Antifungal Agents

Question 1

For many years _____ drug was the only efficacious antifungal drug available for systemic use

Answer 1

Amphotericin B

Question 2

Azole drugs comes with what formations?

Answer 2

Oral and parenteral

Question 3

The only available route of administration of echinocandins

Answer 3

Parenteral administration

Question 4

___ drugs are antifungal antibiotics produced by streptomyces nodosus

Answer 4

Amphotericin A and B

Amphotericin A is not in clinical use

Question 5

___ is an amphoteric polyene macrolide.

Answer 5

Amphotericin B

Question 6

Is effective only on fungi within the lumen of the tract an cannot be used for treatment of systemic disease

Answer 6

Oral amphotericin B

Question 7

___ is a cell membrane sterol, is found in the cell membrane of fungi

Answer 7

Ergosterol

Question 8

The predominant sterol of bacteria and human cell is?

Answer 8

Cholesterol

Question 9

In what sterol does amphoericin B binds to?

Answer 9

Ergosterol

Question 10

MOA of the drug:

Binds to ergosterol and alters the permeability of the cell by forming amphotericin B-associated pores in the cell membrane. The pore allows the leakage of intracellular ions and macromolecules, eventually leading to cell death

Answer 10

Amphotericin B

Question 11

A drug that remains as the anti fungal agent with the broadcast spectrum of action. Has activity against candida albicans, cryptococcus neoformans, pathogenic molds.

Answer 11

Amphotericin B

Question 12

A drug that remains a useful agent for all nearly life-threatening mycotic infections

Answer 12

Amphotericin B

Question 13

Topical drops as well as direct subconjunctival injection of amphotericin B can cure?

Answer 13

Mycotic corneal ulcer and keratitis

Question 14

Two broadcast categories of toxicity in amphotericin B

Answer 14

Infusion-related toxicity
- nearly universal and consists of fever, chills, muscle spasms, vomiting, headache
Cumulative toxicity
- renal damage, most significant toxic reaction

Question 15

A potent antifungal agent that was discovered in 1957 during a search for novel antineoplastc agents. Its spectrum of action is much NARROWER that that of amphotericin B

Answer 15

Flucytosine

Question 16

ROA of flucytosine

Answer 16

Only in oral formulation

Question 17

MOA

Taken up by fungal cells via the enzyme cytosine permease. It is converted intracellularly first to 5-FU and then to 5-fluorodeoxyuridine monophosphate and fluoridine triphosphate, which inhibit DNA and RNA synthesis

Answer 17

Flucytosine

Question 18

Enzyme that takes up flucytosine

Answer 18

Fungal cells via enzyme cytosine permease.

Question 19

Conversion of flucytosine

Answer 19

1. 5-fluroacil
2. 5-fluorodeoxyuridine monophosphate (FdUMP)
3. Fluorouridine triphosphate

Question 20

Spectrum of activity of ____ is restricted to C neoformans and some candida sp

Answer 20

Flucytosine

Question 21

Bone marrow toxicity, with anemia, leukopenia and thrombocytopenia

What drug has this kinds of common adverse effect?

Answer 21

Flucytosine

Question 22

Are systemic compounds that can be classified as either imidazole or triazoles according to the number of nitrogen atoms in the five-membered azole ring

Answer 22

Azoles

Question 23

Examples of imidazole

Answer 23

Ketoconazole
Miconazole
Clotrimazole

Question 24

Examples of triazoles

Answer 24

Itraconazole
Fluconazole
Voriconazole
Isavuconazole
Posaconazole

Question 25

The first oral azole introduced into clinical use, is is less selective for fungal P450 than are the newer azoles

Answer 25

Ketoconazole

Question 26

Is the azole of choice for treatment of disease due to dimorphic fungi histoplasma, basltomyces and sporothrix

Answer 26

Itraconazole

Question 27

An azole that is extensively used in the treatment of dermatophytoses and onychomycosis

Answer 27

Intraconazole

Question 28

An azole that has the widest therapeutic index of the azoles , permitting more aggressive dosing in a variety of fungal infections

Answer 28

Fluconazole

Question 29

The azole of choice in the treatment and secondary prophylaxis of cryptococcal meningitis

Answer 29

Fluconazole

Question 30

An azole agent that is most commonly used for the treatment of mucocutaneous candidiasus

Answer 30

Fluconazole

Question 31

Available forms of: Keto Itra Fluco Vori Posa Isavu

Answer 31

Keto - PO Itra - PO, IV Fluco - PO, IV Vori - PO, IV Posa - liquid oral formulation Isavu - PO, IV

Question 32

Treatment of choice for invasive aspergillosis and some environmental molds

Answer 32

Voriconazole

Question 33

A similar spectrum of action in triazoles that has an excellent activity agaist candida sp and dimorphic fungi

Answer 33

Voriconazole and itraconzaole

Question 34

An azole that was originally available only in liquid oral formulation. IV form and sustained acting tabled are now available

Answer 34

Posaconazole

Question 35

The broadest spectrum member of the azole family, with activity against most species of candida and aspergillus

Answer 35

Posaconazole

Question 36

the first azole with significant activity against the agent of mucormycosis

Answer 36

Posaconazole

Question 37

A prodrug o the newest triazole

Answer 37

Isavuconazole

Question 38

___ has an antifungal spectrum similar to that of posaconzole

Answer 38

Isavuconazole

Question 39

The newest class of antifungal agents to be developed. Theya re large cyclic peptides linked to a long-chain FA

Answer 39

Echinocandins

Question 40

The only echinocandins that are only the licensed agents in the category of antifungals

Answer 40

Caspofungin, micafungin and anidulafungin

Question 41

The only available form of echinocandins

Answer 41

IV formulation

Question 42

Micafungin Dose of 150mg/d treats? Dose of 100mg treats? Dose of 50mg treats?

Answer 42

150 - esophageal candidiasis 100 - candidemia 50 - prophylaxis of fungal infections

Question 43

HL of Caspofungin Micafungin Anidulafungin

Answer 43

C - 9-11hrs M - 11-15 hrs A - 24-48 hrs

Question 44

MOA of echinocandins

Answer 44

Inhibits the synthesis of B(1-3) glucan resulting in desruption of the fungal cell wall and cell death.

Question 45

Caspofungin is licensed for use in?

Answer 45

Invasive aspergillosis

Question 46

Micafungin is licensed for use in?

Answer 46

Mucocutaneous candidiasis, candidemia and prophylaxis of candidal infections

Question 47

Anidulafungin is approved for use in?

Answer 47

Esophagel candidiasis, invasive candidiasis, candidemia

Question 48

Very insoluble fungistatic drug derived from species of penicillium

Answer 48

Griseofulvin

Question 49

Griseofulvin is only use in the systemic treatment of?

Answer 49

Dermatophytosis

Question 50

ROA of griseofulvin

Answer 50

Microcrystalline oral form

Question 51

MOA It is deposited in newly forming skin where it binds to keratin, protecting the sin from new infection

Answer 51

Griseofulvin

Question 52

A synthetic allylamine that is used in the treatment of dermatophytoses especially onychomycosis

Answer 52

Terbinafine

Question 53

MOA Inhibits fungal enzyme squalene epoxidase, leads to the accumulation of the sterol squalene, which is toxic to the organism

Answer 53

Terbinafine

Question 54

Like griseofulvin, terbinafine is a keratophilic medication, but unlike griseofulvin, it is ____

Answer 54

Fungicidal

Question 55

A polyene macrolide much like amphotericin B, too toxic for parental administration and is only used topically

Answer 55

Nystatin

Question 56

Nystatin is commonly used for suppression of __ infection

Answer 56

Local candidal infection

Question 57

Two azole that are most commonly used topically are?

Answer 57

Clotrimazole and miconazole

Question 58

Pleasant-tasting Alternative to nystatin, they are available for treatment of oral thrush.

Answer 58

Oral clotrimazole

Question 59

Allymines available as topical creams. Bot are effective for treatment of tinea cruris and tinae corporis

Answer 59

Terbinafine and naftifine