Anti-fungals pt. 2 Flashcards
T or F
Polyenes contains conjugated -ene system of double bonds yet no activity against bacteria, rickettsia, or viruses and highly potent, broad spectrum antifungals.
True
Isolated from Streptomyces natalensis.
Natamycin
Brand name of Natamycin
Pimaricin, Natacyn
___-membered ring polyenes cause potassium ion leakage and cell lysis at same concentration.
26-membered ring
Uses of Natamycin 5% ophthalmic suspension.
Treatment for fungal conjunctivitis, blepharitis, and keratitis.
Isolated from Streptomyces noursei in 1951
Nystatin
Which of the following is True about Nystatin?
I. Not absorbed systematically when orally administered
II. Too toxic for parenteral administration
III. Tx of GI monolial infections by Candida spp
IV. Cream, ung, powder for cutaneous and mucocutaneous candidiasis
a. I, II, IV
b. II, III, IV
c. I, II, III, IV
d. III, IV
C. I, II, III, IV
Brand name of Nystatin
Mycostatin
Oral Tablets are used for vaginal candidiasis. Oral tablets and troches are used for GI and oral candidiasis.
A. First statement is correct.
B. Second statement is correct.
C. Both of the statements are correct.
D. Both of the statements are incorrect.
B. Second statement is correct,
Vaginal Tablets are used for vaginal candidiasis. Oral tablets and troches are used for GI and oral candidiasis.
T or F
Nystatin + Tetracycline can be used for prevention of monilial overgrowth.
True
Amphotericin B is purified from fermentation beer of a soil culture of _______ ______ in Venezuela
Streptomyces nodosus
What is the mechanism of action of Amphotericin B?
Interact with ergosterol in fungi to produce an aggregate that forms a transmembrane channel.
Parenteral Amphotericin B can be used for treatment of?
For treatment of severe, potentially life-threatening: Coccidioidonycosis Cryptococcosis Aspergillosis Sporotrichosis Histoplasmosis Mucormycosis
CCASHM
Grisactin, Gris-PEG, Grifulvin
Griseofulvin
Griseofulvin is isolated from what specie in 1939?
Penicillium griseofulvum
MOA of Griseofulvin
Rapidly arrests cell division in metaphase.
Rapid, reversible dissolution of the mitotic spindle apparatus, probably by binding with the tubulin dimer that is required for microtubule assembly.
Adverse effects (6) of Griseofulvin.
Rash, urticaria, GI upset, headache, dizziness, insomnia
In 1959, Griseofulvin was introduced to human medicine for systemic tx of tinea infections.
After systemic absorption, griseofulvin is carried by the systemic circulation and capillary beds to the skin, nails, and hair follicles, where it concentrates in keratin precursor cells, which are gradually exfoliated and replaced by healthy tissue.
A. First statement is correct.
B. Second statement is correct.
C. Both of the statements are correct.
D. Both of the statements are incorrect.
C. Both of the statements are correct.
Tolnaftate is an allylamine antimycotic agent that inhibits what?
Squalene epoxidase
The following is true about Tolnaftate, EXCEPT:
A. 1% in cream, powders, aerosols, gels, sol’n for tx of ringworm, jock itch, athlete’s foot.
B. Used with artificial fingernails that decreases ringworm of nail beds.
C. Has brand name of Naftin
C. Has brand name of Naftin
Correct answer:
Brand names of Tolnaftate: Tinactin, Aftate, NP-27
This antifungal is fungicidal at high concentration and fungistatic at low concentration.
Azole Antifungals
Lotrimin, Gyne-Lotrimin, Mycelex
Clotrimazole
The following are true about Clotrimazole, EXCEPT:
I. Has narrow-spectrum
II. Soln’ in PEG400, lotion, 1% cream – tinea pedis, tinea cruris, tinea capitis, tinea versicolor
III. 1% vaginal cream, 100mg or 500mg tabs for vulvovaginal candidiasis
IV. For systemic infections, protein bound, optimally bioavailable.
A. III, IV
B. I, IV
C. I, II, III
D. II, IV
B. I, IV
Clotrimazole has BROAD spectrum and NOT for systemic infections, protein bound, and NOT OPTIMALLY bioavailable.
Brand name of Butoconazole Nitrate
Femstat
Has the brand name of Spectazole and contains 1% cream for topical tx of local tinea infections and cutaneous candidiasis.
Econazole Nitrate
Butoconazole Nitrate is effective against C. albicans. Uses 2% salt in vaginal cream.
A. First statement is correct.
B. Second statement is correct.
C. Both of the statements are correct.
D. Both of the statements are incorrect.
C. Both of the statements are correct.
Uses of Exelderm
GN: Sulconazole nitrate
1% in solution and cream for tx of jock itch, athlete’s foot, ringworm
Uses of Oxistat
GN: Oxiconazole Nitrate
1% in cream, lotion for tx of tinea pedis, tinea corporis, tinea capitis
Uses of Vagistat
GN: Tioconazole
5% in vaginal ointment and effective against Torulopsis glabrata.
Antifungal polyene available as cream, lotion, powder, or spray that is used for tinea infections and cutaneous candidiasis. It is also available in free bases injectable form.
Miconazole Nitrate
Miconazole Nitrate is solubilized with PEG and Castor Oil for serious systemic fungal mycoses.
Has the brand name of Monistat and Micatin
A. First statement is correct.
B. Second statement is correct.
C. Both of the statements are correct.
D. Both of the statements are incorrect.
C. Both of the statements are correct.
Administered orally for treatment of systemic mycoses.
Ketoconazole
T or F
High doses of Ketoconazole lower testosterone and corticosterone levels and enhances responses to cyclosporine and coumarin.
True
Ketoconazole is enzyme inhibitor of cyclosporine, ________, and __________
Cyclosporine, phenytoin, and terfenadine
Brand name of Ketoconazole
Nizoral
The following are true about Ketoconazole, EXCEPT:
I. Antagonizes amphotericin B.
II. 2% in cream and shampoo for cutaneous and tinea infections.
III. Orally active alternative to Itraconazole
IV. NOTA
IV. NOTA
Terconazole (Terazol) is exclusively for vulvovaginal moniliasis caused by what specie?
C. albicans and Candida spp.
T or F
Terconazole is available as suppositories and creams.
True.
80 mg suppositories
0.4% cream for 7-day tx and 0.8% cream for 3-day tx
I. Itraconazole is orally active alternative to ketoconazole.
II. Acidic environment for optimal solubilization
III. More effective and better tolerated than ketoconazole
IV. Hepatotoxic, has adrenal or testicular suppression
V. CYP450 inhibitor, decreases plasma levels of Terfenadine and Astemizole.
A. Two of the statements are true.
B. Three of the statements are true.
C. All of the statements are true.
D. None of the statements are true.
B. Three of the statements are true.
I. Itraconazole is orally active alternative to ketoconazole.
II. Acidic environment for optimal solubilization
III. More effective and better tolerated than ketoconazole
IV. NOT Hepatotoxic, NO adrenal or testicular suppression
V. CYP450 inhibitor, INCREASES plasma levels of Terfenadine and Astemizole.
True or False
Itraconazole is orally active alternative to ketoconazole.
True
Itraconazole is used for the treatment of systemic infections caused by these species.
Blastomycosis, histoplasmosis, nonmeningeal coccidioidomycosis, sporotrichosis
Sporanox is the brand name of Fluconazole. T or F.
False!
Sporanox - Itraconazole
Diflucan - Fluconazole
Fluconazole has the presence of ___________ which is sufficient aqueous solubility to balance lipophilicity of the 2,4-difluorophilicity
two weakly basic triazole ring
Fluconazole is the agent of choice for treatment of cryptococcal _______ and cryptococcosis prophylaxis in _______ patients.
Meningits, AIDS Patients
Which of the following is NOT true about Fluconazole?
I. Oral administration is affected by alteration in GI acidity or food.
II. 27-34 half-life but do not penetrates body cavities and CSF.
III. Agent of Choice for tx of cryptococcal meningitis and cyptococcosis prophylaxis in AIDS px
IV. >10% protein bound, little to no hepatic metabolism and is excreted unchanged
A. I, II, IV
B. I, III, IV
C. I, II, III
D. II, III, IV
A. I, II, IV
Correct Answers:
I. Oral administration is NOT affected by alteration in GI acidity or food.
II. 27-34 half-life, penetrates body cavities and CSF.
III. Agent of choice for tx of cryptococcal meningitis and cyptococcosis prophylaxis in AIDS px
IV. <10% protein bound, little to no hepatic metabolism and is excreted unchanged
I. Voriconazole is more potent that fluconazole to newer and rare fungal pathogens.
II. Posaconazole is used in clinical trials and has high oral BA.
III. Syn2869 has novel-broad spectrum with piperazine-phenyl-triazolone side chain and has better activity than itraconazole.
A. One of the statements is true.
B. Two of the statements are true.
C. All of the statements are true.
D. None of the statements are true.
C. All of the statements are true.
Review:
- Act as noncompetitive inhibitors of (1,3)-beta-d-glucan synthase
- Percentage of econazole used for candidiasis
- Most effective agent in the treatment of systemic fungal infection especially in immunocompromised patients
- Caspofungin
- 1% econazole nitrate
- Fluconazole