L33 - Drugs Flashcards

1
Q

Explain beta-lactamases resistance

A

Hydrolyze beta lacatam ring
Inactivates the drug
= penicillinases

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2
Q

What are 2 common alterations to the binding site that confer resistance

A

PBP2a from mecA
vanA (B, C)
= lives with the threat by changing the drug’s target site

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3
Q

Adverse event for penicillin

A

HST

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4
Q

Adverse event for vanco

A

Red Man

Nephro-oto-toxicity

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5
Q

Adverse event for daptomycin

A

Rhabdomyolysis

Eosinophilic pneumonia

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6
Q

Which drugs work ONLY on g+

A

Nafcillin
Vanco
Dapto
Bacitracin

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7
Q

Which drugs work ONLY on g-

A

Aztreonam

Polymyxins

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8
Q

Drugs active against MRSA

A

Ceftaroline
Vanco
Dapto

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9
Q

4 beta lactam agents

A

Penicillins
Cephalosporins
Carbapenems
Monobactams

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10
Q

Explain B lactam activity

A

Mimics d-ala-d-ala terminal end of peptidoglycan monomer NAM
Can’t cross link NAG and NAMs via transpeptidases
ALSO no remodeling after autolysins come in and cut bonds
Net = cell lysis from osmotic pressure as cell wall (peptidoglycan layer) is weakened

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11
Q

Penicillin bacteriocidal or static

A

Cidal

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12
Q

Explain the reasons penicillin is a good drug of choice vs bad

A
Good:
- High therapeutic index
- Good tissue penetration
Bad:
- Renally excreted --> dosing
- Short 1/2 life --> frequent dosing 
- Bugs can be resistant easily via beta lactamases
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13
Q

What bugs does penicillin work against - draw the parallel to the clinical usage

A

GN cocci only - N.meningitis
GP broad - strep –> dental abscesses/human bites
Spirochetes - syphilis

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14
Q

IV & PO forms of the semi-synthetic penicillins (penicillinase resistant)

A
IV = Nafcillin 
PO = Dicloxacillin
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15
Q

What kinds of bacteria do Nafcillin & Dicloxacillin target?

A

G+ ONLY

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16
Q

How do bugs become resistant to semi-synthetic penicillin?

A

mecA gene –> PBP2a

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17
Q

What are the IV & PO aminopenicillins?

A
IV = Ampicillin
PO = Amoxicillin
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18
Q

Which bacteria do aminopenicillins target?

A

G+ cocci & anaerobes

G- b/c R group is more polar allowing entry through porins

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19
Q

What is unique about Piperacillin? Downside?

A

G- w/ PSEUDO
G+
Limited use b/c of resistance (beta-lactamase) –> almost always used in combo (beta-lactamase inhibitor)

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20
Q

When do you give B lactamase inhibitors?

A

Give w/ resistant infections b/c extends the activity of penicillins

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21
Q

Ampicillin-sulbactam

A

IV
Conquers:
- Penicillinase S.aureus
- B-lactamase G- & anaerobes

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22
Q

Amoxicillin-clavulanic acid

A

PO
Conquers:
- Penicillinase S.aureus
- B-lactamase G- & anaerobes

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23
Q

Piperacillin-tazobactam

A

Conquers:

  • Penicillinase S.aureus
  • B-lactamase G- & anaerobes including PSEUDO!!
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24
Q

Which bugs are resistant to cephalosporins as a general rule?

A

Intrinsic resistance:
- Pseudo
- Enterococci
Altered PBP: MRSA

25
Q

1st generation cephalosporin IV & PO forms

A
IV = Cefazolin 
PO = Cephalexin
26
Q

1st generation cephalosporin spectrum of activity

A

G+

Some G-

27
Q

When do you use cefazolin/cephalexin?

A

SURG PROPHYLAXIS

28
Q

2nd generation cephalosporin IV & PO

A
IV = Cefoxitin 
PO = Cefotetan
29
Q

2nd generation cephalosporin spectrum of activity

A

G+
More G-
Good anaerobic activity

30
Q

When do you use 2nd gen cephalo?

A

Intra-ab surgery prophylaxis

31
Q

3rd gen cephalosporins

A

IV

  • Ceftriaxone
  • Ceftazidime
32
Q

3rd gen cephalo spectrum of activity & pros

A

G+
Excellent G-
- Ceftazidime covers pseudo!
Long half life!!!

33
Q

When do you use ceftriaxone?

A

CA pneumo/meningitis

Serious inpatient infections

34
Q

Cefepime

A
4th gen cephalo
IV only
Broad
- G+
- G- w/ pseudo 
Good b/c resistant to beta-lactamases
35
Q

Ceftraroline

A

5th gen cephalo
G+ - only one that works vs MRSA!
- B/c can binds PBP2a
Some G- (similar to gen 3 levels)

36
Q

Cephalo + B lactamase inhibitors

A

Ceftolozane/tazobactam
Ceftazidime/avibactam

G- covers pseudo
UTI & intra-ab infections

37
Q

3 names of carbapenems

A

Imipenem
Meropenem
Ertapenem

38
Q

Carbapenems spectrum of activity & clinical use

A
VERY BROAD
G+
G- w/ pseudo
Anaerobes 
Use: serious & resistant infections
39
Q

How is Ertapenem’s spectrum of activity different than other carbapenems?

A

No pseudo/acinetobacter

40
Q

What drug should you use if penicillin allergy?

A

Carbapenems

41
Q

IV form of monobactam

A

Aztreonam

42
Q

Monobactam coverage

A

GN ONLY w/ pseudo

43
Q

When are you using monobactam

A

For people with beta-lactam allergy

Unlikely to be your first choice otherwise b/c resistance & decreased efficacy

44
Q

What is the glycopeptide you know

A

Vanco!

45
Q

Vanco mechanism

A

Binds D-ala-D-ala of cell wall –> no cell wall synthesis (constant remodeling)

46
Q

Vanco resistance

A
VanA gene - D-Ala-D-Lac 
- Leads to VRE
VanB-E
Thickened cell wall - vanco gets stuck there 
- VISA
47
Q

Cidal or static for vanco? IV ir PO? Concerns for dosing?

A

Cidal
Mostly IV b/c PO doesn’t penetrate GI
Renally excreted

48
Q

Vanco adverse events!

A
  1. Red Man Syndrome
  2. Nephrotoxic
  3. Ototoxic - dose dependent
49
Q

Vanco spectrum of activity

A

G+ only! w/ MRSA & anaerobes

50
Q

How are you using vanco?

A

PO for C.Diff
1st choice = B lactams, but move to vanco if:
- Resistant G+ infection
- B lactam allergy

51
Q

Cyclic lipopeptide you know

A

Daptomycin

52
Q

Dapto mechanism

A

Tail = lipophilic
Into cell membrane –> depol –> K+ efflux
Cell death w/o lysis
BACTERICIDAL

53
Q

What do you AVOID using dapto for

A

Pneumonia!

Inhibited by pulmonary surfactant - won’t work!

54
Q

Dapto adverse events

A
  1. Eosinophillic pneumonia
  2. Elevated creatinine phosphokinase test/rhabdomyolysis
    - Probably b/c dosing BID
55
Q

Dapto spectrum of activity

A

G+ ONLY

  • MRSA
  • VRE
  • Anaerobes
56
Q

Polymyxins

A

IV only
GN only
Nephrotoxic
Only use for serious GN infections that you don’t have a better option for

57
Q

Bacitracin

A

G+ only

Topical - cuts and scrapes!

58
Q

Fosfomycin

A

Oral powder

UTI only