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ID > Cao - Antifungals > Flashcards

Cao - Antifungals Flashcards

1
Q

a substance intended for use as a component of a medicine but not a device or a component, part, or accessory of a device

A

drugs

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2
Q

Science that deals with the origin, nature, chemistry, effects, and uses of drugs including pharmacognosy, PK, PD, pharmacotherapeutics, and toxicology

A

pharmacology

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3
Q

It is concerned with the development, identification, and interpretation of the mode of action of biologically active compounds at the molecular level

A

medicinal chemistry

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4
Q

It is concerned with the study, identification and synthesis of the metabolic products of these drugs and related compounds

A

medicinal chemistry

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5
Q

What are the two fungal categories?

A

superficial mycoses and deep seated mycoses

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6
Q

What is superficial mycoses?

A

dermatophytoses (skin or mucous membrane)
- contagious skin infections that are limited to the epidermis regions

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7
Q

What is deep-seated mycoses?

A

systemic mycoses (systemic fungal infections)
– lung or central nervous system

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8
Q

3 reasons for fungal infection

A
  1. overuse of abx
  2. immune compromised
  3. translocation
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9
Q

How are superficial mycoses caused?

A

relatively homogenous group of fungi, dermatophytoses, specialized saprophytic molds that unusually digest keratin of the skin

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10
Q

Where does systemic mycoses occur?

A

they invade the skin, lungs and lymphatic tissue

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11
Q

Name the systemic mycosis

A

histoplasmosis
blastomycosis
sporotrichosis
coccidiomycosis

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12
Q

systemic mycosis causative agents

A

free-living saprophytes

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13
Q

fx of fungal cell wall

A

Critical for cell viability and pathogenicity

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14
Q

Fungal cell wall is a critical site for…

A

exchange and filtration of ions and proteins, as well, as metabolism and catabolism of complex nutrients

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15
Q

T/F
mammalian cells have a cell wall so are not an ideal target for anti-fungal therapy

A

false - mammalian cells lack a cell way and it also represents an ideal and specific target for anti-fungal therapy

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16
Q

human cell membrane contains cholesterol and fungal cell membrane contains …

A

ergosterol

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17
Q

Do lipid bilayers form a stable or unstable structure?

A

it forms an unstable structure that cannot retain its shape and functions.

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18
Q

What lies within the lipid bilayer and what do they do?

A

Sterols lie within the lipid bilayer and act as stiffening agents

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19
Q

What are the predominant sterol in many pathogenic fungi?

A

ergosterol

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20
Q

What is a problem for designing drugs?

A

to be selective for the toxic fungal cell but not effect the host

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21
Q

What does the disruption of the fungi’s protein/carbohydrate matrix result in?

A

It results in structurally defective cell wall thus rendering the fungal cell sensitive to osmotic lysis

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22
Q

Drugs that target on the synthesis of ergosterol will lead to…

A

death of fungi

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23
Q

Allylamines

A

Naftifine and Terbinafine

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24
Q

Benzylamine

A

Butenafine

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25
Q

Imidazoles

A

Miconazole, Clotrimazole, Ketoconazole

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26
Q

Triazoles

A

Fluconazole, Itraconazole, Posaconazole, Voriconazole, Isavuconazole

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27
Q

Polyenes

A

Nystatin, natamycin (Pimaricin), Amphotericin B

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28
Q

Echinocandins

A

Caspofungin, Anidulafungin, Micafungin

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29
Q

Other anti-fungals

A

Griseofulvin, Flucytosine. Tolnaftate

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30
Q

MOA for Allylamine and Benzylamine

A

Inhibition of ergosterol biosynthesis at the level of squalene epoxidase

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31
Q

MOA for Azoles and Triazoles

A

Inhibition of CYP450-dependent enzymes (particularly C14a-demethylase) involved in the biosynthesis of ergosterol

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32
Q

Polyene MOA

A

Interaction with sterols in the cell membrane to form channels through which small molecules leak from inside the fungal cell leading to death.

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33
Q

Echinocandin MOA

A

Act as [ ]-dependent noncompetitive inhibitors of beta-1,3 glucan synthase

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34
Q

what is an essential component of the cell wall of susceptible filamentous fungi that’s absent in mammalian cells

A

beta-1,3 glucan synthase

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35
Q

Where did Polyenes get their name from?

A

alternating conjugated double bonds that constitute a part of their macrolide ring structure

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36
Q

Which species are polyenes a product of?

A

Streptomycin species

37
Q

What did Elizabeth Hazel and Rachel Brown propose/prove?

A

bacterial and fungi seem to keep each other in check and bacterial should be useful in identifying anti-fungal agents

38
Q

Which class of anti-fungals are the only fungicidal agent?

A

Polyenes

39
Q

What is the toxicity most likely due to for fungicides?

A

polyenes bind to cholesterol, although they have a 500X affinity for ergosterol over cholesterol

40
Q

First broad-spectrum anti-fungal agent

A

Nystatin

41
Q

Nystatin dosage forms

A

topical Cream, oral suspension, pill

42
Q

Nystatin is absorbed ______________ and is used for the treatment of fungal ____________. It’s also widely used as a “natural” anti-fungal ______ ___________.

A

systemically; keratitis; food additive

43
Q

Amphotericin B dosage forms

A

injectable, pil

44
Q

Why is Amphotericin B use limited?

A

due to its toxicity in the liver and kidneys
- should never be given with other nephrotoxic drugs

45
Q

Which formulation of Amphotericin B limits the toxic liability?

A

formulation with liposomes

46
Q

Liposomal amphotericin B

A

AmBisome

47
Q

Amphotericin B lipid complex

A

ABLC, Abelcet

48
Q

Amphotericin B colloidal dispersion

A

ABCD, Amphotec (AmBisome)

49
Q

MOA for Polyenes

A
  1. bind to ergosterol in the cell membrane
  2. results in membrane formation of pores –> eventually leading to cell death
50
Q

Polyenes attach with higher affinity to…

A

ergosterol

51
Q

higher [ ] of amphotericin B binds to…

A

cholesterol in mammalian cell membranes leading to various organ toxicities

52
Q

Most common adverse effects of amphotericin B

A

Nephrotoxicity (MOST COMMON)
Hypokalemia, Hypomagnesemia, bones marrow suppression

53
Q

Allylamine organic compound formula

A

C3H5NH2

54
Q

Naftifine is the first..

A

anti-fungal allylamine , against tinea

55
Q

Which anti fungal is stronger against tinea and onychomycosis (oral)

A

Terbinafine

56
Q

Butenafine is active against

A

Candida albicans in tolnaftate resistant cases

57
Q

Naftifine is a potential _____________ inhibitor and inhibits __________ ____________. Also represent the first member of the __________ class of antifungals

A

serotonin reuptake; squalene epoxidase; allylamine

58
Q

who am I?
active in vitro against a number of different fungal species, cleared very slowly so only used for topical indications, and a plasma half life of 60hrs

A

Naftifine (Naftin)

59
Q

WHO AM I?
readily absorbed in the GI tract w/ 40% oral availability; high level of metabolism by multiple CYP isoforms and high protein binding; plasma t1/2 of 36h; accumulates in the nails with a t1/2 of 300hrs; active against a broad spectrum of fungal strains

A

Terbinafine (Lamisil)

60
Q

WHO AM I?
similar activity profile as Naftifine; currently only used for topical indications; active against a number of different external infections.

A

Butenafine

61
Q

WHO AM I?
a thiocarbamate that can be made very inexpensively; active for athlete’s foot, ring worm, and jock itch indications by inhibiting squalene epoxidase; not active against Candida and other fungal infection; only used topically

A

Tolnaftate (Tinactin)

62
Q

WHO AM I?
onychomycosis treatment that disrupts other enzymes; only used topically but can be combined with systemic Terbinafine to improve efficacy of both

A

Amorolfine (Loceryl/Curanail)

63
Q

Imidazole antifungals are typically used for what?

A

external fungal infections

64
Q

Triazole antifungals are more commonly used for…

A

systemic infections

65
Q

WHO AM I?
First Azole discovered; not well-absorbed; available as cream, aerosolized spray and solution for fungal ear infection

A

Clotrimazole (Lotrimin)

66
Q

WHO AM I?
2nd member of the azole class of antifungals; exert their activity against 14a-sterol demethylase (CYP450); the most widely used OTC anti-fungal primarily for superficial mycoses; also can be used for neonatal thrush; racemic compound

A

Miconazole (Desenex/Monistat)

67
Q

WHO AM I?
generally used for exterior (non-systemic) indications; differs from Miconazole only by chlorine substitution pattern

A

Isoconazole (Travogen)

68
Q

WHO AM I?
Chlorine substitution analog widely available in the US and around the world; exists only as a cream

A

Econazole (Spectazole)

69
Q

WHO AM I?
first azole to be used to treat systemic Candida infections. Has poor PK (moderate absorption, high protein binding; relatively short t1/2)

A

Ketoconazole (Nizoral)

70
Q

WHO AM I?
Better PK than Ketoconazole; readily metabolized by CYP 3A4; highly protein bound that protects it from rapid metabolism and clearance

A

Itraconazole

71
Q

WHO AM I?
one of the most active triazole anti fungal agents for systemic fungal infections

A

Posaconazole

72
Q

WHO AM I?
Contains 2 triazole units and does not contain a chiral center making it less expensive and less likely to have an undesired SE by a “spectator” isomer; broad-spectrum antifungal; not highly metabolized; inhibit CYP 2C9 and 3A4; DO NOT MIX WITH CHOLESTEROL DRUGS

A

Fluconazole (Diflucan/Forcan)

73
Q

WHO AM I?
broad-spectrum triazole is available as a tablet and an IV formulation

A

Voriconazole (Vorzu/Vfend)

74
Q

Voriconazole Adverse effects and DI’s

A

hepatotoxicity, visual disturbances (common), hallucinations, and dermatologic rxns. Prolong QT interval
numerous DI notably with certain immunosuppressants used after organ transplantation.

75
Q

WHO AM I?
Acts through the inhibition of 14a-sterol demethylase (same target as azaleas). Shows limited antibacterial activity suggesting more than 1 MOA

A

Abafungin (Abasol)

76
Q

triazoles that are available for systemic use

A

fluconazole, itraconazole, Voriconazole, posaconazole, isavuconazole

77
Q

imidazole available for systemic use

A

Ketoconazole

78
Q

What class am I?
anti fungal drugs that inhibit the synthesis of gluten in the cell wall via noncompetitive inhibition of the enzyme 1,3-B glucan synthase; called penicillin f antifungals

A

Echinocandins

79
Q

which Echinocandin blocks B-1,3-glucan synthase (an enzyme necessary for cell wall formation)

A

Caspofungin
Micafungin
Anidulafungin

80
Q

Echinocandins are potently ___________ against most clinically important Candida sp but are considered ___________ against Aspergillus

A

fungicidal; fungistatic

81
Q

Echinocandins adverse effects

A

hepatitis and rash

82
Q

WHO AM I?
Not viable as an oral drug and must be administered intravenously. t1/2 10h - single daily injection is suitable

A

Caspofungin

83
Q

WHO AM I?
Metabolized by CYP3A4 on the hydrophobic tail, leading to decreased toxicity. no DDI problems which makes it useful for treatment of severely immunocompromised patients

A

Micafungin

84
Q

WHO AM I?
only metabolism through hydrolysis (no CYP) and no DDI. excellent therapeutic index

A

Anidulafungin

85
Q

t1/2 of 9h and metabollzied by beconjugation rather than any CYP itxns

A

Griseofulvin

86
Q

Nucleic acid analog, water soluble and well-absorbing after oral administration

A

Flucytosine

87
Q

Flucytosine AEs

A

bone marrow suppression (thrombocytopenia & leukopenia), hepatotoxicity, and enterocolitis

88
Q

Known to have anti fungal activity for 40yrs but MOA is still unknown. Typically used in combination with an azalea or allylamine anti-fungal agent

A

Ciclopirox

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