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Pharm exam 2 > Inhibitors of Protein Synthesis (IPS) > Flashcards

Inhibitors of Protein Synthesis (IPS) Flashcards

1
Q

Prokaryotic ribosome subunits

A

50s and 30s (combined = 70s)

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2
Q

7 Inhibitors of PS

A
  1. Macrolides
  2. ketolides
  3. Clindamycin
  4. Streptogramins
  5. Oxazolidinones
  6. Aminoglycosides
  7. Broad spectrum abx
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3
Q

Inhibits 30s

A

Aminoglycosides & tetracyclines

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4
Q

Macrolide drugs

A

Erythromycin (oral, IV)
Clarithromycin (oral)
Azithromycin (oral, IV)

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5
Q

Macrolide properties

A

G+
reversibly bind to 50s
bacteriostatic; concentration/organism dependent
Oral absorption, biliary excretion, fecal elimination

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6
Q

Macrolide elimination

A

Fecal

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7
Q

H. pylori alternative tx with macrolide

A

clarithromycin + omeprazole (+ ampicillin)

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8
Q

DOC for macrolides

A

Chlamydia- azithromycin (or tetracylcine)
Mycoplasma pneumonia (erythromycin or tetracycline)
Legionella spp (azithromycin + rifampin or quinolone)
Syphilis in those allergic to Pen G

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9
Q

Resistance to macrolide

A

efflux pump

methylation of drug binding site (ribosome)

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10
Q

Toxicity of macrolide

A 
GI sx (clarithro-least, Erythro- most)
QT prolongation- torsades
Ototoxicity (IV erythro)
hepatic changes (jaundice, hyperbillirubinemia, abnormal LFT)
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11
Q

QT wave

A

time for heart to contract and refill; represents depolarization and repolarization of ventricles

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12
Q

macrolide with least drug interaction

A

Azithromycin

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13
Q

Drug with worst drug interactions

A

Erythromycin

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14
Q

Erythromycin

A

potent inhibitor of CYP3A4; inhibits hepatic metabolism of other drugs that require CYP3A4, increasing their serum concentrations and potential toxicity

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15
Q

Erythromycin drug interactions

A 
Carbamazepine
Clozapine
Cyclosporine
Methadone
Quinidine
Protease inhibitors
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16
Q

Macrolide with worst QT prolongation

A

Azithromycin

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17
Q

Increased QT when erythromycin is administered with

A

cisapride or pimozide

sparfloxacin or grepafloxacin

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18
Q

GI macrolides

A

clarithro < azithro < erythro

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19
Q

Drug interactions macrolide order

A

azithro < clarithro = erythro

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20
Q

Ketolide drug

A

Telithromycin (ketek)

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21
Q

MOA of telithromycin

A

bind to TWO sites on 50s to inhibit protein synthesis

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22
Q

Telithromycin properties

A

BROAD-SPECTRUM
static
50s
Good against repiratory pathogens including erythromycin and PCN-resistant pneumococci
activity against intracellular and atypical bacteria
VERY HEPATOTOXIC

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23
Q

Kinetics of telithromycin

A

oral
metabolized by CYP3A4
side effects: diarrhea, GI

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24
Q

Contraindication of telithromycin

A

myasthenia gravis

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25
Q

Telithromycin use

A

only CAP (not DOC: use macrolide)

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26
Q

Clindamycin properties

A 
oral, parenteral and topical
50s 
G+ cocci, anaerobic G-/G+
Resistant: G- aerobes and enterococci
static or cidal
metabolized by liver, minimally excreted by kidneys
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27
Q

Clindamycin use

A

Strep (not enterococci), staph (MRSA); gram + anaerobes (clostridia);
TSS (w/ vanco, nafcillin, or first gen cephalosporin)
OSTEOMYELITIS- obtains high concentration in bone
Toxoplasma encephalitis

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28
Q

Toxoplasma encephalitis tx

A

clindamycin

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29
Q

Osteomyelitis tx

A

clindamycin

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30
Q

Clindamycin toxicity

A 
well-known cause of pseudomembranous colitis
crosses placenta (avoid in prego and nursing)
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31
Q

Streptogramin drug

A

Dalforpristin; quinupristin (synercid) (IV)

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32
Q

Synercid mechanism

A

Dalfopristin: inhibits early protein synthesis
Quinupristi: inhibits late protein synthesis
BACTERICIDAL TOGETHER

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33
Q

Synercid use

A

Aerobic G + including:
PCN-resistant pneumonia, MDR-strep
compicated skin infections due to MSSA or MRSA
VRE

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34
Q

VRE tx

A

synercid

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35
Q

Adverse reaction of synercid

A

hepatotoxicity

inhibit P450 system (CYP3A4), many metabolic interactions (warfarin, diazepam)

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36
Q

Drug interactions of synercid

A

warfarin, diazepam

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37
Q

Contraindication of synercid

A 
breast-feeding
children
hepatic disease
pregnancy
streptogramin hypersensitivity
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38
Q

Linezolid (oxazolidinones) activity

A

aerobic G+ organisms

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39
Q

MOA of linezolid

A

bind to 50s, preventing formation of 70s ribosome;
bacteriostatic (except for in strep)
Reversible, non-selevtive inhibitor of MAO

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40
Q

Inhibitor of MAO

A

linezolid

41
Q

Linezolid use

A 
G+ infections:
bacterial pneumonia
skin infections
VRE
MRSA
42
Q

Kinetics of linezolid

A

IV/oral

metabolized via oxidation but oxidation is non-enzymatic and does not involve hepatic microsomal oxidative system

43
Q

Doesn’t require enzymes fro oxidation

A

Linezolid

44
Q

Adverse reactions of linezolid

A

GI
insomnia, constipation, rash, dizziness, fever
MAO inhibitor Sx
superinfection

45
Q

Contraindications of linezolid

A

hypersensitivity

PHEOCHROMOCYTOMA

46
Q

pheochormocytoma is a contraindication for

A

Linezolid

47
Q

Drug interaction of Linezolid

A

beta-blockers, anesthetics, MAO inhibitors;
antidepressants (amoxapine, maprotiline, mirtazapine, trazodone, tricyclics, SSRIs)
tyramine rich foods (aged cheese, pork, smoked/pickeld foods)

48
Q

Aminoglycoside drugs

A 
streptomycin (IV/IM)
gentamicin (IV/IM/Topical)
Tobramycin (IV/IM/topical)
Amikacin (IV/IM)
Neomycin (IV/IM)
49
Q

Topical aminoglycosides

A

gentamicin, neomycin, tobramycin

50
Q

Oral aminoglycoside

A

Neomycin

51
Q

Streptomycin

A

TB, second line (isoniazid is first line)

52
Q

Aminoglycoside spectrums

A

G-, most combo

53
Q

Aminoglycoside properties

A

polycations, high polarity

54
Q

MOA of aminoglycosides

A

Irreversibly inhibit protein synthesis by bind to 30s; bactericidal

55
Q

Bactericidal PSI

A

Synercid, aminoglycosides

56
Q

Functions of aminoglycosides

A
  1. block initiation of protein synthesis
  2. blocks translation and elicits premature termination
  3. incorporation of incorrect AA
57
Q

Uptake of aminoglycosides

A

must be ACTIVELY TRANSPORTED (oxygen requiring) to enter and bind 30s

58
Q

Spectrum of aminoglycosides

A

AEROBIC G- enteric bacteria (rods) (usually combined w/ beta-lactam) or when there is suspicion of sepsis or endocarditis

59
Q

Streptomycin use

A

tularemia
bubonic plague
TB (2nd line)
endocarditis (combo)

60
Q

Gentamicin/tobramycin/amikacin

A

effective against P. aeruginosa

61
Q

Neomycin and gentamycin

A

topical application of wounds and burns cause by gram-negative organism

62
Q

Enterococcus species DOC

A

aminoglycoside + PCN

63
Q

Synergism of aminoglycoside

A

PCN

64
Q

Toxicity of aminoglycosides

A

ototoxicity
nephrotoxicity
neuromuscular weakness

65
Q

Aminoglycoside kinetics

A

concentration-dependent killing; PAE (single large dose)
IM/IV/topical
none is absorbed enough for oral administration
none penetrates CSF readily
normal kidney rapidly excretes all

66
Q

Resistance to aminoglycosides

A

deficiency of ribosomal receptors
lack of permeability of drug into bacteria
enzymatic modification by the bacteria

67
Q

Broad spectrum abx

A

Chloramphenicol
Tetracylcines
Glycylcyclines

68
Q

Chloramphenicol

A

broad spectrum (synthetic)

69
Q

MOA of chloramphenicol

A

reversibly bind to 50s inhibiting protein synthesis;
bacteriostatic
inhibits mitochondrial protein synthesis in mammalian cells (adverse effects)

70
Q

Inhibit mammalian mitochondria

A

chloramphenicol

71
Q

Spectrum of chloramphenicol

A

broad spectrum: G+/-, aerobes, anaerobes, atypicals

72
Q

Chloramphenicol use

A

LIFE-THREATENING CONDITIONS ONLY:
typhoid fever
meningitis (Hib, n. meningitidis, s. pneumoniae)
Rickettsia, Brucellosis, Rockey mountain, meliodosis
Bacterial conjunctivitis

73
Q

Chloramphenicol kinets

A 
parenteral
widely distributed (eyes and CNS)
metabolized in liver; CONJUGATED W/ GLUCURONIC ACID
excreted in kidney
potent inhibitor of CYP3A4 and CYP2C19
74
Q

Conjugated with glucuronic acid

A

Chloramphenicol

75
Q

100% CNS penetration

A

Chloramphenicol

76
Q

Inhibitors of CYP3A4

A

synercid, erythromycin, chloramphenicol

77
Q

Toxicity of chloramphenicol

A

hetpatopoietic problems:
dose dependent: bone marrow supression
dose-independent: fatal aplastic anemia
Gray baby syndrome

78
Q

Gray baby syndrome

A

Chloramphenicol- inadequate activity of glucuronyl transferase in premature or newborn liver (w/i 48 hours; discontinue tx to recover)

79
Q

Resistance to chloramphenicol

A

acetyl transferase: acetylates and inactivates chloramphenicol
binding site modified (acetylated)
efflux pumps

80
Q

Tetracycline drugs

A

Tetracycline (oral, topical)
Doxycycline (oral)
Minocycline (oral)

81
Q

MOA of tetracycline

A

inhibition of protein synthesis (30s); bacteriostatic

82
Q

Spectrum of tetracyclines

A

broad

83
Q

Organisms resistant to tetracyclines

A

B. fragilis, proteus, pseudomonas

84
Q

Tetracycline use

A 
H. pylori: (w/ metronidazol + Bismuth)
cholera (DOC)
mycoplasma pneumonia  (DOC, erythro)
Chlamydia (DOC, Azithro/erythro)
Rickettsia (DOC)
Lyme disease (early)
Vibrio (DOC)
85
Q

Lyme disease DOC

A

Early- doxycycline, amoxicillin

Late- ceftriazone

86
Q

Resistance to tetraycline

A

efflux pump

87
Q

Tetraycycline resistant strains may be susceptible to

A

doxycycline, minocycline, tigeycline (poor substrates for efflux pumps)

88
Q

Tetracycline kinetics

A

oral is adequate but incomplete (D and M are better)
Chelation with Ca, Fe, Al
Deposit in bone and teeth (Ca)
metabolized by liver, excreted through urine and some bile (except doxycycline)
D and M are slowly excreted (less frequent

89
Q

Long acting tetracyclines

A

Doxycycline and Minocycline

90
Q

Deposit in bone and teeth

A

Tetracyclines

91
Q

Chelation with Ca, Fe, Al

A

Tetracyclines

92
Q

Adverse reactions of tetraycyclines

A 
normal flora changes
bone and teeth
photosensitivity
liver damage
Fanconi syndrome
93
Q

Contraindications of tetracyclines

A

pregnant women

CHILDREN <8 YO

94
Q

<8 YO don’t give

A

Tetracyclines

95
Q

Gylcylcycline drug

A

Tigecycline

96
Q

Synthetic derivative of minocycline; developed to circumvent resistance mechanism

A

Tigecycline

97
Q

Tigecycline

A

IV

binds to 30s; static

98
Q

Tigecycline spectrum

A 
broad spectrum (like tetracyclines) but also active against tetracycline-resistant organisms
MRSA, MRSE, PRSP, VRE
99
Q

Side effects of tigecycline

A

similar to tetracyclines; main effect: N/V

Pharm exam 2 (6 decks)

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