Antibiotics Flashcards

1
Q

Antibiotics that are time dependent?

A

Beta Lactams:
Penicillins
Cephalosporins
Carbapenems

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2
Q

Antibiotics that are concentration dependent?

A

Fluoroquinilones
Aminoglycosides
Daptomycin
Macrolide

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3
Q

What does “cidal” mean?

A
  • Defined as having a 2 log drop in your bacteria over a 24 hr period
  • Beta lactams are categorized as these
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4
Q

4 categories of Beta Lactams

A
  1. Cephalosporins
  2. Penicillins
  3. Carbapenems
  4. Aztreonam
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5
Q

Penicillins

A
  • Categories include natural, amino, anti-staph and extended spectrum with combo beta lactamase inhibitors
  • Kill gram positives (MSSA)
  • Work at the PBP on the peptidoglycan bacterial wall to cause apoptosis
  • Primarily cidal drugs
  • Generally have poor BA
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6
Q

3 major side effects of Penicillins

A

Hypersensitivities
Blood dyscrasias
Lower seizure threshold

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7
Q

T/F: When beta lactams can be given with continuous infusion they should be.

A

TRUE

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8
Q

T/F: GAS is completely susceptible to amoxicillin, ampicillin and penicillin

A

TRUE

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9
Q

Best way to administer penicillin?

A

Less drug and slow infusion allows you to reach better targets to treat your patients

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10
Q

What drug in combo with Penicillin will drastically increase Penicillin’s concentration in the body?

A

Probenecid

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11
Q

Ceftriaxone

A
  • DOC for Strep pneumo
  • IV only
  • Treats diseases of the biliary tract because it is primarily biliary eliminated
  • BAD drug to give in neonates can –> hyperbilirubinemia –> developmental delay
  • May see calcium precipitation with this drug
  • Normally given once daily unless meningitis (twice)
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12
Q

Third generation cephalosporins target?

A

Gram - bacteria

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13
Q

Fourth generation cephalosporins target?

A

Gram + and - bacteria (cefepime)

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14
Q

Fifth generation cephalosporins are important for?

A

Binding to the mutated site of the PBP site created by MRSA

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15
Q

Which drugs fit this description?

  • Lumped under second generation cephalosporins but they also cover anaerobes
  • Cephamycins
A

Cefotetan and Cefoxitin

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16
Q

Cephalosporin PEARLS

A
  • Cephamycin’s have enhanced gram-negative anaerobic activity
  • Third and fourth generation have enhanced CSF penetration (e.g. ceftriaxone, ceftaz, cefepime)
  • Poor BA
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17
Q

Cephalosporins do NOT have activity against _______?

A

Enterococcus

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18
Q

Cephalosporins that can treat meningitis?

A

3rd and 4th generation

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19
Q

What 3 cephalosporins can be administered during dialysis?

A

Cefazolin, cefepime and perhaps ceftazidime

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20
Q

Ceftaroline

A
  • 5th generation cephalosporin
  • Activity vs. MRSA and gram-negatives
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21
Q

Two cephalosporins that should only be used with patients who have significant drug resistant infections.

Sometimes seen with CF and LVADS

A

Ceftazidime/Avibactam & Ceftolozane/Tazobactam

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22
Q

Mainly developed to treat gram negative bacterial infections

INCLUDE:
Imipenem/Cilastatin
Meropenem
Ertapenem
Doripenem

A

Carbapenems

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23
Q

PEARLS of Carbapenems

A
  • IV only
  • Worst offender of lowering the seizure threshold
  • Lower the valproic acid level in your body drastically (DDI)
  • Ertapenem has no pseudomonal activity
  • Imipenem/Cilastatin duo may have better activity against gram positive bacterium
  • Should be renally adjusted
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24
Q

How does Imipenem/Cilastin combo work?

A

Gives Imipenem a longer half life by inhibiting kidney enzymes!

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25
Q

Which carbapenem does not cover Pseudemonas?

A

Ertapenem

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26
Q

The beta lactamase inhibitors include:

A
  • Clavulanic acid
  • Tazobactam
  • Sulbactam
  • Avibactam
  • Vaborbactam
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27
Q

Lone monobactam
Does not work AT ALL against gram + bacterium
Can give the drug inhaled for isolated pneumonia

A

Aztreonam

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28
Q

Aztreonam only treats which type of bacteria?

A

Gram -

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29
Q

Potential side effect for Azetreonam?

A

Transaminitis

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30
Q

There might be cross reactivity between aztreonam and ______ but otherwise, there is no cross-reactivity between aztreonam and beta lactams

A

Ceftazidime

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31
Q

First generation cephalosporin that is the “go to” oral Abx

A

Cephalexin

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32
Q

First generation cephalosporin that is the “go to” IV Abx

A

Cefadroxil

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33
Q

ABx that binds directly to the amino acid (Alanine) present on the bacterial cell wall of all gram positive bacteria, not the PBP

Does not have good activity to gram negative bugs
Acts against MRSA, strep and enterococcus
Cidal
Drug of choice against C diff and MRSA
AUC/MIC >400
Very high serum concentrations

A

Vancomycin

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34
Q

Targets of Vancomycin?

A

Gram + bacteria

MRSA

C. diff

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35
Q

Why does Vanco not have good activity against gram - bacterium?

A

The drug cannot fit through the channels of the double layered membrane

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36
Q

How is Vanco administered for C Diff?

A

Orally

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37
Q

2 ideal treatments for MSSA?

A
  1. anti Staph penicillins
  2. Cefazolin
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38
Q

ADEs of Vancomycin?

A
  • Red Mans syndrome
  • Thrombocytopenia
  • Neutropenia
  • Ototoxicity
  • Nephrotoxicity
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39
Q

Vancomycin may have DDI with?

A

Aminoglycosides and Nephrotoxic Agents

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40
Q

Risk factors for nephrotoxicity while on Vancomycin include…

A

High doses
Obesity
Hypotension
Concurrent nephrotoxins
Concurrent beta lactams (piperacillin)

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41
Q

When dosing and monitoring Vancomycin you must take into account _______ dose and _______ dose

A

Loading and maintenance dose

you must ALSO take into account weight and renal function

42
Q
  • Used for efficacy, not so much toxicity
  • 30 mins prior to 4th does
  • Make sure patient is in steady state before ordering
  • Done every week to two weeks after the initial monitoring is done because the patient maintains relatively stable concentrations
A

Trough concentrations

43
Q
  • Lipoglycopeptide
  • IV
  • Predominately gram positive
  • Inhibits cross-linking and peptidoglycan formation (D-Ala-D-Ala) and causes membrane depolarization
  • Highly protein bound
  • Patient’s with bad kidneys did not have good results with this drug
  • Chalky taste and foamy urine
  • Decreases blood clotting
  • Can be used for MRSA but not used over Vanc
  • AUC/MIC
A

Telavancin

44
Q
  • 2nd generation lipoglycopeptides
  • Treat staph and strep (MRSA)
  • Long acting IV injections because of their very large half lives
  • Used to treat osteomyelitis
A

Dalbavancin and Oritavancin

45
Q

Has cidal activity except with enterococcus
Concentration dependent
Causes a membrane depolarization leading to an inhibition of DNA, RNA and protein synthesis
May cause musculoskeletal atrophy (statins may also increase CPK levels)
Weight based dosing
Do not use to treat any sort of pulm infection

A

Daptomycin

46
Q

Route of administration for Daptomycin?

A

IV

47
Q

What does Daptomycin treat?

A

Predominately gram positive including MRSA and VRE

NOT enterococcus

48
Q

Daptomycin ADE?

A

May cause muscle toxicity with an increase in CPK

49
Q

Daptomycin DDI?

A

Statins (might also increase CPK)

50
Q

Work predominantly on gram negative bacterium because there are no holes on the gram positive membrane
Concentration dependent
Nephrotoxicity and ototoxicity
Very high PAE
Need to be cautious with this drug; therapeutic drug monitoring
Gram positive synergy (e.g. vanc)

A

Aminoglycosides

51
Q

Aminoglycosides MOA?

A

Irreversible 30s subunit binding

52
Q

Aminoglycosides- Why can we use/Why do we use?

A

Peak/MIC ration predictive of cidal activity
High peaks do not equal toxicity
Less nephrotoxicity
PAE
Less monitoring (once daily dosing)

53
Q

Atypical pathogens?

A

Mycoplasma, Chlamydia, Legionella

54
Q

Abx that work on atypcials?

A

Tetracyclines, Microlides and Fluoroquinilones

55
Q
  • Works against atypical pathogens (mycoplasma, chlamydia and legionella)
  • Works against some gram negatives
  • Limited with anaerobes
  • STIs
  • Strep pneumonia and staph areus
  • Activity against C diff
A

Tetracyclines

56
Q

Tetracycline MOA?

A

Works on the 30s ribosomal subunit; static

57
Q

Tetracyclines used for treating S. aureus activity?

A

Doxycycline and Minocycline

58
Q

Tetracycline ADE?

A
  • GI dyspepsia
  • Binding with multivalent cations
  • Tooth discoloration
  • Sun sensitivity

Minocycline: vertigo, discoloration, hepatitis, lupus, leukopenia, pericardial effusion

59
Q

T/F: tetracyclines have really good tissue penetration but really poor serum concentrations

(Aka would not use to treat blood stream infections)

A

TRUE

60
Q

Vancomycin-Resistant Enterococcal UTI’s

A

Doxy > Tetra > Mino

61
Q

Tetracycline that treats SIADH (syndrome of inappropriate ADH secretion)

A

Demeclocycline

62
Q

Tigecycline

A
  • Tetracycline that binds to two sites on the ribosome
  • Enhanced minocycline
  • Broad spectrum but doesn’t work well in pts because it rapidly leaves blood stream and penetrates tissues greatly
  • Rarely ever used
  • Biliary excretion is the primary route of elim
  • Been to work well with mycobacterium infections and severe C diff
63
Q

The Tetracyclines include?

A

Doxycycline, Tetracycline, Minocycline, Tigecycline

64
Q

Tigecycline can be given in what situation?

A

ICU patients with severe drug resistance

65
Q

Tigecycline ADE?

A

Profuse projectile vomiting

66
Q

Tigecycline route of administration?

A

IV only

67
Q
  • Binding at the 23S and 50S ribosomal subunit
  • Static activity and time dependent
  • Oral and IV BA 100% (1:1)
  • Good to use for vancomycin resistant bugs
  • No renal adjustment
  • Very high tissue penetration so it has never been clinically proven to be better than Vanco
A

Linezolid

68
Q

Linezolid works against?

A

Gram positive, MRSA, VRE, Mycobacterium, C. Diff

69
Q

Linezolid ADE?

A
  • Hematologic (RBC,WBC and platelets)
  • Peripheral neuropathies (weakness, numbness, pain in hands and feet)
  • Arthralgia in hands and knees
  • Optic neuritis
  • May see drug drug interactions with SSRI’s because it is a MAO inhibitor; reduce SSRI to lowest effective dose
  • Caution with tyramine containing foods; increase in BP
70
Q
  • Inhibits DNA gyrase and topoisomerase at the site of DNA replication
  • 40% resistance of E coli
  • Avoid use in “simple uncomplicated infections”
A

Fluoroquinilones

71
Q

What do fluoroquinilones work against?

A

Gram +, gram -, pseudo, anaerobes, atypicals

72
Q

ADE for fluoroquinilones?

A

Sun sensitivity, tendon rupture, Cipro Psychosis, dysglycemia, PN, QT prolong

73
Q
  • Not renally adjusted
  • Activity against anaerobes
  • Activity against atypical organisms
A

Moxifloxacin

74
Q
  • Does not have 1:1 BA like the other fluoroquinolones
  • Has MRSA activity
A

Delafloxacin

75
Q

The fluoroquinilones include?

A

Ciprofloxacin, Levofloxacin, Moxifloxacin, Delafloxacin

76
Q

What 3 fluoroquinolones have pseudemomas activity?

A

Ciprofloxacin, Levofloxacin, and Delafloxacin

77
Q

DNA gyrase is more common in which bugs?

A

Gram +

78
Q

Topoisomerase is more common in which bugs?

A

Gram -

79
Q
  • Fluoroquinolone with higher topoisomerase activity in comparison to DNA gyrase
  • Higher affinity for gram negative organisms
  • DOES get into the lungs, it just doesn’t treat gram positive strep pneumo
A

Ciprofloxacin

80
Q

The Macrolides include?

A

Azithromycin, Erythromycin, Clarithromycin

81
Q

What is the MOA of macrolides?

A

Binding at 50s ribosomal subunit (dissociation of tRNA from ribosome)

82
Q

What do macrolides cover?

A

Broad spectrum:
Atypical, strep, MSSA, STI, mycobacterium, Helicobacter Pylori

83
Q

Because of their action on the ribosome, macrolides have a long half life, but….

A

This may breed resistance

84
Q

ADE of macrolides?

A
  • GI
  • Dysgeusia
  • Cardiotoxicity
85
Q

Which macrolide does not have GI effects and why?

A

Azithromycin- does not bind to gastrin

86
Q

Clarithromycin and Erythromycin both….

A

Inhibit 3A4

Therefore you see large increases in statin!

87
Q

All Macrolides also have ________ properties

A

Anti inflammatory

88
Q

Clindamycin is antagonistic with ________?

A

Macrolides

89
Q

Clindamycin predominately treats?

A

Strep and Staph- including MRSA

90
Q

Clindamycin BA?

A

Really good! Penetrates well into most body tissues except CSF

Time dependent killing

91
Q

Biggest ADE for Clindamycin?

A

Severe diarrhea, high risk for C. Diff*

92
Q

Clindamycin clinical uses with really bad staph and strep infections?

A

Clindamycin binds toxins and reduce toxin production of staph and strep

Recommended with limb or life threatening staph or GAS

93
Q

Drug that interferes with human follic acid metabolism?

A

SMX/TMP

94
Q

SMX and TMP treats?

A

MRSA, Gram +

95
Q

SMX and TMP are the DOC for?

A

Nocardia and PJ

96
Q

SMX/TMP ADE?

A

Bone marrow suppression (anemia)
Hyperkalemia
High serum Creatine

97
Q

2 treatments for UTIs?

A

Fosfomycin
Nitrofurantoin

98
Q

Side effects of Fosfomycin?

A

NONE works directly at the bladder and is exreted in the urine

99
Q

DOC for invasive MSSA?

A

Nafcillin (or Oxacillin) and Cefazolin

100
Q

Beta lactam that works against MRSA and why?

A

Ceftaroline- affinity for mutated site PBP 2a

101
Q

DOC for MRSA?

A

Vancomycin