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PC2 > Carbapenems > Flashcards

Carbapenems Flashcards

1
Q

Cilastatin is

A

DHP1 inhibitor

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2
Q

Carbapenems came from

A

imipenem

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3
Q

Carbapenem base structure

A

beta-lactam ring fused with a 5 C ring and sulfur is not in the ring

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4
Q

CARBapenems

A

presence of many carbons

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5
Q

Modifications at C3 and C4

A

improve stability, spectrum of activity, and lower epileptogenic potential

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6
Q

Imipenem is vulnerable to

A

renal DHP1 and has epileptogenic potential

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7
Q

Meropenem benefits:

A

stable to renal DHP1 (improved bt 1 beta methyl group on C4), less epileptogenic potential, and increased gram - activity

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8
Q

Carbapenem MOA:

A

bind to and inactivate multiple PBP resulting in inhibition of cell wall synthesis and initiating autolysis

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9
Q

Carbapenem spectrum of activity varies depending on

A

affinity to PBP

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10
Q

Doripenem 1/2 life

A

short

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11
Q

Doripenem elimination

A

renal 70%

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12
Q

Imipenem/cilastatin 1/2 life

A

short

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13
Q

Imipenem/cilastatin elimination

A

renal 70%

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14
Q

Meropenem 1/2 life

A

short

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15
Q

Meropenem elimination

A

renal 70%

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16
Q

Carbapenem tissue penetration

A 
peritoneal fluid
urine
lung
bone
CSF dosing is different for meningitis
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17
Q

Carbapenem CSF penetration

A

very low with no inflammation and not the best with inflammation but meropenem would work the best out of all of them

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18
Q

Carbapenems are bactericidal/bacteriostatic

A

bactericidal

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19
Q

What PD property is used for carbapenems?

A

% Time> MIC

20
Q

Carbapenems have the _____ % Time >Mic requirement

A

shortest

21
Q

What is the % requirement for carbapenems to have bactericidal activity?

A

40%

22
Q

Carbapenem spectrum coverage

A

dark purple: streptococcus, s. pneumoniae, viridans, MSSA/MSSE, E. faecalis
dark red: Neisseria, h. influenzae, m. catarrhalis, E. coli, klebsiella, p. mirabilis, morganella, enterobacter, citrobacter, serratia, p. aeruginosa, acinetobacter
anaerobes: ++ oral and gut
Misc: stable against ESBL and AmpC, activity against mycobacterium, inactive against s. maltophilia

23
Q

Carbapenems do not cover

A

MRSA/MRSE and e. faecium

24
Q

Common carbapenems include

A

doripenem, imipenem/cilastatin, meropenem

25
Q

Ertapenem is unique because

A

it has anionic character that results in decreased penetration into porin channels found in pseudonomas

26
Q

Ertapenem also has

A

increased protein binding and increased 1/2 life

27
Q

Ertapenem does not cover

A

acinetobacter, p. aeruginosa, MRSA, enterococcus

28
Q

Ertapenem 1/2 life

A

medium/long 4 hours

29
Q

Ertapenem elimination

A

renal

30
Q

Hemodialysis can remove ___% of Ertapenem

A

30

31
Q

Ertapenem spectrum coverage

A

dark purple: streptococcus, s. pneumoniae, viridans, MSSA/MSSE
dark red: Neisseria, h. influenzae, m. cattarhalis, E. coli, klebsiella, p. mirabilis, Morganella, enterobacter, citrobacter, serratia
anaerobe: ++ (oral and gut)
Misc: stable against ESBL and AmpC, inactive against S. maltophilia

32
Q

Carbapenem resistance

A
  • stable from hydrolysis from numerous beta lactamases
  • enterobacteriaceae/acinetobacter inactivate the drug by carbapenem-hydrolyzing enzymes
  • pseudonomas decreased outer membrane permeability (altered porin channels) and active efflux
  • mutant or acquired altered PBPs
33
Q

Addition of beta-lactamase inhibitor to carbapenems advantage:

A

expands coverage

34
Q

Meropenem/vaborbactam advantage:

A

expanded activity against CRE (KPCs)

35
Q

Vaborbactam does/does not enhance activity against pseudomonas aeruginosa or acinetobacter that are resistant to carbapenems due to efflux or porin mutations

A

does NOT

36
Q

Imipenem/cilastatin/relebactam advantage:

A
  • expanded activity against CRE (KPCs and some OXA-type) and carbapenem resistant pseudomonas aeruginosa
  • may have a role in treatment of nontuberculous mycobacterial infections
37
Q

Adverse events related to to carbapenems

A 
CNS
GI
hepatic
renal
skin
hematologic
anaphylaxis
38
Q

Drug interactions with carbapenems

A

-effect on valproic acid (loss of seizure control)
should consider alternative antibacterial or anticonvulsant
-probenecid interferes with tubular secretion of all carbapenems

39
Q

Antipseudomonal Carbapenem indications

A
  • ESBL/AmpC infections
  • strong propensity for selecting for resistant organisms (increasing incidence of carbapenem-resistant enterobacteriaceae)
  • should be considered in cefepime or pipercilln/tazobactam resistant gram - bacilli
  • clinical worsening while receiving extended spectrum penicillin or cephalosporins
40
Q

Ertapenem dosing

A

QD, eases transition to home

41
Q

Ertapenem indications

A

stable against ESBL and AmpC beta-lactamases
intra-ab infections
skin/skin structure infections
CA pneumonia
UTI
pelvic infections
surgical prophylaxis in colorectal surgery

42
Q

Antipseudomonal carbapenems include

A

doripenem, morepenem, imipenem/cilastatin

43
Q

Carbapenem/beta lactamase inhibitor indications

A
  • expanded activity against carbapenem-resistant enterobacteriaceae (CRE)
  • utilization is driven by susceptibility profile and should be used as definitive therapy
44
Q

Carbapenem/beta lactamase inhibitor drugs are

A

EXPENSIVE

45
Q

Carbapenems are broad/narrow spectrum

A

broad

PC2 (18 decks)

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