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pharma > 32.antifungal drugs > Flashcards

32.antifungal drugs Flashcards

1
Q

what are antifungal drugs used for?

A

for treatment of mycoses

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2
Q

which are the types of mycoses

A

1.superficial
2.subcutaneous
3.systemic

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3
Q

describe the fungal cell

A
  1. eukaryotic
  2. cell wall made of chitin
  3. cell membrane made of ergosterol
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4
Q

how many main group are the antifungal drugs classified into

A

1- synthetic antifungal drugs
2- antibiotics with antifungal activity

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5
Q

how many subgroups does synthetic antifungal drugs contain

A

1-azoles
2-allylamines
3-echinocandins
4-antimetabolite antifungals
5-others

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6
Q

name the drugs in the azole group

A
  1. Imidazoles
    1.1. ketoconazole - tab.200mg, cream 2%15g
    1.2 myconazole - oral gel 2% 40g
    1.3 econazole - cream 1% 15g
    1.4 clotrimazole - cream 1% 20g

2.Triazoles
2.1 fluconazole - caps.50,100,150mg
2.2 voriconazole - tab.200mg, flac 200mg
2.3 itraconazole - caps.100mg

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7
Q

name the allylamines (squalene epoxidase inhibitors)

A

1.terbinafine (lamisil) - tab.250mg, cream 1%15g

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8
Q

name the echinocandins

A

1.micafungin - flac.100mg
2.caspofungin - flac.50mg

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9
Q

name the antimetabolite antifungals

A

1.flucytosine - caps.500mg

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10
Q

name other synthetic antifungal drugs

A
  1. ciclopirox - cream 0,77%
  2. tolnaftate - cream 1%15g
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11
Q

name meds from the second group - antibiotics with antifungal activity

A

1.nystatin - tab 500.000IU, vag.100.000IU
2.amphotericine B - flac.50m.g (only i.v)

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12
Q

MOA of azoles

A
  1. are fungistatic
  2. inhibit ergosterol synthesis by inhibiting C14-a-demethylase (a cyt.450 enzyme),
    disrupting cell membrane function and structure and by that inhibiting the fungal cell growth
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13
Q

Spectrum of action of Azoles

A

broad
-against systemic and cutaneous mycoses

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14
Q

application of Imidazoles for?

A

topical for cutaneous infections

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15
Q

SOA of triazoles

A

systemically given for treatment and prophylaxis of systemic mycoses

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16
Q

Which is the least active of all triazoles?

A

fluconazole

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17
Q

SOA of fluconazole

A

yeast
1.candida
2.cryptococcus
3.dimorphic fungi

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18
Q

SOA of Voriconazole

A

1.broader SOA
2.against invasive Candida and Aspergillus in severely immunocompromised patients

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19
Q

Application of Imidazoles

A

topical - oral gels, creams, ointments

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20
Q

Application of Ketoconazole?

A

oral application

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21
Q

Application of Triazoles?

A

oral or i.v - NO topical forms

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22
Q

Absorption of Triazoles is better in which medium?

A

acidic (low gastric pH)

23
Q

How do proton pump inhibitors affect the absorption of triazoles?

A

reduce it because they affect the gastric pH

24
Q

Distribution of Azoles

A
  1. have a large volume of distribution
  2. distribute widely to all body fluids and tissues
  3. penetrate BBB and placental barrier
25
Q

Where does Itraconazole accumulate?

A

in nails and skin in higher concentrations and is released slowly

26
Q

Metabolism and Excretion of Azoles

A

1.in liver
2. excretion via urine + bile

27
Q

Excretion of Fluconazole?

A

unchanged via the urine — means that its dosage should be lower in patients with renal dysfunction

28
Q

ADRs of Azoles

A

1.GI disturbances e.g nausea and vomiting
2.Endocrine disorders e.g gynecomastia, decreased libido
3.Hepatotoxicity - increased serum hepatic transaminases

29
Q

ADRs of Itraconazole

A

negative ionotropic effect - hypokalemia, hypertension, edema

30
Q

ADRs ofVoriconazole

A

visual and auditory hallucinations

31
Q

MOA of Allylamines ( squalene epoxidase inhibitors)

A

1.inhibit squalene epoxidase
2.accumulation of squalene
3.increased permeability
4.death of fungal cells

32
Q

SOA of allyalmines

A

active against agents that cause cutaneous and nail fungal infections
e.g Trichophyton
Epidermophyton
Candida

-fungicidal or static depending on the organism

33
Q

Application of Terbinafine

A

oral and topical

34
Q

Bio-availability of Terbinafine

A

40% due to first pass metabolism (well absorbed)

35
Q

Where is Terbinafine deposited?

A
  1. skin+hair follicles (after 24hrs)
  2. nails
  3. adipose tissue
36
Q

Metabolism and excretion of Terbinafine?

A

1.by CYP450 isoenzymes
2.excreted via urine

37
Q

ADRs of Allylamines

A

1.GIT disturbances
2.increased serum hepatic transaminases
3.Taste and visual disturbances
4.Rash

38
Q

MoA of Echinocandins

A

inhibit fungal cell wall synthesis - lysis + cell death

39
Q

SOA of Echinocandins

A

narrow - candida + aspergillus

40
Q

Administration of Echinocandins

A

i.v

41
Q

metabolism of Echinocandins

A

liver + spontaneous degradation

42
Q

ADRs of Echinocandins

A

1.fever
2.rash
3.phlebitis
4.histamine like reactions (flushing)

43
Q

MoA of polyene antifungal Antibiotic

A

1.bind to ergosterol in the fungal cell membrane where they form pores
2.pores distrupt the membrane function, allowing electrolytes K+ to leak from the cell - cell death

44
Q

SOA of Amphotericin B

A
  1. fungicidal or static depending on the organism and concentration of the drug
  2. effective against a wide range of fungi
  3. used for systemic mycoses
45
Q

Nystatin SoA

A

for cutaneous and oral candida infections

46
Q

how is Amphotericin B administered?

A

slow i.v infusion

47
Q

Amphotericin B volume of distribution

A

1.extensively plasma protein bound
2.distributed through the body
3. low BBB penetration but penetrates the placenta

48
Q

Amphotericin B elimination

A

via the urine over a long period of time

49
Q

Absorption of Nystatin

A

not absorbed from GIT

50
Q

Is nystatin used parenterally?

A

no, because of systemic toxicity

51
Q

how is nystatin administered?

A

1.orally - for oropharyngeal candidiasis
2.intravaginally - for vulvovaginal candidiasis
3.topically - for cutaneous candidiasis

52
Q

therapeutic index of amphotericin B?

A

low

53
Q

ADRs of antifungal antibiotics

A

1.GI disturbances
2.rash
3.fever 1-3hrs after start of i.v
4.renal impairment: decreased GFR and renal tubular function
5.hypotension and hypokalemia

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