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MOD > Antibiotics > Flashcards

Antibiotics Flashcards

1
Q

Definition of antibiotic

A

substance or compound that kills or inhibits growth of bacteria

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2
Q

Endogenous antibiotic

A

lysozyme from mucus and tears

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3
Q

selective toxicity

A

ability of antibiotic to cause harm to bacteria without causing damage to the host

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4
Q

Antibiotic potential targets

A

cell wall synthesis, membrane integrity, folate synthesis, DNA/RNA synthesis, protein synthesis

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5
Q

Bactericidal

A

kills bacteria, does not rely on immune system for clearance

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6
Q

Bacteriostatic

A

bacteria “lassoed,” not propagating or proliferating, immune system able to overwhelm bacteria

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7
Q

Spectrum

A

broad: targets a variety of species
Narrow: targets a very specific species

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8
Q

Antibiotic resistance

A

bacteria resist actions of frequently used drugs, can mutate

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9
Q

Major cause of abx resistance

A

over prescription and misuse

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10
Q

Prevention of abx resistance

A

appropriate abx, use as indicated(!)

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11
Q

Synergy

A

inhibitory or killing effects of two or more abx in combination are greater than their effects individually

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12
Q

Antagonism

A

inhibitory or killing effects of two or more abx in combo are less than their effects individually

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13
Q

Cell wall synthesis inhibitors

A

Beta lactams (penicillins, cephalosporins, carbapenems), monobactams, glycopeptides and lipoglycopeptides

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14
Q

How do glycopeptides and lipogylcopeptides differ from beta lactams?

A

glyco/lipoglyco peptodes: inhibit cell wall synthesis by binding to D-alanyl-Dalanine terminus
Beta lactams: interact with transpeptidase

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15
Q

Which antibiotic relies on renal dipeptidase inhibitor celastatin?

A

carbapenems, imipenem

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16
Q

What differentiates second gen cephalosporins from cephamycins?

A

cover both G+ and G- while cephamycins are active against B. fragilus and some Serratius spp.

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17
Q

What is the general sprectrum of coverage for monobactam aztreonam?

A

mostly G-, aerobic bacteria

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18
Q

How does resistance to methicillin happen in MRSA?

A

transpeptidase (penicillin binding protein) mutation prevents methicillin binding

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19
Q

Protein Synthesis Inhibitors

A

50s: oxazolidinones, macrolides, ketolides, streptogramins
30s: tetracyclines, aminoglycosides, glycylcyclines

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20
Q

What is the difference in MOA between oxazolidinones and streptogramins?

A

streptogramins: prevent translation by binding to 50s
oxazolidinones: prevent initiation

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21
Q

DNA/RNA synthesis inhibitors

A

Fluoroquinolones

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22
Q

What proteins do fluoroquinolones inhibit?

A

Topoisomerase II in G+ bacteria, Topoisomerase IV in G- bacteria

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23
Q

Membrane integrity and folate synthesis inhibitors

A

membrane integrity: polymyxins

Folate synthesis: sulfonamides and benzylbiyrimidines

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24
Q

Why are sulfonamide and benzylpyrimidines synergistic?

A

both inhibit folate, sulfonamide inhibits PABA, benzylpyrimidines inhibit dihydrofolate reductase

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25
Q

Are polymyxins active against G+ bacteria?

A

no, target LPS on G- bacteria

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26
Q

Penicillin MOA

A

interfere with transpeptidation reaction, inhibiting cell wall synthesis by preventing cross linking of components

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27
Q

Method of penicillin resistance

A

Beta lactamases break down beta lactam ring; porin and PBP structure alteration; increased efflux

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28
Q

Method of Penicillin G resistance

A

beta lactamases

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29
Q

Spectrum of Penicillin G activity

A

G+ coccii (strep spp.), G- coccii (N. meningitidis), T. pallidum, non-B-lactamase anaerobes (C. perfringens)

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30
Q

Penicillin G AE

A

hypersensitivity reactions (anaphylaxis), N/V/D

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31
Q

Aminopenicillins MOA

A

cell wall synthesis inhibitors

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32
Q

Aminopenicillins mechanism of resistance

A

Beta-lactamases

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33
Q

Spectrum of aminopenicillins

A

G-, G+; E. coli and other enterics; H. influenzae, Klebsiella spp., Proteus spp., B. fragilis

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34
Q

Penicillinase resistant penicillins drugs

A

methicillin, nafcillin, oxacillin,dicloxacillin

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35
Q

Resistance to penicillinase resistant penicillins

A

reduced affinity for med in binding pocket of transpeptidase

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36
Q

Spectrum of penicillinase resistant penicillins

A

staphylococcal spp.

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37
Q

Antipseudomonal penicillins drugs

A

carboxypenicillins, ureidopenicillins

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38
Q

Mechanism of resistance for antipseudomonal penicillins

A

beta-lactamase (although should be co-formulated with tazobactam to inhibit beta-lactamase)

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39
Q

Spectrum of antipseudomonal penicillins

A

P. aeruginosa, G- bacilli, E. coli, H. influenzae, and B fragilis

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40
Q

Cephalosporin MOA

A

inhibits transpeptidation reaction by binding and inhibiting transpeptidase

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41
Q

Cephalosporin mechanism of resistance

A

beta-lactamases, altering porins and molecular structure of transpeptidase, efflux pumps

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42
Q

Cephalosporin AE

A

maculopapular rash, eosionophilia, fever

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43
Q

First generation cephalosporin drugs

A

cefadroxin, cephalothin, cephradine, cefazolin, cephalexin

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44
Q

Spectrum of first gen cephalosporins

A

G+ cocci (S. aureus); NOT MRSA, B. fragilis, enterococci, or S. epidermidis; G- bacteria such as M. catarrhalis, K. pneumonie, E. coli, Proteus mirabilis

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45
Q

Second generation cephalosporin drugs

A

cefuroxime, loracarbef, cefonicid, cefamanadole, cefalcor, cefoxitin

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46
Q

Spectrum of second gen cephalosporins

A

H. influenzae, N. meningitidis, S. pneumonia, cefoxitin and cefotetan are active against B. fragilis and some Serratia spp.; NO enterobacter spp.

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47
Q

Third generation cephalosporin drugs

A

cefotaxime, cefixime, cefdinir, ceftibuten, ceftazimide, ceftriaxone

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48
Q

Spectrum of third gen cephalosporins

A

expansion of G- coverage, slightly less active against G+ like Strep and Staph spp.; work well against Neisseria and Haemophilus spp. (Not Acinetobacter, Serratia, Enterobacter spp.)

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49
Q

Only third gen cephalosporin active against P. aeruginosa

A

ceftazidime

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50
Q

Cefdinir is active against….

A

E. coli, S. pyogenes, H. influenzae, P. mirabilis

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51
Q

Ceftriaxone AE

A

biliary pseudolithiasis, jaundice

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52
Q

Fourth gen cephalosporin drugs

A

cefepime

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53
Q

Spectrum of cefepime

A

P. aeruginosa, Enterobacter spp.; Poor activity against B. fragilis

54
Q

Fifth gen cephalosporin drugs

A

ceftaroline fosamil, ceftolozane

55
Q

Spectrum of fifth gen cephalosporins

A

MRSA, Pseudomonas spp.; Pseudomonas spp.

56
Q

Carbapenem drugs

A

ertapenem, meropenem, imipenem

57
Q

Carbapenems MOA

A

bind to and inhibit transpeptidase, inhibiting cell wall synthesis

58
Q

Carbapenem resistance

A

shrinking of porin channels, upregulation of degradation enzymes

59
Q

Carbapenem spectrum

A

gram-negative and positive bacteria

60
Q

Imipenem spectrum

A

G+ anaerobes, and most G- rods; P. aeruginosa, Listeria, staphylococci, enterococci, streptococci, Acinetobacter, B. fragilis

61
Q

Bugs resistant to Imipenem

A

B. cepacia, C. diff. MRSA, E. faecium

62
Q

Ertapenem spectrum does not include…

A

P. aeruginosa, Acinetobacter spp. and enterococcus

63
Q

AE with imipenem

A

skin rashes, diarrhea, vomiting, nausea; if the pt is in renal failure imipenem may cause seizures

64
Q

Monobactam available in the US

A

Aztreonam

65
Q

Aztreonam MOA

A

inhibits G- transpeptidase, preventing cell wall synthesis

66
Q

Aztreonam spectrum

A

G- aerobic bacteria, enterobacteriaceae, P. aeruginosa, H. influenzae

67
Q

Aztreonam AE

A

pts allergic to ceftazidime will also have a sensitivity; elevations of serum aminotransferases, skin rashes

68
Q

Glycopeptide drug

A

vancomycin

69
Q

Glycopeptide MOA

A

bind to D-alanyl-Dalanine terminus of cell wall precursor which prevents linking of peptidoglycans

70
Q

Lipoglycopeptide MOA

A

dimerize and imbed their structure into the bacterial cell membrane, increasing potency of glycopeptide

71
Q

Glycopeptide resistance

A

E. faecium; change in glycopeptide vinding site

72
Q

Glycopeptide spectrum

A

G+ bacteria (including drug resistant strep and enterococci, MRSA)

73
Q

Bacteria resistant to glycopeptides

A

G- bacilli and mycobacterium, Lactobacillus

74
Q

Glycopeptide administration

A

must be thru IV, cannot be absorbed across GI mucosa

75
Q

Glycopeptide AE

A

infusion reactions, nephrotoxicity, hypotension, tachycardia and flushing (Red man syndrome)

76
Q

Beta lactamase inhibitors drugs

A

not antibiotics; clavulanic acid, sulbactam, tazobactam

77
Q

Beta lactamase MOA

A

inhibit beta lactamase

78
Q

Spectrum of Beta lactamase coverage

A

dependent on paired antibiotic such as aminopenicillins and piperacillin

79
Q

Oxazolidinone drugs

A

linezolid

80
Q

Oxazolidinone MOA

A

protein synthesis inhibitor, bind to P site on 50S ribosome

81
Q

Oxazolidinone restriction

A

point mutation on 23S rRNA

82
Q

Oxazolidinone spectrum

A

G+ bacteria, poor coverage of G-

83
Q

Oxazolidinone AE

A

myelosuppression, mitochondrial toxicity, drug-drug interactions

84
Q

Myelosuppression in oxazolidinone AE

A

thrombocytopenia

85
Q

Mitochondrial toxicity in oxazolidinone AE

A

lactic acidosis, optic neuritis, peripheral neuropathy

86
Q

Drug-drug interactions in oxazolidinone AE

A

SSRIs, MAOs–can lead to serotonin syndrome (HA, palpitation, hypertensive crisis)

87
Q

Macrolides that are clinically used

A

erythromycin, clarithromycin, azithromycin, fidaxomicin

88
Q

Macrolides MOA

A

prevents tRNA translocation from A site to P site, inhibits 50S, and conformational protein change

89
Q

Macrolide resistance

A

drug efflux, methylase enzyme production protects ribosome, macrolide degradation, 50S mutations

90
Q

Erythromycin spectrum

A

all gram positive bacilli, some gram negatives (Bartonella, T. pallidum, Neisseria); inactive against most aerobic enteric G- bacilli

91
Q

Azithromycin spectrum

A

M. catarrhalis, Chalmydia spp., B. burgdorferi, H. pylori, H. influenzae

92
Q

Clarithromycin spectrum

A

streptococci, staphylococci, H. influenzae

93
Q

Fidaxomicin spectrum

A

C. difficile

94
Q

Macrolide AE

A

N/V/D, anorexia, epigastric distress, arrhythmias, hepatotoxicity; skin eruptions, eosinophilia, and fever

95
Q

Streptogramin drugs

A

streptogramin A and B

96
Q

Streptogramin MOA

A

inhibit protein synthesis by binding 50S, inhibits elongation and induces early termination

97
Q

Streptogramin resistance

A

enzymatic inactivation, altered binding sites, drug efflux

98
Q

Streptogramin spectrum

A

gram positive cocci, M. pneumoniae, C. pneumoniae, Legionella spp.; NOT G- bacteria, not E. faecium

99
Q

Streptogramin AE

A

pain and arthalgia-myalgia syndrome

100
Q

Tetracycline drugs

A

minocycline, demeclocycline, doxycycline

101
Q

Glycylcycline drug

A

tigecycline

102
Q

Tetra/glycylcycline MOA

A

bind 30S ribosome and prevent tRNA from entering A site, inhibiting protein synthesis

103
Q

Tetra/glycylcycline resistance

A

decrease influx or increase efflux, upregulation of a protein that dislodges tetracyclines, enzymatic inactivation

104
Q

Tetracycline spectrum

A

more active against G+; anaerobes, chlamydiae, mycoplasmas and rickettsiae; MRSA, B. anthracis, L, monocytogenes, V. cholera, Legionella, Plasmodium, T. pallidum

105
Q

Glycylcycline spectrum

A

same activity as tetracyclines but greater activity against enterococci, enterobacteriaceae, Acinetobacter spp., B. fragilis

106
Q

Tetra/Glycylcycline AE

A

GI irritation, pts at increased risk for C. diff, bind well to developing bones and teeth (will develop a permanent brown stain)

107
Q

Aminoglycoside drugs

A

streptomycin, gentamicin, neonmycin, kanamycin

108
Q

Aminoglycoside MOA

A

bind to 30S subunit and act as an irreversible inhibitor (inhibit initiation, continuation of translation, introduction of errors in developing protein)

109
Q

Aminoglycoside resistance

A

enzymatic inactivation, decreased influx, mutations in 30S subunit prevent binding

110
Q

Aminoglycoside spectrum

A

aerobic G- bacteria; Enterobacter spp., E. coli, K. pneumoniae, P. aeruginosa, Serratia spp.

111
Q

Aminoglycoside AE

A

nephrotoxic (Gentamicin, neomicin), ototoxic (Gentamicin and streptomycin cause vestibular damage)

112
Q

Fluoroquinolones drugs

A

norfloxacin, ciprofloxacin, ofloxacin, gatifloxacin

113
Q

Fluoroquinolone MOA

A

inhibit transcription and replication of DNA by binding topoisomerase II

114
Q

Fluoroquinolone resistance

A

mutations in binding region on DNA gyrase, active efflux, or upregulation of proteins that shield DNA gyrase

115
Q

Fluoroquinolone spectrum

A

active against G+ and G-; Campylobacter spp., Enterobacter spp., Shigella, Proteus, E. coli, Legionella, Chlamydia

116
Q

Levofloxacin is a good drug for what bacteria

A

S. pneumon iae

117
Q

Ciprofloxacin is a good drug for what bacteria

A

P. aeruginosa

118
Q

Fluoroquinolone AE

A

GI side effects, increased C. diff risk, tendon rupture, QT prolongation

119
Q

Sulfonamide drug

A

sulfamethoxazole

120
Q

Benzylpyrimidine drug

A

trimethoprim

121
Q

Trimethoprim MOA

A

inhibits dihydrofolate reductase (cannot make purines)

122
Q

Sulfamethoxazole MOA

A

inhibit dihydropteroate synthase, cannot produce folate

123
Q

Sulfamethoxazole resistance

A

bacterial overproduction of PABA, reduced binding to enzyme, decrease influx

124
Q

Trimethoprim resistance

A

reduced bacterial permeability, upregulation of dihydrofolate reductase, reduced binding affinity to enzyme

125
Q

Timethoprim monotherapy

A

can be used to treat UTIs, but combination therapy is more likely

126
Q

TMP/SMX spectrum

A

S. epidermidis, S. aureus, S. pyogenes, Viridians, Serratia, shigella, salmonella, enterobacter, P. mirabilis, Nocardia, P. jiroveci, Haemophilus, M. catarrhalis

127
Q

TMP/SMX AE

A

anemia, leukopenia, granulocytopenia, N/V, photosensitivity, fever, urticaria, Stevens-Johnson syndrome

128
Q

Polymyxin MOA

A

Disrupt G- membrane, bind to and inactivate endotoxin

129
Q

Polymyxin resistance

A

rare, only an issue in some Klebsiella and Acinetobacter spp.

130
Q

Polymyxin spectrum

A

G- bacteria, aerobes; NOT proteus or serratia, neisseria, burkholderia spp.

131
Q

Polymyxin AE

A

nephrotoxicity, slurred speech, vertigo, paresthesia, apnea, muscle weakness

MOD (34 decks)

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