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Pharmacology > Protein Synthesis Inhibitors > Flashcards

Protein Synthesis Inhibitors Flashcards

1
Q

This typically prokaryotic ribosomal subunit is found in mitochondria of mammalian cells

A

70S

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2
Q

Protein synthesis inhibitor that penetrates the mitochondria, leading to extensive toxicity

A

Chloramphenicol

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3
Q

Streptomycin is this type of protein synthesis inhibitor

A

Aminoglycoside (30S inhibitor)

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4
Q

Neomycin is this type of protein synthesis inhibitor

A

Aminoglycoside (30S inhibitor)

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5
Q

Aminoglycosides have this charge

A

Positively charged

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6
Q

Aminoglycosides enter bacteria through this

A

Negatively charged pores

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7
Q

The entrance of positively charged aminoglycosides into bacteria through negatively charged pores is disrupted by these 2 things

A

Low pH and metal ions (divalent cations)

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8
Q

Internalized aminoglycoside changes the permeability of the membrane under these conditions

A

Aerobic conditions

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9
Q

The action of internalized aminoglycoside to change membrane permeability is disrupted by this

A

Low oxygen

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10
Q

As initial entry into bacteria is via pores, prior use of these increases overall permeability to aminoglycosides and is a synergistic antibiotic action

A

Cell wall synthesis inhibitors (penicillins)

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11
Q

Aminoglycosides inhibit this

A

Protein synthesis - 30S subunit

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12
Q

Is aminoglycoside action concentration-dependent?

A

Yes

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13
Q

Effect of treatment with aminoglycosides that is related to the formation of frozen initiation complex resulting in formation of “streptomycin monosomes” (ribosomes stuck irreversibly on mRNA)

A

Post-antibiotic effect

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14
Q

Spectrum of action of Aminoglycosides

A

Broad
Effective against aerobic gram negative, staphylococci and mycoplasma

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15
Q

3 mechanisms of resistance against aminoglycosides

A

Increased degradation of aminoglycosides
Alterations in ribosomal proteins
Altered permeability

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16
Q

Aminoglycosides concentrate in these 2 structures

A

Renal and inner ear

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17
Q

Adverse effect of aminoglycosides that is generally reversible, dose and time related, and additive with other toxic drugs

A

Nephrotoxic

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18
Q

Nephrotoxicity, Ototoxicity, and neuromuscular blockage are adverse effects of this

A

Aminoglycosides

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19
Q

The distribution of aminoglycosides leads to these two toxicities

A

Nephrotoxicity, Ototoxicity

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20
Q

Why does neuromuscular blockage occur with use of aminoglycosides?

A

Because of decreased acetylcholine release at neuromuscular junction (due to Ca2+ sequestration)

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21
Q

3 black box warnings of aminoglycosides

A

Nephrotoxicity, Ototoxicity, Neuromuscular blockage

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22
Q

Are aminoglycosides safe during pregnancy?

A

No

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23
Q

Type of drugs that may enhance permeability for aminoglycosides, enhancing activity

A

Cell wall synthesis inhibitors (penicillins, cephalosporins, vancomycin)

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24
Q

30S inhibitor that is bactericidal at high doses

A

Aminoglycosides

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25
Q

30S protein inhibitor that is bacteriostatic

A

Tetracyclines

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26
Q

Are these short or long acting tetracyclines:
Tetracycline, Oxytetracycline

A

Short acting (half life ~8 hours)

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27
Q

Are these short or long lasting tetracyclines:
Doxycycline, Minocycline, Demeclocycline

A

Long lasting (>12 hours)

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28
Q

MOA of tetracyclines

A

Bind 30S and block tRNA binding to A site

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29
Q

Selective toxicity of this protein synthesis inhibitor is related to specific energy-dependent transport and accumulation systems found in bacteria

A

Tetracyclines

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30
Q

Protein synthesis inhibitor that binds to 30S subunit and blocks tRNA binding to A site

A

Tetracyclines

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31
Q

Tetracyclines oral absorption is impaired by food and metal ions, except for these 2

A

Doxycycline and minocycline (less polar tetracyclines)

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32
Q

Doxycycline and minocycline are exceptions to this characteristic of tetracyclines

A

Are NOT impaired by food and metal ions

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33
Q

Tetracyclines are distributed in body tissues and fluids according to this

A

Lipid solubility (and protein binding)

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34
Q

Short acting tetracyclines are more or less polar?

A

More
Poorest lipid solubility and protein binding

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35
Q

Long acting tetracyclines are more or less polar?

A

Less polar
Best lipid solubility and protein binding

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36
Q

Elimination of tetracyclines

A

Renal elimination
Except doxycycline which is excreted in the feces and may be preferred in patients with renal problems

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37
Q

Doxcycline is an exception to this characteristic of tetracyclines

A

is NOT renally excreted
Is excreted in the feces

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38
Q

Tetracycline that is excreted in the feces and may be preferred in patients with renal problems

A

Doxycyline

39
Q

Spectrum of action of tetracyclines

A

Broad spectrum of action
Commonly used for acne and Chlamydia

40
Q

Tetracyclines have a broad spectrum of action and are commonly used for these 2 conditions

A

Acne and Chlamydia

41
Q

Tetracyclines accumulate in these 2 places

A

Teeth and bone

42
Q

Should tetracyclines be used during pregnancy?

A

No
Also not in children under 8 years of age
Use during pregnancy may result in yellow to brown discoloration of teeth and potential weakening of teeth and bones

43
Q

Teeth and bone accumulation is characteristic of this protein synthesis inhibitor

A

Tetracyclines

44
Q

Photosensitivity is an adverse effect of this protein synthesis inhibitor

A

Tetracyclines

45
Q

MOA of chloramphenicol

A

Binds 50S to prevent peptide bond formation (transpeptidate reaction)

46
Q

Spectrum of action of chloramphenicol

A

Broad

47
Q

Elimination of chloramphenicol

A

Inactivation by conjugation before excretion
Alternative biotransformation pathways are noted in neonates and young children but are inadequate to handle normal dosing regimens

48
Q

Chloramphenicol is inactivated by this before excretion

A

Conjugation

49
Q

Protein synthesis inhibitor that is inactivated by conjugation before excretion

A

Chloramphenicol

50
Q

Protein synthesis inhibitor with bone marrow depression and gray baby syndrome as adverse effects

A

Chloramphenicol

51
Q

Reversible dose related anemia and idiosyncratic aplastic anemia are adverse effects of this protein synthesis inhibitor

A

Chloramphenicol

52
Q

Onset of this may be delayed months after therapy with chloramphenicol is stopped

A

Idiosyncratic aplastic anemia (not dose related)

53
Q

Gray baby syndrome involves undeveloped newborn conjugation processes, allowing blood levels to increase, and is associated with this protein synthesis inhibitor

A

Chloramphenicol

54
Q

Why does Gray baby syndrome occur?

A

Undeveloped newborn conjugation processes allow blood levels of chloramphenicol to increase
Is potentially fatal

55
Q

Depression and suicide risk must be assessed with use of this protein synthesis inhibitor

A

Chloramphenicol

56
Q

Appropriate use (hospitalize patients and monitor for hematological toxicity) and blood dyscrasias are black box warnings of this protein synthesis inhibitor

A

Chloramphenicol

57
Q

Erythromycin is this type of protein synthesis inhibitor

A

Macrolides

58
Q

Clarithromycin is this type of protein synthesis inhibitor

A

Macroldies

59
Q

Azithromycin is this type of protein synthesis inhibitor

A

Macrolides

60
Q

MOA of macrolides

A

Bind 50S and inhibit translocation

61
Q

Spectrum of action of macrolides

A

Broad
Relatively few indications

62
Q

Motility increased in GI tract, arrhythmia risk, cholestatic hepatitis, rash, and eosinophilia are adverse effects of this protein synthesis inhibitor

A

Macrolides

63
Q

risk of this is elevated by macrolide inhibition of CYP3A4

A

Sudden cardiac death risk

64
Q

Sudden cardiac death risk elevated by this inhibition of CYP3A4

A

Macrolide

65
Q

Sudden cardiac death risk elevated by macrolide inhibition of this

A

CYP3A4

66
Q

5 adverse effects of macrolides

A

Motility increased in GI tract
Arrhythmia risk elevated by prolonged QT interval
Cholestatic hepatitis
Rash
eOsinophilia

67
Q

Macrolide indicated for Clostridium difficile-associated diarrhea

A

Fidaxomicin

68
Q

Fidaxomicin is this type of protein synthesis inhibitor

A

Macrolide

69
Q

Indication of Fidaxomicin

A

C. difficile

70
Q

Protein synthesis inhibitor that inhibits bacterial transcription by targeting RNA polymerase sigma

A

Fidaxomicin

71
Q

MOA of Fidaxomicin

A

Targets RNA pol sigma
Cidal

72
Q

Spectrum of action of Fidaxomicin

A

Very narrow: gram + aerobes and anaerobes, used primarily for C. diff

73
Q

MOA of clindamycin

A

Binds 50S to inhibit translocation

74
Q

Lincosamide antibiotic that binds to 50S ribosomal subunit to inhibit translocation

A

Clindamycin

75
Q

Spectrum of action of clindamycin

A

Narrow gram positive

76
Q

Pseudomembranous colitis is a black box warning for this protein synthesis inhibitor

A

Clindamycin

77
Q

Black box warning for Clindamycin

A

Pseudomembranous colitis

78
Q

Look for this in order to determine if Pseudomembranous colitis is caused by C. diff or drug-induced

A

C. diff toxin

79
Q

The depletion of this is an important marker for Streptogramin action (Quinupristin-Dalfopristin Combination)

A

Free tRNA
Cidal

80
Q

Quinupristin-Dalfopristin Combination:
Component that disrupts early protein synthesis steps (blocks aminoacyl-tRNA binding)

A

Quinupristin

81
Q

Quinupristin-Dalfopristin Combination
Component that disrupts later protein synthesis steps to promote premature dissociation of complex

A

Dalfopristin

82
Q

The MOA of Quinupristin-Dalfopristin Combination results in this

A

Decreased free tRNA in cell (cidal)

83
Q

Quinupristin-Dalfopristin Combination generally binds this ribosomal subunit

A

50S

84
Q

2 adverse effects of Quinupristin-Dalfopristin Combination

A

Joint and muscle pain
Hepatotoxicity

85
Q

Joint and muscle pain, and hepatotoxicity are adverse effects of this protein synthesis inhibitor

A

Quinupristin-Dalfopristin Combination (bactericidal streptogramin class)

86
Q

Protein synthesis inhibitor with these limited indications:
MRSA, Vancomycin-resistant enterococcus (black box)
Complicated skin and skin-structure infections
Drug-resistant pneumococci

A

Quinupristin-Dalfopristin Combination (bactericidal streptogramin class)

87
Q

Spectrum of action of Linezolid

A

Narrow gram positive
Primary use is vancomycin-resistant enterococcal infections

88
Q

Reversible bone marrow depression, peripheral neuropathy, and dangerous drug interactions due to inhibition of monoamine oxidase (dangerous hypertension or serotonin syndrome) are adverse effects of this protein synthesis inhibitor

A

Linezolid

89
Q

MOA of Linezolid

A

Binds 50S and blocks formation of functional tRNA-ribosome-mRNA complex that initiates protein synthesis

90
Q

Peripheral neuropathy is an adverse effect of this protein synthesis inhibitor

A

Linezolid

91
Q

Protein synthesis inhibitor that inhibits monoamine oxidase, leading to dangerous drug interactions

A

Linezolid

92
Q

Dangerous hypertension or serotonin syndrome (muscle rigidity, hyperthermia, autonomic instability) are results of drug interactions involving this protein synthesis inhibitor

A

Linezolid

93
Q

Protein synthesis inhibitor that has concentration dependent actions with postantibiotic activity

A

Aminoglycosides

Pharmacology (14 decks)

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