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DRUGS/CHEMOTHERAPY
A. Drugs acting on the cell membrane
1. Disrupts the integrity of the cell
membrane by binding to ergosterol
DRUGS/CHEMOTHERAPY
2. Interacts with C-14, demethylase to
block demethylation of lanosterol to
ergosterol
Imidazole (Clotrimazole,
Ketoconazole, miconazole)
Triazole (Fluconazole, itraconazole))
DRUGS/CHEMOTHERAPY
B.Nuclear division blocker Griseofulvin
(fungistatic)
C. DNA synthesis blocker 5
flurocytosine/ 5FC (fungistatic)
SUPERFICIAL MYCOSES:
TREATMENT
SUPERFICIAL
MYCOSES
TREATMENT
1. Pityriasis
Versicolor
2. Tinea Nigra
(Tinea nigra
palmaris)
3. Black piedra
4. White piedra
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
nail
Foot Infections
1.
Acute phase = soak in potassium permanganate
1: 5,000
until acute inflammation subsides
2. Chronic phase = apply antifungal drug
NYSTATIN
MOA OF NYSTATIN
GRISEOFULVIN
Fungistatic in activity.
MOA:
Inhibits fungal cell mitosis by being
accumulated in
the newly-synthesized keratincontaining tissue, thus producing multinucleated
defective cells that bind to the microtubules, thereby
disrupting mitotic spindle.
Pharmacokinetic profile:
ADR:
Headache, lethargy, fatigue, blurred vision,
insomnia, GI upset, hepatotoxicity.
GRISEOFULVIN
Drug Interactions:
IMIDAZOLES:
Ketoconazole
Azoles
FLUCONAZOLE
ITRACONAZOLE
Administered PO or IV.
May produce teratogenic effects.
DOC for Cryptococcus neoformans.
DOC for blastomycosis, aspergillosis, sporotrichosis,
histoplasmosis, and paracoccidioidomycosis.
Orally administered.
With teratogenic capability.
VORICONAZOLE
Caspofungin
Others: Micafungin
Anidulafungin
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:
TOPICAL IMIDAZOLE:
Clotrimazole
ADR:
urticaria.
TOPICAL IMIDAZOLES:
Econazole & Butoconazole
ECONAZOLE
BUTOCONAZOLE
Derivative of miconazole.
Used for the treatment of tinea pedis, tinea cruris, tinea
corporis, tinea versicolor, and cutaneous candidiasis.
ADR:
Burning, itching, rash.
TERBINAFINE
NAFTIFINE
AMOROLFINE
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.
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).
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).
CLIOQUINOL, OXICONAZOLE,
SULCONAZOLE, TERCONAZOLE
CLIOQUINOL
OXICONAZOLE
SULCONAZOLE
TERCONAZOLE