ABs- inhibitors of Protein synthesis Flashcards

1
Q

what are the 7 ABs that act by protein synthesis inhibition?

A

Aminoglycosides, Tetracyclines, Chloramphenicol, Clindamycin, Erythromycin (macrolides), Quinupristin/ dalfopristin, and Linezolid

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2
Q

what is the only AB that binds to the 30s part of the ribosome

A

Tetrecyclines, but some Aminoglycosides bind to 30s too!

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3
Q

Aminoglycoside MoA cidal or static

A

bind to 30s or 50s, inhibit tRNA attachment, and polysome breakdown
cidal

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4
Q

Tetracylcline MoA, static or CIdal

A

Tetracycline bind to 30s blocking tRNA binding to mRNA

static

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5
Q

Aminoglycoside spectrum?

A

Aminoglycosides are effective against GRAM NEG only! especially pseudomonas

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6
Q

How can Aminoglycosides be used to treat Gram pos?

A

Aminoglycoside + B lactam= effective against Gram +

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7
Q

the 6 aminoglycoside drugs

A

streptomycin, kanamycin, gentamicin, tobramycin, amikacin, neomycin

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8
Q

Clinical use of streptomycin

A

Streptomycin = drug resistant TB.

Use penicillin + streptomycin to treat endocarditis (outdated)

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9
Q

Kanamycin clinical use

A

Kanamycin NOT used in the US

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10
Q

Gentamicin, Tobramycin, and Amikacin uses?

A

Gram neg infections, septicemia, meningitis, endocarditis, pneumonia
possible use against gram + w B lactams

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11
Q

Neomycin uses?

A

Neomycin effective for topical tx of burns, wounds, infected dermatoses and oral use for prep for bowl surgery

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12
Q

Aminoglycoside absorption, distrib, metabolism/ excretion

A

Aminoglycosides are given IV and IM. Poor distribution, don’t enter CNS, renal excretion

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13
Q

Aminoglycoside Toxicity

A

Aminoglycosides are DOSE RELATED!!

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14
Q

Aminoglycoside toxicities

A

Aminoglycosides cause ototoxicity (cochlear hair death), Nephrotoxicity and Neuromuscular blockage

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15
Q

What is important for treat pts with myaesthenia Gravis

A

Aminoglycosides cause neuromuscular blockage- muscle weakness and respiratory depression

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16
Q

What are the 3 concentration dependent drugs

A

Aminoglycosides, quinolones, and daptomycin

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17
Q

what are the 3 Time dependent drugs

A

B lactams, Vancomycin, and quinolones (quinolones also Time dependent)

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18
Q

what do ahminoglycosides exhibit

A

aminoglycosides exhibit a post antibiotic effect- actions occur long after the drugs have cleared the blood

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19
Q

tetracylines bind to what part of the ribosome? are static or cidal?

A

tetracyclines bind to 30s part of ribosome and are STATIC

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20
Q

what is the specificity of tetracyclines

A

tetracyclines accumulate preferentially in bacteria through an energy dependent transporter lacking in mammalian cells

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21
Q

What are tetracyclines effective against

A

rickettsiae, mycoplasma, chlamydia and protozoa

GRAM - and GRAM + . 1st BROAD spectrum AB

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22
Q

tetracyclines are now considered a what due to resistance and toxicities

A

tetracyclines are 2nd line of defense for acne, outpatient mycoplasma, urethritis

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23
Q

resistance to tetracyclines are due to what

A

tetracyclines resistance are due dec influx, INC efflux, DEC binding to ribosomes

24
Q

what don’t you use Tetracyclines with

A

dont admin tetracyclines with MILK or antacids

25
what is a concern with the distribution of Tetracyclines
Tetracylines are sequestered in the bone with some penetration into CNS
26
Tetracyclines are what concern for the mouth
Tetracyclines causes yellowing browning of the teeth, don't admin in the pregnant or young!
27
are tetracyclines photosensitive? | whats a special toxicity of tetracyclines?
YES tetracyclines are photosensitive! | tetracyclines= fanconi syndrome: renal tubular dysfunction after admin outdated tetracyclines
28
What is a newer Tetracycline agent that is static and binds to 30s part of ribosome
Tigecycline: monocycline and Glycylcycline
29
Tigecycline spectrum? and what is the difference between tigecycline and tetracyclines?
Tigecycline is BROAD spectrum effective against gram - and gram + including anaerobes. Tigecycline is not effected by the same resistance mechanisms as tetracycline
30
Tigecycline is used against what bacteria
Tigecycline used against bacteria resistant to B lactams, vancomycin, and tetracyclines
31
what is a limiting toxicity of Tigecycline
Tigecycline causes nausea
32
what is the clinical use of Tigecycline
Tigecycline is used for complicated intra abdominal and skin and skin structure infections
33
What is a nitrobenzene analog that has very limited clinical use
Chloramphenicol
34
Chloramphenicol is very limited clinically why?
Chloramphenicol causes a fatal side effect: aplastic anemia
35
What is chloramphenicol's spectrum
Chloramphenicol is BROAD spectrum effective against Gram - and Gram +
36
What is Chloramphenicol used for when tetracyclines are ineffective
Chloramphenicol is used to treat rikettsial infections when tetracyclines are ineffective
37
What is the resistance of chloramphenicol
Chloramphenicol resistance develops due to acetylation of the drug, dec uptake, change in ribosome structure
38
what is the fatal toxicity of chloramphenicol
Aplastic anemia!
39
What is the other serious toxicity of chloramphenicol
Chloramphenicol is responsible for Gray Baby syndrome- bc neonates can't glucoronidate chloramphenicol which accumulates inhibition of mitochondrial protein synthesis- abdominal destination, cyanosis = high mortality
40
what are the 3 macrolides
erytrhomycin, azithromycin, clarithromycin
41
Spectrum of macrolides? | macrolides are effective against what?
Static some cidal against gram + Macrolides effective against Mycoplasma pneumonia, Legionnaires, Chlamydial infections, other respiratory infections, pneumoniae middle ear and sinus infections in children
42
What are the resistance to Macrolides
Macrolide resistance from methylation of 50s ribosome, enhanced efflux pump, chromosome mutations of 50s, macrolide hydrolysis by esterases
43
What is used the least out of the 3 macrolides
Erythromycin is the least used bc has the shortest half life, narrowest spectrum and least desirable effects
44
What is a semisynthetic Erythromycin analog that binds to the 50s ribosomal subunit
Ketolide - Telithromycin
45
Ketolide- Telithromycin spectrum: What infection specifically?
Broad spectrum. TX of RTI, community acquired pneumonia | and effective against Macrolide resistant strains
46
What is the toxicity warning of Telithromycin
Liver Toxicity= Ketolide
47
Clindamycin spectrum
Clindamycin effective against Gram + bacteria and anaerobes: S pyogenes
48
What two drugs are for anaerobic infections
Clindamycin and Metronidazole
49
What is Clindamycin used to treat specifically?
Clindamycin used to treat Penicillin resistant infections and gram + anaerobes
50
what is the specific toxicity that comes with Clindamycin use, making it a rarely used AB
Clindamycin causes pseudomembraneous colitis by toxin form from C difficile. C difficile is resistant to Clindamycin
51
If a pseudomembraneous colitis develops from use of Clindamycin then what do you treat this C difficile infection with?
Metronidazole
52
The combo of what two drugs is effective against mainly gram + organisms and is bactericidal
Quinopristin/ dalfopristin
53
Quinopristin/ dalfopristin is used specifically to treat what infections
VRE and MRSA type infections
54
What AB is Broad spectrum against gram + (staph, strep, enterococcus) and has poor activity against gram - and anaerobes
Linezolid
55
What is Linezolid specifically used to treat?
VRE and MRSA infections
56
What inhibits isoleucyl tRNA synthetase and is bacteriocidal
Mupirocin
57
What is Mupirocin effective against
Gram + and some gram -. Skin infections including MRSA