CD 14 Flashcards

1
Q

Fungal infections Associated with

A

Skin
Mucous membranes
but Minor in healthy people

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2
Q

Fungal infections serious when

A
Systemic infections
Tinea pedis (Athlete’s foot)
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3
Q

Does Fungi are complex?

A

complex and evolved than bacteria

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4
Q

Do fungi is Clinically important?

A

Yes and Opportunistic pathogens

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5
Q

What is Amphotericin B?

A
  • Polyene antibiotic
  • Binds to ergosterol in fungal membrane
  • Helps to penetrate the wall
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6
Q

What is the Pharmacokinetics of Amphotericin (B)?

A

Used topically, systemic i.v. infusion

Excreted via by kidneys

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7
Q

What are the Unwanted effect of Amphotericin (B)?

A

Renal toxicity (80% of patients)
Hypokalemia (20%)
thrombophlebitis (Blood clots)

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8
Q

What are the clinical Usages of Amphotericin (B)?

A

Candida oesophagitis (HIV/AIDS)
Mucormycosis (weakened immune system e.g. organ transplant)
Meningitis

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9
Q

What is the mechanism of Nystatin?

Pharmacokinetics of Nystatin

A

Nystatin binds to ergosterol, a major component of the fungal cell membrane.It forms pores in the membrane that lead to K+ leakage, acidification, and death of the fungus.

Pharmacokinetics: Not absorbed from the GI tract, skin, or vagina good for ‘topical’ use

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10
Q

What are the Unwanted effects of Nystatin?

A

None to note however, Allergic reactions very uncommon

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11
Q

What is the Therapeutic Use of Nystatin?

A

Only for candidiasis (thrush)

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12
Q

What are the Griseofulvin?

A

FungiSTATIC and Narrow spectrum

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13
Q

What is the Pharmacokinetics of Griseofulvin?

A
  • Given orally
  • Taken up selectively by newly formed skin, concentrated in keratin
  • t1/2=24h (retained much longer)
  • CYP1A2 inducer Clinically significant drug interactions with warfarin
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14
Q

What are the Unwanted effects of Griseofulvin?

A
  • GI upset
  • Photosensitivity

Caution: Not for use in pregnant women (teratogenic)

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15
Q

What are the unwanted effect of amphotericin B

A

Infusion-related toxicity and nephrotoxicity

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16
Q

What Echinocandins inhibit? e.g. Caspofungin, micafungin, anidulafungin

A

Inhibit synthesis of 1,3-β-D-glucans↓structural integrity=>death
• FungiCIDAL

17
Q

Pharmacokinetics of Echinocandins

A

given i.v.
Don’t penetrate into CSF (cerebrospinal fluid)
No renal clearance
(little effect on [drug] plasma in renal impairment

18
Q

Unwanted effects of Echinocandins

A

Remarkably well tolerated
Phlebitis at injection site (caspofungin)
Histamine-like effects (rapid infusion)

19
Q

Therapeutic Use of Echinocandins

A

Deeply invasive candidiasis

Salvage therapy* for invasive aspergillosis

20
Q

Caspofungin and micofungin are mild inhibitors of CYP3A4

A

↑[drug]plasma tacrolimus

21
Q

rifampicin is inducers of CYP3A4?

A

↓[drug]plasma of caspofungin

22
Q

Azoles (e.g fluconazole, itroconazole, miconazole, voriconazole, posaconazole)

A
  • Inhibit 14-α-sterol demethylase

* FungiSTATIC (broad spectrum)

23
Q

Pharmacokinetics of Azoles

A

Can be given orally or i.v.
Short t1/2 ~6-8h (miconazole., voriconazole)
• Long t1/2 ~30-40h (fluconazole., itroconazole, posaconazole)

24
Q

Unwanted effects of Azoles

A

• Nausea
• Headache
Teratogenic: avoid during pregnancy
Need effective contraception during treatment

25
Therapeutic Use of Azoles
- Candidiasis - Seborrheic dermatitis - Cryptococcal meningitis (AIDS)
26
Fluconazole, Voriconazole is
CYP3A4 CYP2C9 CYP2C19 inhibitor
27
itraconazole, Posaconazole is
CYP3A4 inhibitor
28
clotriamzole
OTC topical treatment Superficial fungal infections Thrush (candidiasis), tinea, fungal keratitis, nappy rash
29
Flucytosine
Converted to 5-fluorouracil in fungi • 5-FU inhibits thymidylate synthetase and DNA synthesis • Limited spectrum, combined with amphotericin and/or azoles • Resistance common
30
Pharmacokinetics of Flucytosine
Given by i.v. infusion, can also be given orally • t1/2 ~3-5h • 90% excreted unchanged by kidney • Dosage should be reduced in renal impairment
31
Unwanted effects of Flucytosine
* Anaemia, * Neutropenia * GI disturbances
32
Terbinafine (Lamisil)
ergosterol (fungir cell membrane e thaky) synthesis inhibitor • FungiCIDAL
33
Pharmacokinetics of Terbinafine (Lamisil)
Topical or oral • Well absorbed (↓ bioavailability due to first pass metabolism) • Accumulates in skin, hair and nails • Metabolised in liver, excreted in urine
34
Unwanted effects of Terbinafine (Lamisil)
Low incidence of GI distress, headache or rash Not recommended in hepatic failure Systemic therapy avoided during pregnancy
35
Therapeutic Use of Terbinafine (Lamisil)
Nail onychomycosis (oral) Tinea (cream or spray)
36
Terbinafine (Lamisil) increase blood plasma of which drugs?
Rifampin ↓ | Cimetidine ↑