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Ok Pharmacology... Let's Do This... Be Gentle > Protein Synthesis Inhibitors > Flashcards

Protein Synthesis Inhibitors Flashcards

1
Q

what are the 4 protein synthesis inhibitors

A
  1. macrolides
  2. tetracyclines
  3. clindamycin
  4. aminoglycosides
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2
Q

macrolides selectively bind the __ ribosomal subunit

and block translocation of ___

A

50s

peptidyl tRNA

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3
Q

macrolides are __

but are not __

and enter by

A

bacteriostatic

actively transported

passive diffusion

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4
Q

macrolides are a weak __

that are more active at an __ pH

A

base

alkaline

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5
Q

resistance to macrolides is via

A

methylation of 23s rRNA of 50s ribosome

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6
Q

what gene prevents macrolide binding

A

ermB

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7
Q

rates of resistance to macrolides is increasing for what 2 bacteria

A

strep pneumo

h.flu

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8
Q

how is strep pneumo developing resistance to macrolides

A

via multi drug efflux transporter

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9
Q

what gene is associated with strep pneumo resistance to macrolides

A

mefA

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10
Q

all macrolides cover

A

(+) cocci → staph (including MRSA/MSSA), strep

(-) cocci → m. catarrhalis

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11
Q

which macrolide covers corynebacterium diptheriae

A

erythromycin

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12
Q

which macrolide covers chlamydia

A

azithromycin

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13
Q

all macrolides cover which atypical bacteria

A

mycoplasma pneumoniae

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14
Q

macrolides do not work well for what infxn

A

UTIs

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15
Q

which gram negative bacilli do all macrolides work against

A

bortadella pertussis

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16
Q

azithromycin is good for what 4 gram (-) bacilli

A

h.flu

bortadella pertussis

legionella

c. jejuni

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17
Q

clarithromycin is good for what 2 gram negative bacilli

A

h. flu
h. pylori

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18
Q

what abx is used for neisseria gonorrheae

A

ceftriaxone

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19
Q

what abx are used for chlamydia trachomatis and mycoplasma hominum

A

azithromycin/doxycycline

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20
Q

what abx is used for trichomonas

A

metrondiazole

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21
Q

azithromycin should be taken

A

on an empty stomach

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22
Q

clarithromycin can be taken

A

without any regard to meals

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23
Q

erythromycin absorption

A

varies depending on salt form

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24
Q

free base erythromycin is

A

destroyed by stomach acid

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25
Q

stearate erythromycin is

A

acid-resistant and well absorbed

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26
Q

__ erythromycin is better abosrbed

than __ erythromycin

A

stearate

free base

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27
Q

azithromycin and clarithromycin accumulate in __

in the (5)

A

skin

lungs

tonsils

cervix

sputum

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28
Q

macrolides have ___ distribution,

including to the __

A

wide

fetus

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29
Q

macrolides do not distribute as widely to the __

and __

A

brain

CSF

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30
Q

azithromycin is not metabolized and is excreted via the __

A

liver

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31
Q

azithromycin has high tissue penetration and binding with slow release and may be dosed __

A

daily

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32
Q

clarithromycin is __ and excreted

via the __

so __ dosing may be necessary

A

metabolized

kidneys

renal

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33
Q

erythromycin is metabolized in the __

and excreted in __

A

liver

bile

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34
Q

all the macrolides are excreted via the liver except for

A

clarithromycin

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35
Q

what are 2 adverse effects of macrolides

A
  1. GI disturbances
  2. prolonged QT interval
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36
Q

which macrolide directly stimulates gut motility

A

erythromycin

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37
Q

which 2 macrolides inhibit CYP450

A

clarithromycin

erythromycin

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38
Q

in what cardiac pt population should you use macrolides cautiously

A

ventricular arrhythmias

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39
Q

relative to erythromycin, clarithromycin has

A

greater duration of activity

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40
Q

tetracyclines bind __ and

prevent access of ___

A

30s ribosome

aminoacyl tRNA to mRNA site

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41
Q

how do tetracyclines inhibit bacteria

A

bacteriostatic

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42
Q

how are drugs resistant to tetracyclines

A

insertion of MDR transporters that move drug out of the cell

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43
Q

MDR plasmid is associated with

A

tetracyclines

sulfonamides

aminoglycosides

macrolides

44
Q

which tetracycline is not affected by ribosomal protection of proteins that block tetracycline

A

tigecycline

45
Q

most gram negative cocci and gram negative rods are

A

resistant to tetracyclines

46
Q

which tetracycline can be used against bacillus anthracis

A

doxycycline

47
Q

which tetracycline can be used against atypical organisms, including chlamydia and mycoplasma pneumoniae (CAP)

A

doxycycline

48
Q

which tetracyclines are used against p. acnes

A

minocycline

doxycycline

49
Q

which tetracyclines are used against chlamydia trachomatis and mycoplasma hominum

A

azithromycin

doxycycline

50
Q

which tetracyclines have 95-100% bioavailability

A

doxycycline

minocycline

51
Q

which macrolide has incomplete absorption and is best given on an empty stomach

A

tetracycline

52
Q

which tetracycline alters intestinal flora and contributes to superinfections

A

tetracycline

53
Q

tetracycline absorption is impaired by

A

cations → form salts that can’t be absorbed

dairy

54
Q

penetration of tetracyclines into most tissues-fluids is __,

including __

A

excellent

placental and fetal

55
Q

excretion of doxycycline and minocycline is concentrated in the __

and secreted into __

A

liver

bile

56
Q

tetracycline is excreted into __

and should be avoided in pt’s with __ dz

A

urine

renal

57
Q

which tetracyclines are long acting

A

doxycycline

minocycline

58
Q

which tetracycline is short acting

A

tetracycline

59
Q

what is the main 2 adverse rxn of tetracyclines

A

teeth and bone

60
Q

tetracyclines should be avoided in what 2 pt populations

A

later half of pregnancy

children < 8 yo

61
Q

tetracyclines are a pregnancy risk factor __

A

D

62
Q

GI disturbance is more common in which tetracycline

A

tetracycline → not as well absorbed as the other 2

63
Q

besides GI disturbance and teeth/bone, what are 2 other adverse rxns of tetracyclines

A
  1. candidal overgrowth → thrush and vaginitis
  2. photosensitivity
64
Q

what 2 drugs do tetracyclines react with

A

antacids

iron supplements

65
Q

phenytoin, barbituates, and carbamazepine can caused increased absorption of which tetracycline

A

doxycycline

66
Q

the regimen of choice for tx of urogenital gonorrhea is

A

IM ceftriaxone and oral azithromycin

67
Q

clindamycin binds to __

and prevents translocation of ___

to prevent

A

50s ribosome

peptidyl tRNA (ECN binding site)

peptide bond formation

68
Q

clindamycin is ___

but can be __ against certain organisms at higher concentrations

A

bacteriostatic

bactericidal

69
Q

clindamycin is ineffective against which anaerobe

A

c.diff

70
Q

clindamycin is a good alternative for streptococci and MSSA if a pt is

A

PCN allergic

71
Q

clindamycin has good coverage against __

for intraabdominal and brain abscesses

A

bacteroides fragilis

72
Q

__% of clindamycin is orally absorbed

and absorption is not __

A

90%

affected by food

73
Q

clindamycin penetrates __ especially well

but not __

A

bone

CSF

74
Q

clindamycin is metabolized by the __

and has __ excretion

A

liver

biliary

75
Q

is renal dosing required for clindamycin

A

no

76
Q

is clindamycin excreted in breast milk

A

yes

77
Q

what common adverse rxn’s are associated w. clindamycin (3)

A
  1. nausea
  2. diarrhea
  3. skin rashes
78
Q

what serious side effect is associated w. clindamycin

A

pseudomembranous colitis → toxigenic c. diff

79
Q

amiinoglycosides bind ___

to __ and alter interaction of mRNA with subunit

A

irreversibly

30s

80
Q

name 3 MOA for aminoglycosides

A
  1. produce inhibition of protein synthesis
  2. break up polysomes
  3. misread the code → produce lethal proteins
81
Q

how do aminoglycosides kill bacteria

A

bactericidal

82
Q

aminoglycosides require __

and are not effective against __

A

O2

anaerobes

83
Q

what is the method of resistance against aminoglycosides

A

chemical modifications of aminoglycosides that impair ribosomal binding and drug reuptake

84
Q

__ mediated transfer of AG modifying enzymes

is of major importance to __

A

plasmid

gram (-) pathogens

85
Q

gentamicin, tobramycin, and amikacin have good activity against what 2 gram negative rods

A

pseudomonas

e. coli

86
Q

if combined with a __

aminoglycosides have good activity against __

A

cell wall synthesis inhibitor

enterococci

87
Q

gentamicin plus __

work well against __

A

cell wall inhibitor (PCN or vanco)

enterococci

88
Q

aminoglycosides are high __

and are not well absorbed via __

A

polar

oral administration

89
Q

aminoglycosides have rapid and complete absorption via __ administration,

and have peak plasma concentrations in __

A

IM

30-90 minutes

90
Q

aminoglycoside distribution in the body is limited to

A

extracellular fluid

91
Q

aminoglycoside distribution is excluded from the __

A

CNS

92
Q

aminoglycosides selectively accumulate in the __

and the __,

predisposing these areas to __

A

renal cortex

inner ear

toxicity

93
Q

aminoglycosides are eliminated via the __

and have a normal half life of __

A

kidneys

2-3 hours

94
Q

aminoglycosides require __ dosing

A

renal

95
Q

is once daily dosing possible for aminoglycosides

A

yes

96
Q

what is concentration dependent killing

A

greater plasma concentration kills greater proportion of bacteria at a faster rate → seen with aminoglycosides

97
Q

what is a postantibiotic effect

A

bactericidal effect persists beyond plasma half-life

98
Q

what 2 properties of aminoglycosides allow for daily dosing

A
  1. concentration dependent killing
  2. postantibiotic effect
99
Q

with aminoglycosides, __ levels predict efficacy

and __ levels predict toxicity

A

peak

trough

100
Q

what is a trough level

A

time above threshold

101
Q

what irreversible auditory adverse rxn is associated with aminoglycosides

A

8th CN damage

102
Q

8th CN damage related to aminoglycosides can cause __

and __

A

tinnitus

vestibular → dizzy, n/v, vertigo

103
Q

what drug potentiates ototoxicity of aminoglycosides

A

loop diuretics

104
Q

can aminoglycosides cause renal toxicity

A

yes

105
Q

what is the earliest sign of aminoglycoside-induced nephrotoxicity

A

increased blood creatinine

106
Q

aminoglycosides are not effective against __ bacteria

A

(+)

Ok Pharmacology... Let's Do This... Be Gentle (6 decks)

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