50S Protein Synthesis Inhibitors - Fitzpatrick Flashcards

1
Q

Macrolides - drugs (3)

A
  • Erythromycin
  • Clarithromycin
  • Azithromycin
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2
Q

Ketolides - drug (1)

A

Telithromycin

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3
Q

Erythromycin - treats what?

In respiratory medicine, used when?

A
  • Gram (+) cocci (Staph, Strep)
  • SYPHILIS (treponema pallidum)

If Penicillin allergy - for strep throat, strep. pneumonia, etc.

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4
Q

Clarithromycin - treats what?

A
  • Gram (+) cocci (NOT MRSA)
  • Some gram (-)
  • Chlamydia, Legionella, Moraxella
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5
Q

Azithromycin - DOC for what?

A

Legionella (Legionnaires’ disease)

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6
Q

Telithromycin (Ketolide) - DOC for what?

A

Multi-drug resistant Strep. Pneumoniae

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7
Q

A major indication for Macrolide/Ketolides = _______

A

URI’s, community acquired pneumonia

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8
Q

TYPICAL respiratory infection organisms covered by Macrolides

A
  • Strep. pneumonia
  • Haemophilus
  • Moraxella
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9
Q

ATYPICAL respiratory infection organisms covered by Macrolides

A
  • Legionella
  • Chlamydia
  • Mycoplasma
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10
Q

Most commonly used Macrolide? Why?

A

Azithromycin - long half life, effective, additional gram (-) coverage

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11
Q

Macrolides - MoA

A

Bind 50S ribosome, inhibit translocation of growing peptide along the ribosome to make room for next tRNA

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12
Q

Mechanisms of resistance to Macrolides (2)

A
  • Methylation of ribosome (“erm” genes) - MORE resistant

- Macrolide efflux pumps (“mef” genes) - PARTIAL resistant

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13
Q

Organisms naturally resistant to Macrolides

Why?

A
  • Enterobacter
  • Pseudomonas
  • Acinetobacter

Decreased permeability of outer cell envelope

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14
Q

Adverse effects of Macrolides/Ketolides

A
  • QTc prolongation (blocking inward rectifying K+ channels)

- CYP 3A4 drug interactions

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15
Q

_____ is most associated with increased risk of sudden cardiac death due to QT prolongation / Torsades

This risk is increased in who?

A

Erythromycin

Pt’s taking CYP 3A4 inhibitors –> Erythromycin around longer

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16
Q

A pregnant woman needs a Macrolide for a respiratory infection. Which ones?

A

Erythromycin, Azithromycin

17
Q

Clindamycin - drug class

A

Lincosamides

18
Q

Clindamycin is similar to ____ in terms of MoA, resistance mechanisms, and usage w/ gram (+) cocci

A

Erythromycin

19
Q

Clindamycin - clinical uses (main ones) (2)

A
  • Abdominal ANAEROBES - MAIN ONE (Ex. B. fragilis via gunshot/stab)
  • Toxin-producing bacteria (toxic shock syndrome, PVL toxin, SEB toxin, etc.)
20
Q

Adverse effect of Clindamycin

A

C. diff. overgrowth –> pseudomembranous colitis

21
Q

Treatment of Clindamycin-induced C. Diff. infection

A

Metronidazole + Vancomycin ORALLY (not absorbed)

22
Q

When might Clindamycin be used WITH a Beta-Lactam? Why?

At FIRST glance, why might this be counterintuitive?

A

An infection that is secreting a damaging toxin of some kind
- Clindamycin –> inhibits protein synthesis –> inhibits TOXIN synthesis

NORMALLY, not good to combine a bacteriocidal w/ a bacteriostatic (exception in this case)

23
Q

Chloramphenicol - spectrum?

A

WIDE spectrum (Gram + and Gram -)

24
Q

Chloramphenicol - clinical use?

A

Almost none - life-threatening infections w/ no alternative

25
Q

Chloramphenicol - toxicities

A
  • Aplastic anemia (or hemolytic anemia in G6PD deficiency)
  • Gray Baby Syndrome
    • Abd. distention, diarrhea, vomiting, gray color, death
26
Q

Chloramphenicol - MoA

A

Binds 50S subunit, inhibits peptidyl transferse

27
Q

How is Chloramphenicol toxic to us?

A

Enters our cells and inhibits mitochondrial protein synthesis

28
Q

Linezolid - drug class

A

Oxazolidinones

29
Q

Linezolid - clinical use?

A

Vancomycin-resistant organisms

30
Q

Linezolid - MoA

A

Inhibits 50S subunit from hooking together with the 30S subunit in the initiation complex

31
Q

Linezolid - adverse effect

A

MAO interaction –> peripheral neuropathy