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Cephalosporins Flashcards

1
Q

Cephalosporin nucleus

A

beta-lactam ring linked to a dihydrothiazine ring

4 ring then 6 ring with a sulfur in the 6 ring

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2
Q

C3 alterations

A

change pharmacokinetics

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3
Q

C7 alterations

A

change spectrum of activity

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4
Q

Cephalosporins MOA:

A

interfere with transpeptidase PBP which disrupts the cross linking which also weakens cell wall and initiates lytic cycle

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5
Q

Cephalosporins are bactericidal/bacteriostatic

A

bactericidal

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6
Q

Bactericidal activity of cephalosporins depends on

A

duration of time that free drug levels exceed MIC

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7
Q

Cephalosporins have the ____ % time> MIC requirement

A

longest; needs to be 60-70 %

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8
Q

General rule for cephalosporin activity in terms of this order and gram + and gram -

cefazolin 1st
cefuroxime 2nd
ceftriaxone 3rd
cefepime 4th
ceftaroline anti MRSA
A

gram + : activity decreases as you go down but increases for ceftaroline so it has 2 triangles touching each other at the tips where cefepime is

gram - : increase as you go down the list and tapers off at ceftaroline, it looks like a stiletto shaped nail

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9
Q

First generation cephalosporins include:

A

cefazolin, cephalexin, cefadroxil

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10
Q

Cefazolin oral absorption:

A

poor IV only

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11
Q

Cefazolin 1/2 life

A

short but the longest in terms of 1st gen cephalosporins

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12
Q

Cefazolin eliminination

A

renal

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13
Q

Cephalexin oral absorption

A

high

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14
Q

Cephalexin 1/2 life

A

short

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15
Q

Cephalexin elimination

A

renal

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16
Q

Cefadroxil oral absorption

A

high

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17
Q

Cefadroxil 1/2 life

A

short

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18
Q

Cefadroxil elimination

A

renal

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19
Q

1st Generation tissue penetration

A

skin
bone/joint
urine
lung-variable

CSF is POOR due to active efflux from BBB

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20
Q

1st Generation spectrum coverage

A

dark purple: streptococcus, viridans, MSSA/MSSE
dark red: E. coli, klebsiella, p. mirabilis
light red: Neisseria
anaerobes: +/- (just oral)

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21
Q

Important: Cephalosporins do not cover which organism?

A

enterococcus

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22
Q

1st Generation indications

A 
skin/skin structure infections (MSSA, s. pyogenes/s. agalactiae)
UTI (E. coli)
surgical prophylaxis (cefazolin)

definitive therapy for MSSA

  • endocarditis
  • osteomyelitis
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23
Q

Second generation cephalosporins include:

A

cefprozil, cefaclor, cefuroxime, cefotetan, cefoxitin

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24
Q

Second generation cephalosporins used for respiratory infections:

A

cefprozil, cefaclor, cefuroxime

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25
Cefprozil oral absorption
high
26
Cefprozil 1/2 life
short
27
Cefprozil elimination
35-45 %
28
Cefaclor oral absorption
high
29
Cefaclor 1/2 life
short
30
Cefaclor elimination
70% renal
31
Cefuroxime oral absorption
52% (axetil)
32
Cefuroxime 1/2 life
short
33
Cefuroxime elimination
90% renal
34
Second generation cephalosporins that are cephamycins
cefotetan and cefoxitin
35
Cefotetan oral absorption
poor IV only
36
Cefotetan 1/2 life
longer 3.5 hrs
37
Cefotetan elimination
75% renal
38
Cefoxitin oral absorption
poor IV only
39
Cefoxitin 1/2 life
short
40
Cefoxitin elimination
80% renal
41
2nd Generation tissue penetration
``` skin bone/joint urine respiratory intra-ab ``` CSF is variable- cefuroxime IV penetrates but is clinicaly inferior to ceftriaxone/cefotaxime for meningitis
42
2nd Generation spectrum coverage for respiratory
dark purple: streptococcus, s. pneumoniae, viridans, MSSA/MSSE dark red: h. influenzae, m. catarrhalis, E. coli, klebsiella, p. mirabilis light red: Neisseria, morganella anaerobes: +/- (just oral)
43
2nd Generation spectrum coverage for cephamycins
dark purple: streptococcus, s. pneumoniae, viridans, MSSA/MSSE dark red: h. influenzae, m. catarrhalis, E. coli, klebsiella, p. mirabilis light red: Neisseria, morganella anaerobes: + active against most but some resistance found in b. fragilis
44
2nd Generation cephalosporin indications
upper and lower respiratory infections otitis media UTI cephamycins: intra-ab infections mycobacterial infections (cefoxitin) surgical prophylaxis
45
Third Generation cephalosporins include
cefixime, cefdinir, cefpodoxime, ceftriaxone, cefotaxime
46
Cefixime oral absorption
50% so fair
47
Cefixime 1/2 life
longer 3-4 hours
48
Cefixime elimination
35-45% renal
49
Cefdinir oral absorption
21% poor
50
Cefdinir 1/2 life
short
51
Cefdinir elimination
20% renal
52
Cefpodoxime oral absorption
50% so fair
53
Cefpodoxime 1/2 life
short
54
Cefpodoxime elimination
30% renal
55
Ceftriaxone oral absorption
none IV only
56
Ceftriaxone 1/2 life
long 8.5 hours
57
Ceftriaxone elimination
30-65% renal
58
Cefotaxime oral absorption
none IV only
59
Cefotaxime 1/2 life
short
60
Cefotaxime elimination
60% renal
61
3rd Generation cephalosporin tissue penetration
``` skin bone/joint urine respiratory intra-ab CNS ```
62
3rd Generation cephalosporin spectrum coverage
dark purple: streptococcus, s. pneumoniae, viridans light purple: MSSA/MSSE dark red: Neisseria, h. influenzae, m. catarrhalis, E. coli, klebsiella, p. mirabilis, morganella light red: eneterbacter, citrobacter, serratia (all 3 of these induce AmpC and led to ESBL) anaerobes: +/- (oral only) Misc: no activity against ESBL, poor activity against AmpC
63
3rd Generation cephalosporin indications
``` upper and lower respiratory infections otitis media UTI CNS intra-ab infections skin and soft tissue infections bone and joint infections ```
64
Common dosing for meningitis using ceftriaxone
1-2 gm IV q12h
65
Common resistance for cephalosporins
AmpC beta-lactamases - encoded on chromosomes of enterobacteriaceae and P. aeruginosa - inducible by enterobacter - resistance observed to all 3 generations ESBL - e.coli and klebsiella - resistance observed to all 3 generations Altered target binding in gram positive cocci
66
Adverse events for cephalosporins
``` CNS with 3rd gen GI hyperbilirubinemia renal skin anaphylaxis cross reactivity with PCN allergy hematologic disulfiram reaction ```
67
Adverse events to remember for cephalosporins
- CNS with 3rd generation - cross reactivity in patients with PCN allergy, DO NOT USE in patients who get anaphylaxis to PCN - Disulfiram reaction with alcohol (cefotetan mostly)
68
Drug interactions in cephalosporins
- probenecid (block tubular secretion, so increases serum concentration/1/2 life) - cetriaxone with calcium (forms insoluble precipitate) and contraindicated in neonates 28 day or younger - iron supplement should be separated from cefdinir by 2 hours before or after (decreased absorption)
69
All cephalosporins (1,2,3 gen) do not cover
MRSA, enterococcus, P. aeruginosa, and acinetobacter
70
Ceftazidime is an
anti-pseudomonal cephalosporin
71
Ceftazidime structure differences help to
increase activity against gram - bacilli, increase stability against some beta-lactamase and increases pseudomonas activity, zwitterionic properties
72
Ceftazidime is generally unstable against
ESBL, AmpC, carbapenemases
73
Cefepime is an
anti-pseudomonal cephalosporin
74
Cefepime structure causes it to be
zwitterion at neutral pH
75
Ceftazidime is a ____ generation cephalosporin
3rd
76
Cefepime is a _____ generation cephalosporin
4th
77
Ceftazidime oral absorption
poor IV only
78
Ceftazidime 1/2 life
short 2 hours
79
Ceftazidime elimination
renal
80
Cefepime oral absorption
poor IV only
81
Cefepime 1/2 life
short 2.2 hours
82
Cefepime elimination
renal
83
Ceftazidime/Cefepime tissue distribution
``` skin bone/joint urine lung CNS with inflammation intra-ab ```
84
Ceftazidime spectrum coverage
light purple: streptococcus, s. pneumoniae dark red: h. influenzae, m. catarrhalis, E. coli, klebsiella, p. mirabilis, morganella, p. aeruginosa light red: Neisseria, enterobacter, citrobacter, serratia anaerobes: +/- (oral only) Misc: activity against achromobacter and s. maltophilia, unstable against ESBL and AmpC
85
Cefepime spectrum coverage
dark purple: streptococcus, s. pneumoniae, MSSA/MSSE light purple: viridans dark red: Neisseria, h. infleunzae, m. catarrhalis, e. coli, klebsiella, p. mirabilis, Morganella, enterobacter, citrobacter, serratia, p. aeruginosa light red: acinetobacter anaerobes: +/- (oral) Misc: stable against AmpC, poor activity against S. maltophilia and achromobacter
86
Ceftazidime/Cefepime indications
healthcare associated infections like pneumonia, CNS, skin and skin structure, intra-ab, UTI Cefepime is often preferred to improve gram + activity and it has better activity against MSSA
87
Cephalosporin/inhibitor agents
ceftazidime/avibactam, ceftolozane/tazobactam
88
Avibactam is a ____ inhibitor
non suicidal; able to be recycled
89
Avibactam is a
non-beta-lactam beta-lactamase inhibitor and improves binding affinity
90
Avibactam inhibits
ESBL, AmpC, and some OXA-type
91
Ceftolozane/tazobactam structure
C7 side chain allows for enhanced gram - coverage | C3 side chain improves p. aeruginosa activity
92
Tazobactam provides some stability against
ESBL
93
Ceftazidime/avibactam oral absorption
poor IV only
94
Ceftazidime/avibactam 1/2 life
2/2.7 so short
95
Ceftazidime/avibactam elimination
renal
96
Ceftolozane/tazobactam oral absorption
poor IV only
97
Ceftolozane/tazobactam 1/2 life
2.8/1 so short
98
Ceftolozane/tazobactam elimination
renal
99
Ceftazidime/avibactam and Ceftolozane/tazobactam tissue penetration
``` skin bone/joint urine respiratory intra-ab ```
100
Ceftazidime/avibactam spectrum coverage
dark purple: MSSA light purple: streptococcus, s. pneumoniae dark red: h. influenzae, m. catarrhalis, E. coli, klebsiella, p. mirabilis, morganella, enterobacter, citrobacter, serratia, P. aeruginosa light red: Neisseria anaerobes: +/- (oral) Misc: ceftazidime has poor activity against b. fragilis, has activity against KPC, ESBL, AmpC
101
Ceftolozane/tazobactam spectrum coverage
dark purple: streptococcus light purple: s. pneumoniae, viridans dark red: h. influenzae, m. catarrhalis, E. coli, klebsiella, p. mirabilis, morganella, citrobacter, serratia, p. aeruginosa light red: Neisseria, enterobacter, acinetobacter anaerobes: +/- (oral) Misc: cetfolozane has poor activity against b. fragilis, is active against carbapenem resistant pseudomonas
102
Ceftazidime/avibactam indications
- predominant role will be KPC-producing organisms | - has activity against ESBL and AmpC producing organisms but not better than carbapenems
103
Ceftolozane/tazobactam indications
P. aeruginosa, especially carbapenem resistant isolates
104
Cefiderocol is a ____ cephalosporin
siderophore
105
Cefiderocol has a novel MOA
binds to free extracellular ferric iron and actively transports itself across the outer cell membrane of bacteria into periplasmic space using siderophore iron uptake mechanism (Trojan horse)
106
Cefiderocol is bactericidal/bacteristatic
bactericidal
107
Cefiderocol is bactericidal through
inhibiting cell wall synthesis through binding to PBP
108
Cefiderocol oral absorption
poor IV only
109
Cefiderocol 1/2 life
2-3 hours so medium/short
110
Cefiderocol elimination
renal
111
Cefiderocol spectrum coverage
ONLY GRAM - dark red: h. influenzae, m. catarrhalis, E. coli, klebsiella, p. mirabilis, morganella, enterobacter, citrobacter, serratia, p. aeruginosa, acinetobacter light red: Neisseria Misc: active against carbapenem- resistant pseudomonas and enterobacteriaceae and s. maltophilia active against ESBL, AmpC, KPC, OXA-type, MBL carbapenemases
112
Cefiderocol indications
multi-drug-resistant gram - infections like UTI, pneumonia, bacteremia
113
Anti-staphylococcal cephalosporin
ceftaroline
114
Ceftaroline is a
pro drug
115
phosphono group was added to Ceftaroline to
improve solubility
116
Ceftaroline has enhanced activity against
PBP2a and MRSA
117
Ceftaroline's structure allows it to be
zwitterion
118
Ceftaroline oral absorption
poor IV only
119
Ceftaroline 1/2 life
2-3 so medium/short
120
Ceftaroline elimination
40-70% renal
121
Ceftaroline tissue penetration
``` skin bone/joint urine respiratory intra-ab CNS (animal models) ```
122
Ceftaroline spectrum coverage
Same as ceftiaxone + MRSA dark purple: streptococcus, s. pneumoniae, viridans, MSSA/MSSE, MRSA/MRSE dark red: Neisseria, h. influenzae, m. catarrhalis, E. coli, klebsiella, p. mirabilis, morganella light red: enterobacter, citrobacter, serratia anaerobes: +/- (oral) Misc: no activity against ESBL, poor activity against Ampc
123
Ceftaroline does not cover
enterococcus and p. aeruginosa and acinetobacter
124
Ceftaroline indications
pneumonia, bacteremia, skin and skin structure
125
Ceftaroline adverse events
``` CNS GI renal skin anaphylaxis hematologic ```
126
Which drugs improved activity against nosocomial pathogens including p. aeruginosa?
cefepime and ceftazidime and ceftolozone/tazobactam
127
Cefepime has improved
gram + coverage
128
Which drug has improved activity against carbapenem resistant pseudomonas, enterobacteriacae, and acinetobacter?
cefiderocol
129
Cefiderocol does not have reliable ____ coverage
gram + and anaerobic
130
Valuable drug for MRSA management
Ceftaroline

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