed in the liver to 6-methyl-griseofulvin; urinary
excr. ADR: Headache, lethargy, fatigue, blurred vision,
insomnia, GI upset, hepatotoxicity.
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MOA of Griseolfulvin and the Echinocandins
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GRISEOFULVIN
Drug Interactions: With anticoagulants reduced effectiveness of
anticoagulants because of enhanced metabolism. With barbiturates enhanced metabolism of
griseofulvin. With alcohol tachycardia and flushing; potentiation
of intoxicating effects of alcohol. With oral contraceptives amenorrhea, increased
breakthrough bleeding.
Therapeutic Use: For tinea infections of the skin, hair, nails including athlete’s foot and ringworm caused by Microsporum, Epidermophyton, and Trichophyton (oral).
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IMIDAZOLES:Ketoconazole
Broad antifungal activity; fungistatic agent. MOA: Selectively increases fungal cell membrane
permeability by blocking the demethylation of lanosterol to ergosterol.
(effective only in growing cells) MOR: Mutation in the C14 -demethylase gene
decreased azole binding; fungi’s ability to pump the azole out of the cell.
Orally given; readily absorbed under acidic pH. ADR: NAV, diarrhea, rash, itching, dizziness,
constipation, fever, chills, and headache; gynecomastia and impotence;
hepatocellular toxicity. Therapeutic Uses: Rx of systemic and vaginal candidiasis,
mucocandidiasis, oral thrush, histoplamosis, chromomycosis, coccidioidomycosis, dermatophytosis.
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Azoles FLUCONAZOLE
Administered PO or IV. May produce teratogenic effects. DOC for Cryptococcus neoformans.
ITRACONAZOLE DOC for blastomycosis, aspergillosis, sporotrichosis,
histoplasmosis, and paracoccidioidomycosis. Orally administered. With teratogenic capability.
VORICONAZOLE Administered orally and effective for invasive aspergillosis
and serious infections caused by Scedosporium apiospermum and fusarium species.
ADR: Transient visual disturbance.
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Caspofungin First of the echinocandins class of antifungal drugs. MOA: Interferes with the synthesis of the fungal
cell wall by inhibiting the synthesis of -D- glucan cell lysis and death.
ADR: Fever, rash, nausea, phlebitis, flushing.
Others: MicafunginAnidulafungin
For aspergillosis, Pneumocystis carinii infection
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SYSTEMIC & TOPICAL IMIDAZOLE: Miconazole Administered both parenterally and topically.
Therapeutic Uses: For Rx of candidal and dermatophytic infections of
the skin and for vaginal candidiasis (topical). For severe systemic fungal infections unresponsive
or not tolerant to Amphotericin B (IV).
ADR: Local burning, itching, and rash (topical).NAV, anemia, anaphylactoid reactions,
CNS toxicity, hyponatremia, phlebitis (IV).
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TOPICAL IMIDAZOLE:Clotrimazole
Broad antifungal activity.
Therapeutic Uses: Vulvovaginal candidiasis (topical)Oropharyngeal candidiasis (topical
oral)
ADR: Erythema, blistering, edema, pruritus, urticaria.
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TOPICAL IMIDAZOLES:Econazole & Butoconazole
ECONAZOLE Derivative of miconazole. Used for the treatment of tinea pedis, tinea cruris, tinea
corporis, tinea versicolor, and cutaneous candidiasis. ADR: Burning, itching, rash.
BUTOCONAZOLE Azole cream for vaginal use and is effective against vaginal
infections caused by Candida albicans and Candida tropicalis.
May cause vulvovaginal burning and itching.
OTHER TOPICAL ANTIMYCOTIC AGENTS Undecylenic acid, haloprogin.
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TERBINAFINE NAFTIFINEAMOROLFINE
TERBINAFINE Fungicidal agent that acts by selectively inhibiting
squalene epoxidase that is involved in the synthesis of ergosterol from squalene in the fungal cell wall accumulation of squalene toxicity to organism.
Given orally or topically for fungal infections of the nails.
ADR: GI disturbances, rashes, pruritus, headache, dizziness, joint and muscle pains,
hepatitis.Related drug: Naftifine
AMOROLFINE A morpholine derivative that interferes with fungal
sterol synthesis. Given orally for fungal infections of the nails.
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BUTENAFINE A synthetic benzylamine.
MOA Alters fungal membrane permeability and growth
inhibition. Interferes with sterol biosynthesis by allowing
squalene to accumulate within the cell.
Therapeutic Uses Dermatophytoses, including tinea corporis, tinea
cruris, and tinea pedis (1% cream).
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CICLOPIROX
MOA: Intracellular depletion of amino acids and
ions necessary for normal cellular function.
Therapeutic Uses: Tinea pedis, tinea cruris, tinea corporis,
tinea versicolor, cutaneous candidiasis (topical).
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CLIOQUINOL, OXICONAZOLE, SULCONAZOLE, TERCONAZOLE
CLIOQUINOL Available in 3% ointment for tinea pedis and cruris. May cause local irritation, rash, and sensitivity reactions.
OXICONAZOLE Available in 1% cream or lotion for tinea cruris, corporis,
mannum, and pedis and tinea versicolor. SULCONAZOLE
Imidazole derivative available in 1% cream or solution and used for tinea corporis, cruris, pedis, versicolor and impetigo.
TERCONAZOLE Imidazole derivative available in vaginal cream and
suppository and used for vulvovaginal candidiasis.
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A blissful Christmas and a blessed 2014!