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antibacterials Flashcards

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1
Q

folic acid synthesis and reduction

A

DNA methylation,

PABA inhibitors: sulfonamides,
DHF inhibitor: trimethoprim

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2
Q

peptidoglycan synthesis inhibitors

A

glycopeptides ( vancomycin, bacitracin)

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3
Q

peptidoglycan x-link inhibitors

A

pencillinase-sensitive, pencillinase-resistant, antipseudomonals, cephalosporin (I-V), Carbapenems, Monobactams

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4
Q

Pencillinase sensitive

A

pencillin G,V; ampicillin; amoxicillin

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5
Q

penicillinase resistant

A

oxacillin, nafacillin, dicloxacillin

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6
Q

antipseudomonals

A

ticarcillin, pipercillin

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7
Q

cephalosporin I

A

cefazolin

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8
Q

cephalosporin II

A

cefoxitin

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9
Q

cephalosporin III

A

ceftriaxone

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10
Q

cephalosporin IV

A

cefepime

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11
Q

cephalosporin V

A

ceftaroline

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12
Q

Carbapenems

A

imipenem, meripenem, ertapenem, doripenem,

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13
Q

monobactam

A

aztreonam

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14
Q

DNA integrity inhibitor (via free radicals)

A

metronidazole

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15
Q

mRNA synthesis inhibitor (via RNA polymerase)

A

rifampin

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16
Q

DNA gyrase inhibitor

A

FQN, quinolone

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17
Q

FQN

A

ciprofloxacin, levofloxacin

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18
Q

quinolone

A

nalidixic acid

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19
Q

50s protein synthesis inhibitors

A

chloramphenicol, clindamycin, linezolid, macrolides, streptogramins

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20
Q

macrolides

A

azmycin, cymcin, emycin

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21
Q

streptogramins

A

quinupristin, dalfopristin

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22
Q

30s subunit inhibitors

A

aminoglycosides, tetracyclines

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23
Q

aminoglycosides

A

gentamicin, neomycin, amikacin, tobramycin, streptomycin

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24
Q

PCN G/V mechanism

A

D-ala-D-ala structural analog. Binds PBP.

blocks PBP xlink of peptidoglycan in cell wall.

activates autolytic enzymes

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25
Q

PCN G/V use

A

G+ organisms, syphilis and gonorrhea

bacteriocidal

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26
Q

PCN G/V ADR

A

hypersensitivity rxns, direct Coombs + hemolytic anemia

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27
Q

PCN G/V resistance

A

pencillinase in bacteria cleaves b-lactam ring

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28
Q

penicillinase-resistant PCN MOA

A

same as PCN; narrow spectrum

pencillinase resistant b/c bulky R group blocks access of B-lactamases

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29
Q

penicillinase-resistant PCN use

A

MSSA

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30
Q

penicillinase-resistant PCN ADR

A

hypersensitivity rxns, interstitial nephritis

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31
Q

penicillinase-sensitive PCN MOA

A

same as PCN, wider spectrum

pencillinase sensitive. also combine with clavulanic acid to protect against destruction by b-lactamase

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32
Q

penicillinase-sensitive PCN use

A

extended-spectrum pencillin

H. influenzae, H pylori, E. coli, listeria monocytogenes, Proteus mirabilis, salmonella, shigella, enterococci

“Ampicillin/amoxicillin HHELPSS kill enterococci”

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33
Q

penicillinase-sensitive PCN ADR

A

pseudomembranous colitis, rash, hypersensitivity rxns

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34
Q

penicillinase-sensitive PCN mechanism of resistance

A

penicillinase in bacteria cleaves b-lactam ring

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35
Q

antipseudomonal PCN MOA

A

same as pcn, extended specturm

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36
Q

antipseudomonal PCN ADR

A

pseudomonas, gram - rods

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37
Q

antipseudomonal PCN codrug

A

susceptible to penicillinase. need B-lactamase inhibitors

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38
Q

antipseudomonal PCN ADR

A

hypersensitivity rxns

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39
Q

B-lactamase inhibitors

A

clavulanic acid, sulbactam, tazobactam

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40
Q

cephalosporin MOA

A

b-lactam drugs that inhibit cell wall synthesis, but are less susceptible to penicillinase

bactericidal

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41
Q

organisms not covered by 1-4 generation

A

(“Lame”)

Listeria, Atypicals (chlamydia, mycoplasma), MRSA, and Enterococci

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42
Q

1st generation cephalosporin use

A

cefazolin, cephalexin

gram + cocci; PEK

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43
Q

Cefazolin surgical use

A

prophylaxis to prevent S aureus wound infections

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44
Q

2nd generation cephalosporin use

A

cefaclor, cefoxitin, cefuroxime (“Fake fox fur”)

gram + cocci; HENS PEK

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45
Q

HENS

A

H influenzae, Enterobacter aerogenes, Neisseria, Serratia

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46
Q

PEK

A

proteus mirabilis, E coli, Klebsiella pneumoniae

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47
Q

3rd generation cephalosporin use

A

ceftriaxone, cefotaxime, ceftazidime

serious gram - infections resistant to other B-lactams

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48
Q

Ceftriaxone use

A

meningitis, gonorrhea, disseminated Lyme disease

49
Q

Ceftazidime use

A

pseudomonas

50
Q

4th generation cephalosporin use

A

cefepime

gram - organisms, inc activity against Pseudomonas and gram + organisms

51
Q

5th generation cephalosporin use

A

ceftaroline

broad +/- coverage, including MRSA; no pseudomonas

52
Q

cephalosporin ADR

A

hypersensitivity rxns, autoimmune hemolytic anemia, disulfiram-like rxn, vitamin K deficiency.

53
Q

cephalosporin drug interactions

A

exhibit x-rxn with PCN

inc nephrotoxicity with aminoglycosides

54
Q

cephalosporins mechanism of resistance

A

structural changes in PBP

55
Q

Imipenem (carbapenems) MOA

A

broad-spectrum, B-lactamase-resistant.

always administered with cilastatin to decrease inactivation of drug in renal tubules

56
Q

imipenem use

A

G+ cocci, G - rods, and anaerobes.

wide spectrum, but significant ADR limit use

57
Q

meropenem

A

dec risk of seizures and is stable to dehydropeptidase I

58
Q

carbapenem adr

A

GI distress, skin rash, seizures at high plasma levels

59
Q

monobactams MOA

A

prevents peptidoglycan x-linking by binding to PBP 3. synergistic w/ aminoglycosides.

no cross allergenicity w/ PCN

60
Q

monobactam use

A

G- only

used in PCN allergic pts, and those with renal insufficiency

61
Q

vancomycin MOA

A

inhibits cell wall peptidoglycan formation by binding to D-ala-D-ala precursor.

Bacteriocidal (except C. Diff –> bacteriostatic)

62
Q

vanc use

A

gram + only

63
Q

vanc ADR

A

red man sx; nephrotoxicity, ototoxicity, thrombophlebitis

64
Q

vanc resistance

A

bacteria change walls to d-ala-d-lac

65
Q

protein synthesis inhibitors

A

specifically target smaller bacterial ribosome (70s, made of 30s and 50s), leaving human ribosomes unaffected

66
Q

30s inhibitors

A

aminoglycosides (bactericidal); tetracyclines (bacteriostatic)

67
Q

50s inhibitors

A

Chloramphenicol, Clindamycin (bacteriostatic)
Erythromycin (bacteriostatic)
Linezolid (variable)

68
Q

protein synthesis inhibitors mnemonic

A

Buy AT 30, CCEL at 50

69
Q

aminoglycosides MOA

A

bactericidal;

irrev. inhibition of initiation complex thru binding of 30s subunit.

Can cause misreading of mRNA; block translocation.

Require O2 for uptake–>INACTIVE AGAINST ANAEROBES

70
Q

aminoglycosides use

A

severe G- rod infections. synergistic w/ b-lactam abx

71
Q

neomycin

A

prophylaxis for bowel surgery

72
Q

aminoglycoside ADR

A

nephrotoxicity, neuromuscular blockade, ototoxicity

teratogen

73
Q

aminoglycoside method of resistance

A

bacterial transferase enzymes inactivate drug by acetylation, phosphorylation, or adenylation

74
Q

tetracyclines

A

(bacteriostatic) bind 30s and prevent attachment of aminoacyl-tRNA;

limited CNS penetration

75
Q

Doxycycline pts

A

can be used in pts with renal failure due to fecal elimination

76
Q

Tetracycline drug interactions

A

milk, antacids, iron preparations b/c divalent cations inhibit drugs absorption in drugs

77
Q

tetracycline use

A

Borrelia burgdorferi, M pneumoniae

accumulates intracellularly –> Rickettsia, Chlamydia

acne tx

78
Q

tetracycline ADR

A

discoloration of teeth and inhibition of bone growth in children

photosensitivity

contraindicated in pregnancy

79
Q

Chloramphenicol MOA

A

blocks peptidyltransferase at 50s (bacteriostatic)

80
Q

Chloramphenicol use

A

Meningitis, Rocky mounted spotted fever

81
Q

chloramphenicol ADR

A

anemia, aplastic anemia, *gray baby syndrome

82
Q

gray baby sx cause

A

premie infants bc lack liver UDP-glucuronyl transferase

83
Q

Chloramphenicol mech. of resistance

A

plasmid-encoded acetyltransferase inactivates drug

84
Q

Clindamycin MOA

A

blocks peptide transfer (translocation) at 50s (bacteriostatic)

85
Q

Clindamycin use

A

anaerobic infections (aspiration pneumonia, lung abscesses, oral infections)

invasive GAS infection

86
Q

Clindamycin versus metronidazole

A

clindamycin treats ABOVE diaphragm

metronidazole BELOW diaphragm

87
Q

Clindamycin ADR

A

pseudomembranous colitis, fever, diarrhea

88
Q

Linezolid MOA

A

inhibit protein synthesis by binding 50s and preventing formation of initiation complex

89
Q

Linezolid use

A

G+ including MRSA and VRE

90
Q

Linezolid ADR

A

bone marrow suppression (thrombocytopenia); peripheral neuropathy; serotonin syndrome

91
Q

linezolid mech of resistance

A

pt mutation of ribosomal RNA

92
Q

macrolides MOA

A

inhibit protein synthesis by blocking translocation; bind to 23s rRNA of 50s (bacteriostatic)

93
Q

macrolides use

A

atypical pneumonia (Mycoplasma, Chlamydia, Legionella), STIs (chlamydia), gram + cocci, B pertussis

94
Q

Macrolides ADR

A

GI motility issue; arrhythmia (prolonged QT interval); acute cholestatic hepatitis; rash; eosinophilia

95
Q

Macrolides drug interactions

A

increases serum concentration of theophylline, oral anticoag.

Clarithromycin and emycin inhibit cyp450

96
Q

Macrolides mechanism of resistance

A

methylation of 23S rRNA-binding site prevents binding of drug

97
Q

Sulfonamides MOA

A

inhibit dihydropteroate synthesis, thus inhibiting folate synthesis (bacteriostatic)

98
Q

when does sulfonamide become bacteriocidal?

A

combined with trimethoprim

99
Q

sulfonamide use

A

G+/-, nocardia, chlamydia

100
Q

SMX use

A

simple UTI

101
Q

Sulfonamide mech of resistance

A

altered enzyme (bacterial dihydropteroate synthase), dec uptake, inc PABA synthesis

102
Q

Dapsone MOA

A

similar to sulfonamides, but structurally distinct agent

103
Q

Dapsone use

A

leprosy, pneumocystis jirovecii prophylaxis

104
Q

Dapsone ADR

A

hemolysis if G6PD deficient

105
Q

Trimethoprim MOA

A

inhibits bacterial dihydrofolate reductase (bacteriostatic)

106
Q

Trimethoprim use

A

used in combo with SMX, causing sequential block of folate synthesis

combo tx: UTI, shigella, salmonella, pneumocystis tx and prophylaxis, toxo prophylaxis

107
Q

trimethoprim ADR

A

megaloblastic anemia, leukopenia, granulocytopenia

108
Q

FQN MOA

A

inhibit prokaryotic enzymes Topoisomerase II (dna gyrase) and topoisomerase IV. (bacteriocidal)

109
Q

FQN drug interaction

A

CANT use antacids

110
Q

FQN use

A

G - rods of urinary and GI tracts, Neisseria, some + positive organisms

111
Q

FQN ADR

A

contraindicated in pregnant women, nursing mothers, and kids under18 for cartilage damage

tendonitis in 60+ and in pts taking pred

112
Q

FQN mechanism of resistance

A

Chromosome-encoded mutation in DNA gyrase, plasmid-mediated resistance, efflux pumps.

113
Q

Daptomycin MOA

A

lipopeptide that disrupts cell membrane of gram + cocci

114
Q

daptomycin use

A

MRSA skin infections, bacteremiam endocarditis, VRE

115
Q

Daptomycin cant be used in what dx?

A

pneumonia, inactivated by surfactant

116
Q

Daptomycin ADR

A

myopathy, rhabdomyolysis

117
Q

Metronidazole use

A

forms toxic free radical metabolites in the bacterial cell that damage DNA. (bactericidal, antiprotozoal)

118
Q

Metronidazole use

A

Tx Giardia, Entamoeba, Trichomonas, Gardnerella vaginalis, anaerobes (Bacteroides, C diff).

Used with PPI and clarithromycin for triple therapy against H pylori

119
Q

Metronidazole ADR

A

disulfiram-like rxn (severe flushing, tachycardia, hypotension)

HA, metallic taste

step 1 microbiology (7 decks)

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