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Respiratory Medicine-Unit 2 > Pharmacology of antifungal drugs (Fitz) > Flashcards

Pharmacology of antifungal drugs (Fitz) Flashcards

1
Q

Amphotericin B is this type of anti-fungal:

A

polyene

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2
Q

what is the MOA of amphotericin B?

A

penetrate cell membrane –> bind to ergosterol –> create pores –> Disrupt membrane integrity –> increase osmotic fragility

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3
Q

What is the therapyutic index of Amphotericin B? What are some adverse effects at onset of infusion? Later onset?

A

therapeutic index: poor ~1.5-2x

onset at infusion: Chills, fever, anemia, hypotension

later onset: nephrotoxicity –> direct damage to distal tubule membrane; Na, K, mg wasting, hypokalemia; Decreased GFR (arteriole constriction)

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4
Q

Amphotericin B aggravates the nephrotoxicity of other drugs, particularly these types of pts:

A

transplant, allograft pts: cyclosporine, sirolimus, tacrolimus

HIV pts: Foscarnet, pentamidine

Serious infx: Gram -, MRSA (Aminoglycosides, vancomycin)

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5
Q

What type of anti fungal drug is Fluconazole?

A

1st generation Triazole

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6
Q

what is the MOA of Azoles?

A

create deficit of ergosterol –> disrupt sterol content (create Lanosterol surplus, inhibit formation of ergosterol)

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7
Q

what are indications for Fluconazole?

A

Narrow spectrum
Candida albicans (candidemia, local candidiasis)
Cryptococcus (meningitis, with AMP-B)

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8
Q

what are limitations of Fluconazole?

A

NO activity vs Aspergillus

2nd line vs most true pathogens

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9
Q

What is the clearance of Fluconazole?

A

renal (75%)

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10
Q

what is the bioavailability and absorption of Itraconazole?

A 
Poor bioavailability (50%)
Poor solubility (requires acid)
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11
Q

what type of CSF access does Itraconazole have? Does it have any interaction with CYP450?

A

poor CSF access

Strong CYP450 inhibitor

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12
Q

This triazole is the drug of choice/recommended for Aspergillus spp

A

Voriconazole

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13
Q

This triazole is the drug of choice/recommended for histoplasmosis, coccidioides, and blastomycoses:

A

Itraconazole

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14
Q

this triazole is resistant to “other” candida and can be used for cryptococcus:

A

fluconzaole

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15
Q

list some fungal resistance mechanisms to azoles:

A
  • mutation of lanosterol-14a-demethylase
  • overexpression of lanosterol-14a-demethylase
  • energy-dependent efflux systems
  • changes in sterol and/or phospholipid composition of fungal cell membrane (decreased permeability)
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16
Q

Caspofungin is what type of anti-fungal?

A

Echinocandin

17
Q

what is the MOA of Caspofungin

A

Inhibits B(1,3) glucan synthase

18
Q

Describe the pharmacokinetics of Caspofungin:

A
  • Well-tolerated
  • Hepatic metabolism
  • Few drug interactins
19
Q

what are some therapeutic indications for Caspofungin?

A

Opportunistic infx (serious) –> invasive candidiasis, candidemia; Invasive aspergillosis

20
Q

What are some therapeutic limitations of Echinocandins (Caspofungin)? i.e., what are they not effective against?

A

Histoplasmosis
Coccidioidomycosis
Fusarium spp

21
Q

What are therapeutic indications of triazoles for opportunistic infx? Pathogenic infx?

A

opportunistic –> aspergillus, candida, rhizopus, cryptococcus

pathogenic –> histoplasma, coccidioides, blastomyces, paracoccidiodies

22
Q

what are some indications for Itraconazole?

A

Broad spectrum –> covers candida, some activity vs aspergillus

Front line/recommended for histoplasmosis, coccidioides, blastomycoses, true pathogenic infx

23
Q

what is a major adverse effect of Ketoconazole?

A

Gynecomastia and decreased libido

inhibits human adrenal and gonadal steroid synthesis

24
Q

what are some “pros” for absorption and distribution of Voriconazole and Fluconazole?

A

both are readily absorbed (>90% bioavailability) with excellent distribution including CSF

25
Q

What are some “cons” for absorption and distribution of Itraconazole?

A

Like ketoconazole; it requires gastric acidity to dissolve. Poor CSF penetration

26
Q

these triazoles are strong inhibitors of hepatic CYP450 and enhance renal toxicity:

A

voriconazole and itraconazole

27
Q

what are common and rare side effects of vori/flucon/itraconazole?

A

avoid all triazoles in pregnancy
all triazoles can damage liver
genetics alter voriconazole clearance
voriconazole disturbs vision

28
Q

This is the drug of choice for Mucormycosis (zygomycosis)

A

Amphotericin B

that Joplin slide

29
Q

this is the drug of choice for cryptococcal meningitis

A

Amphotericin B

lipid formulations and in combo with 5-FC

Respiratory Medicine-Unit 2 (5 decks)

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