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PR3151 CA1: Antibiotics (NUS Pharmacy) > Antifungal Agents > Flashcards

Antifungal Agents Flashcards

1
Q

Classification by Mechanism of Action

A
  1. Polyenes (Amphotericin B, Nystatin)
  2. Antimetabolite (5 Flucytosine, Terbinafine)
  3. Echinocandins
  4. Azoles (Triazoles, Imidazoles)
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2
Q

Classification by Site of Infection

A
  1. Subcutaneous and Systemic Mycotic Infections (Amphotericin B, 5 Flucytosine, Echinocandins, Triazoles)
  2. Cutaneous Mycotic Infections (Nystatin, Imidazoles, Terbinafine)
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3
Q

Parenteral Antifungals

A
  1. Amphotericin B
  2. Echinocandins
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4
Q

Oral antifungals

A
  1. 5 Flucytosine
  2. Itraconazole
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5
Q

Oral and parenteral antifungals

A

Triazoles

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6
Q

Topical and Vaginal Suppositories

A
  1. Imidazole
  2. Nystatin (Oral also)
  3. Terbinafine (Oral also)
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7
Q

Terbinafine MOA as Squalene epoxidase inhibitor and Administration?

A

Inhibit squalene conversion to lanosterol and thus biosynthesis of ergosterol, reducing cell membrane function. Toxic accumulation of squalene increases membrane permeability and fungal cell death

Oral and Topical (Cream, gel)

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8
Q

Terbinafine antifungal activity against _______ and is indicated in treatment of ___________________

A

Trichophyton - Cause tinea

Onychomycosis, Tinea capitis (Scalp) - Oral

Tinea corporis (Ringworm), Tinea cruris (Groin), Tinea pedis (Foot) - Topical

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9
Q

Why are onychomycosis and tinea capitis treated by terbinafine orally?

A

Accumulation in the keratin is necessary

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10
Q

Can terbinafine be used in renal and hepatic impairment?

A

To be avoided

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11
Q

Why is terbinafine bioavailability 40%?

A

Extensive CYP450 metabolism and excretion by urine

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12
Q

Terbinafine ADR?

A
  1. GI disturbance
  2. Headache, rash
  3. Elevated LFTs
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13
Q

Terbinafine is contraindicated in ________ but is it safe in pregnancy?

A

Breastfeeding (Accumulation in milk)

Safe in pregnancy

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14
Q

Nystatin oral administration instructions

A

Swish and swallow or Swish and spit

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15
Q

Nystatin is indicated for use in …

A
  1. Oropharyngeal candidiasis (Thrush)
  2. Vulvulovaginal candidiasis
  3. Cutaneous candidiasis
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16
Q

Why is nystatin not given parenterally?

A

Acute infusion-related adverse effects and nephrotoxicity can occur (Systemic toxicity)

17
Q

Nystatin ADR

A

Well tolerated. Some skin irritation for topical and vaginal formulations

18
Q

How long does miconazole stay on the skin and how deep it penetrates?

A

Stratum corneum for more than 4 days

19
Q

Miconazole is indicated in …

A
  1. Tinea pedis (Foot)
  2. Tinea cruris (Groin)
  3. Tinea versicolor
  4. Vulvulovaginal candidiasis
20
Q

Clotrimazole is used for …

A
  1. Dermatophyte infections (Cutaneous candidiasis)
  2. Vulvulovaginal candidiasis
  3. Oropharyngeal candidiasis
21
Q

Imidazole ADRs

A

Contact dermatitis, vulvulovaginal irritation, edema

GI disturbance

Elevated liver enzymes (Clotrimazole oral)

22
Q

Which triazole requires dose adjustment in renal impairment?

A

Fluconazole

23
Q

How are each triazole cleared?

A
  1. Fluconazole - Renally excreted unchanged
  2. Posaconazole - Fecal excretion
  3. Itraconazole - Hepatic metabolism and renally excreted
  4. Voriconazole - Hepatic metabolism and renally excreted
24
Q

Which triazole is taken orally only?

A

Itraconazole

25
Q

Oral administration counselling points for posaconazole, itraconazole and voriconazole?

A

Take with high fat meal (Dairy product) - Posaconazole

Avoid antacids, PPI, H2RAs

Best taken on empty stomach - Itraconazole, Voriconazole

26
Q

Azole inhibit hepatic CYP450 3A4 and enhance the activity of which drugs?

A

Warfarin, cyclosporine, oral hypoglycemic agents

27
Q

Can azoles be used in pregnancy?

A

Teratogenic - Avoid in pregnancy

28
Q

How are echinocandins cleared?

A

Hepatic metabolism by hydrolysis and N-acetylation and excreted in urine and feces

29
Q

Echinocandin ADR

A

Well tolerated, sometimes GIT, fevers, chills, rashes, skin flushing, thrombocytopenia

30
Q

Mycotic Drugs with good CSF penetration

A

Fluconazole, Voriconazole, 5 Flucytosine

31
Q

How does conventional amphotericin B cause nephrotoxicity?

A

Despite low drug levels excreted in the urine, conventional amphotericin B causes renal vasoconstriction and reduces GFR by more than half

32
Q

Amphotericin B ADRs

A

Fever and chills, Nephrotoxicity, Electrolyte imbalances (Hypotension), Thrombophlebitis, Bone Marrow Suppression (Anemia)

PR3151 CA1: Antibiotics (NUS Pharmacy) (11 decks)

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