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Test > Macrolides And Ketolide > Flashcards

Macrolides And Ketolide Flashcards

1
Q

Are Macrolides/Ketolides bacteriostatic or -icidal?

A

Bacteriostatic. Rely on adequate T/B cells and complement defense
-suppress cellular activity
Except they are bactericidal to strep pneumonia and strep pyrogenes

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2
Q

Are Macrolides/ketolides concentration dependent or time dependent?

A

Concentration dependent

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3
Q

What is the bacteriostatic nemonic?

A

We’re ECSTaTIC about bacteriostatics!
Erythromycin, Clinda, Sulfa, Trimethorprim, Tetracyclines, chloramphenicol

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4
Q

What is the bactericidal nemonic?

A

Very Finely Proficient At Cell Murder
-Vanc, Fluoroquinolones, PCNs, Aminoglycosides, Cephalosporins, Metronidazole

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5
Q

What class of drug to erythromycin, clarithromyacin, and azithromyacin fall under?

A

Macrolides; Protein Synthesis Inhibitors

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6
Q

What is the MOA of Macrolides?

A

Inhibit protein synth by binding to domain II and V on 50s ribosomal subunits; makes the bacteria not work as well

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7
Q

Macrolides share domain binding sites with what other abx, and, therefore, should not be used together?

A

Clindamycin, lincomycin, chloramphenicol, streptogramins

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8
Q

Macrolides offer good coverage for what atypical bacteria?

A

Mycoplasma pneumonia and legionella
-mycoplasmas like to hide in cells and Macrolides offer good cell penetration.
-mycoplasmas don’t have cell walls, so cell wall synthesis inhibitors can’t work on them

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9
Q

What Gram + bugs to Macrolides cover?

A

Group A strep, strep pneumonia, strep pyogenes, strep viridans, staph aureus MSSA (NOT MRSA*), listeria

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10
Q

What Gram - coverage to Macrolides offer?

A

Bordatella purtussis, campylobacter, clamydia, H. influenzae, H. Pylori, legionella, MAC (except eryth), gonorrhea, shigella, S. Typhi

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11
Q

What three drugs are used to treat H. Pylori

A

Clarithromyacin, amoxicillin, and a PPI

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12
Q

What are the general uses for Macrolides?

A
  • upper and lower resp infections (otitis media, pharyngitis (s. Pyogenes), sinusitis, CAP)
  • Cervicitis, chlamydia, bacterial COPD exacerbations, whooping cough (pertussis)
  • bacterial conjunctivitis, corneal ulceration, prophylaxis of ophthalmia neonatorum
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13
Q

What is the mechanism of resistance against Macrolides?

A
  • Methylation of guanine reside on the rRNA, making them less effective at protein synth, but also making Macrolides less effective or
  • mutation of domain V, causing reduced binding to eryth and clarith or
  • efflux pumps kicking the abx out
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14
Q

Which Macrolide has the most convenient dosing schedule?

A

Azithromyacin; Zpack is 500mg per day, 250mg 2-5d.
- longest half life of Macrolides: 68h

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15
Q

Which macrolide has the least convenient dosing schedule?

A

Erythromycin. 250-500mg q6h

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16
Q

What are the SE for azithromyacin?\

A
  • GI upset
  • QT prolong
  • bad taste, hearing loss
  • antacids decrease levels
17
Q

What are the SE of clarithromyacin?

A

Bad taste, GI upset, QT prolong; adjust for renal fx, hearing loss, hold statins dt tendon rupture risk

18
Q

What are the SE of erythromycin?

A

Diarrhea (the worst), QT prolong, SJS, hearing loss
- contra w myasthenia gravis, liver disease, pimozide, and alkaloids can cause ergot tox

19
Q

What is azithromyacin’s relationship with CYP3A4?

A

No interaction

20
Q

What is clarithromyacin’s relationship with CYP3A4?

A

Moderate inhibito

21
Q

What is erythromyacin’s relationship with CYP3A4?

A

MAJOR inhibitor

22
Q

Fidaxomicin is used for?

23
Q

Which Macrolides do you use opthalmically?

A

Erythromycin and azithromyacin (use DuraSite as it’s an aqueous solution)

24
Q

What is the main difference between Macrolides and ketolide?

A

Ketolide lacks the 3-L-cladinose side group, binds to domains II and V on the 23s rRNA of the 50s subunit
- this different retains its activity against methylation of domain V that causes resistance to other Macrolides
- allows it to work against MDR S. Pneumoniae, CAP, and bacterial infections of chronic bronchitis

25
Q

Ketolides work against which gram + bugs?

A

Group A strep, strep pneumonia, ***MDRSP, strep pyogenes, strep viridans, staph aureus (MSSA)

26
Q

Ketolides work against which Gram - bugs?

A

H. Influenzae, m. Catarrhalis
- also good atypical coverage

27
Q

Which drug is a Ketolides and what are its SEs?

A

Telithromycin
- visual disturbances, liver tox, QT prolong

28
Q

Telithromycin is contraindicated in which cases?

A
  • Dt being a CYP3A4 inhibitor stop: lovastatin, simvastatin, atorvastatin; caution with dig and metoprolol
  • contra with myasthenia gravis
  • renal adjustment

Test (13 decks)

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