Ribosomal Agents Flashcards

1
Q

30s ribosome

A

spectinomycin, aminoglycan, tetracyclines

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2
Q

50s ribosome

A

Chloramphenicol, macrolides, lincosamides, strettogramins, linezolid

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3
Q

Spectinomycin MOA

A
  • Inhibit initiation complex
  • bacteriostatic
  • bind to 30s subunit
  • Parenteral
  • Only indication = Gonorrhea
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4
Q

Aminoglycosides Examples

A

Streptomycin, gentamicin, tobramycin, Neomycin, Amikacin, Netilmicin

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5
Q

Aminoglycosides MOA & MOR

A
  • Bind to 30s subunit
  • Prevents initiation AND causes misreading of codon
  • bactericidal
  • O2 dependent –> needs high pH and aerobic conditions»better activity at high pH
  • Resistance = group transferases (acetyl-,adenyl-, phospho-)
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6
Q

If there is resistance to gentamicin, what agent would you use?

A

Amikacin

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7
Q

Aminoglycosides adverse effects

A

-OTOTOXICITY
-NEPRHOTOXICITY (must monitor renal function)
(same toxicity as vancomycin)
- Neuromuscular blockade
- Skin reactions

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8
Q

Aminoglycosides indications

A

AEROBIC gram -

usually combine with beta-lactam

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9
Q

Tetracycline examples

A

Tetraycline, Doxycycline, MInocycline, Tigecycline, Demeclocycline

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10
Q

Tetracyclines MOA & MOR

A
  • Bind to 30s subunit
  • Inhibit binding of aminoacyl-tRNA
  • Resistance: efflux protein pump
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11
Q

Tetracyclines indications

A
  • Broad spectrum antibiotics ( gram - & gram +)
  • Respiratory ifx (atypical): Mycoplasma, Legionella, Chlamydophila
  • Bronchitis: H. flu, pneumococcus
  • *Rickettsiae,
  • *STDs!! (chlamydia, PID, ureaplasma, chancroid)
  • *Lyme disease
  • *Acne
  • Drug resistent falciparum malaria (doxy)
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12
Q

Chloramphenicol MOA & MOR

A
  • 50s subunit
  • inhibit peptidyl transferase
  • Resistance: acetyltransferase
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13
Q

Chloramphenicol adverse effects

A
  • gray baby syndrome
  • Bone marrow suppression (dose-dep)
  • Aplastic anemia
  • Decreased iron incorporation into Hgb
  • Rare hypersensitivity
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14
Q

Chloramphenicol Indications

A
  • Broad spectrum (but not for staph or pseudomonas)
  • typhoid fever (if other unable to use other tx)
  • MENINGITIS & Brain Abscess (only if other agents can’t be used)
  • Bac conjunctivitis (topical)
  • Oral meningitis tx when IV can’t be used
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15
Q

Macrolides Examples

A

Erythromycin, claritrhomycin, azithromycin, Telithromycin

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16
Q

Macrolides MOA & MOR

A
  • Binds to 50s
  • prevents translocation
  • Resistance: Methylation (use Telitrhomycin in such cases)
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17
Q

Macrolide adverse effect

A
  • GI problems

Macrolides are oral agents

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18
Q

Macrolide indications

A
  • broad spectrum

- respiratory ifx

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19
Q

Lincosamides examples

A

lincomycin, clindamycin

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20
Q

Lincosamides MOA & MOR

A
  • Bind to 50s subunit
  • prevent translocation
  • Resistance methylation
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21
Q

Lincosamides Indications

A
  • anaerobic ifx

- aerobic gram +

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22
Q

Streptogramins MOA & MOR

A

-Binds to 50s
-Prevents translocation
-Bactericidal
Resistance = methylation
-Example = synercid

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23
Q

Streptogramins indications

A

PRSP, MRSA, VRSA, VRE tx

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24
Q

Linezolid MOA & MOR

A
  • bactericidal
  • Unique site binding to 50s (23s)
  • Inhibits initiation AND translocation
  • No cross resistance ( resistance only with mutation of 23s binding site)
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25
Q

Linezolid Indications

A

PRSP, MRSA,VRA, VRE tx
Enterococci tx
not active against G- or anaerobes

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26
Q

only topical or oral aminoglycoside antibiotic

A

Neomycin–b/c of high nephrotoxicity

all others parenteral

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27
Q

second line drug for tx of drug resistant TB

A

Streptomycin

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28
Q

Tetracylines adverse effects

A

absorption inhibited by milk, antacid, Ca+, Iron (metals)

  • CONTRAINDICATED: renal failure and pregnant women & children
  • teeth discoloration and concentration in bones
  • GI effects
  • Hepatotoxicity
  • Doxy –> esophageal ulcerations, photosensitivity
  • Tetra, Mino–> pre-renal azotemia
  • Mino –> Vertigo
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29
Q

Erythromycin Indications

A

Treatment for:

  • *Legionnaire’s disease
  • *Mycoplasma pneumonia
  • *Chlamydia ifx
  • *Corynebacterium diphtheria
  • *Bordatella pertussis
  • *Campylobacter Enteritis
  • Use w/ neomycin for surgical bowel prep
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30
Q

This drug exacerbates Myasthenia gravis

A

Telithromycin

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31
Q

This drug is associated with pseudomembranous colitis

A

Clindamycin

32
Q

Mupirocin MOA

A

formely called pseudomonic acid

  • topical ointment
  • Interfers w/ bac RNA & protein synthesis
33
Q

Rifampin

A

Cheif use for tx of TB

  • Also for staph ifx involving bone and prosthetic devices
  • ALWAYS combined with another antimicrobial
  • Reddish discoloration of urine
34
Q

Rifaximin Indications

A
  • prevention and therapy of traveler’s diarrhea due to non-invasive E. coli
  • Px/tx of hepatic encephalopathy (dec ammonia production by gut bac)
  • Tx of refractory C. diff colitis
35
Q

This class has minimal protein binding and cleared unchanged into urine by glom. filtration

A

Aminoglycosides

36
Q

Aminoglycoside distribution

A
  • Low in CNS, Sputum, Bile, and Prostate

- Excellent in urine

37
Q

this drug can be taken orally to decrease gut flora before GI surgery or in liver failure

A

Neomycin

38
Q

Initial DOC for serious aerobig gram neg rod infections

A

Gentamicin, tobramycin, amkacin
(can be swapped with drugs w/ less toxicity later when org ID/sensitivity is known)
-Good to give w/ beta lactams for synergy, spectrum (hit gram +), and resistance issues

39
Q

Aminoglycoside with highest nephrotoxicity

A

Neomycin

40
Q

Aminoglycoside with highest vestibular toxicity

A

Streptomycin

FYI: Balance probs–provide enough light to compensate visually

41
Q

Aminoglycoside with highest Cochlear toxicity

A

Neomycin

42
Q

Factors that increase risk of aminoglycoside nephrotoxicity

A
  • Severe infection
  • Decreased renal blood flow (e.g. in spetic shock, dec cardiac output)
  • Dehydration, diuretic use
  • Underlying renal dz
43
Q

Average half-life for aminoglycosides

A

2-3 hrs

50-110 hours in anephric!

44
Q

Spectinomycin half-life

A

1-2 hours

45
Q

Short-acting Tetracycline

A

Tetracycline O, IV

T1/2=8hrs

46
Q

Long-Acting Tetracyclines

A

Doxycycline O, IV (T1/2=18 hrs)

Minocycline O, IV (T1/2=16 hrs)

47
Q

This class of drugs is metabolized by liver, concentrated in bile, but excreted by kidneys

A

Tetracyclines

except Doxy: excreted mainly in poop

48
Q

First class of glycyclines-derivatives of minocyclines

A

Tigecycline

49
Q

This drug is IV only, has half-life of 36 hours, and primarily cleared by liver

A

Tigecycline

50
Q

Tigecycline MOA

A
  • Binds to 30S
  • Inhibits protein synthesis
  • STATIC
51
Q

Tigecycline Spectrum

A

Very broad spectrum

  • All Gram + (even MRSA & VRE)
  • Most Gram -, bu NOT pseudomonas and proteus
  • Most anaerobes
  • Atypical orgs: mycoplasma, mycobacteria, but NOT Legionella
52
Q

Tigecycline Indications

A
  • Complicated skin and soft tissue infections

- Complicated intra-abdominal infections

53
Q

Tigecycline Toxicity

A
  • N & V

- Contraindicated in preg & young kids (like tetracyclines)

54
Q

T1/2 Erthromycin

A

1.4 hrs

55
Q

Erythromycin oral preparations

A
  • E. Base
  • E. Ethylsuccinate (EES)
  • E Estolate
  • E. Stearate
56
Q

Erythromycin pharmacokinetics

A
  • Wide distribution EXCEPT in CNS & Eye
  • Much is metabolized in liver
  • Some excreted in bile
  • 10% excreted in urine
57
Q

Erythromycin Spectrum

A
  • Similar to pen G (good substitute in allergic pts)
  • AVOID in serious infections
  • Good for Strep, Staph (non-MRSA), pen-sensitive anaerobes
  • NOT good for GC or Syph
58
Q

Erthromycin toxicity

A
  • GI upset
  • Cholestatic hepatitis (mimics gallbladder attack)
  • Phlebitis
  • Cardiac rhythm disturbances
  • Drug interactions (drugs met by liver)
  • Hypersensitivity uncommon
59
Q

Clarithromycin indications

A
  • Similar to erythro and azithro but mainly for RESPIRATORY infections (concentrates in resp tissues)
  • atypical mycobac infection (esp m. avium)
60
Q

Clarithomycin Toxicity

A
  • Same as erythromycin except…
  • Less GI
  • Bad taste in mouth
  • Contraindicated in preg
  • Possibly cardiac rhythm
  • Drug interactions
61
Q

This macrolide has a half-life of three days when taken orally

A

Azithromycin

Now also available in IV

62
Q

Azithromycin Indications

A
  • H. Flu & Moraxella catarrhalis (ear infections)
  • Chlamydia (single dose tx)
  • Mainly resp infections
  • Atypical mycobac infections (m. avium)
63
Q

Azithromycin Toxicity

A
  • Mild GI
  • Possible cardiac rhythm
  • Tinnitus/deafness (high doses)
  • Drug interactions
64
Q

Telithromycin Indications

A
  • Mild-moderate COMMUNITY-onset pneumonia (not bronchitis, otitis, or sinusitis) b/c of severe toxicity
  • S. pneumo (resistant strains too)
  • E. Faecalis
  • S. aureus
65
Q

Telithromycin Toxicity

A
  • Mainly GI (taken orally)
  • Drug interactions: CYP 450 3A4
  • Rare Fatal hepatotoxicity (met by liver)
  • MG exacerbation
  • Contraindicated in pts w/ MG or liver dz
66
Q

Clindamycin pharmacokinetics

A

-T1/2= 2.5 hrs
-Oral, IM, IV, Topical
-Cleared mainly by liver and intestine
-Wide distribution, but no CNS, eye, and ? prostate
» Gets into BONE and works in abscesses!!

67
Q

Clindamycin indications

A
  • MRSA skin/soft tissue infections
  • DOC for Anaerobic infections
  • staphylococcal osteomyelitis
  • Acne (topical)
  • Pen alternative for staph, strep, anaerobes
  • NOT FOR AEROBIC GRAM (-)
68
Q

Clindamycin Toxicity

A
  • Hypersenstivity
  • Mild hepatotoxicity
  • GI upset
  • Pseudomembrane colitis
69
Q

Mupirocin Indications

A
  • Topical tx of superficial skin infections due to staph and strep (Impetigo)
  • Nasal application for S. aureus carriage (esp MRSA)
70
Q

Mupirocin Toxicity

A

Local irritation

71
Q

This drug has a half-life of 5 hrs and does not need to be adjusted in renal failure

A

Linezolid
(largely met in liver, excreted in urine)
Oral and IV administrations

72
Q

Linezolid Toxicity

A
  • SEROTONIN Syndrome when taken w/ antidepressants
  • Inc BP when taken w/ adrenergic agents or high tyramine
  • mild GI
  • occasional thrombocytopenia & neutropenia
  • Also, super expensive :(
73
Q

Rifaximin MOA

A
  • Drug related to rifampin

- Blocks RNA synth: Binds to beta sub-unit of RNA polymerase

74
Q

Rifaximin Toxicity

A
  • Minimal/sim to placebo

- Preg Category C (teratogenic in rats)

75
Q

Chloramphenicol Pharmacokinetics

A
  • Oral or IV
  • T1/2= 2-3 hr (doubles in renal failure)
  • Inactivated in liver and excreted in urine
  • Great distribution, even in CNS!!