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Antibiotics > Protein Synthesis Inhibitors > Flashcards

Protein Synthesis Inhibitors Flashcards

1
Q

Protein synthesis inhibitors 7

A 
Aminoglycosides
Macrolides
Tetracyclines
Chloramphenicol
Clindamycin
Linezolid
Streptogramins
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2
Q

Aminoglycosides 5

A 
Gentamicin
Neomycin
Amikacin 
Tobramycin
Streptomycin
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3
Q

Aminoglycosides MOA

A

Bind bacterial ribosome at 30S

Misreading of genetic code-> some of misread proteins go to cell membrane, make it more permeable to salt and water—> cell death

Aminoglycosides are bacteriocidal

Require O2 for tx into cells- NOT FOR ANAEROBES

NOT TRANSFERRED INTO CELLS NOT EFFECTIVE FOR INTRACELLULAR ORGS (rickettsia, chlamydia)

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4
Q

Aminoglycosides use

A

Streptomycin used in combo for M. Tb

Neomycin preop for bowel surgery- poorly absorbed, give with erythromycin

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5
Q

Aminoglycosides + beta lactam synergy

A

Combo more effective than sum of either alone

Vancomycin/gentamicin for endocarditis

Ampicillin/gentamicin for newborn meningitis

Pip/tazo + tobramycin for CF pts with pseudomonas

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6
Q

Aminoglycoside resistance

A

Aminoglycoside modifying enzymes - bacteria acquire enzymes that modify drug structure, modified structure binds poorly to ribosomes

Aminoglycoside kinases- phosphorylation
Transferases- adenylation/acetylation

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7
Q

Aminoglycosides AES

A

Ototoxicity
Nephrotoxicity- ATN
Neuromuscular blockade- can block/limit ACh release at NMJ
CANNOT USE IN PREGNANCY

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8
Q

Macrolides

A

Azithromycin
Clarithromycin
Erythromycin

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9
Q

Macrolides MOA

A

Bind 50s ribosome and block translocation

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10
Q

Macrolides uses

A

GP, especially strept
Some GN

Concentrated in macrophages and cells
EFFECTIVE AGAINST INTRACELLULAR PATHOGENS 
- Chlamydia (obligate)
- Legionella (facultative)
— both are good for atypical PNA

Community acquired PNA
Safe in pregnancy

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11
Q

Gonorrhea tx

A

Macrolide + ceftriaxone

Chlamydia and gonorrhea often coninfect

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12
Q

Macrolides in GI infection

A

Erythromycin- binds motillin receptors, stimulates smooth muscle contraction, can be used in GI motility dx

Clarithromycin- part of triple tx for H pylori

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13
Q

Macrolide resistance

A

Methylate abx binding site on 50s ribosome

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14
Q

Macrolide AEs 5

A

N/V/D

QT prolongation

Acute cholestatic hepatitis
- contraindicated for pts w liver dysfunction

Maculopapular rash

P450 ENZYME INHIBITORS
- raise warfarin and theophylline levels

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15
Q

Tetracyclines

A

Tetracycline
Doxycycline
Demeclocyline
Minocycline

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16
Q

Tetracycline MOA

A

Bind 30s ribosome

17
Q

Demeclocycline use

A

Not used as abx
ADH antagonist- treat SIADH
Causes nephrogenic DI to reverse SIADH

18
Q

Doxycycline use

A

MC used in tetracycline family

Accumulates intracellularly

Covers zoonotic and atypical bacteria (chlamydia)

Treats acne vulgaris (minocycline)

19
Q

Tetracycline absorption impaired by

A

Minerals and antacids
Calcium, magnesium, iron, dairy

Chelate the drug

Cannot be taken with antacids or milk

20
Q

Tetracycline resistance

A

Decrease influx or increase efflux

Plasmid encoded transport pumps

21
Q

Tetracycline AEs

A 
GI distress
Photosensitivity 
DO NOT GIVE TETRACYLCINES TO KIDS:
Discoloration of teeth
Inhibit bone growth in peds
CONTRAINDICATED IN PREGNANCY
22
Q

Chloramphenicol MOA

A

Inhibits peptidyl transferase at 50s ribosome

23
Q

Chloramphenicol use

A

Rickettsia and ehrlichia in pregnancy- only 1 and 2 trimester

Meningitis in developing world
- less effective but cheap

24
Q

Chloramphenicol AEs

A

Aplastic anemia- irreversible, fatal

Gray baby syndrome- infants lack liver enzyme to metabolize drug-> skin turns GREY, hypotension, fatal

25
Q

Clindamycin MOA and resistance

A

Same as macrolides:
Binds 50s ribosome

Methylation of abx binding site

26
Q

Clindamycin use

A

Anaerobes above diaphragm:
Aspiration PNA
Lung abscesses
Oral infections

B fragilis highly resistant to clindamycin, use metronidazole

27
Q

Clindamycin AEs

A

C diff—> pseudomembranous colitis

Antibiotic assoc diarrhea- milder than c diff, osmotic diarrhea

28
Q

Linezolid MOA and use

A

Binds 50s ribosome

Vancomycin resistant enterococcus (VRE)

29
Q

Linezolid AE

A

Serotonin syndrome- linezolid is monoamine oxidase inhibitor

High risk if given with SSRI

Serotonin syndrome- fever, confusion, agitation, hyperreflexia

30
Q

Streptogramins

A

Quinupristin/dalfopristin

31
Q

Streptogramins MOA and use

A

Block 50s ribosome

Used for vancomycin resistant bacteria- VRSA, VRE

32
Q

What protein synthesis inhibitor abx are bacteriocidal?

A

Aminoglycosides
- misread proteins travel to membrane and increase permeability

All others are bacteriostatic

Antibiotics (8 decks)

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