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Protein synthesis inhibitors Flashcards

1
Q

How do AGs work?

A

They block translocation and termination of peptides

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2
Q

How do tetracyclines work?

A

They block AA-tRNA

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3
Q

How do macrolide work?

A

They lock translocation of peptides

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4
Q

How do oxazolidinones (linezolid) work?

A

Block 50 S binding

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5
Q

CLEan TAG

A

50s: chloramphenicol, clindamycin, linezolid, erythromycin
30s: tetracyclines and aminoglycosides

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6
Q

Name the aminoglycosides

A

Gentamicin and tobramycin

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7
Q

What are aminoglycosides good at covering?

A

aerobic GNRs

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8
Q

What formulary is available for AGs?

A

Only IV

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9
Q

What are the side effects of aminoglycosides?

A

Nephrotoxic and ototoxic. Lots of kids given gentamicin develop irreversible hearing loss which is why we don’t often use it.

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10
Q

Describe concentration dependent killing versus time dependent killing

A

Concentration dependent=Exposure to higher concentration for a short time

Time dependent=Longer exposure with more dosings is more efficient

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11
Q

Which drugs rely on concentration dependent killing?

A

Aminoglycosides
fluoroquinolones
metronidazole

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12
Q

Which drugs rely on time dependent killing?

A

penicillins

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13
Q

Extended interval dosing:

A

Give lots of smaller doses throughout the day to keep toxicity low but remain in efective range

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14
Q

How to tetracyclines work?

A

They bind to 30S unit and block the aminoacyl tRNA too

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15
Q

What are the major situations in which we would use a tetracycline?

A

Rocky mountain spotted fever and lyme dz

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16
Q

How do macrolides develop resistance?

A

23S rRNA nucleotide mutation

Efflux

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17
Q

When do we use macrolides?

A

Respiratory tract infections

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18
Q

What is unique about the metabolism of macrolides?

A

They have a very long half life

19
Q

What are the side effects of macrolides?

A

Ototoxicity

20
Q

What do the macrolides cover?

A
  1. GPC (staph and strep often resistant)
  2. mycoplasma
  3. legionella
  4. chlamydia, mycobacteria
  5. H. flu
    - –>basically all the atypicals
21
Q

How does clindamycin work?

A

Binds to 23S rRNA binding site, preventing peptide bond formation

22
Q

What drug should you NOT prescribe with clindamycin? Why?

A

Macrolides–because will have mutual interference

23
Q

Is clindamycin bacteriostatic or bacteriocidal?

A

bacteriostatic. Almost all of the protein synthesis inhibitors are bacteriostatic EXCEPT the aminoglycosides

24
Q

What is clindamycin effective against?

A

GPC and oral/bowel anaerobes

25
Q

How does linezolid work?

A

Prevents 50S from binding the 30S unit

26
Q

What is linezolid effective against?

A

VRE, VRSA, MRSA

27
Q

How do sulfa drugs work?

A

They inhibit dihydropteorate synthesis

28
Q

How does trimethoprim work?

A

Inhibits DHFR

29
Q

Is bactrim static or cidal?

A

static

30
Q

What are the contraindications to bactrim?

A

erythema multiforme rxn
Pregnancy***
Can cause bone marrow suppression

31
Q

What is bactrim good for?

A

S pneumo

H flu, E coli, pneumocystis

32
Q

How do fluoroquinolones work?

A

They inhibit DNA gyrase

33
Q

What are three mechanisms of resistance with fluoroquinolones?

A
  1. Reduced binding to DNA topoisomerase (gyrase)
  2. Protection by QnR protein
  3. Impaired permeability and drug efflux
34
Q

Are fluoros cidal or static?

A

cidal

35
Q

Cipro is used for:

A

Uti and STD (mostly gram negative coverage)

–Cipro has better penetration of the urinary tract

36
Q

Mox/levo is used for:

A

pneumonia (good gram positive coverage too unlike cipro)

37
Q

How does metronidazole work?

A

Damages DNA by forming a nitro radical

38
Q

What is metronidazole used for?

A

Anaerobes (bowel, oral)
C difficile infection
Giardia
Amoeba

39
Q

What are the side effects of metronidazole?

A

Metallic taste
GI upset
CNS: ataxia/vertigo
teratogen

40
Q

How does Rifampin work?

A

Binds to RNA polymerase and inhibits

41
Q

What is Rifampin good for?

A

It’s broad spectrum and good for: GP and GN coverage

Mycobacterium especially

42
Q

How does rifampin resistance develop?

A

Mutation of the RNA poly binding site. Resistance develops very easily, so never use alone

43
Q

How do you treat pertussis?

A

Azithromycin

–can also use bactrim

ID (24 decks)

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