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Lippincotts pharmacology 6th edition > Ch. 39 Protein synthesis inhibitors > Flashcards

Ch. 39 Protein synthesis inhibitors Flashcards

1
Q

may cause toxic effects as a result of interaction with mitochondrial mammalian ribosomes

A

chloramphenico or the tetracyclines

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2
Q

ribosomes composed of 30S and 50S subunits

A

bacterial ribosomes

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3
Q

ribosomes composed of 40S and 60S subunits

A

mammalian ribosomes

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4
Q

consists of 4 fused rings with a system of conugated double bonds

A

tertracyclines

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5
Q

enter susceptible organisms via passive diffusion and also by an energy-dependent transport protein mechanism unique to the bacterial inner cytoplasmic membrane

A

tetracyclines

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6
Q

binds reversibly to the 30S subunit of the bacterial ribosome , preventing binding of tRNA to the mRNA-ribosome complex, thereby inhibiting bacterial proetin synsthesis

A

tetracyclines

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7
Q

bacteriostatic antibiotics
against : gram(+) and (-)
protozoa, spirochetes , mycobacteria , atypical

A

tetracyclines

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8
Q

tetrayclines treatment

A

acne and chlamydia infections (doxycycline)

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9
Q

naturally occuring resistance to tetracyclines

A

efflux pump that expels drug out of the cell

-prevents intracellular accumulation

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10
Q

Spirochete: Lyme disease : cause , s/s (signs and symptoms), treatment

A

Borrelia burdorferi, bite of infected ticks,

skin lesions, headache and fever, followed by meningoencephalitis and evetually arthritis

bull’s eye pattern rash with a red outer ring (erhema migrans.

doxycycline

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11
Q

Cholera

cause , s/s (signs and symptoms), treatment

A

fecally contaminated food or water (vibrio cholerae)

enterotoxin that produces diarrhea

doxycycline

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12
Q

Chlamydial infections

cause , s/s (signs and symptoms), treatment

A

Chlamydia trachomatis
-nongonococcal , urethritis, PID, lymphogranuloma venerum

Chlamydia psittaci
-pneumonia, hepatitis, myocarditis , coma

doxycyline or azithromycin

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13
Q

mycoplasma pneumoniae

cause , s/s (signs and symptoms), treatment

A

mycoplasma pneumoniae
community-acquired pneumonia
—-military camps
Macrolide or doxycycline

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14
Q

Rocky Mountain Spotted fever

cause , s/s (signs and symptoms), treatment

A

rickettsia rickettsii
-fever, chills, aches in bones and joints
tetracyclines-started early in the disease process

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15
Q

dairy products will create nonabsorbable chelates thus decrease oral absorption for ?
-divalent and trivalent cations: mg and aluminum anta acids or iron supplements

A

tetracyclines

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16
Q

tetracyclines that are oral and IV

A

minocycline and doxycycline

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17
Q

where do tetracyclines concentrate?

A

bile, liver, kidney, gingival fluid, and skin

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18
Q

minocycline and doxycycline achieve therapeutic levels in the

A

CSF

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19
Q

achieves high levels in saliva and tears, eradicating the meningococcal carrier state

A

minocycline

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20
Q

tetracycline is primarily eliminated unchanged in

A

urine

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21
Q

not hepatically metabolized

A

tetracycline and doxycycline

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22
Q

undergoes hepatic metabolism

A

minocycline

- lesser extent in kidney

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23
Q

in renally compromised patients we prefer?

because?

A

doxycycline

because eleminated via bile into feces

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24
Q

adverse effects of tetracyclines

A

gastric discomfort, calcified tissues, hepatotoxicity , phototxicity (severe sunburn), vestibular dysfunction, pseudotumor cerebri,

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25
Q

Contraindication of tetracyclines:

A

less than 8yrs of age
pregnant
lactation

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26
Q

tetracycline should be taken on an empty or full stomach?

A

empty stomach

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27
Q

why is tetracycline CI in the kids less than 8yrs of age

A

deposition in the bone and primary dentition occurs during the calcification process in growing children

-discoloration and hypoplasia of teeth and temporary stunting of growth

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28
Q

why do people taking tetracycline and demeclocycline need to wear adequate sun protection?

A

phototoxicity

–severe sunburn

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29
Q

minocycline and doxycycline have a common adverse effect, what is it?

A

vestibular dysfunction,

dizziness, vertigo, and tinnitus

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30
Q

benign intracranial hypertension : headache and blurred vision

A

tetracyclines

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31
Q

Protein inhibitor Group: tetracyclines

A

demeclocycline
doxycycline
minocycline
tetracycline

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32
Q

Protein inhibitor Group: Aminoglycosides

A

drivin a “Stang”!

Streptomycin, tobramycin, amikacin, neomycin, amikacin, gentamicin

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33
Q

Protein inhibitor Group: Macrocyclic

A

think “Mother Fucker”
thus, Macrocyclic:

-Fidaxomicin

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34
Q

Protein inhibitor Group: Macrolides/Ketolides

A

azithromycin,
clarithromycin
erythromycin
telithromycin

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35
Q

Protein inhibitor Group: Lincosamides

A

clindamycin

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36
Q

Protein inhibitor Group: oxazolidinones

A

linezolid

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37
Q

Protein inhibitor Group: others

A

cloramphenicol

quinupristin/dalfopristin

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38
Q

what are the Protein inhibitor Group?

A 
tetracyclines
glycylcyclines
aminoglycosides
macrolides/ketolides
macrocyclic
oxazolidinones
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39
Q

Protein inhibitor Group: Glycylcyclines

A

tigecyclines

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40
Q
  • minocycline derivative
  • treatment of complicated skin and soft tissue infections
  • intra-abdominal infections
A

Tigecycline

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41
Q

tigecycline MOA:

A

bacteriostatic

  • reversibily binding 30S ribosomal subunit
  • inhibits protein synthesis
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42
Q
A

Tigercycline

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43
Q

tigecycline is not active against

A

morganella
proteus
providencia
pseudomonas species

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44
Q

resistance of tigecycline is due to

A

overexpression of efflux pumps

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45
Q

dose reduction is recommended in sever hepatic dysfunction

A

tigecycline

-route of elimination is biliary/fecal

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46
Q

poor option for bloodstream infections

A

tigecycline

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47
Q

acute pancreatitis , fatality, nausea, vomiting , photosensitivity, pseudotumor cerebri, discoloration of permanent teeth when used during tooth development, teratogenic

A

adverse effects for tigecycline

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48
Q

elevation in liver enzymes and creatinine

A

tygecycline

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49
Q

decrease the clearance of warfarin and increase prothrombin time

A

tygecycline

-monitor closely when tigecycline is coadministered with warfarin.

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50
Q

aminoglycosides treatment

A

serious infections due to aerobic gram(-) bacilli

-clinical utility is limited by serious toxicities

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51
Q

diffuse through porin channels in the outer mebrane of susceptible organisms

A

aminoglycosides

52
Q

bind the 30S ribosomal subunit

  • interfere with assembly of the functiional ribosomal appartus
  • cause the 30S subunit of the completed ribosome to misread the genetic code
  • distrupt protein synthesis
  • bacteriostatic
A

aminoglycosides

53
Q

Cmax (concentration max) is 8-10 times the MIC (minimum inhibitory concentration)

  • exhibit postantiobiotic effect (PAE)
  • –larger the dose . longer the PAE
A

aminoglycosides

54
Q

dosages for aminoglycosides

A

a single dose daily

-reduces risk of nephrotoxicity

55
Q

effective:
aerobic gram(-) bacilli (AeG(-)b)
multi drug resistance (MDR): P. aueruginosa, Klebsiella pneumoniae, Enterobacter sp,

A

aminoglycosides

56
Q

cobined with B-lactam antibiotic provides synergistic effect, treatment of Enterococcus faecalis, and enterococcus faecium infective endocarditis

A

aminglycosides

57
Q

4 commonly used aminoglucosides

A

I have my “GATS” locked and loaded

streptomycin, tobramycin, amikacin, gentamicin

58
Q

efflux pumps, decreased uptake or modificiation and inactivation by plasmid associated synthesis of enzymes

A

resistance to aminoglycoside

59
Q

all aminoglycosides must be given parenterally except

A

neomycin

60
Q

neomycin administration

why?

A

-topically for skin infections or
-orally for bowel preparation prior to colorectal surgery
parental will cause severe nephrotoxicity

61
Q

concentrations in the CSF are inadequate

-CNS infection which route?

A 
aminoglycosides
intrathecal route (IT)
62
Q

dose adjustments due to renal dysfunction

A

aminoglycosides

63
Q

while on aminoglycosides the elderly are

A

susceptible to nephrotoxicity and ototoxicity

64
Q

adverse effects of aminoglycosides are

A

ototoxicity
nephrotoxicity
neuromuscular toxicity
allergic reactions

65
Q

accumulates in the endolmph and perilymph of the inner ear

A

ototoxicity
adverse effects of aminoglycosides
-cisplatin or loop diruretics

66
Q

distrupts calcium-mediated transport process of the PCT cells

A

adverse effects of aminoglycosides

-nephrotoxicity

67
Q

calcium gluconate or neostigmine can reverse the block that causes

A
  • neuromusclar paralysis caused by aminoglycosides

- myasthenia gravis patients are at risk

68
Q

contact dermititis is common reaction

A

adverse effects of aminoglycosides
neomycin
allergic reaction

69
Q

alternative for individuals with an allergy to B lactam antibiotics

A

macrolides

-erythromycin

70
Q

macrocyclic lactone structure

- one or more deoxy sugars

A

macrolides

71
Q

methylated for of erythromycin

A

clarithromycin

72
Q

have larger lactione ring

A

azitrhromycin

73
Q

first ketolide antimicrobial agent

A

telithromycin

74
Q

active against many macrolide-resistant gram(+) strains

A

Ketolides

-telithromycin

75
Q

bind irreversibly to 50S subunit of bacterial ribosome, inhibiting translocation steps of protein synthesis

A

microlides/ketolides

76
Q

Cornybacterium Diphtheriae

A

Erythromycin or penicillin

77
Q

Legionnaires disese

-Legionnellosis

A

fluroquinoloones or azithromycin

78
Q

Mycoplasma pneumonia

A

atypical pneumonia

azithromycin or doxycycline

79
Q

mycobacterium avium complex

MAC

A

azithromycin in combination with:
rifampin and ethambutol

-once weekly azithromycin is used as MAC prophylaxis in patients with AIDS

80
Q

Chlamydial infections

A

Azithromycin or doxycycline

81
Q
  • used in patients with penicillin allergy

- effective towards many of the same organisms as penicilin G

A

Erythromycin

-penicillin G alternative

82
Q

effective against Haemophilus influenzae

A

erythromycin similairity

clarithromycin

83
Q

chlamydia, legionella, moraxella, ueraplasma species, helicobacter pylori, erythromycin

A

Clarithromycin

84
Q

less active against streptococci and staphylococci than erythromycin , far more active against respiratory infections due to H. inflenzae and moraxella catarrhalis

A

AZITHROMYCIN

85
Q

extensive use of azithromycin results in

A

growing streptococcus pneumoniae resistance

86
Q

resistance to macrolides is associated with

A

the inability of the organisms to take up the antibiotic
presens of efflux pumps decreaseed affinity of the 50Sribosomal subunit for the antibiotic, methylation of an adenine in the 23Sbacterial ribosomal RNAin gram(+) organisms presence of gram(-) organisms such as enterbacteriaceae

87
Q

clarithromycin and azithromycin share some cross-resistance with

A

erythromycin

88
Q

telithromycin may be effective against

A

macrolide organisms

89
Q

erythromycin and azithromycin are available in

A

IV

enteric coated tablets

90
Q

interaction with the cytochrome P450 system

-interference with theophyllline statins , antiepileptics reported for clarithromycin

A

erythromycin and telithromycin

91
Q

adverse effects of macrolides/ketolides

A

-GI distress and motility
-cholestatic jaundices
—-erythromycin
-ototoxity
—erythromycin (high dosages)
——Azithromycin
-

92
Q

contraindications of macrolides/ketolides

A
  • hepatic dysfunction( erythromycin, telithromycin, azithromycin)
  • proarrhythmic agents
93
Q

Drug interactions of macrolides/ketolides

A

interaction with digoxin

-inhibit hepatic metbolism

94
Q

macrocyclic antibiotic

A

Fidaxomicin

95
Q

distrupting bacterial transcription

A

fidaxomicin

96
Q

very narrow spectrum of activity limited to gram(+) aerobes and anaerobes

A

fidaxomicin

97
Q

used primarily for colstridium difficile

-remains with the GI tract

A

fidaxomicin

98
Q

angioedema, dyspnea and pruritis hypersensitivity

A

fidaxomicin

99
Q

restricted to life-threateninng infections for which no alternatives exist

A

chloramphenicol

100
Q

binds revisebly to bacterial 50S ribosomal subunit and inhibits protein syntheses at the peptidyl transferase reactions

A

chloramphenicol

101
Q

high chloramphenicol level circulating

A

bone marrow toxicity

102
Q

chlamydiae, rickettsiae, spirochetes, and anaerobes

-bacteriostatic

A

chloramphenicol

103
Q

decreased ability to penetrate the organism and ribosomal binding site alterations

A

resistance of chloramphenicol

104
Q

adverse effects of chloramphenicol

A

anemias, gray baby syndrome, drug interactions with warfarin and phenytoin(elevates concentration)

105
Q

gray baby syndrome

A

cyanosis
deperessed breathing, cardiovascular collapse and death,
adults can exhibit this if taken in high doses

106
Q

anemia from AE of chloramphenicol

A
  • glucose-6-dehydrogenase deficiency and dose-realted anemia

- hemolytic anemia

107
Q

clidamycin treat

A

infections cause by gram(+) organisms, includin MRSA and streptococcus and anaerobic bacteria

108
Q

C. difficile is always resistant to

A

clindamycin

109
Q

common adverse effect of clindamycin

A

diarrhea caused by overgrowth of c. difficle

110
Q

treatment of c. difficle?

A

metronidazole and vancomycin

111
Q

quinupristin/dalfopristin is reserved for the treatment of ?

-in the absence of other therapeutic options

A

vancmycin-resistent enterococcus faecium VRE

112
Q

distrupts enlongation interfering with addition of new amino acid to the peptide chain

A

dalfpristin and quinupristin

113
Q

active primarily against gram positive cocci . primary treats E. faecium , VRE strains
-not effective against E. faecalis

A

quinupristin/dalfopristin

114
Q

plasma mediated actyltransferase inactivates

active efflux pump can decrease levels of the antibiotics

A

dalfopristin

-resistance mechanism

115
Q

injected intravenously

-excretion in feces=hepatic metabolism

A

quinupristin/dalfopristin

116
Q

excretion in feces

A

hepatic metabolism

biliary route

117
Q

adverse effects of quinuprist/dalfopristin

A

hyperbilirubinemia

25%

118
Q

comats ressitant gram(+) organisms such as methicillin resistant staphylococcus aureus , VRE, penicillin resistant streptococci

A

linezolid

119
Q

binds to the bacterial 23S ribosomal RNA of the 50S subunit, inhibiting formation of the 70S intiation complex

A

linezolid

120
Q

against corybacterium and listeria monocytogenes

moderately active against M tuberculosis
-bacteriostatic

A

linezolid

121
Q

alternative to daptomycin for infections caused by VRE

A

linezolid

122
Q

linezolid is not recommended to treat

A

MRSA bacteremia

123
Q

resistance to S. aureus and enterococcus sp

cross-resistance with other protein inhibitors does not occur

A

Linezolid

-resistance

124
Q

oral administration, iv, metabolized via oxidation, no dose adjustments for renal or hepatic dysfunction

A

linezolid

125
Q

Adverse Effects of linezolid

A

GI upset, nausea, diarrhea, headach, rash

  • thrombocytopenia–>10 days
  • irreversible peripheral neuropathies and optic neuritis (BLINDNESS)—-> 28 days
126
Q

possesses nonselective monoamine oxidases activity and leads to serotonin syndrome if given with tyramine-containing foods, selctive serotonin reuptake inhibitors, or MAO inhibitors

A

linezolid

Lippincotts pharmacology 6th edition (6 decks)

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