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PC2 > Penicillins > Flashcards

Penicillins Flashcards

1
Q

Pure penicillin is ____ to degradation by acids.

A

highly susceptible; pH was 5-7

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2
Q

Serial passages of penicillin over ____and ____ results in resistant organisms.

A

staphylococcus; streptococcus species

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3
Q

Organisms that are inherently resistant to penicillins

A

Gram - bacilli

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4
Q

Peniciilins have a ___ safety margin compared to other available compounds.

A

WIDE

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5
Q

Structure of Penicillin: nucleus

A

beta-lactam and thiazolidine rings

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6
Q

Nucleus is important because:

A

required for biological activity

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7
Q

Breakdown of beta-lactam by beta-lactamase results in

A

loss of activity

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8
Q

Acyl side chain modifications

A

change spectrum of activity, stability to enzymes, and pharmacokinetic properties

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9
Q

MOA for Penicillin

A

PEN inhibits transpeptidase responsible for cross-linking peptide chains resulting in a dysfunctional wall

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10
Q

Normal function of PBP:

A

synthesize peptidoglycan, maintain cell shape, and septum formation

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11
Q

Disruption of cell wall stimulates

A

autolysis and cell death

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12
Q

Penicillin G could be given:

A

orally, IV, IM

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13
Q

Penicillin G benefits over other agents:

A

readily distributed into multiple tissues and wide therapeutic index (safe)

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14
Q

Penicillin G challenges:

A

rapid acid degradation, susceptibility to beta-lactamases, narrow spectrum of activity

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15
Q

Natural Penicillins oral absorption:

A

PCN VK (60%) >PCN G (30%)

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16
Q

Natural Penicillins 1/2 life

A

short

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17
Q

Natural Penicillins route of elimination

A

renal

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18
Q

Natural Penicillins CSF distribution

A

better into inflamed than non-inflamed but still poor

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19
Q

Natural Penicillins protein binding

A

50

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20
Q

PCN VK is more/less stable than PCN G

A

more, produces 2-5x greater serum concentration

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21
Q

Natural Penicillins can/cannot be removed by hemodialysis

A

can

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22
Q

Bacterialcidal activity for beta-lactams is measured by

A

T>MIC; duration of time that free drug levels exceed MIC

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23
Q

for stasis:

for cidal:

A

30%

50%

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24
Q

Spectrum coverage for Natural PCNs

A

dark purple: streptococcus spp, S. pneumoniae, E. faecalis
light purple: viridans strep
dark red: Neisseria spp
anaerobes: +/- (oral +)
Misc: T. pallidum (syphillis), B. burgdorferi (Lyme)

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25
Q

Common indications for Natural PCNs

A 
syphilis (dosing depends on stage of syphilis)
neurosyphilis 
endocarditis
meningitis
streptococcal pharyngitis
streptococcal toxic shock
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26
Q

Long acting parenteral agents:

A

Penicillin G procaine, penicillin G benzathine (Bicillin LA), penicillin G benzathine/procaine (Bicillin CR)

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27
Q

Long acting parenteral agents administration

A

IM; avoid IV due to increased risk of cardiac arrest

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28
Q

Purpose for developing PCN long acting parenteral agents

A

developed in response to short half-life and poor oral absorption of PCN

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29
Q

Penicillinase resistant penicillins active against penicillinase producing staph aureus:

A

Oxacillin and Nafcillin

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30
Q

Spectrum coverage for oxacillin and nafcillin:

A

GRAM + ONLY
dark purple: streptococcus, s.pneumoniae, MSSA/MSSE
light purple: viridans

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31
Q

Nafcillin/Oxacillin oral absorption:

A

poor oral, IV only

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32
Q

Nafcillin/Oxacillin 1/2 life:

A

short

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33
Q

Nafcillin/Oxacillin Route of elimination:

A

hepatic, biliary

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34
Q

Nafcillin/Oxacliin distribution

A 
skin
joint
lung
urine
CSF with inflammation
bile
peritoneal
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35
Q

Nafcillin/Oxacliin dosing

A

the same for both and varies with infection; can be administered as continuous infusion

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36
Q

Nafcillin/Oxacliin challenges

A

poor oral absorption due to gastric acid breakdown

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37
Q

Dicloxacillin oral bioavailability

A

increased 50% from Nafcillin/Oxacliin

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38
Q

Dicloxacillin protein binding

A

high

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39
Q

Dicloxacillin 1/2 life

A

short

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40
Q

Purpose of isoxazoyl group in dicloxacillin

A

mitigates penicillinase and gastric acid breakdown

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41
Q

Dicloxacillin used for

A

treatment of mild bacterial skin/skin structure infections

42
Q

Resistance mechanisms for penicillins

A

alterations in PBPs (s. pneumo/neisseria, enterococcus)

PCN penicillinase (s.aureus)
Oxacillin/methicillin resistance by altering PBP2 (s.aureus)
43
Q

Adverse effects for Pencillins

A 
well tolerated
neurologic
GI
hepatic
renal
allergy
electrolyte abnormalities
hematologic
thrombophlebitis
44
Q

Penicillins have a ____ spectrum of activity

A

narrow

45
Q

Penicillins are primarily used as ___ therapy

A

definitive

46
Q

Penicillins are bactericidal/bacteriostatic

A

bactericidal

47
Q

Extended spectrum penicillins include

A

aminopenicillins and ureidopenicillins

48
Q

Clinical needs for extended spectrum penicillins

A

safe antimicrobials

improved gram - activity by enhancing penetration through outer membrane and having higher affinity for PBP

49
Q

Ampicillin has enhanced cell wall penetration because it is a

A

zwitterion at neutral pH

50
Q

Zwitterions penetrate through ____ within the cell membrane

A

porins

51
Q

Ampicillin oral absorption:

A

50% (fair)

52
Q

Ampicillin elimination:

A

RENAL

53
Q

Ampicillin 1/2 life:

A

short

54
Q

Ampicillin is associated with which side effect:

A

diarrhea

55
Q

Ampicillin has saturable

A

absoprtion

56
Q

Ampicillin tissue penetration

A

lung, bone, CNS with inflammation

57
Q

Amoxicillin is administered

A

orally only in the US

58
Q

Amoxicillin oral absorption

A

75% so higher than ampicillin

59
Q

Amoxicillin has ____ frequency of diarrhea

A

reduced

60
Q

Amoxicillin is primarily used for

A

URI

61
Q

Amoxicillin has activity against ____ so it can be used for URI

A

s. pneuomoniae

62
Q

Amoxicillin dosing depends on

A

indication

63
Q

Ampicillin/Amoxicillin spectrum coverage:

A

dark purple: streptococcus, S. pneumoniae, E. faecalis
light purple: viridans, E. faceium
dark red: Neisseria
light red: H. influenzae, E. coli, P. mirabilis
anaerobes: +/- (oral +)
Misc: L. monocytogenes, H. pylori, Salmonella, Shigella

** not stable against penicillinase **

64
Q

Common indications for Ampicillin/Amoxicillin

A 
Empiric therapy: 
Group A strep
s.pneumoniae (high dose amoxicillin)
H.pylori
Listeria (especially CNS) use ampicillin

Definitive therapy:
Enterococcus
S. pneumoniae
H. influenzae (beta-lactamase negative)

65
Q

Sulbactam is added to ampicillin to

A

minimize impact of beta lactamases

66
Q

Sulbactam is a _____ inhibitor

A

suicide

67
Q

Suicide inhibitor

A

permanently inactivates beta-lactamases and cannot be recycled
also has minor PBP inhibitory properties

68
Q

Spectrum of inhibition for ampicillin/sulbactam

A

penicillinases (MSSA)
cephalosporinases (klebsiella)
broad spectrum beta lactamases (E. coli)

69
Q

Sulbactam has weak intrinsic activity against

A

Neisseria and acinetobacter

70
Q

Ampicillin/sulbactam oral absorption

A

50/20

71
Q

Ampicillin/sulbactam 1/2 life

A

short

72
Q

Ampicillin/sulbactam elimination

A

RENAL

73
Q

Ampicillin/sulbactam is administered

A

IV only as combo in 2:1 ratio

74
Q

Sulbactam tissue penetration

A

CSF- similar to ampicillin in inflamed cases
lung- similar to ampicillin
bone- 15% so less than ampicillin

75
Q

Clavulanate is a ____ inhibitor

A

suicide

76
Q

Clavulanate extends amoxicillin’s spectrum of activity through

A

inhibition of beta-lactamases

77
Q

Clavulanate does not have activity against

A

acinetobacter

78
Q

Clavulanate has activity against

A

s. aureus, h. influenzae, E. coli, klebsiella, p. mirabilis, salmonella, shigella, norcardia, and some mycobacterium

79
Q

Amoxicillin/clavulanate oral absorption

A

high 75/75

80
Q

Amoxicillin/clavulanate 1/2 life

A

short

81
Q

Amoxicillin/clavulanate elimination

A

renal/ hepatic-renal

82
Q

Amoxicillin/clavulanate adverse effects

A

diarrhea! from clav component and less diarrhea is seen with newer formulations

83
Q

Amoxicillin/clavulanate dosage forms

A

tablet, ER tablets, liquid

84
Q

Aminopenicillin + inhibitor spectrum coverage:

A

dark purple: streptococcus, s. pneumoniae, MSSA/MSSE, e. faecalis
light purple: viridans, e. faecium
dark red: Neisseria, h. influenzae, m. catarrhalis, E. coli, klebsiella, p. mirabilis
light red: morganella
anaerobes: ++ (oral and gut b. fragilis)
Misc: similar to ampicillin for acinetobacter

85
Q

Ampicillin/sulbactam indications

A

empiric use:
surgical prophylaxis for intra-ab surgery
head and neck infections
sinus infections
XDR acinetobacter infections (due to sulbactam activity)

definitive:

  • intra-ab infections
  • gynecologic infections
  • head and neck infections
86
Q

Amoxicillin/clavulanate indications

A

URI like sinusitis, outpatient community acquired pneumonia, otitis media, strep throat

87
Q

Ureidopenicillins have a ___ spectrum of activity

A

broader

88
Q

Ureidopenicillins have

A

enhanced cell wall penetration and improved binding affinity to multiple PBP

89
Q

Ureidopenicillin drug

A

pipercillin/tazobactam

90
Q

Pipercillin/tazobactam oral absorption

A

poor

91
Q

Pipercillin/tazobactam administration

A

IV only

92
Q

Pipercillin/tazobactam 1/2 life

A

short

93
Q

Pipercillin/tazobactam elimination

A

renal: 68/80 mostly renal
biliary: 20/20

94
Q

Pipercillin/tazobactam penetration into CNS

A

not good

95
Q

Pipercillin/tazobactam penetration into tissues

A

bile, lung, skin, urine, bone, peritoneum

96
Q

Pipercillin/tazobactam spectrum coverage:

A

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

97
Q

Pipercillin/tazobactam indications

A

healthcare associated infections (suspicion for multi drug resistant organisms)
intra-ab infections
pneumonia
complicated skin/skin structure infections
fever and neutropenia
NOT GOOD FOR CNS/MENINGITIS

98
Q

Pipercillin/tazobactam adverse effects

A 
well tolerated
neurologic
GI
hepatic (kcholestatis jaundice is higher than other PCNs)
renal
allergy
electrolyte imbalance (sodium overload)
hypokalemia
hematologic
thrombophlebitis
99
Q

Which organism do all PCN drugs not cover?

A

MRSA/MRSE

100
Q

Which PCN drug/derivative covers p. aeurginosa and acinetobacter?

A

pipercillin/tazobactam

101
Q

Which PCN drug/derivative covers B. fragilis (gut anaerobes)?

A

pipercillin/tazobactam and aminopenicillins+inhibitor

102
Q

In the hospital setting _____ is the most used PCN agent due to its broad spectrum of activity

A

pipercillin/tazobactam

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