Antibiotics Flashcards

1
Q

What are some 30S inhibitors?

A

Aminoglycosides

Tetracycline

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2
Q

Are

linezolid

macrolides

chloramphenicol

clindamycin

quinupristin/dalfopristin

30S or 50S inhibitors?

A

50S inhibitors

*NOTE* linezolid, tetracycline and chloramphenicol interfere with mitochondrial ribosomes - do have effect on us, ie, bone marrow suppression.

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3
Q

What part of translation do linezolid and aminoglycosides inhibit?

A

Initiation

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4
Q

What part of translation do aminoglycoside, tetracycline, macrolide, chloramphenicol, clyndamycin, quinupristin/dalfoprisitin inhibit?

A

Elongation

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5
Q

Where else does aminoglycoside inhibit translation?

A

termination

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6
Q

Are most ribosome inhibitors bacteriostatic or bacteriocidal?

how about things that affect the cell wall?

A

bacteriostatic.

those would be bactericidal

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7
Q

What do linezolid, tetracycline, and chloramphenicol interfere with?

A

mitochondrial ribosomes (bone marrow suppression)

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8
Q

What are the steps of prokaryote translation initiation?

A

1) Initiation factors associate with the 30S ribosomal subunit.
2) Formylmethionine initiator tRNA and mRNA bind to 30S subunit.
3) 50S ribosome then binds and you have the complete initiation complex.

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9
Q

Where does Linezolid bind?

A

P-site on the 50S subunit

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10
Q

where do aminoglycosides bind and what do they do?

A

bind to 30S ribosome and freeze initiation complex

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11
Q

Elongation:

Aminoacyl tRNA is inserted in the acceptor site. ____________ interfere here and prevent aminoacyl tRNA attachment to the acceptor site.

A

TETRACYCLINES

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12
Q

Elongation:

  1. The peptide bond is formed. ____________ inhibits peptide bond formation.
A

Chloramphenicol

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13
Q

Elongation:

  1. fmet tRNA is released from the P site. In prokaryotes, an exit site called the E site binds tRNA after it’s displaced from the P site
  2. Translocation. A dipeptide tRNA moves from the A to the P site and the ribosome moves one codon along the mRNA. _______________________________ inhibit translocation.
  3. Another amino acyl tRNA is put in the A site and elongation continues.
A

Macrolides, Streptotagmins, Clindamycin

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14
Q

what antibiotics should you not use with newborns?

A

Chloramphenicol (can’t glucuronidate)

Erythromycin (piloric stenosis)

Sulfonimides

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15
Q

What antibiotics can you not use in children?

A

Tetracyclines

Fluoroquinolones

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16
Q

What antibiotics should you not use during pregnancy?

A

Tetracycline

Aminoglocosides,

Clarithromycin

Fluoroquinolones

Chloramphenicol

Sulfonimides

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17
Q

What do you need to do with antibiotics for the elderly?

A

Adjust for reduced renal funtion:

the half life of

beta-lactams

aminoglycosdes

and fluoroquinolones

will be increased

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18
Q

Where do Aminoglycosides

Streptomycin

Neomycin

Amikacin

Gentamicin

Tobramycin

do in Protein Synthesis?

Are they bactericidal, bacteriostatic?

A

BacterioSTATIC…act on 30S ribosome

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19
Q

What do the Tetracyclines -

Doxycycline,

Minocycline

Demeclocycline

Tetracycline

do in protein synthesis?

Are these bacteriostatic or bactericidal?

A

inhibit - act on 30S Ribosome

BacterioSTATIC

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20
Q

Where do Macrolides -

erythromycin

azithromycin

clarithromycin

cindamycin

chloramphenicol act in Protein Synthesis?

Are they bacteriostatic or bactericidal?

A

act on 50S ribosome…

Bacteriostatic

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21
Q

Resistance mechanism that prevents drug from reaching its target in

Beta-lactams
Rifampin
Fluoroquinolones
Sulfonamides
Trimethoprim

Linezolid
Aminoglycosides
Erythromycin, clindamycin, quinupristin/dalfopristin
Tetracyclines

are due to:

A

alteration of target

Beta-lactams – altered penicillin binding proteins (MRSA)
Vancomycin- altered target
Rifampin - DNA dependent RNA polymerase
Fluoroquinolones - DNA topoisomerase II or IV
Sulfonamides - Dihydropteroate synthetase
Trimethoprim - Dihydrofolate reductase

Linezolid – altered ribosome
Aminoglycosides – altered ribosome (uncommon)
Erythromycin, clindamycin, quinupristin/dalfopristin – methyltransferase modified ribosome
Tetracyclines – production of proteins that interfere with ribosomal binding

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22
Q

Resistance mechanism that prevents drug from reaching its target in

Sulfonamindes

is due to:

A

Upregulation of target or its substrate

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23
Q

Resistance mechanism that prevents drug from reaching its target in

penicillins

Cephalosporins

Aminoglycosides

Chloramphenicol

Tetracyclines

Macrolides

Clindamycin

quinupristin/dalfoprintin, metronidazole

is due to:

A

Enzymatic alteration of the antibiotics

this can sometimes occur in Bacitracin and Polymyxins as well

24
Q

Which drugs are reserved for difficult to treat drug resistant bacteria?

(Like MRSA or VRE - vancomycin resistant enterococcus)

A

5th gen cephalosporin- ceftaroline,

vancomycin,

TMP-SMX,

daptomycin,

Quinupristin-Dalfopristin,

Linezolid

25
Q

Dihydropteroate synthetase targeted

A

Sulfonamides

26
Q

Production of proteins that interfere with ribosomal bindng

A

tetracyclines

27
Q

Resistance mech that prevent drug from reaching its target in

Tetracyclines
Sulfonamides
Aminoglycosides
Chloramphenicol

is due to:

A

primarily decreased uptake

28
Q

Resistance mechanism that prevents drug from reaching its target in

Cephalosporins
Aztreonam
Tetracyclines (most impt), minocycline the exception
Macrolides
Quinupristin/dalfopristin
Fluoroquinolones
Sulfonamides

is:

A

increased efflux

29
Q

What are some differences between RNA and DNA translation?

A

RNA starts with formyl-methionine and the Shine Delgarno Sequence

DNA starts with just methionine…invovles a 5’Cap

30
Q

What is notable about quinupristin/dalfopristin?

A

They’re 2 seperate drugs, but always used in combination

31
Q

What antibiotic inhibits at all 3 steps of mRNA -> protein translation?

A

aminoglycosides (which is why they’re bacteriocidal - most ribosome inhibs. are bacteriostatic: they just interfere with one step)

32
Q

What are concentration-dependent drugs?

A

Concentrations > 10 times above the MIC most effective at killing the organism

33
Q

What are time-dependent drugs?

A

effect depends on time above the MIC

34
Q

are aminoglycosides time or concentration dependent?

A

Concentration - they’re administered as a single large dose

35
Q

Are B-lactams time or concentration-dependent?

A

Time - must have multiple doses

36
Q

What drugs should be used on Mycoplasma pneumonia?

A

atypical pneumonia - use

Doxycycline

Azithromycin

Levofloxacin

(B-lactams not effective)

37
Q

What should you use for Lymes?

A

amoxycillin or doxycycline….use Johns Hopkins guide

38
Q

Enterococcuw drug resistance examples

(Gram + organism)

A
39
Q

What agents may cause hemolysis in patients with glucose-6-phosphate dehydrogenase deficiency?

A

sulfonamides (trimethoprim/sulfamethoxazole)

40
Q

which antibiotic may cause seizures?

A

beta-lactam (esp. carbapenems)

41
Q

what antibiotic may cause hepatotoxicity?

A

rifampin

42
Q

what antibiotic may cause nephrotoxicity?

A

sulfonamides

aminoglycosides

vancomycin

43
Q

what antibiotic may cause Ototoxicity?

A

aminoglycosides

vancomycin

44
Q

what antibiotic may cause QT interval prolongation?

A

macrolides, fluoroquinolones

45
Q

what antibiotic may cause anemia?

A

chloramphenicol

trimethoprim

46
Q

what antibiotic may cause arthralgia?

A

quinupristin/dalfoprisin

fluoroquinolones

47
Q

what antibiotic may cause disulfiram-reaction when taken with alcohol?

A

metronidazole

2nd gen. cephalosporin w/methylthiotetrazole groups

48
Q

what antibiotic may cause superinfections?

A

clindamycin

fluoroquinolones

3rd gen. cephalosporin

ampicillin

49
Q

Which drugs are patients commonly hypersensitive to?

A

sulfonamides (shouldn’t take other sulfa drugs like diuretics)

B-Lactam (can use skin test to see, and then work on desensitization)

clindamycin

50
Q

what are common drug-drug interactions?

A

rifampin induces drug metabolizing enzymes (uses up other drugs faster)

clarithroycin and erythromycin inhib. hepatic metabolism

51
Q

Why treat with Trimethoprim-Sulfamethoxazole?

A

Inhibits multiple steps in folate synthesis

52
Q

Why treat with Aminoglycoside+Penicillin?

A

Penicillin increases permeability of cell membranes increasing the ability of aminoglycosides to enter the cell

53
Q

Why are

Ampicillin-sulbactam,

Amoxicillin-clavulanate,

Piperacillin-tazobactam,

Ticarcillin-clavulanate

Imipenem-cilastatin

used in sets like that?

A

Addition of inhibitors to prevent degradation of the enzyme

(for example, that last set blocks renal dehydropeptidase)

54
Q

What happens if you use Vancomycin and Aminoglycosides together?

A

each alone have some nephrotoxicity. If given together you get marked renal impairment.

55
Q

Should you use penicillin or penicillin + tetracycline in treating pneumoccal meningitis?

A

Penicillin - 21% mortality
Penicillin + Tetracycline - 79% mortality

(antagonism occurs)