Allylamines, Azole, Echinocandins and Pneumocandins, Antiprotozoal Agents Flashcards
1
Q
• inhibits squalene epoxidase resulting to shutting down of biosynthesis of ergosterol and cause an accumulation of squalene, which destablizes the fungal cell membrane
A
MOA of Allylamines Related Compounds
2
Q
• Naftin®
• supplied in a 1% concentration in a cream and in a gel for the topical treatment of ringworm, athlete’s foot and jock itch
A
Naftifine
3
Q
• Lamisil®
• available in 1% cream for topical administration for the treatment of tinea pedis, tinea corporis, and tinea cruris
A
Terbinafine
4
Q
• Tinactin®, Aftate®, NP-27®
• not an allylamine but has MOA the same with allylamine compounds
• formulated into preparations intended to be used with artificial fingernails to counteract the increased chance of ringworm of the nail beds
A
Tolnaftate
5
Q
- interacts with C-14-demethylase to block demethylation of lanosterol to ergosterol, the principal sterol of fungal membranes. This inhibition disrupts membrane function and increases permeability
A
MOA of Azole Antifungal Agents
6
Q
- effective against most fungi that cause superficial infections of the skin and mucous membrane
- also exhibit activity against yeasts that cause systemic infections
A
Antifungal Spectrum
7
Q
basic structural requirement for members of the azole class is a weakly basic imidazole or _____
A
1,2,4-triazole ring
8
Q
the most potent antifungal azoles possess _____
A
2 or 3 Aromatic Rings
9
Q
- Lotrimin®, Mycelex®
- a broad-spectrum antifungal drug that is used topically for the treatment of tinea infections and candidiasis
- 1% vaginal cream and tablets of 100 mg and 500 mg for vulvovaginal candidiasis
- extremely stable, with a shelf-life of more than 5 years
A
Clotrimazole
10
Q
- Spectazole®
- 1% cream for the topical treatment of local tinea infections and cutaneous candidiasis
A
Econazole
11
Q
- Femstat®
- supplied as vaginal cream intended for vaginal candidiasis
A
Butoconazole
12
Q
- Exelderm®
- supplied in 1% concentration for the
treatment of local tinea infections, such as jock itch, athlete’s foot, and ringworm
A
Sulconazole
13
Q
- Oxistat®
- used in cream and lotion
dosage forms in 1%
concentration for the
treatment of tinea infections
A
Oxiconazole
14
Q
- Vagistat®
- used for the treatment of
vulvovaginal candidiasis
A
Tioconazole
15
Q
- Monistat®, Micastin®
- used as treatment for tinea infections and cutaneous candidiasis, vaginal candidiasis
- can be used also for systemic infections but can cause thrombophlebitis, pruritis, fever and GI upset
A
Miconazole
16
Q
- Nizoral®
- a broad-spectrum antifungal that is administered orally for the treatment of systemic fungal infections
- inhibits androgen and andrenal steroid synthesis
- has endocrine effects: gynecomastia, decreased libido, impotence, and
menstrual irregularities - absorption is increased with acidic foods
- recommended for the treatment of the following systemic infections: candidiasis (oral thrush and chronic mucocutaneous form), coccidioidomycosis, blastomycosis, histoplasmosis, chromomycosis and
paracoccidioidomycosis
A
Ketoconazole
17
Q
- used orally to treat severe refractory cutaneous dermatophytic infections not responsive to topical therapy and oral griseofulvin
- used topically in 2% concentration in a cream and shampoo for the
management of cutaneous
candidiasis and tinea infections - S/E: (additional) hepatotoxicity
A
Ketoconazole
18
Q
- Terazol®
- used exclusively for the control of vulvovaginal moniliasis caused by
Candida spp. - available in creams containing 0.4% and 0.8% of the free base intended
for 7-day and 3-day treatment periods, respectively
A
Terconazole
19
Q
- Sporanox®
- an orally active, broad-spectrum antifungal agent that has become an important alternative to
ketoconazole - lacks the endocrinologic effects of ketoconazole
- DOC for tinea ungium
A
Itraconazole
20
Q
- Diflucan®
- administered orally and intravenously
- has excellent penetrability into the CSF
- drug of choice for Cryptococcal meningitis (Cryptococcus neoformans) - can be diagnosed through negative staining using Negrosin ink/India ink
A
Fluconazole
21
Q
- can be acquired through pigeon droppings
- HIV patients (+ headache)
A
Cryptoccocal Meningitis
22
Q
KIF SYS
* for subcutaneous and SYStemic fungal infections
A
Ketoconazole
Itraconazole
Fluconazole
23
Q
MEC SUP
*for SUPerficial mycoses
A
Miconazole
Econazole
Clotrimazole
24
Q
VP- Newer Antifungal Agents
A
- Voriconazole
- Posaconazole
25
* act as non-competitive inhibitors of (1,3)--d-glucan synthase, an enzyme complex that forms stabilizing glucan polymers in the fungal cell wall
MOA of Echinocandins and
Pneumocandins
26
* Capsebon®
* supplied as shampoo for the treatment of dandruff or seborrheic dermatitis
Caspofungin
27
* produced from Aureobasidium pullulan
MOA:
acts as a tight-binding noncompetitive inhibitor of the enzyme inositol phosphorylceramide
synthase (IPC synthase), which is an essential enzyme for fungal sphingolipid biosynthesis
Aureobasidins
28
Common Pathogenic Protozoa (under Antiprotozoal Agents)
* Entamoeba histolytica
* Balantidium coli
* Giardia lamblia
* Trichomonas vaginalis
* Pneumocystis carinii (now a fungi)
* Toxoplasma gondii
* Trypanosoma cruzi
* Trypanosoma brucei
* Leishmania donovani (Kala-azar)
29
* Flagyl®, Protostat®, Metro IV®
* the most useful nitroimidazole derivative
for Amoebiasis, Trichominiasis and Giardiasis
* also has antibacterial activity
* S/E: disulfiram-like effect, metallic aftertaste
* MOA: formation of reactive intermediate that binds to the DNA of microorganism
Metronidazole
30
* used in the treatment of asymptomatic carriers of Entamoeba histolytica
Diloxanide
31
* recommended for acute and chronic intestinal amebiasis but is not effective in extraintestinal disease
* S/E: neuropathy
Iodoquinol
32
* obtained by extraction from ipecac (Caephalis ipecacuanha)
* MOA: inhibits protein synthesis in protozoal and mammalian cells by preventing protein elongation
* S/E: severe GI distress, CV diseases,
neuromuscular effects
* I: Amoebiasis, balantidial dysentery, fluke infestations (fascioliasis, paragonimiasis)
Emetine & Dehydroemetine
33
* NebuPent®, Pentam 300®
* used for the treatment of pneumonia caused by the opportunistic pathogenic protozoan P. carinii, a frequent secondary
invader associated with AIDS
* used for the prophylaxis and treatment of African trypanosomiasis and visceral leishmaniasis
Pentamidine
34
* Mepron®
* MOA: may act as antimetabolite and
interfere with the function of electron transport enzymes
* S/E: GI distress
* originally for malaria but now used against P. carinii (alternative for TMP-SMX)
Atovaquone
35
* used for the treatment of West African sleeping sickness, caused by Trypanosoma brucei gambiense
* Indicated for the
meningoencephalitic stage of the disease
* S/E: myelosuppression (anemia, leukopenia, thrombocytopenia)
Eflornithine
36
* Lampit®
* used for the treatment of South American trypanosomiasis caused
by Trypanosoma cruzi (Chagas disease)
Nifurtimox
37
* Radanil®, Rochagan®
* used in the treatment of Chagas Disease
Benznidazole
38
* Mel B®, Arsobal®
* DOC for the treatment of the later stages of both forms of African trypanosomiasis
* should be monitored for signs of arsenic toxicity
Melarsoprol
39
* Pentostam
* a pentavalent antimonial compound intended primarily for the treatment of various forms of leishmaniasis
Sodium Stibogluconate
40
* used as a long-term prophylactic agent for trypanosomiasis
* also used for prophylaxis of onchocerciasis
Suramin
41
