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Unit 2- Pharm > Inhibitors of Protein Synthesis I/II > Flashcards

Inhibitors of Protein Synthesis I/II Flashcards

1
Q

7 inhibitors of protein synthesis

A

SMACKBO

streptogramins

macrolides

aminoglycosides

clindamycin

ketolids

broad spectrum antibiotics

oxazolidinones

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2
Q

3 Macrolide drugs

A

ACE
erythromycin - oral, IV

clarithromycin - oral

azithromycin - oral, IV

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3
Q

Macrolides: G+/G-

A

G+

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4
Q

Which subunit of ribosomes do macrolides bind to?

A

50S

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5
Q

What is the spectrum of macrolides similar to?

A

Pen G

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6
Q

Erythromycin, Clarithromycin, azithromycin: bacteriostatic or cidal

A

Static

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7
Q

A majority of G- organisms are resistant to what macrolides?

A

erythromycin

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8
Q

Clarithromycin + Omeprazole + amp is one option for trearing

A

H pylori

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9
Q

Erythromycin is DOC for which urogenital infection occurring when?

A

Chlamydia occurring during pregnancy

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10
Q

Azithromycin is an alternative to tetracycline in treating uncomplicated _____ infections.

A

Chlamydia

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11
Q

Erythromycin or tetracycline is effective at treating what “atypical” disease?

A

Mycoplasmal pneumonia

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12
Q

Erythromycin is effective in treating what STD when people are allergic to Pen G

A

Syphilis

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13
Q

Azithromycin is effective at treating (DOFC) what disease?

A

Legionnaire’s Disease

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14
Q

How does resistance work in macrolides?

A

Efflux pumps (drug leaves cell quickly and in increased concentrations)

Methylation of drug binding site on ribosome so drug no longer recognizes binding site

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15
Q

Adverse side effects of macrolides?

A

diarrhea

QT prolongation

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16
Q

What is the problem with QT prolongation?

A

time it takes heart to contract and then refill with blood before beginning next contraction – if QT is too long, there is the potential for torsades

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17
Q

Drug interactions of erythromycin/clarithromycin? (Azithromycin has less of this drug interaction)

A

potent inhibitor of CYP3A4 - increases serum concentrations of other drugs that require CYP3A4 potentially causing toxicity

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18
Q

Drug interactions of erythromycin/clarithromycin: prolonged ______. Azithromycin is more favorable.

A

QT segment

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19
Q

Macrolides; diarrhea side effect?

A

Erythromycin - most

Azithromycin - next highest

Clarithromycin - least

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20
Q

Macrolides: drug interactions due to CYP3A4 inhibition

A

Most: Clarithromycin and Erythromycin

Least: Azithromycin

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21
Q

Macrolides: QT prolongation

A

Most: Azithromycin

Least: Clarithro, Erythro

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22
Q

Ketolides: bind tightly to how many sites on ribosomal RNA?

What does this mean when comparing to macrolides?

A

2 binding sites

Stronger

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23
Q

Name of ketolides

A

Telithromycin

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24
Q

Telithromycin is what kind of spectrum antibiotic

A

Broad

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25
Q

Telithromycin: static or cidal?

A

static

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26
Q

Telithromycin binds to what ribosomal subunit

A

50S

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27
Q

During what specific type of infections do we use telithromycin?

A

good against respiratory pathogens including erythromycin and penicillin resistant pneumococci

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28
Q

How do you take telithromycin?

A

orally - very effective as a once a day dose

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29
Q

Telithromycin is metabolized by what hepatic cytochrome

A

CYP3A4

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30
Q

Telithromycin can cause what adverse side effects (2)

A

diarrhea

hepatotoxicity - severe - only on market for community acquired pneumonia

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31
Q

Despite serious hepatotoxicity, why is telithromycin still on the market?

A

community acquired pneumonia

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32
Q

Clindamycin reversibly binds to

A

50S ribosomal subunit

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33
Q

Clindamycin is active against what three types of bacteria (general - not names)

A

aerobic G+ cocci

anaerobic G-

anaerobic G+

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34
Q

Clindamycin: static or cidal?

A

both - depends on concentration and specific susceptibility of organism

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35
Q

Clindamycin - used with vanco, nafcillin, or first gen cephalosporin to treat what?

Why used together?

A

Toxic Shock Syndrome

Because the toxin is produced by the bacteria. If you just used a cidal drug, the bacteria would rupture and toxins would seep out. If you use a protein inhibitor first, the toxins die - then lyse the cells with a cidal drug

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36
Q

Clindamycin is used to treat _____. Why?

A

osteomyelitis -obtains high concentration in bones

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37
Q

Clindamycin is a well-known cause of:

A

pseudomembranous colitis - overgrowth of c-diff. switch to metronidazole

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38
Q

Clindamycin can/cannot be used while pregnant/breast-feeding?

A

cannot

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39
Q

Streptogramins: used together

A

Dalfopristin and Quinupristin – to make Synercid

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40
Q

How do streptogramins work?

A

inhibit protein syn by blocking ribosomal function

Dalfopristi - binds to 50S early

Quinupristin 0- binds to 50S late

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41
Q

How is synercid administered?

A

IV infusion - two antibiotics act synergistically

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42
Q

Independently, dalfopristin and quinupristin are ______. Together, they are ______.

A

static

cidal

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43
Q

Spectrum of synercid

A

aerobic G+

MDR

MSSA

MRSA

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44
Q

Oxazolidinones

A

Linezolid

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45
Q

Linezolid spectrum

A

aeorbic G+

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46
Q

Linezolid: mechanism of action

A

inhibits protein syn

binds to 50S ribosome

prevents formation of 70S ribosome complex

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47
Q

Linezolid is static/cidal?

A

static

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48
Q

Linezolid is a:

relates to MAO

A

reversible, non-selective inhibitor of monoamine oxidase?

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49
Q

Linezolid indicated for:

Save it for:

A

G+ infections

MDR strains (like MRSA)

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50
Q

Unique bioavailability property of linezolid

Can also be given

A

oral bioavailability 100%

IV

51
Q

How is linezolid metabolized?

A

oxidative - does not involve hepatic microsomal oxidative system

52
Q

Important drug interactions

A

beta-blockers, anesthetics, SSRIs (IMPORTANT ONE), MAO inhibitors

53
Q

Important contraindications for linezolid (2)

A

hypersensitivity

pheochromocytoma (IMPORTANT - on test)

54
Q

5 aminoglycosides

A

streptomycin

gentamycin

tobramycin

amikacin

neomycin

55
Q

Aminoglycosides: special physical characteristic

A

really large

really polar

polarity responsible for pharmacokinetic properties

56
Q

Aminoglycosides: mechanism of action

A

irreversibly inhibit protein syn of susceptible microorganisms by inhibiting the 30S subunit

57
Q

Aminoglycosides - which subunit of ribosomes

A

30S

58
Q

Aminoglycosides: cidal/static under aerobic conditions

A

cidal

59
Q

Aminoglycosides: active transport and O2

to be effective, aminoglycosides first must be _____ ____ (requiring ____) into susceptible bacteria and bind to what subunit?

A

actively transported

oxygen

30S

60
Q

Are aminoglycosides effective against aerobes or anaerobes? Think mechanism of action.

A

AEROBES

61
Q

Aminoglycosides spectrum

A

aerobic G- enteric bacteria

sepsis

endocarditis

62
Q

When do you use gentamycin, tobramycin, amikacin

A

P. aeruginosa

63
Q

When are neomycin and gentamycin used?

A

topical application to wounds and burns

64
Q

DOC: aminoglycosides + antipseudomonal penicillin for:

A

p. aeurginosa (immunocompromised)

Tularemia

65
Q

Why do you use two cidal drugs to attack p. aeruginosa?

A

Bacteria is an opportunistic infection –> there is synergy that occurs that makes sure the immune system of host does not have to fight (because it cannot)

66
Q

DOC: aminoglycoside + penicillin

A

enterococci

67
Q

How do aminoglycosides and penicillins work together?

A

Penicillins create hole in membrane so aminoglycosides (which are very polar and can’t get in by themselves) can get through and reach protein for protein inhibition

68
Q

What two types of toxicity are aminoglycosides known for?

A

ototoxicity

nephrotoxicity

69
Q

What do the levels of ototoxicity and nephrotoxicity depend on?

A

duration of time the concentration of drug is above threshold

70
Q

Aminoglycosides: concentration-dependent killing

A

increasing concentrations kill an increasing population of bacteria and an increased rate

71
Q

Do aminoglycosides have a post-antiobiotic effect? If they do, what does this mean?

A

Yes – this means that a single large dose has better efficacy than multiple smaller doses - this reduces toxic side effects

72
Q

By giving aminoglycosides only once/day, time spent over the threshold concentration is more/less?

What does this mean?

A

Less

Less toxic effects.

73
Q

Pharmacokinetics of aminoglycosides

administration?

CNS penetration?

excretion?

A

IM, IV, topical

NOT GIVEN ORALLY

DO NOT penetrate CNS

Normal kidney excretion

74
Q

Cross resistance of aminoglycosides?

A

bacteria that acquire resistance to one amino-glycoside may exhibit cross-resistance to all aminoglycosides

75
Q

How does resistance to aminoglycosides occur?

A

deficiency of ribosomal receptors

lack of permeability of drug into bacteria

enzymatic modification by bacteria

76
Q

Aminoglycosides are usually given alone/in combination with other antibiotics?

A

in combo

77
Q

What is important when treating pseudomonas?

A

never give only one antibiotic!

78
Q

3 classes of broad spectrum antibiotics

A

chloramphenicol

tetracyclines

glycylcyclines

79
Q

Chloramphenicol: what special “broad spectrum” characteristics does it have?

A

one of the best broad spectrum but also really toxic – saved for really serious infections when you don’t have other choices

80
Q

What fatal adverse effect of chloramphenicol is it known for?

A

fatal aplastic anemia

81
Q

Chloramphenicol: mechanism of action

A

reversibly binds to 50S subunit –> protein synthesis is inhibited

82
Q

Chloramphenicol: static or cidal

A

static

83
Q

Chloramphenicol:

can also inhibit:

A

mitochondrial protein synthesis in mammalian cells – this is thought to be the basis of their adverse effects

84
Q

Chloramphenicol: what kind of spectrum?

A

broad - G+, G-, anaerobes, aerobes, atypicals

85
Q

Can be used for what infections? Is it the DOFC?

A

Typhoid fever, Meningitis, Rocky Mountain Spotted Fever,

NOT drug of first choice

86
Q

How is Chloramphenicol adminstered?

A

IV, parenterally

87
Q

What drug has the best CNS penetration without inflammation?

A

Chloramphenicol

88
Q

What must occur for chloramphenicol to be eliminated/excreted?

A

metabolized in the liver and conjugated with glucuronic acid to form inactive metabolite which is excreted in the kidney

89
Q

Chloramphenicol: toxicity

hematopoietic problems: dose-dependent

A

bone marrow suppression - leads to anemia, leukopenia

90
Q

Chloramphenicol toxicity

hematopoietic problems: dose-independent

A

fatal aplastic anemia – can develop months after drug has been discontinued OR from a single dose

CAN BE LETHAL

91
Q

Chloramphenicol: what syndrome is associated with this drug and infants?

A

gray baby syndrome

92
Q

Chloramphenicol: Gray Baby Syndrome occurs how?

A

inadequate activity of glucuronyl transferase in premature or newborn liver –> cannot be excreted so increased concentrations

93
Q

Chloramphenicol: Resistance works how?

A

acetyl transferase produced by resistant organisms acetylates and inactivates chloramphenicol - this leads to binding sites being modified.

Efflux pumps

94
Q

Can you give Chloramphenicol to pregnant mothers?

A

Yes - will not cross placenta

95
Q

Tetracyclines: 3 drugs in this class

A

tetra, doxy, mono

96
Q

Tetras: which subunit?

A

30S

97
Q

Tetras: cidal or static?

A

static

98
Q

Tetras MOA

A

inhibition of bacterial protein synthesis; binds to 30S and prevents addition of amino acids to the growing peptide chain

99
Q

Spectrum of the tetras?

A

G+, G-, anaerobes, aerobes, atypicals

100
Q

What are the three organisms resistant to tetras?

A

B gragilis

proteus

pseudomonas

101
Q

Because tetras are widely used….

A

resistance is high

102
Q

Tetras:

H. pylori treated how

A

with metronidazol and bismuth

103
Q

Tetras: DOC for what diarrheal disease?

A

cholera

104
Q

Tetras: used but not DOC for what atypical pneumonia?

A

mycoplasma pneumonia

105
Q

Tetras: used but not DOC for what STD?

A

chlamydia

106
Q

Tetras: used but not DOC for what type of “outdoorsy” infection?

A

rickettsial infection

107
Q

Doxy is the DOC for what?

A

rocky mountain spotted fever

108
Q

Tetras: treats what stage of lyme disease?

A

early

109
Q

Tetras: DOC for what species?

A

vibrio

110
Q

Tetras: resistance occurs how?

A

efflux pumps

111
Q

Are all tetras (tetra, doxy, mono) susceptible to same resistance?

A

No - if efflux pumps are mode of resistance, you can still potentially use mono or doxy. Therefore, tetra resistant strains may be susceptible to doxy, mono, tigecycline.

112
Q

Which of the following is worst for chelation with Ca2+, Fe2+, and Al3+

A

Tetracycline

113
Q

Which of the tetras has the worst oral absorption?

A

tetracycline

114
Q

Tetras deposit themselves where?

A

bone and teeth

115
Q

Which of the tetras are the longest lasting?

A

Doxy, Mino

longer half life and less frequent administered

116
Q

Adverse effects of tetras?

A

normal flora changes

bone and teeth issues

photosensitivity

117
Q

To whom should you not give tetras? Why?

A

prengnat women or children below age of 8

can cross placenta and excreted in breast milk

bone issues in young children

118
Q

Glycylcyclines: name

A

Tigecycline

119
Q

Glycylcyclines: tigecycline

binds to what subunit

static or cidal

A

30S

static

120
Q

Glycylcyclines: tigecycline

spectrum similar to what?

A

tetras; however, tigecycline shows activity against tetra-resistant organisms

121
Q

How is glycylcyclines: tigecycline administerd?

A

IV

122
Q

Glycylcyclines: tigecycline has activity against wide variety of resistant pathogens

A

MRSA

MRSE

PRSP

VRE

123
Q

Why is ampicillin given with clavilanate but not vanco?

A

Vanco does not have beta-lactam ring

Unit 2- Pharm (9 decks)

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