| 1 Schonlein and Gruby identified __
2 Langenbeck identified __
3 Isolated fungus responsible for the favus on
potato slices, rubbed it on the head of a child, and
produced the disease. __ | 1 Trichophyton schoenleinii in 1839
2 Candida albicans
3 Gruby |
| 1 Acidic, fatty substance with natural
antifungal agent
2 all fatty acids and their salts have __ properties
3 Nonvolatile are for __ application | 1 sebum
2 fungicidal properties
3 topical |
| Non irritating and nontoxic
Present in sweat/perspiration in low
concentration ( around 0.01%) | PROPIONIC ACID |
| Anhydrous form and monohydrate
Its salt is unstable to moisture> zinc
hydroxide and propionic acid
Used as fungicide, particularly on adhesive
tape | Zinc propionate |
| Its salt is unstable to moisture | zinc hydroxide and propionic acid |
| Prepared from caprylic acid, component of
coconut and palm oils
Treat superficial dermatomycoses | Sodium Caprylate |
| Viscous yellow liquid
Obtained from destructive distillation of
castor oil
Use concentration is up to 10%
Used for Athlete’s foot (Tinea pedis) | Undecylenic acid
Other name: 10-Undecenoic acid (Desenex, Cruex) |
| 1) benzoic acid 6% and salicylic acid 6%, in a petroleum base
2) 1% cream for superficial tinea, photosensitive, expensive
3) A 3% ointment or cream has been used vaginally as a treatment for Trichomonas vaginalis vaginitis. | 1 Whitfield’s ointment, USP
2 Haloprogin (Halotex),USP
3 Clioquinol( Vioform),USP |
| Clioquinol( Vioform),USP is the best use for __ | topical treatment of fungal infections such as athlete’s foot and jock itch. |
| agent of use for treatment of cutaneous candidiasis, tinea
infections,
2nd line treatment of onychomycosis (ringworn in nails) | Ciclopirox olamine (Loprox) |
| Narrow spectrum, orally active
Used in combination with Amphotericin B for the treatment
of systemic mycoses and meningitis caused by Cryptococcus neoformans and Candida | Nucleoside Antifungals: Flucytosine
Other Names:
5-Fluorocytosine, 5-FC,
4-amino-5-Fluoro-2(1H)-pyrimidinenone,
2-hydroxy-4-amino-5-fluoropyrimidine (Ancobon) |
| Flucytosine Mode of Action | Flucytosine is converted to antimetabolite 5-fluorouracil (5-FU) by the fungus, not human. 5-FU is subsequently converted to 5-fluorodeoxyuridine monophosphate (5-FdUMP)which inhibits THYMIDYLATE SYNTHETASE ENYZYME and thus DNA synthesis.
Resistant mutant may occur. Thus, not used alone
Shortened:
5-FdUMP or 5-fluorodeoxyuridine monophosphate inhibits Thymidylate Synthetase Enzyme (DNA Synthesis) |
| Antifungal antibiotics | A. Polyenes
B. Griseofulvin |
| 1) Isolated from soil bacteria genus Streptomyces
Structure: conjugated double bonds in a
macrocyclic lactone rings
2) 26 membered ring
3) 38 membered ring | 1) POLYENES
2) Natamycin
3 Amphotericin B and Nystatin: |
| 1 smallest macrocycle
2 hexene
3 heptene
4 POLYENES Chemical structure description | 1 Natamycin
2 Nystatin
3 Amphotericin
4
A. series of hydroxyl group
B. glycosidically linked deoxyaminohexose
mycosamine |
| Polyenes Characteristics | bacteria, rickettsia, or viruses (-)
but they are highly potent, broad-spectrum
antifungal agents.
protozoa, such as Leishmania spp. (+)
They are effective against pathogenic yeasts,
molds, and dermatophytes. |
| Low concentrations of the polyenes in vitro will
inhibit | 1 Candida spp.
2 Coccidioides immitis
3 Cryptococcus neoformans
4 H. capsulatum
5 Blastomyces dermatitidis
6 Mucor mucedo
7 Aspergillus fumigatus,
8 Cephalosporium spp.
9 Fusarium spp |
| 1 Polyenes are limited used in tx of systemic infections
due to:
2 treatment for systemic infections, must be solubilized with detergent | 1 toxicity, low water solubility, poor
chemical stability
2 Amphotericin B |
| AMPHOTERICIN B MODE OF ACTION | 1 AMPHOTERICIN B interacts hydrophobically with ergosterol in the fungal cell membrane, forming a spore.
2 Potassium and other small molecules are lost through the pore, causing cell death |
| Amphotericin B
1 Low concentration: __
2 High concentration: __ | 1 Fungistatic
2 Fungicidal |
| BN: Fungizone
1956: Gold et al.
Streptomyces nodosus, isolated from
Venezuela
Use: Drug Of Choice for systemic mycoses (severe, life
threatening), CNS: mix with CSF
S/E: nephrotoxic, pain at site of injection,
thrombophlebitis of IV
Never administer thru IM
Liposomal dosage form | Amphotericin B |
| BN: Mycostatin
1951: Streptomyces noursei by Hazen and Brown
Aglycone: nystatinolide
Not absorbed systemically: Topical agent
Used for the tx of local and GI monilial infections
caused by C. albicans
Administered as an oral agent for tx of oral
candidiasis | Nystatin |
| BN: Pimaricin, Natacyn
Streptomyces natalensis
Drug: 5% ophthalmic suspension for tx of
fungal conjunct, blepharitis, and keratitis | Natamycin |
| Natamycin at low and high concentration: __ | Leakage of Potassium Ions |
| BN: Grisactin, Gris-PEG, Grifulvin
1939: Oxford et al
Fungus: Penicillum griseofulvum
“Curling factor in plants”
Fungistatic agent
Absorption is increased by fatty
foods
Mitotic spindle poison | Other antifungal antibiotic: Griseofulvin |
| GRISEOFULVIN MODE OF ACTION | 1 Enters the fungal cell
2 Binds to tubulin and prevents formation of microtubules
3 Cause arrest of mitosis
4 Inhibits Fungal cell division
5 Fungistatic action |
| GRISEOFULVIN is used for a long time for the systemically delivered treatment of refractory ringworm infections of
the body, hair, nails, and feet caused by species
of dermatophytic fungi including __
Micronized (ultramicrosized, microsized) griseofulvin | 1 Trichophyton
2 Microsporum
3 Epidermophyton |
| Fungicidal:
dermatophytes and other filamentous fungi, but their action
against pathogenic yeasts, such as Candida spp., is
largely fungistatic. | Allylamine and Related compounds |
| 1) 1% concentration for topical agents
2) 1% conc, for topical administration | 1 Naftidine (Naftin) and Terbinafine (Lamisil)
2 Tolnaftate ( Tinactin, Aftate, NP-27) |
