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FOM > Week 4 - Nucleic Acid Inhibitors > Flashcards

Week 4 - Nucleic Acid Inhibitors Flashcards

1
Q

What is the mechanism of action for Rifampin?

A

bactericidal – binds RNA pol at the active center, blocks elongation

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2
Q

What is Rifampin used to treat?

A

TB

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3
Q

What drug has the side effect of turning body fluids orange-red?

A

Rifampin

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4
Q

Why would Rifampin not be prescribed for someone who is taking organ rejection meds?

A

induction of Cyp450 enzyme can induce metabolism of other drugs at higher rate, leading to lower drug amounts in your system

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5
Q

How does impaired liver function lead to higher blood levels of Rifampin?

A

no deacetylation –>Rifampin remains hydrophobic–>decreased excretion through feces–>build up in blood

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6
Q

What is the mechanism of action for Fidaxomicin?

A

bactericidal - inhibits RNA pol

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7
Q

What is the spectrum for Fidoxamicin?

A

narrow, Gram + anaerobes (C. diff)

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8
Q

Why is Fidoxamicin used to treat C. diff?

A

low absorption

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9
Q

What are the fluoroquinolones?

A

Ciprofloxacin, levofloxacin, moxifloxacin

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10
Q

What is the mechanism of action for the fluoroquinolones?

A

Bactericidal – bind topo II and IV

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11
Q

What is the spectrum for Fluoroquinolones?

A

broad, Gram+ and Gram -

Mycoplamsa, hospital acquired Pneumonia

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12
Q

Resistance of Fluoroquinolones:

A

overprescribed for UTIs, resp, and acute GI infections

  • active efflux of drug
  • mutations in Topo
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13
Q

Which topo inhibition strategy is most important for each of the classes of bacteria?

A 
Topo II (gyrase)- Gram -
Topo IV - Gram +
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14
Q

How do fluoroquinolones lead to cell death?

A

cause dsDNA breaks

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15
Q

What are a few adverse effects for fluoroquinolones?

A

arthropathy (don’t use with kids or prego)
confusion and photosensitivity
C. diff, fungal infections

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16
Q

What shouldn’t be consumed with fluoroquinolones?

A

calcium, ion, aluminum, zinc because they can prevent drug absorption by binding drug
-avoid milk, fortified juice

17
Q

What is the general mechanism of action for Sulfonamides and Trimethoprim?

A

indirect inhibition of DNA synthesis by blocking dihydrofolic acid synthesis

18
Q

What is the mechanism of action for sulfamethoxazole?

A

bacteriostatic - it is a PABA analog, acts as a competitive inhibitor for Dihydropteroate synthetase

19
Q

Adverse effects of Sulfonamides:

A

Hypersensitivity (Stevens-Johnson), crystalluria, hemolysis if G-6-P dehydrogenase deficient, Kernicterus (jaundice in newborns)

20
Q

Mechanism of action for Trimethoprim:

A

bacteriostatic - inhibits dihydrofolate reductase (low affinity for mammalian)

21
Q

What is the sequential blockade used to treat UTIs and Pneumocystis?

A

TMP-SMX = Bactrin

  • blocks folate synthesis twice to be bactericidal
  • don’t use with sulfa allergy
22
Q

What is the mechanism for Metronidazole/tinidazole?

A

bactericidal - drug is reduced to generate free radicals that lead to DNA strand breaks and cell death

23
Q

Spectrum fro Metronidazole:

A

anaerobic, includes C. diff and Protozoa

24
Q

What is a unique side effect of Metronidazole?

A

disulfiram-like rxn when taken with alcohol – it blocks ALDH
**avoid with prego

25
Q

Why doesn’t metronidazole work on aerobes?

A

metro needs reduced form of ferredoxin

-aerobes have mostly oxidized ferredoxin

26
Q

Mechanism of Nitrofurantoin:

A

bactericidal – drug is reduced by flavoproteins to reactive intermediates –>alters/inactivates ribosome
-inhibits DNA, RNA, cell wall, and protein synthesis

27
Q

What is the spectrum for nitrofurantoin?

A

broad, rapidly excreted in active form so used primarily for UTIs

28
Q

Resistance mechanisms for nitrofurantoin:

A

none known right now – blocks many vital processes

29
Q

What would be the best empiric treatment for a patient showing symptoms of UTI?

A

TMP/SMX

30
Q

What drugs will have increased efflux as the resistance mechanism?

A

Fluoroquinolones, Sulfonamides

31
Q

What drugs will have decreased uptake as the resistance mechanism?

A

Sulfonamides

32
Q

What drugs will have an altered target as the resistance mechanism?

A

Rifampin, Fluoroquinolones, Sulfonamides, Trimethoprim

FOM (11 decks)

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