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Pharm Final > ABs- inhibitors of Protein synthesis > Flashcards

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Use penicillin + streptomycin to treat endocarditis (outdated)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
Q

what is a concern with the distribution of Tetracyclines

A

Tetracylines are sequestered in the bone with some penetration into CNS

26
Q

Tetracyclines are what concern for the mouth

A

Tetracyclines causes yellowing browning of the teeth, don’t admin in the pregnant or young!

27
Q

are tetracyclines photosensitive?

whats a special toxicity of tetracyclines?

A

YES tetracyclines are photosensitive!

tetracyclines= fanconi syndrome: renal tubular dysfunction after admin outdated tetracyclines

28
Q

What is a newer Tetracycline agent that is static and binds to 30s part of ribosome

A

Tigecycline: monocycline and Glycylcycline

29
Q

Tigecycline spectrum? and what is the difference between tigecycline and tetracyclines?

A

Tigecycline is BROAD spectrum effective against gram - and gram + including anaerobes. Tigecycline is not effected by the same resistance mechanisms as tetracycline

30
Q

Tigecycline is used against what bacteria

A

Tigecycline used against bacteria resistant to B lactams, vancomycin, and tetracyclines

31
Q

what is a limiting toxicity of Tigecycline

A

Tigecycline causes nausea

32
Q

what is the clinical use of Tigecycline

A

Tigecycline is used for complicated intra abdominal and skin and skin structure infections

33
Q

What is a nitrobenzene analog that has very limited clinical use

A

Chloramphenicol

34
Q

Chloramphenicol is very limited clinically why?

A

Chloramphenicol causes a fatal side effect: aplastic anemia

35
Q

What is chloramphenicol’s spectrum

A

Chloramphenicol is BROAD spectrum effective against Gram - and Gram +

36
Q

What is Chloramphenicol used for when tetracyclines are ineffective

A

Chloramphenicol is used to treat rikettsial infections when tetracyclines are ineffective

37
Q

What is the resistance of chloramphenicol

A

Chloramphenicol resistance develops due to acetylation of the drug, dec uptake, change in ribosome structure

38
Q

what is the fatal toxicity of chloramphenicol

A

Aplastic anemia!

39
Q

What is the other serious toxicity of chloramphenicol

A

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
Q

what are the 3 macrolides

A

erytrhomycin, azithromycin, clarithromycin

41
Q

Spectrum of macrolides?

macrolides are effective against what?

A

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
Q

What are the resistance to Macrolides

A

Macrolide resistance from methylation of 50s ribosome, enhanced efflux pump, chromosome mutations of 50s, macrolide hydrolysis by esterases

43
Q

What is used the least out of the 3 macrolides

A

Erythromycin is the least used bc has the shortest half life, narrowest spectrum and least desirable effects

44
Q

What is a semisynthetic Erythromycin analog that binds to the 50s ribosomal subunit

A

Ketolide - Telithromycin

45
Q

Ketolide- Telithromycin spectrum: What infection specifically?

A

Broad spectrum. TX of RTI, community acquired pneumonia

and effective against Macrolide resistant strains

46
Q

What is the toxicity warning of Telithromycin

A

Liver Toxicity= Ketolide

47
Q

Clindamycin spectrum

A

Clindamycin effective against Gram + bacteria and anaerobes: S pyogenes

48
Q

What two drugs are for anaerobic infections

A

Clindamycin and Metronidazole

49
Q

What is Clindamycin used to treat specifically?

A

Clindamycin used to treat Penicillin resistant infections and gram + anaerobes

50
Q

what is the specific toxicity that comes with Clindamycin use, making it a rarely used AB

A

Clindamycin causes pseudomembraneous colitis by toxin form from C difficile. C difficile is resistant to Clindamycin

51
Q

If a pseudomembraneous colitis develops from use of Clindamycin then what do you treat this C difficile infection with?

A

Metronidazole

52
Q

The combo of what two drugs is effective against mainly gram + organisms and is bactericidal

A

Quinopristin/ dalfopristin

53
Q

Quinopristin/ dalfopristin is used specifically to treat what infections

A

VRE and MRSA type infections

54
Q

What AB is Broad spectrum against gram + (staph, strep, enterococcus) and has poor activity against gram - and anaerobes

A

Linezolid

55
Q

What is Linezolid specifically used to treat?

A

VRE and MRSA infections

56
Q

What inhibits isoleucyl tRNA synthetase and is bacteriocidal

A

Mupirocin

57
Q

What is Mupirocin effective against

A

Gram + and some gram -. Skin infections including MRSA

Pharm Final (13 decks)

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