06b: Antibac and Antifungal Agents II Flashcards

1
Q

Antifolates, such as (X), are (bacteriostatic/bactericidal).

A

X = Sulfonamides/Trimethorpim

Bacteriostatic

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2
Q

Antifolates are used primarily in (hospital/community) settings due to (good/poor) oral absorption and (many/few) adverse effects.

A

Community; good; few (hypersensitivity, hematologic, and photosensitivity)

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3
Q

Sulfonamides are in (X) class of drugs and work by (stimulating/inhibiting) (Y).

A

X = antifolates;

Inhibit (PABA structural analog) dihydropteroate synthetase

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4
Q

Trimethoprim is in (X) class of drugs and work by (stimulating/inhibiting) (Y).

A

X = antifolates;

Inhibit DHF reductase (thus inhibiting DNA synthesis/cell replication)

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5
Q

Antifolates spectrum includes gram (pos/neg) (aerobes/anaerobes). Give some special examples of its coverage.

A

Pos and neg aerobes;

MRSA, Listeria, P. jiroveci (PCP), Shigella

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6
Q

T/F: Sulfonamide/Trimethoprim can’t be used for CNS infections due to poor distribution into CSF.

A

False - good CSF distribution

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7
Q

List three clinical diseases that antifolates are typically used for.

A
  1. UTI (concentrate in urine)
  2. PCP
  3. S. aureus skin/soft tissue infections
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8
Q

List two examples of first-line antimycobacterial agents.

A
  1. Rifampin

2. Isoniazid

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9
Q

Rifampin mechanism of action.

A

Blocks RNA Pol (transcription)

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10
Q

Rifampin has (narrow/broad) spectrum of activity and is usually given as (mono/combination) therapy.

A

Broad;

COMBINATION! All anti-mycobacterial agents given in combo

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11
Q

Rifampin is (bacteriostatic/bactericidal). It acts (slowly/quickly) on (replicating/non-replicating) cells.

A

Bactericidal;
Slowly;
Both

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12
Q

T/F: Rifampin and Isoniazid should only be given via IV.

A

False - good oral absorption

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13
Q

(X) anti-mycobacterial agent has many drug interactions since it’s an (inducer/inhibitor) of CYP450 enzymes.

A

X = Rifampin

Inducer

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14
Q

T/F: Rifampin and Isoniazid should only be given in combo therapy due to their broad spectrum of activity.

A

False - isoniazid SELECTIVE for mycobac;

Given in combo therapy to avoid development of resistance

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15
Q

Isoniazid mechanism of action is to (stimulate/inhibit) (X). It’s (bacteriostatic/bactericidal) and acts on (replicating/non-replicating) cells.

A

Inhibit;
X = mycolic acids of mycobac cell wall

Bactericidal;
Rapidly growing

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16
Q

(Rifampin/Isoniazid) is metabolized by liver.

A

Both

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17
Q

A malnourished individual may develop (X) adverse effect when taking (Y) antibiotic. This can be avoided with vitamin (Z) supplementation.

A
X = peripheral neuropathy
Y = Isoniazid
Z = B
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18
Q

List the four types of anti-fungals and a prototype of each.

A
  1. Polyene (Amphotericin B)
  2. Azoles (Fluconazole)
  3. Echinocandins (caspofungin)
  4. Flucytosine
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19
Q

“Gold standard” antifungal.

A

Amphotericin B

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20
Q

Amphotericin B mechanism of action.

A

Binds ergosterol, inserts itself into membrane and increases its permeability

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21
Q

Amphotericin B is (fungicidal/fungistatic) and (time/conc)-dependent.

A

Fungicidal;

Conc-dependent

22
Q

T/F: Amphotericin B is only given via IV.

A

True - poor oral absorption

23
Q

Amphotericin B is mainly (hydrophilic/lipophilic) and has (good/poor) distribution.

A

Lipophilic; good (wide)

24
Q

Reluctancy to use amphotericin B largely due to which reason?

A

Adverse effects/toxicity (esp nephrotoxicity)

25
Q

K an Mg wasting can be seen in (X) drug adverse effect. Why does this happen?

A

X = amphotericin B

Drug binds to our cells’ cholesterol (instead of ergosterol of fungi membrane)

26
Q

Amphotericin B lipid products can be given to (increase/decrease) free drug concentrations and thus (increase/decrease) (X). What’s a limiting factor for these drugs?

A

Decrease (drug released slowly from lipid carrier);
Decrease
X = nephrotoxicity

Expensive!

27
Q

T/F: Over the years, use of amphotericin B has decreased due to lower incidence of fungal infections.

A

False - due to availability of less toxic agents

28
Q

Azoles, such as (X), mechanism of action is to (stimulate/inhibit) (X).

A

X = fluconazole
Inhibit
Y = fungal CYP450 (which converts lanosterol to ergosterol)

29
Q

T/F: Azoles are all fungistatic and metabolized in liver.

A

True

30
Q

Fluconazole mainly covers which species?

A

Candida and Cryptococcus

31
Q

T/F: All azoles can be used for mucocutaneous candidiasis.

A

True

32
Q

Voriconazole is first-line therapy for (X).

A

X = invasive aspergillosis

33
Q

T/F: All azoles cover aspergillus species.

A

False - voriconazole and itraconazole do, but not fluconazole

34
Q

T/F: All azoles cover candida species.

A

True

35
Q

(X) antifungal is second-line therapy for cryptococcal meningitis.

A

X = fluconazole

36
Q

(X) antifungal should not be used in patients with (Y) disease due to hypokalemia, edema, and negative inotropic adverse effects.

A
X = Itraconazole (an azole)
Y = HF
37
Q

T/F: All azoles are CYP450 inhibitors.

A

True

38
Q

T/F: Fluconazole is the most toxic of the azole antifungals.

A

False - generally very well tolerated

39
Q

When giving patient a loading dose of (X) antifungal, it’s important to warm him/her about potential hallucinations until maintenance doses are given.

A

X = voriconazole

40
Q

T/F: Azoles don’t treat histoplasmiosis.

A

False - itraconazole does

41
Q

Echinocandins, such as (X), are (fungistatic/fungicidal) and work by (stimulating/inhibiting) (Y).

A

X = caspofungin
Fungicidal;
Inhibiting;
Y = glucan synthase (thus cell wall synthesis)

42
Q

(X) antifungal, the second-line treatment for (Y) is not FDA approved for this disease.

A
X = caspofungin 
Y = invasive aspergillosis
43
Q

Caspofungin has broad coverage of (X) species.

A

X = Candida

44
Q

T/F: Caspofungin is given OTC for Candida infections.

A

False - only IV

45
Q

T/F: Caspofungin has wide distribution and is generally very well tolerated.

A

True

46
Q

Flucytosine (stimulates/inhibits) (X) process after undergoing (amination/deamination/acetylation/deacetylation) in cell.

A

Inhibits;
X = fungal DNA/RNA synthesis;
De-amination (to 5-flurouracil)

47
Q

Flucytosine covers which species of fungi?

A

Candida and Cryptococcus

48
Q

(X) is the “Rifampin” of the fungal world. This is because…

A

X = flucytosine

It’s given in combo therapy with amphotericin B

49
Q

T/F: Flucytosine usually given in combo therapy due to poor oral absorption and distribution.

A

False - rapid oral absorption and wide distribution (including CSF)

50
Q

Why might flucytosine/amphotericin B combo be especially problematic in patients with (hepatic/renal) dysfunction?

A

Renal;
Amp is nephrotoxic and flucytosine 90% excretion in urine (unchanged)

SO must monitor/adjust carefully!