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Pharmacology > Antibiotics > Flashcards

Antibiotics Flashcards

1
Q

which penicillins are penicillinase sensitive (3)

A

penicillin G and V
ampicillin
amoxicillin

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2
Q

which penicillins are penicillinase resistant (3)

A

oxacillin
naficillin
dicloxacillin

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3
Q

mechanism penicillin

A

blocks cross-linking of peptidoglycan by binding penicillin-binding proteins (transpeptidases)

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4
Q

clinical use penicillin (3)

A
  1. gram positive (S. pneumo, S. pyogenes, Actinomyces)
  2. N. meningitidis
  3. Syphillis
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5
Q

is penicillin bactericidal or bacteriostatic?

A

bactericidal

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6
Q

side effects penicillin (2)

A
  1. hypersensitivity

2. hemolytic anemia

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7
Q

mechanism of resistance to penicillin

A

penicillinase (beta-lactamase) cleaves beta-lactam ring

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8
Q

ampicillin / amoxicillin mechanism

A

blocks cross-linking of peptidoglycan by binding penicillin-binding proteins (transpeptidases)

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9
Q

what do you combine ampicillin / amoxicillin with?

A

clavulanic acid (protect against beta-lactamase)

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10
Q

which has greater oral bioavailability, amoxicillin or ampicillin?

A

amoxicillin

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11
Q

which has wider spectrum, penicillin or ampicillin/amoxicillin?

A

ampicillin/amoxicillin

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12
Q

clinical use ampicillin / amoxicillin

A 
H. influenzae
E. coli
Listeria
Proteus
Salmonella
Shigella
Enterococci
(HELPSS kill enterococci)
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13
Q

side effects ampicillin / amoxicillin (2)

A
  1. hypersensitivity

2. pseudomembranous colitis

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14
Q

mechanism of resistance to ampicillin / amoxicillin

A

penicillinase (beta-lactamase) cleaves beta-lactam ring

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15
Q

what are three penicillinase-resistant penicillins?

A
  1. oxacillin
  2. nafcillin
  3. dicloxacillin
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16
Q

mechanism of penicillinase-resitstant penicillins

A

blocks cross-linking of peptidoglycan by binding penicillin-binding proteins (transpeptidases)

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17
Q

which has a wider spectrum, penicillin or penicillinase-resistant penicillins?

A

penicillin

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18
Q

why are penicillinase-resistant penicillins resistant to penicillinase?

A

bulky R group blocks beta-lactamase access to ring

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19
Q

clinical use penicillinase-resistant penicillins

A

S. aureus (except MRSA)

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20
Q

how is MRSA resistant to penicillinase-resistant penicillins?

A

altered penicillin-binding protein target site

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21
Q

side effects penicillinase-resistant penicillins

A
  1. hypersensitivity

2. interstitial nephritis

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22
Q

what two drugs are antipseudomonals?

A
  1. ticarcillin

2. piperacillin

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23
Q

mechanism antipseudomonals

A

blocks cross-linking of peptidoglycan by binding penicillin-binding proteins (transpeptidases)

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24
Q

which has a wider spectrum, penicillin or antipseudomonals?

A

antipseudomonals

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25
Q

clinical use antipseudomonals (2)

A
  1. Pseudomonas

2. gram-negative rods

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26
Q

what do you give antipseudomonals with?

A

beta-lactamase inhibitors (antipseudomonals are susceptible to penicillinase)

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27
Q

side effect antipseudomonals

A

hypersensitivity

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28
Q

what are three beta-lactamase inhibitors?

A
  1. clavulanic acid
  2. sulbactam
  3. tazobactam
    (CAST)
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29
Q

what do beta-lactamase inhibitors do

A

protect penicillin antibiotics from destruction by beta-lactamase (penicillinase)

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30
Q

cephalosporin mechanism

A

beta-lactam drugs –> inhibit cell wall synthesis

less susceptible to penicillinases

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31
Q

are cephalosporins bacteriostatic or bactericidal?

A

bactericidal

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32
Q

organisms not covered by cephalosporins

A 
Listeria
Atypicals (chlamydia, mycoplasma)
MRSA
Enterococci
(LAME)
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33
Q

what cephalosporin covers MRSA?

A

ceftaroline

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34
Q

what are two 1st generation cephalosporins?

A
  1. cefazolin

2. cephalexin

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35
Q

what are three 2nd generation cephalosporins?

A
  1. cefoxitin
  2. cefaclor
  3. cefuroxime
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36
Q

what are three 3rd generation cephalosporins?

A
  1. ceftriaxone
  2. cefotaxime
  3. ceftazidime
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37
Q

what is one 4th generation cephalosporin?

A

cefepime

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38
Q

what is one 5th generation cephalosporin?

A

ceftaroline

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39
Q

clinical use 1st generation cephalosporins (5)

A
  1. gram positive cocci
  2. Proteus
  3. E. coli
  4. Klebsiella
  5. prior to surgery to prevent S. aureus wound infections
    PEcK
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40
Q

clinical use 2nd generation cephalosporins (7)

A
  1. H. influenzae
  2. Enterobacter
  3. Neisseria
  4. Proteus
  5. E. coli
  6. Klebsiella
  7. Serratia
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41
Q

clinical use 3rd generation cephalosporins

A

serious gram-negative infections (resistant to other things

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42
Q

clinical use ceftriaxone (2)

A
  1. meningitis

2. gonorrhea

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43
Q

clinical use ceftazidime

A

Pseudomonas

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44
Q

clinical use 4th generation cephalosporins

A
  1. greater activity against Pseudomonas

2. greater activity against gram positive

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45
Q

clinical use 5th generation cephalosporins

A

broad coverage, including MRSA

does NOT cover Pseudomonas

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46
Q

side effects cephalosporins

A
  1. hypersensitivity
  2. vitamin K deficiency
  3. increases nephrotoxicity of aminoglycosides
    (low cross-reactivity with penicillins
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47
Q

mechanism aztreonam

A

prevents peptidoglycan cross-linking by binding penicillin-binding protein 3
–> resistant to beta-lactamases

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48
Q

does aztreonam have any cross-allergenicity with penicillins?

A

NO!!!

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49
Q

what other antibiotic is aztreonam synergistic with?

A

aminoglycosides

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50
Q

what two groups of people is it useful to use aztreonam for?

A
  1. penicillin allergies

2. renal insufficiency who can’t use aminoglycosides

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51
Q

is aztreonam susceptible to beta-lactamases?

A

NO!!

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52
Q

clinical use aztreonam

A

ONLY gram negative rods

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53
Q

side effect aztreonam

A

GI upset

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54
Q

what are four carbapenems?

A
  1. imipenem
  2. meropenem
  3. ertapenem
  4. doripenem
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55
Q

mechanism imipenem

A

broad-spectrum, beta-lactamase resistant carbapenem

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56
Q

what do you administer imipenem with?

A

cilastatin (inhibits renal dehydropeptidase I to decrease inactivation of drug in renal tubules)

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57
Q

what is cilastatin?

A

inhibits renal dehydropeptidase I to decrease inactivation of imipenem in renal tubules

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58
Q

clinical use carbapenems (3)

A
  1. gram-positive cocci
  2. gram-negative rods
  3. anaerobes
    ONLY use in life-threatening infections b/c of side effects
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59
Q

which carbapenem has a decreased risk of seizures

A

meropenem

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60
Q

side effects carbapenems (3)

A
  1. GI distress
  2. rash
  3. CNS toxicity (seizures)
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61
Q

vancomycin mechanism

A

inhibits cell wall peptidoglycan formation by binding D-ala D-ala

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62
Q

is vancomycin bacteriostatic or bactericidal?

A

bactericidal

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63
Q

clinical use vancomycin

A

gram-positive ONLY

use for multidrug-resistant organisms (i.e. MRSA, enterococci, and C. difficile)

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64
Q

how do you administer vancomycin to treat pseudomembranous colitis?

A

oral

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65
Q

side effects vancomycin (4)

A
  1. Nephrotoxicity
  2. Ototoxicity
  3. Thrombophlebitis
    NOT
  4. red man syndrome
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66
Q

what drug causes red man syndrome

A

vancomycin

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67
Q

how do you prevent red man syndrome

A

pretreatment with antihistamines

slow infusion rate

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68
Q

mechanism of resistance to vancomycin

A

modification of D-ala D-ala to D-ala D-lac in cell wall precursors

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69
Q

what protein synthesis inhibitors act on the 30S subunit?

A

Aminoglycosides

Tetracyclines

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70
Q

are aminoglycosides bacteriostatic or bactericidal?

A

bactericidal

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71
Q

are tetracyclines bacteriostatic or bactericidal?

A

bacteriostatic

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72
Q

what protein synthesis inhibitors act on the 50S subunit?

A

Chloramphenicol
Clindamycin
Erythromycin (macrolides)
Linezolid

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73
Q

is chloramphenicol bacteriostatic or bactericidal?

A

bacteriostatic

74
Q

is clindamycin bacteriostatic or bactericidal?

A

bacteriostatic

75
Q

is erythromycin bacteriostatic or bactericidal?

A

bacteriostatic

76
Q

what are five aminoglycosides?

A
  1. Gentamicin
  2. Neomycin
  3. Amikacin
  4. Tobramycin
  5. Streptomycin
    GNATS
77
Q

mechanism aminoglycosides

A

inhibit formation of initiation complex
cause misreading of mRNA
block translocation

78
Q

are aminoglycosides useful against anaerobes?

A

NO!!

require O2 for uptake into cells

79
Q

are aminoglycosides bacteriostatic or bactericidal?

A

bactericidal

80
Q

clinical use aminoglycosides

A

severe gram-negative rods

81
Q

what are aminoglycosides synergistic with?

A

beta-lactam antibiotics

82
Q

what drug is useful for bowel surgery?

A

neomycin

83
Q

side effects aminoglycosides (4)

A
  1. Nephrotoxicity (esp. if use with cephalosporins)
  2. Neuromuscular blockade
  3. Ototoxicity (esp. if use with loop diuretics)
  4. Teratogen
84
Q

mechanism of resistance to aminoglycosides

A

bacterial transferase enzymes inactivate the drug (via acetylation, phosphorylation, or adenylation)

85
Q

what are three tetracyclines?

A
  1. tetracycline
  2. doxycycline
  3. minocycline
86
Q

are tetracyclines bacteriostatic or bactericidal?

A

bacteriostatic

87
Q

mechanism tetracyclines

A

prevent attachment of aminoacyl-tRNA

88
Q

do tetracyclines enter the CNS well?

A

NO!!!

89
Q

what type of patients is doxycycline useful for?

A

renal failure (doxycycline is fecally eliminated)

90
Q

what should you not eat when taking tetracyclines?

A

milk (Ca), antacids (Ca or Mg), or iron-containing preparations
divalent cations inhibit tetracycline absorption from gut

91
Q

clinical use tetracyclines (3)

A
  1. Borrelia burgdorferi
  2. M. pneumoniae
  3. Chylamydia and Rickettsia (accumulates intracellularly)
92
Q

side effects tetracyclines (3)

A
  1. GI distress
  2. discoloration of teeth and inhibition of bone growth in children
  3. photosensitivity
93
Q

who are tetracyclines contraindicated in?

A

pregnancy

94
Q

mechanism of resistance to tetracyclines

A

decrease uptake or increase efflux out of bacterial cells by plasmid-encoded transport pumps

95
Q

how is resistance to tetracyclines encoded?

A

plasmid

96
Q

what are three macrolides

A
  1. azithromycin
  2. clarithromycin
  3. erythromycin
97
Q

mechanism macrolides

A

block translocation

bind to the 23S rRNA of the 50S ribosomal subunit

98
Q

are macrolides bacteriostatic or bactericidal?

A

bacteriostatic

99
Q

clinical use macrolides (3)

A
  1. atypical pneumonia (Mycoplasma, Chlamydia, Legionella)
  2. STDs (Chlamydia)
  3. gram-positive cocci (strep in pts allergic to penicillin)
100
Q

side effects macrolides (5)

A
  1. GI Motility issues
  2. Arrhythmias (prolonged QT
  3. acute Cholestatic hepatitis
  4. Rash
  5. eOsinophilian
    MACRO
101
Q

what do macrolides increase the serum concentration of?

A

theophyllines (oral anticoagulants)

102
Q

mechanism of resistance to macrolides

A

mehylation of 23S rRNA binding site

103
Q

mechanism chloramphenicol

A

blocks peptidyltransferase

104
Q

is chloramphenicol bacteriostatic or bactericidal?

A

bacteriostatic

105
Q

clinical use chloramphenicol (2)

A
  1. meningitis (H. influenzae, N. meningitidis, S. pneumo)

2. Rocky Mountain spotted fever

106
Q

where is chloramphenicol used?

A

developing countries (side effects)

107
Q

side effects chloramphenicol

A
  1. anemia (dose dependent)
  2. aplastic anemia (dose independent)
  3. gray baby syndrome (premature babies lack liver UDP-glucoronyl transferase)
108
Q

can you use chloramphenicol in premature babies?

A

NO!!

gray baby syndrome (premature babies lack liver UDP-glucoronyl transferase)

109
Q

mechanism of resistance to chloramphenicol

A

plasmid-encoded acetyltransferase inactivates the drug

110
Q

how is resistance to chloramphenicol encoded?

A

plasmid

111
Q

mechanism clindamycin

A

blocks peptide transfer (translocation)

112
Q

is clindamycin bacteriostatic or bactericidal?

A

bacteriostatic

113
Q

clinical use clindamycin (2)

A
  1. anaerobic infections (i.e. Bacteroides, Clostridium perfringens)
    1a. aspiration pneumonia
    1b. lung abscesses
    1c. oral infections
  2. invasive group A strep
114
Q

which part of the body do you treat anaerobes with clindamycin?

A

above the diaphragm

115
Q

which part of the body do you treat anaerobes with metronidazole?

A

below the diaphragm

116
Q

side effects clindamycin (3)

A
  1. pseudomembranous colitis (C. difficile)
  2. fever
  3. diarrhea
117
Q

mechanism sulfonamides

A

inhibit folate synthesis

PABA antimetabolites inhibit dihydropteroate synthase

118
Q

are sulfonamides bacteriostatic or bactericidal?

A

bacteriostatic

119
Q

clinical use sulfonamides

A
  1. gram positive
  2. gram negative
  3. Nocardia
  4. Chlamydia
  5. simple UTI (triple sulfas or SMX)
120
Q

side effects sulfonamides

A
  1. hypersensitivity
  2. hemolysis if G6PD deficient
  3. nephrotoxicity (tubulointerstitial nephritis)
  4. photosensitivity
  5. kernicterus in infants
121
Q

what do sulfonamides do to other drugs?

A

displaces other drugs from albumin (i.e. warfarin)

122
Q

see person take an antibiotic and then get hemolysis, think….

A

sulfonamides in a G6PD deficient person!

123
Q

mechanism of resistance to sulfonamides

A

altered enzyme (bacterial dihydropteroate synthase)
decreased uptake
increased PABA synthesis

124
Q

mechanism trimethoprim

A

inhibits bacterial dihydrofolate reductase

125
Q

is trimethoprim bacteriostatic or bactericidal?

A

bacteriostatic

126
Q

how do you sequentially block folate synthesis?

A

trimethoprim in combo with sulfonamides (TMP-SMX)

127
Q

clinical use TMP-SMX

A
  1. UTIs
  2. Shigella
  3. Salmonella
  4. Pneumocystic jirovecii pneumonia
  5. toxoplasmosis prophylaxis
128
Q

side effects trimethoprim

A
  1. megaloblastic anemia
  2. leukopenia
  3. granulocytopenia
    - -> may alleviate with folic acid
129
Q

what are some fluoroquinolones?

A 
-oxacin
ciprofloxacin
norfloxacin
levofloxacin
ofloxacin
sparfloxacin
moxifloxacin
gemifloxacin
enoxacin
130
Q

what drug is a quinolone?

A

nalidixic acid

131
Q

mechanism fluoroquinolones

A

inhibit DNA gyrase (topoisomerase II) and topoisomerase IV

132
Q

are fluoroquinolones bacteriostatic or bactericidal?

A

bactericidal

133
Q

what should you not take with fluoroquinolones?

A

antacids

134
Q

what two drugs would you not take with antacids?

A
  1. fluoroquinolones

2. tetracycline

135
Q

clinical use fluoroquinolones (3)

A
  1. gram negative rods of urinary and GI tracts (including Pseudomonas)
  2. Neisseria
  3. some gram positive
136
Q

side effects fluoroquinolones (7)

A
  1. GI upset
  2. superinfections
  3. rash
  4. headache, dizziness
  5. tendonitis/tendon rupture (esp. in >60 or pts on prednisone)
  6. leg cramps and myalgias
  7. prolonged QT
137
Q

who are fluoroquinolones contraindicated in?

A

pregnant women
nursing mothers
children < 18 (damage to cartilage)

138
Q

who are at risk of tendon rupture on fluoroquinolones?

A

pts > 60

pts taking prednisone

139
Q

mechanism of resistance to fluoroquinolones

A

chromosome-encoded mutation in DNA gyrase
plasmid-mediated resistance
efflux pumps

140
Q

how is resistance to fluoroquinolones encoded?

A

chromosome and plasmids

141
Q

mechanism metronidazole

A

forms free radical toxic metabolites in the bacterial cell –> damages DNA

142
Q

is metronidazole bacteriostatic or bactericidal?

A

bactericidal

143
Q

clinical use metronidazole

A
  1. Giardia
  2. Entamoeba
  3. Trichomonas
  4. Gardnerella vaginalis
  5. anaerobes (Bacteroides, C. difficile)
  6. H. pylori
    GET GAP
144
Q

what is triple therapy for H. pylori

A
  1. metronidazole
  2. proton pump inhibitor
  3. clarithromycin
145
Q

what is M. tuberculosis prophylaxis?

A

isoniazid

146
Q

what is M. avium-intracellulare prophylaxis?

A

azithromycin, rifabutin

147
Q

what is M. tuberculosis treatment?

A 
Rifampin
Isoniazid
Pyrazinamide
Ethambutol
RIPE
148
Q

what is M. avium-intracellulare treatment?

A

azithromycin OR clarithromycin + ethambutol

can add rifabutin or ciprofloxacin

149
Q

what is M. leprae treatment (tuberculoid)?

A

long-term dapsone and rifampin

150
Q

what is M. leprae treatment (lepromatous)?

A

long-term dapsone and rifampin PLUS clofazimine

151
Q

mechanism isoniazid

A

decrease synthesis of mycolic acids

bacterial catalase-peroxidase (encoded by KatG) needed to convert INH to active metabolite

152
Q

what is needed to activate isoniazid?

A

bacterial catalase-peroxidase (encoded by KatG) needed to convert INH to active metabolite

153
Q

clinical use isoniazid

A

M. tuberculosis

154
Q

how does INH half-life vary?

A

different in fast vs. slow acetylators

155
Q

side effects isoniazid

A
  1. neurotoxicity
  2. hepatotoxicity
  3. lupus
    INH Injures Neurons and Hepatocytes
156
Q

how can you prevent neurotoxicity and lupus from isoniazid?

A

pyridoxine (vitamin B6)

157
Q

what are two rifamycins?

A
  1. rifampin

2. rifabutin

158
Q

mechanism rifamycins

A

inhibits DNA-dependent RNA polymerase

159
Q

clinical use rifamycins (3)

A
  1. M. tuberculosis
  2. M. leprae (delays resistance to dapsone)
  3. prophylaxis in meningococcus and contacts of kids with H. influenzae type B
160
Q

side effects rifamycins

A
  1. minor hepatotoxicity
  2. induces P450
  3. orange body fluids
    rapid resistance if used alone!
161
Q

which rifamycin is better to use in patients with HIV?

A

rifabutin (better than rifampin) because less cytochrome P450 stimulation

162
Q

mechanism pyrazinamide

A

uncertain
may acidify intracellular environment via conversion to pyrazinoic acid
effective in acidic pH of phagolysosomes (where TB eaten by macrophages is)

163
Q

clinical use pyrazinamide

A

M. tuberculosis

164
Q

side effects pyrazinamide (2)

A
  1. hyperuricemia

2. hepatotoxicity

165
Q

mechanism ethambutol

A

decrease carbohydrate polymerization of mycobacterium cell wall by blocking arabinosyltransferase

166
Q

clinical use ethambutol

A

M. tuberculosis

167
Q

side effect ethambutol

A

optic neuropathy (red-green color blindness)

168
Q

prophylaxis for endocarditis with surgical or dental procedures

A

penicillins

169
Q

prophylaxis for gonorrhea

A

ceftriaxone

170
Q

prophylaxis for history of recurrent UTIs

A

TMP-SMX

171
Q

prophylaxis for meningococcal infection

A

ciprofloxacin (drug of choice)

rifampin (children)

172
Q

prophylaxis for pregnant women with group B strep

A

ampicillin

173
Q

prophylaxis for prevention of gonococcal or chlamydial conjunctivitis in newborn

A

erythromycin ointment

174
Q

prophylaxis for prevention of postsurgical infection due to S. aureus

A

cefazolin

175
Q

prophylaxis for strep pharyngitis in child with prior rheumatic fever

A

oral penicillin

176
Q

prophylaxis for syphilis

A

benzathine penicillin G

177
Q

prophylaxis for CD4 < 200

A

TMP-SMX (to prevent Pneumocystis pneumonia)

178
Q

prophylaxis for CD4 < 100

A

TMP-SMX (to prevent Pneumocystis pneumonia and toxoplasmosis)

179
Q

prophylaxis for CD4 < 50

A

azithromycin (to protect against M. avium)

180
Q

MRSA treatment (5)

A
  1. vancomycin
  2. daptomycin
  3. linezolid (can cause serotonin syndrome)
  4. tigecycline
  5. ceftaroline
181
Q

VRE treatment (2)

A
  1. linezolid

2. streptogramins (quinupristin/dalfopristin)

Pharmacology (8 decks)

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