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Pharm Block 12 > Protein Synthesis Inhibitors > Flashcards

Protein Synthesis Inhibitors Flashcards

1
Q

30s drugs

A
  • tetracyclines: doxycycline
  • aminoglycosides: gentamicin

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2
Q

50s drugs

A
  • macrolides: eryhromycin, clarithromycin, azithromycin
  • clindamycin

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3
Q

Protein synthesis overview

A
  1. Imitation: the charged imitation tRNA carries fMet to the ribosome which binds to the AUG start codon
  2. Elongation: a charger tRNA enters the ribosome at the At site, the enzyme peptidyl transferase cleaves the peptide chain form the P site and transfers it to the A site tRNA, the P site tRAN exits the ribosome, the ribosome movies exactly 3 nucleotides (one codon) which moves the tRNA at the A site to the P site (translocation)
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4
Q

Imitation of protein synthesis

A

The charged initator tRNA carriers fMet to the ribosome which binds tot he AUG start codon

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5
Q

Protein elongation

A

A charged tRNA enters the ribosome at the A site, the enzyme peptidyl transferase cleaves the peptide chain from the P site transfers it to the A site tRNA, the P site tRNA exits the ribosome, the ribosome moves exactly 3 nucleotides (codon) which moves the tRNA at the A site and to the P site (translocation)

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6
Q

what is the tetracycline drug

A

Doxycycline.

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7
Q

How many rings are in a tetracycline

A

4 fused ring

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8
Q

MOA of tetracycline (doxycycline)

A
  • bacteriostatic
  • blocks protein synthesis by binding to the 30s ribosomal subunit and blocks the access of tRNA to the A site.

No tRNA can get to A site, no docking occurs

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9
Q

What drugs block translocation

A

Macs
Clundamycin

50s

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10
Q

What do tetracycline do to bacteria

A

Block docking of tRNA

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11
Q

How do AGs inhibit bacteria

A
  1. Formation of initiation complex
  2. Cause misreading of the code
  3. Inhibit translocation
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12
Q

Translocation

A

Moving from A to P

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13
Q

Clinical uses of tetracycline (doxy)

A
  • broad spectrum Abx
  • limited by resistance
  • rickettsia (Rocky Mountain spotted fever) and borrelia (Lyme disease)
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14
Q

What drug is good for treating bacterial infections associated with ticks

A

Tetracycline (doxy)

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15
Q

Resistance of tetracycline (doxy)

A

Widespread

  • accomplished by a Mg++ depends active effluent of the drug by the protein TetA
  • pumps drug right back out
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16
Q

Absorption of tetracycline (doxy)

A
  • should not be taken with dairy food because they chelate with calcium ions
  • cannot take with antacids due to chelation with magnesium and aluminum

Binds metals

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17
Q

Elimination of tetracycline (doxy)

A

By the kidneys (adjust in renal failure)

Doxy is the exception as it is preferentially excreted via the bile (good for renal failure)

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18
Q

What is th exception to renal elimination of tetracycline

A

Doxy can be eliminated by the liver

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19
Q

Adverse effects of tetracyclines (doxy)

A
  • GI discomfort
  • deposition of calcium in bone and teeth
  • causes discoloration of teeth
  • stunts growth in children -
  • phototoxicitiy to exposed skin
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20
Q

Why are tetraclyines not good for children

A

Cause stunted growth

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21
Q

What is the only alone protein synthesis inhibitory that is bactericidal

A

Aminoglycosides (gentamicin)

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22
Q

Is gentamicin 30s or 50s

A

30s

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23
Q

MOA of aminoglycosides (gnetamcicin)

A
  • bactericidal because of all of the different mechanisms
  • entry of drugs into bacterial cells
  • block protein synthesis
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24
Q

How do aminoglycosides gain entry into bacterial cells

A
  • passive diffusion across cell wall
  • active O2 dependent transport (low pH or anaerobic conditions prohibit entry)
  • transport into cells is enchanted by cell wall active drugs like penicillins or vancomycin and is the likely basis for synergism between these compounds
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25
Q

How is transport of a aminoglycosides drug such as gentamicin enhanced

A

With the addition of a penicillin

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26
Q

How do aminoglycosides (gentamicin) block protein synthesis

A
  • bind to 30S ribosomal subunit
  • interfere with a invitation copmplex of peptide formation
  • induce misreading
  • inhibit translocation
  • activities occur simultaneously and overall effect is lethal for the cell
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27
Q

Clinical use of aminoglycosides (gentamicin)

A
  • Active against aerobic gram negative organisms

- synergistic use with penicillins-especially important for organisms like pseudomonas

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28
Q

How do you kill pseudomonas

A

With an aminoglycosides (Gentamicin) + penicillin (pipericillin)

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29
Q

Resistance of aminoglyvosides (gentamicin)

A

Can have some, not super important

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30
Q

Elimination of aminoglycosides (gentamicin)

A

Kidney

Adjust in renal failure

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31
Q

Adverse effects of aminoglycosides (gentamicin)

A

Nephrotoxicity
Ototoxicity
Neuromuscular paralysis

32
Q

Nephrotoxicity in aminoglycosides (gentamicin)

A

Happens when used for more than 5 days

33
Q

Ototoxicity in aminoglycosides (gentamicin)

A
  • auditory damage=tinnitus, high frequency hearing loss
  • vestibular damage-vertigo, ataxia, loss of balance
  • Tx greater than 5 days
  • do not give with loop diuretics
34
Q

Neuromuscular paralysis in aminoglycosides (gentamicin)

A

Can cause respiratory paralysis at very high doses

  • blocks Ach releases
  • Botox like effect
  • not good in MG patients
35
Q

What are the macro lines

A

Erythromycin
Azithromycin
Clarithromycin

“Thromycin”

36
Q

Are the macrolides (thromycin) 30s or 50s

A

50s

37
Q

MO of macrolides (thromycin)

A
  • baceriostatic

- block protein synthesis

38
Q

How do macrolides (thromycin) block protein synthesis

A

Bind to the 50s subunit

-inhibit the translocation reaction

39
Q

Clinical use for macrolides (thromycin)

A
  • community acquired pneumonia due to strep pneumo and atypical such as legionella, chlamydophila, and mycoplasma
  • mycobacterium Avium (MAComplex)
  • chalmydia trachomatis (STD)
  • alternative to B lactams in allergic individuals
40
Q

Resistance of macrolides (thromycin_

A

10-15% of strep pneumonia in the US is completely resistant to macrolides (if the strain is penicillin resistant, then 50% will also be resistance to macrolides)

Resistance happens when the binding site has been methylated

41
Q

Adverse effects of macrolides (thromycin)

A

-epigastric distress, commonly used to increased GI motility and gastric emptying (gastroparesis)

42
Q

What abx is used for people with gastroparesis (such as diabetics)

A

Macrolides (thromycin)

43
Q

Which macrolides are P450 inhibitors

A

Erythromycin and clarithromycin

44
Q

Which macrolides are not P450 inhibitors

A

Azithromycin

Most popular one for this reason

45
Q

Other protein synthesis inhibitors that do not fall into the other groups

A

Clindamycin

46
Q

MOA of clindamycin

A
  • binds to the 50S subunit, inhibits translocation

- macrolides wannabe

47
Q

Clinical use of clindamycin

A

Anaerobes, especially severe infection due to bacteroides

48
Q

What’s the difference between macrolides and clindamycin

A

Used for anaerobes like bacteroides

49
Q

Adverse effects of clindamycin

A

Superinfection of C diff, which causes pseudomembranous colitis
-fever, cramping, abdominal pain

50
Q

What drug can cause a superinfection of C diff

A

Clindamycin

51
Q

How do you treat a superinfection of C diff caused by clindamycin?

A

Metronidazole

52
Q

MOA of metronidazole (flagyl)

A

Don’t really know, think it ends up being a free radial

Targets DNA

53
Q

Is metronidazole bateriostatic or bacteriocoidial

A

Bactericidal

54
Q

Clinical used of metronidazole

A

Anaearobes and some parasites

  • bactericides, clostridium (difficult, non-difficile) DOC
  • trichamonas vaginalis, entamaeba histalytica, giardia lamblia, gardenerella

GET BaC on the METRO, G

55
Q

Elimination of metronidazole

A

Liver

56
Q

Adverse effects of metronidazole

A

Metallic taste

Disulfiram-like effect with alcohol (hangover because of acid aldehyde accumulation)

57
Q

What drugs do we not need to adjust for in renal failure

A

Ceftriaxone
Doxycylcine
Metronidazole
Antisthaph

58
Q

Intro to fluoroquinolones

A

Fluorinated quinolone

Limited to gram negative organisms

59
Q

DOC for bactericides and clostridium

A

Metronidazole

60
Q

MOA of fluoroquinolones

A

Inhibition of DNA gyrase (topoisomerase II)

-makes sure the super coils stay in there and tension will break the DNA

61
Q

Is fluoroquinolones bactericidal or bacterostatic

A

Bactericidal

62
Q

Clinical uses for fluoroquinolones

A

Gram negative

63
Q

Why are fluoroquinolones back up drugs

A

Too many people Rxed I pro for UTIs even though TMX-SFX was DOC
-now there is resistance

64
Q

Generations of fluoroquinolones

A
  1. Not important
  2. Ciprofloxacin
  3. Levofloxacin
  4. Gemifloxacin
65
Q

Of the different generations of fluoroquinolones, which ones are more frame negative and which ones are more gram positive

A

Gram negative for 1st generation

More gram positive as you go towards 4th generation

66
Q

Spectrum of fluoroquinolones

A
  • UTIs
  • gram negative infections
  • CAP (community acquired pneumonia), alt to macs
67
Q

Which fluoroquinolones are used doe community acquired pneumonia

A

3rd and 4th generations

  • levofloxacin
  • gemifloxacin
68
Q

Resistance of fluoroquinolones

A

Mutation of the bacterial DNA gyrase

69
Q

Adverse effects of fluoroquinolones

A
  • black box warning: tendinitis and tendon rupture
  • not for kids or pregos because effects on collagen metabolism and cartilage development
  • phototoxicity
70
Q

Drug interactions of fluoroquinolones

A

Avoid antacid

-chelates metals

71
Q

What drug is a urinary tract antiseptic

A

Nitrofurantoin

72
Q

MOA of nitrofurantoin

A

IDK

73
Q

Spectrum of nitrofurantoin

A

Used for uncomplicated UTIs

-alt to TMP-SMX

74
Q

DOC for neisseria gonrrhea

A

Ceftriaxone

75
Q

Drug of choice for treponema (syphillus)

A

Beneath one Pen G

76
Q

Chlamydia trachomatis

A

Azithromycin (or doxy)

Pharm Block 12 (7 decks)

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