Nucleic Acid Synthesis and Metabolic Inhibitors Flashcards

1
Q

What are the 3 AB that inhibit folate synthesis?

A

Sulfonamides, Trimethoprim, and Dapsone

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2
Q

What is Dapsone used for?

A

PCP prophylaxis in HIV infected person

Alternative to TMP/SMX

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3
Q

What is Sulfisoxazole acetyl marketed for and with?

A

In combo with erythromycin ethylsuccinate for kids w/ otitis media

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4
Q

What is the MOA of TMP/SMX?

A

Inhibits tetrahydrofolate synthesis

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5
Q

What is the MOA of trimethoprim?

A

Inhibits dihydrofolate reductase and in turn reduces it to tetrahydrofolate

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6
Q

In general, sulfonamides exert a (bactericidal/bacteriostatic) effect

A

bacteriostatic

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7
Q

What is the spectrum of activity of TMP/SMX?

A

G+ (strep and staph)
G-
No anaerobes
Pneumocystis jirovecii (PCP)

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8
Q

What is the ratio of TMP:SMX in serum/tissue?

A

1:20

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9
Q

What is the ratio of TMP:SMX in a oral/IV dose?

A

1:5

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10
Q

Where is TMP/SMX distributed to?

A
  1. Urine
  2. Prostate
  3. CSF
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11
Q

Why is the use of TMP/SMX generally limited?

A

Because of resistance

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12
Q

What is the drug of choice for treatment and prophylaxis of Pneumocystis jirovecii pneumonia?

A

TMP/SMX

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13
Q

What are the AEs of TMP/SMX?

A
  1. GI issues
  2. Hematological (most serious)
  3. Skin disorders
  4. Sun sensitivity (due to sulfa)
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14
Q

What is a serious skin disorder from using sulfa drugs?

A

Steven’s Johnson Syndrome

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15
Q

What are the 1st GEN fluoroquinolones?

A

Nalidixic Acid

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16
Q

What are the 2nd GEN fluroquinolones?

A
  1. Ciprofloxacin
  2. Ofloxacin
  3. Norfloxacin
17
Q

What are the 3rd GEN fluroquinolones?

A

Levofloxacin

18
Q

What are the 4th GEN fluroquinolones?

A
  1. Gemifloxacin

2. Moxifloxacin

19
Q

Quinolone antibiotics target what?

A

Bacterial DNA gyrase and topoisomerase IV

G+; target = Topoisomerase
G-; target = DNA gyrase

20
Q

Which quinolones cover Pseudomonas?

A

Cipro + Levofloxacin + Delafloxacin

21
Q

Which quinolones cover S. pneum?

A

Gemifloxacin

22
Q

Which GEN of quinolones has better G+ coverage?

A

3rd and 4th GEN

23
Q

Which GEN of quinolones has better G- coverage?

A

They are all about the same

24
Q

What are the atypicals that are covered by quinolones?

A
  1. Legionella pneumophila
  2. Chlamydia sp.
  3. Mycoplasma sp.
25
Q

Which quinolone has the highest bioavailability?

A

Levofloxacin (99%)

26
Q

Which quinolone has the least bioavailability?

A

Norfloxacin (50%)

27
Q

Quinolones are (concentration/time)-dependent

A

Both

28
Q

What is special about the distribution of quinolones?

A

Extensive tissue distribution (prostate, liver, lung, skin, bone, urinary tract)

29
Q

What are the AE of quinolones? Which one is the black box warning*?

A
  1. Articular Damage
  2. Tendonitis/tendon rupture*
  3. Dysglycemias
  4. Hypersensitivity
  5. Prolongation of QTc interval
30
Q

What medications should you avoid when using quinolones?

A

Class III (block K+) and Class IA (block K+ and Na+) antiarrhythmics or erythromycin

31
Q

What are some drug interactions with quinolones?

A
  1. Anything w/ divalent or trivalent cations (Calcium, aluminum)
  2. Antacids, sucralfate, multivitamins
    * *administer doses at least 2 hrs apart, take quinolone first
32
Q

What kind of drug is Metronidazole?

A

Prodrug; only anaerobes convert Flagyl to its active form

33
Q

What is the spectrum of Flagyl?

A

Anaerobes + Protozoa (Trichomonas vaginalis, amebiasis, and giardiasis)

34
Q

How is Flagyl distributed?

A

Penetrates CSF

35
Q

What is the half-life of Flagyl?

A

6 to 8 hrs

36
Q

What is the drug of choice for P. colitis due to C. difficile?

A

Flagyl

37
Q

What are the AE of Flagyl?

A

Metallic taste

38
Q

Are there any RX interactions w/ Flagyl?

A

Alcohol

39
Q

What is Nitrofurantoin used for?

A

Against G+ or G- infections that cause UTIs