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
1st generation cephalosporin IV & PO forms
``` IV = Cefazolin PO = Cephalexin ```
26
1st generation cephalosporin spectrum of activity
G+ | Some G-
27
When do you use cefazolin/cephalexin?
SURG PROPHYLAXIS
28
2nd generation cephalosporin IV & PO
``` IV = Cefoxitin PO = Cefotetan ```
29
2nd generation cephalosporin spectrum of activity
G+ More G- Good anaerobic activity
30
When do you use 2nd gen cephalo?
Intra-ab surgery prophylaxis
31
3rd gen cephalosporins
IV - Ceftriaxone - Ceftazidime
32
3rd gen cephalo spectrum of activity & pros
G+ Excellent G- - Ceftazidime covers pseudo! Long half life!!!
33
When do you use ceftriaxone?
CA pneumo/meningitis | Serious inpatient infections
34
Cefepime
``` 4th gen cephalo IV only Broad - G+ - G- w/ pseudo Good b/c resistant to beta-lactamases ```
35
Ceftraroline
5th gen cephalo G+ - only one that works vs MRSA! - B/c can binds PBP2a Some G- (similar to gen 3 levels)
36
Cephalo + B lactamase inhibitors
Ceftolozane/tazobactam Ceftazidime/avibactam G- covers pseudo UTI & intra-ab infections
37
3 names of carbapenems
Imipenem Meropenem Ertapenem
38
Carbapenems spectrum of activity & clinical use
``` VERY BROAD G+ G- w/ pseudo Anaerobes Use: serious & resistant infections ```
39
How is Ertapenem's spectrum of activity different than other carbapenems?
No pseudo/acinetobacter
40
What drug should you use if penicillin allergy?
Carbapenems
41
IV form of monobactam
Aztreonam
42
Monobactam coverage
GN ONLY w/ pseudo
43
When are you using monobactam
For people with beta-lactam allergy | Unlikely to be your first choice otherwise b/c resistance & decreased efficacy
44
What is the glycopeptide you know
Vanco!
45
Vanco mechanism
Binds D-ala-D-ala of cell wall --> no cell wall synthesis (constant remodeling)
46
Vanco resistance
``` VanA gene - D-Ala-D-Lac - Leads to VRE VanB-E Thickened cell wall - vanco gets stuck there - VISA ```
47
Cidal or static for vanco? IV ir PO? Concerns for dosing?
Cidal Mostly IV b/c PO doesn't penetrate GI Renally excreted
48
Vanco adverse events!
1. Red Man Syndrome 2. Nephrotoxic 3. Ototoxic - dose dependent
49
Vanco spectrum of activity
G+ only! w/ MRSA & anaerobes
50
How are you using vanco?
PO for C.Diff 1st choice = B lactams, but move to vanco if: - Resistant G+ infection - B lactam allergy
51
Cyclic lipopeptide you know
Daptomycin
52
Dapto mechanism
Tail = lipophilic Into cell membrane --> depol --> K+ efflux Cell death w/o lysis BACTERICIDAL
53
What do you AVOID using dapto for
Pneumonia! | Inhibited by pulmonary surfactant - won't work!
54
Dapto adverse events
1. Eosinophillic pneumonia 2. Elevated creatinine phosphokinase test/rhabdomyolysis - Probably b/c dosing BID
55
Dapto spectrum of activity
G+ ONLY - MRSA - VRE - Anaerobes
56
Polymyxins
IV only GN only Nephrotoxic Only use for serious GN infections that you don't have a better option for
57
Bacitracin
G+ only | Topical - cuts and scrapes!
58
Fosfomycin
Oral powder | UTI only