Antifungal Flashcards
Adults have an acidic, fatty substance in and out of the skin called?
sebum
Higher-molecular-weight fatty acid have the advantage of having (higher or lower) volatility?
lower
It is prepared from caprylic acid, which is a component of coconut and palm oils.
Sodium caprylate
10-Undecenoic acid, obtained from the destructive
distillation of castor oil.
Undecylenic acid
Brand name of undecylenic acid?
Desenex, Cruex
is used externally in ointments and solutions for its antifungal
and keratolytic properties.
Salicylic acid
m-Hydroxyphenol
resorcinol
possesses appreciable antifungal effects, but it cannot
penetrate the outer layer of the skin in infected areas.
benzoic acid
Whitfield’s
Ointment, USP. This ointment contains?
6% benzoic acid, 6%, and salicylic acid, in a petrolatum base
not a phenol but has properties like those of phenols.
ciclopirox olamine
Brand name of clioquinol?
Vioform, used vaginally as a treatment for Trichomonas vaginalis vaginitis.
is considered an agent of choice in the treatment of
cutaneous candidiasis, tinea corporis, tinea cruris, tinea pedis, and
tinea versicolor. It is a second-line for onychomycosis?
Ciclopirox olamine
An active metabolite of the drug Flucytosine?
5-Fluorouracil
What is the mechanism of action of flucytosine in fungal infections?
Conversion to 5-fluorouracil, which inhibits fungal RNA and protein synthesis
One strategy used to decrease resistance and to prolong
the effect of 5-FC is to administer it, with the polyene antibiotic of ?
Amphotericin B
Two classes of antifungal antibiotics, are?
Polyenes and Griseofulvin
True or False
Natamycin, the smallest macrocycle, is
a pentaene; nystatin is a hexaene; and amphotericin B is a heptaene
TRUE
It was purified from the fermentation beer of a soil culture of the actinomycete Streptomyces
nodosus, which was isolated in Venezuela.
Amphotericin B
It binds to ergosterol in the fungal cell membrane, forming pores that cause leakage of ions and molecules, disrupting membrane integrity and leading to cell death.
Amphotericin B
TRUE OR FALSE
Amphotericin B can be administered intramuscularly?
FALSE, poor absorption to muscle tissue causes thrombophlebitis
A polyene antibiotic that was first isolated in 1951 from a strain of the
actinomycete Streptomyces noursei by Hazen and Brown?
Nystatin
A polyene antibiotic obtained from cultures of Streptomyces natalensis?
Natamycin
TRUE OR FALSE
Natamycin, a 26-membered–ring polyenes cause both potassium ion
leakage and cell lysis at the same concentration. Whereas
the 38-membered–ring polyenes cause potassium leakage
at low, fungistatic concentrations and cell lysis at high, fungicidal concentrations.
TRUE
What is the MOA of Griseofulvin?
Involves binding to fungal microtubules, which disrupts the mitotic spindle formation during cell division
It is use for the systemically delivered treatment of refractory
ringworm infections of the body, hair, nails, and feet caused by
species of dermatophytic fungi including
Griseofulvin
Interfere with an early step in ergosterol biosynthesis, namely, the epoxidation of squalene catalyzed by
squalene epoxidase.
Allylamines, such as naftifine and terbinafine
TRUE OR FALSE
Squalene epoxidase forms an epoxide at the C2–C3 position of squalene.
TRUE
Although not an allylamine, it inhibits squalene epoxidase and has a spectrum of activity similar to that of the allylamines.
Tolnaftate
More potent than naftifine and has also
demonstrated oral activity against onychomycosis
(ringworm of the nails).
Terbinafine hydrochloride
A thioester of B-naphthol antifungal
Tolnaftate
Inhibits lanosterol 14- demethylase
Azole Antifungal Agents
TRUE OR FALSE
The basic structural requirement for members of the azole class is a weakly basic imidazole or 1,2,4-triazole
ring (pKa of 6.5–6.8) bonded by a nitrogen–carbon linkage to the rest of the structure
TRUE
TRUE OR FALSE
Fluconazole, possesses two polar triazole moieties, is sufficiently water soluble to be injected intravenously as a solution of the free base
TRUE
Two nitrogen in structure group
Imidazole
TRUE OR FALSE
Clotrimazole and Ketoconazole are triazole?
FALSE
Brand name of Clotrimazole?
Canesten
Brand name of Tioconazole?
Trosyd, more effective against Torulopsis glabrata than other azoles
Brand name of Miconazole?
Daktarin, Monistat, Micatin
Brand name of Ketoconazole?
Nizoral
TRUE OR FALSE
Ketoconazole antagonizes Amphotericin B?
TRUE
Brand name Itraconazole?
Sporanox
Brand name of fluconazole?
Diflucan
TRUE OR FALSE
Hepatotoxicity, most serious adverse effect of ketoconazole.
TRUE
Agent of choice for cryptococcal meningitis and prophylaxis against cryptococcosis in
AIDS patient.
Fluconazole
Approved for the treatment of invasive aspergillosis and refractory infections of
Scedosporium apiospermum and Fusarium spp
Voriconazole
It noncompetitively inhibit (1,3) beta-d-glucan synthase enzyme.
Echinocanadins, such as Micafungin, Anidulafungin, Caspofungin
A cyclic depsipeptide produced by fermentation in cultures of Aureobasidium
pullulan
Aureobasidin A
A noncompetitive inhibitor of enzyme inositol phosphorylceramide synthase
( essential enzyme for fungal sphingolipid biosynthesis)
Aureobasidins A
First line options for the Tx of invasive candidiasis and candidemia
ECHINOCANDINS
First echinocandin option for patients with invasive candidiasis.
* Second line option for invasive aspergillosis
Capofungin
Echinocandins that : indicated for the prophylaxis for invasive Candia infections
Micafungin
Echinocandins that can be administered in severe hepatic dysfunction
Anidulafungin
Give example of CELL MEMBRANE SYNTHESIS INHIBITORS of fungi?
Polyenes such as Amphotericin B, Nystatin, Natamycin
DOC for systemic mycoses
Amphotericin B
MOA: Inhibition of C-14 α-
demethylase
Azoles
TRUE OR FALSE?
Azoles are contraindicated for pregnancy?
TRUE
DOC for the Tx of Blastomycosis, Sporotrichosis,
Paracoccidioidomycosis, Histoplasmosis
Itraconazole
Buccal tablet for the tx of thrush.
Miconazole
Endocrine A/E: Gynecomastia, ↓ libido, Impotence,
Menstrual irregularitites
Ketoconazole
DOC for Onychomycosis
Terbinafine
DNA SYNTHESIS INHIBITORS of fungi?
Flucytosine and Ciclopirox olamine
Inhibits the transport of essential elements in the fungal cell,
disrupting the synthesis of DNA, RNA, and proteins
Ciclopirox olamine
DOC for ringworm or tinea infection
Griseofulvin
TRUE OR FALSE
Griseofulvin absorption is increased by fats.
TRUE
Distorts the hyphae and stunts mycelial growth in susceptible
fungi
Tolnaftate