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House Microbiology > Anti-fungal Agents > Flashcards

Anti-fungal Agents Flashcards

1
Q

Mode of action of some antifungal agents

Amphotericin B binds to _____ creating ____

Azoles inhibits _________ in the fungal cell

5FC converts to ______ , incorporated into ____, _______

A

plasma membrane ; pores

cytochrome P450 enzymes

5FU; RNA; abnormal proteins

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2
Q

Mode of action of some anti fungal agents

Griseofulvin binds _____ proteins, inhibiting ______

Terbinafine is ________ inhibitor useful for ___________

Echinocandins target their action on ______

A

microtubule; cell wall synthesis

an ergosterol ; systemic mycosis

fungal cell wall

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3
Q

Drugs for systemic fungal infections

Polyene antibiotics
-__________
Pyrimidine antimetabolites
-_______
Antifungal azoles
-_______
-________
-______
Echinocandins
______,______, and _______

A

Amphotericin B

Flucytosine

Ketoconazole, Fluconazole, Itraconazole

Caspofungin, micafungin, and anidulafungin

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4
Q

Drugs for superficial fungal infections

Systemic drugs
-_______
-_______

Topical drugs
-_______
-______
-_______
-Azoles (______,_____,_____, etc.)

A

Griseofulvin; Iodide

Nystatin; Haloprogin; Tolnaftate

miconazole, econazole, clotrimazole

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5
Q

Polyenes

are produced from _______

are _______ molecules

Are ______ spectrum

Examples include ____,____,____,____

A

Streptomyces

Cyclic molecules

Broad spectrum

Natamycin
Nystatin
Amphotericin B
Mepartricin

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6
Q

PHARMACOLOGY OF AMPHOTERICIN B
Chemistry

-Amphotericin B is a _____ antibiotic

Mechanism of action
-Binding to ________ present in the membranes of fungal cells leading to Formation of “ ______ ” in the membrane, Leading to ________________ from the cells

A

polyene

ergosterol

pores

leaking of small molecules (mainly K+)

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7
Q

polyene: containing _____________

A

many double bonds

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8
Q

The ultimate effect of amphotericin B is fungistatic?

A

may be fungicidal or fungistatic depending on the organism and on drug concentration.

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9
Q

Antifungal spectrum and resistance of amphotericin B

-Antifungal spectrum includes:
LOL!

Resistance ?

A

Histoplasma capsulatus Coccidioides immitis Paracoccidioidoides braziliensis Aspergillus fumigatus Blastomyces dermatitidis Cryptococcus neoformans Candida albicans
Sporothrix schenckii
Mucor and Rhizopus spp

may occur but is very rare

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10
Q

The TI of Amphotericin B is (wide or narrow?)

A

Very narrow

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11
Q

Adverse effects of Amphotericin B

-Headache, ________ , nausea and vomiting fever and chills, hyperpnea, ____________ (they may appear during IV infusion and may be reduced by concomitant administration of ______ or _______ )
-Malaise, weight loss
-__________
-_______ anemia, likely due to ___________

-_____________
-Delirium, seizures (after intrathecal injection)

A

arthralgias

shock-like fall in blood pressure; antipyretics or meperidine

Nephrotoxicity

Normocytic; decreased production of
erythropoietin (frequent)

Thrombophlebitis

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12
Q

Amphotericin is the drug of choice for:

-Disseminated _______
-Disseminated and meningeal ______ -Disseminated and meningeal _______
-______
-________
-Mucormycosis

A

histoplasmosis; coccidioidomycosis; cryptococcosis

Invasive aspergillosis

Deep candidiasis

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13
Q

Amphotericin is an alternative drug for:
- ________
-______________
-Extracutaneous _______

[Amphotericin is preferred when these mycoses are ________, occur in _____ host or involve the _____]

A

Blastomycosis

Paracoccidioidomycosis

sporotrichosis

rapidly progressive; immunocompromised; CNS

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14
Q

Azole Derivatives

A chemical ______ structure with ___ nitrogen atoms

Water (soluble or insoluble?) except ______

Preferentially inhibit _________

Fungi(static or cidal?)

A

pentacyclic; 2

Insoluble; fluconazole

cytochrome P450 enzymes

static

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15
Q

fluconazole

Water soluble or insoluble

A

Soluble

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16
Q

Azole derivatives

First generation Imidazoles:
_______ and ______

A

Clotrimazole & Miconazole

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17
Q

Clotrimazole

requires (low or high ?) doses

(Well or Poorly?) tolerated

A

High

Poorly

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18
Q

Parenteral dosages no longer available for _____azole

A

Micon

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19
Q

CYP is vital to the formation of _____ and _____

A

cholesterol & steroids

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20
Q

Third generation azoles

Triazole derivatives (contain _____ nitrogen atoms)

A

three

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21
Q

Third generation azoles
Triazole derivatives

List 5!!

A

Fluconazole
Itraconazole
Voriconazole
Posaconazole
Revuconazole

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22
Q

Triazoles have a Satisfactory tolerability

T/F

A

T

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23
Q

Triazoles are not Suitable for systemic use

T/F

A

F

24
Q

PHARMACOLOGY OF ANTIFUNGAL AZOLES

Chemistry
-Imidazole derivatives: ____,____,____,_____

-Triazole derivatives: _____,____

A

ketoconazole, miconazole, econazole,
clotrimazole

itraconazole, fluconazole.

25
Q

PHARMACOLOGY OF ANTIFUNGAL AZOLES

Mechanism of action
-Inhibition of __________________ , a ________-dependent enzyme (has relative selectivity occurs because the affinity for ________ isozymes is less than that for the ______ isozyme)

A

sterol 14-alpha-demethylase

cytochrome P450

mammalian P450 ; fungal

26
Q

Mechanism of action of azoles is to block the ______ of _____ in fungal cell membranes

The ultimate effect may be _____ or ______ depending on _______ and _____

A

Synthesis of ergosterol

fungicidal or fungistatic

the organism and on drug concentration.

27
Q

____azole has been extensively used for yeast infections

A

Flucon

28
Q

Fluconazole is Useful for systemic infections

T/F

A

T

29
Q

Absorption of Fluconazole??

Distribution of Fluconazole

A

It is readily and completely absorbed by gastrointestinal tract

Distributed equally in different organs and tissue

30
Q

_________ is Intrinsically resistant to fluconazole

A

Candida krusei

31
Q

_______azole is used to treat aspergillus infections

A

Itracon

32
Q

Itraconazole is not Entirely metabolized in the liver

T/F

A

F

It is

33
Q

Voriconazole

is a modified _____
A _____ spectrum antifungal agent

_____ absorption after oral administration
Distributes in tissues and body fluids

Metabolized in the ____
Eliminated in the ______ in _____ form

A

fluconazole

broad

Rapid

liver

urine in unchanged

34
Q

Azoles carry some side effects

_________,__________, and _______

______,________ and other hypersensitivity

A

Hepatotoxicity, gastrointestinal and endocrine toxicity

Skin rash, pruritis

35
Q

Cross-resistance between azoles is rare

T/F

A

F

Cross-resistance between azoles is a common finding.

36
Q

Azoles may inhibit certain mammalian cytochrome P450 isozymes and therefore they may
1) inhibit the synthesis of _______ and ———
2) ______ the effects of several drugs including cyclosporine,
phenytoin, terfenadine, astemizole, tolbutamide and warfarin.

A

androgens and of corticosteroids

potentiate

37
Q

Newest class of antifungal agents are the _________

A

Echinocandins

38
Q

Echinocandins

Route of administration: ____________

Mechanism of action: inhibiting ___________

A

Intravenous

the synthesis of (1–3)-glucan

39
Q

Echinocandins are (poorly or Well?) tolerated

A

Well

40
Q

Examples of Echinocandins

List 3

A

Caspofungin Micafungin Anidulafungin

41
Q

Caspofungin

synthesized from _________

A

Glarea lozyensis

42
Q

Caspofungin

is natural , semisynthetic or synthetic?

A

semisynthetic

43
Q

Caspofungin

Appearance is ________, _________ soluble, fungi(static or cidal?)

A

Whitish powder

water & methanol

cidal

44
Q

Caspofungin is Fungicidal against, ______,____, and ______

A

Aspergilli, Candida and P. carinii

45
Q

Presence of cross resistance to Caspofungin amongst strains resistant to Ampho B or azoles

T/F

A

F

No cross resistance

46
Q

Caspofungin is fungicidal against Cryptococcus neoformans, Fusarium & Rhizopus

T/F

A

F

No activity against Cryptococcus neoformans, Fusarium & Rhizopus

47
Q

Caspofungin is Effective against Pneumocystis carinii

T/F

A

T

48
Q

Micafungin and Anidulafungin are widespread

T/F

A

F

Micafungin and Anidulafungin – are under investigation

49
Q

Terbinafine

Has _______ and _____ administrations

Terbinafine inhibits _________

A

Oral and topical (cream) formulations

ergosterol biosynthesis

50
Q

Terbinafine belongs to _______, synthetic, highly lipo____

A

allylamines

philic

51
Q

Terbinafine

Used to treat _____ mycosis but Also useful against _____ mycosis (yeast & other fungi)

A

superficial

systemic

52
Q

Adverse reactions to terbinafine are in general _________ and _____

A

transient and mild

53
Q

Based on one video, antifungal agents can be divided into 5

List them

A

Antibiotics
Azoles
Antimetabolites
Allylamines
Topical agents

54
Q

List the antibiotics antifungal agents

A

Polyenes
Echinocandins
Heterocyclic benzofurun

55
Q

Hamycin is a ______

A

Polyene

56
Q

Examples of antimetabolites anti fungal agents?

A

Flucytosine

57
Q

The only systemic imidazole is??

Rest are ??

A

Ketoconazole

Topical

House Microbiology (93 decks)

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