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Pharmacology Antimicrobials > Beta Lactams > Flashcards

Beta Lactams Flashcards

1
Q

Narrow Spectrum, penicillinase-susceptible penicillins

A

Penicillin G, Penicillin V

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2
Q

Narrow spectrum penicillin resistant organisms

A
  • Most Staph aureus strains

- Many Neisseria gonorrhoeae strains

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3
Q

Very narrow spectrum (anti-staphylococcal), penicillinase-resistant penicillins

A

Methicillin
Oxacillin
Nafcillin

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4
Q

Very narrow spectrum penicillin resistant organisms

A

MRSA

PRSP

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5
Q

Wider spectrum, penicillinase-susceptible penicillins

A 
Piperacilin
Ampicillin
Ticarcillin
Amoxicillin
(fat pata)
-use with beta-lactamase inhibitors
-synergistic w/ aminoglycosides
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6
Q

Enterococcal & listerial infection treatments

A

Ampicillin/aminoglycosides

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7
Q

PCN + Beta-lactamase inhibitors

A

Amox + Clavulanic acid (Augmentin)
Ampi + Sulbactam (Unasyn)
Piper+ Tazobactam (Zosyn)
Ticar + Clavulanic acid (Timentin)

AC, AS, PT, TC

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8
Q

PCN mechanisms of resistance

A

1) Beta lactamase (staph, gram-)
2) PBP modification (MRSA, MRSE, PRSP, eterococci)
3) Changes in Porin (gram-…P. aeruginosa)
4) Efflux pump (salmonella typhimurium)

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9
Q

Cephalosporin mechanisms of resistance

A

1) beta lactamases (less susceptible to staph penicillnases than PCN)
2) PBP modification (MRSA, PRSP)
3) Decrease in drug permeability

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10
Q

1st Generation Cephalosporins

A

Cefazolin
Cephalexin
Cefadroxil

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11
Q

2nd Generation Cephalosporins

A 
Cefaclor
Cefotetan
Cefamandole
Cefoxitin
Cefuroximea
Cefuroxime Axetil
Cefproxil
Loracarbef
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12
Q

3rd Generation Cephalosporins

A 
Cefotaxime
Cefixime
Cefoperazone
Ceftriaxone
Ceftazidime
Cefpodoxime
Cefdinir
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13
Q

4th Generation Cephalosporin

A

Cefepime

Gram + and Gram - coverage

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14
Q

Patterns of cephalosporins from 1st to 3rd generations

A
  • Decrease Gram+ coverage
  • Increase Gram - coverage
  • Increase CNS penetration
  • Increase resistance to B-lactamase
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15
Q

Monobactam

A

Aztreonam

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16
Q

Monobactam coverage

A
  • certain Gram - rods (resistant to B-lactamases produced by rods) including Pseudomonas
  • NO activity against gram + or anaerobes
  • Synergistic w/ aminoglycosides
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17
Q

Carbapenems

A

Imipenem
Meropenem
Ertapenem
Doripenem

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18
Q

Carbapenem coverage

A

-Broadest spectrum of all antibiotics!
> G+ cocci (staph/strep), G- rods (pseudomonas), anaerobes
> resistant to most B-lactamases, but susceptible to METALLO-B-LACTAMASE

-No coverage against:
MRSA, Listeria Monocytogenes, some enterococci, few hospital-strain Gram-
-Ertapenem: low Pseudomonas activity!

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19
Q

B-lactamase Inhibitors

A

Clavulanic acid (w/ Amox & Ticar)
Sulbactam (w/ Ampi)
Tazobactam (w/ Pipera)

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20
Q

MRSA & PRSP Treatment

A

Vancomycin: no B-lactam ring, no binding to PBP

|&raquo_space;PRSP: Vanco + 3G Ceph

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21
Q

Vancomycin coverage

A
  • Active against Gram (+)…MRSR, PRSP

- No coverage against Gram (-), can’t penetrate cell membrane

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22
Q

PCN, Cephalosporin Mechanism of Action

A
  • Bind to PBP b/c they are D-Ala-D-Ala analogs
  • Inhibit transpeptidase (comp. inhibitor)–> inhibit cell wall synth
  • Activate autolysins (bac enzyme that cause lesions in cell memb and wall)
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23
Q

Monobactam, Carbapenem Mechanism of Action

A

-Binds to PBP (PBP3 for monobactam)

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24
Q

Vancomycin Mechanism of Action

A
  • Binds to D-Ala-D-Ala terminus of nascent peptidoglycan pentapeptide
  • Inhibits transglycosylase, sterically hinders ELONGATION of peptido & cross-linking
  • Damages cytoplasmic memb
  • CIDAL for dividing orgs
  • can’t penetrate complex Gram - cell walls
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25
Q

Vancomycin Mechanism of Resistance

A
  • D-Ala-D-Ala modification (VRE, VRSA)

- Change in drug permeability

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26
Q

Daptomycin coverage

A

VRE
VRSA
>CIDAL for Gram+….act on cell memb
> INACTIVE against Gram -

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27
Q

Daptomycin considerations

A 
-Renal elimination
>monitor Creatine phosphokinase activity to watch out for myopathy, esp w/ statins
-Long 1/2 life (9hrs) -->once a day
-predominantly cleared by kidney
-long post-antibiotic effect
-concentration-dependent killing
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28
Q

Fosfomycin Mechanism of Action

A

-Antimetabolite inhibitor of cytosolic enolpyruvate transferase
> prevent N-acetylmuramic acid formation–> block peptido chain formation

29
Q

Fosfomycin Mechanism of Resistance

A

-Decreased intracellular accumulation

30
Q

Fosfomycin Indication

A

-UTI: excreted by kidney & urinary levels exceed MICs for many UTI pathogens

31
Q

Parenteral Cephalosporins

A

1: Cefazolin
2: Cefoxitin, Cefotetan, Cefuroxine
3: Cefaperozone, Ceftriaxone, Ceftazidime, Cefotaxime
4: Cefepime
5: Ceftaroline

32
Q

Oral Cephalosporins

A

1: Cefalexin, Cefadroxil
2: Cefuroxime Axetil, Cefaclor, Cefprozil, Loracarbef
3: Cefpodoxime, Cefdinir, Cefixime

33
Q

Cephalosporin clearance

A

All renal, except for three 3rd gens
Cefotaxime, Cefoperazone (hepatic + renal)
Cefotriaxone (hepatic)

34
Q

Cephalosporins w/ CNS coverage

A

2: Cefuroxine
3: Cefotaxime, Ceftriaxone, Ceftazidime
4: Cefepime

35
Q

Cephalosporins with long half-lives

A

Ceftriaxone (8hours), Cefotetan (3.5)

All others are ~1-2 hrs mostly

36
Q

Ceftaroline Coverage

A

-MRSA, Enterococci!!
(but still NO LISTERIA!)
-Other Strep, Staph
-H.Flu

37
Q

Cefepime Coverage

A

-Strep, Staph
-H.Flu
-Pseudomonas
-Other Gram-
Very broad spectrum: almost everything except ANAEROBES, ENTEROCCI, LISTERIA, and MRSA

38
Q

Cefazolin Coverage

A

Notable for non-MRSA Staph, Strep

> DOC for surgical prophylaxis

39
Q

Cefuroxime Coverage

A
  • Notable for non-MRSA Staph, strep

- Other Gram - (non pseudomonas)

40
Q

Cefoxitin/Cefotetan Coverage

A

Notable for Bacteroides

41
Q

Cefotaxime, Cefitriaxone Coverage

A

Notable for Other Gram -

42
Q

Ceftazidime Coverage

A

Notable for Pseudomonas

43
Q

Cephalosporins that cover Pseudomonas

A

3: Cefoperazone, Ceftazidime
4: Cefepime

44
Q

Cephalosporins that cover Bacteroides

A

2: Cefoxitin, Cefotetan
3: Cefotaxime, Ceftriaxone, Cefoperazone, Ceftazidime
4: Cefepime

45
Q

Tx for Serious Adult Bacterial Pneumonia (except pseudomonas, hospital strains)

A

Cefuroxime

46
Q

Tx for Serious Pediatric Bacterial Pneumonia

A

Cefuroxime

|&raquo_space;CSF penetration protects against meningitis

47
Q

Tx for infections due to combo of anaerobes and community aerobic orgs

A

Cefoxitin and Cefotetan

> Cefotetan has longer half-life

48
Q

Tx for respiratory infections where H. flu and Moraxella suspected (outpatient)

A

Oral 2nd generation cephalosporins

49
Q

Tx for hospital-acquired Gram - (except Pseudomonas)

A

3rd Gen cephalosporins

May need to use w/ clindamycin or metroidazole (effective against anaerobes)

50
Q

DOC for Menigitis (and pneumonia w/ same orgs)

A

Ceftriaxone and Cefotaxime

51
Q

Tx for “hospital-acquired” Gram - INCLUDING pseudomonas

A

Ceftazidime–should be combined w/ aminoglycosides

52
Q

Back-up drugs for respiratory infections and UTI

A

Oral 3rd Gen cephalosporins

53
Q

Tx for skin & soft tissue infections

A

Ceftaroline

54
Q

Tx for community onset pneumonia

A

Ceftaroline: covers strep pneumo and common Gram -, but NOT pseudomonas

55
Q

Monobactam/Carbanepem administration and clearance

A

All given IV and cleared renally

56
Q

This drug combination blocks action of dipeptidase in renal tubule and allows for reasonable urinary concentration in active drug

A

Imipenem-Cilastatin

57
Q

Carbapenem with longest half-life

A

Ertapenem: 4 hours (good for outpatient IV)
Other Carbapenems are 1hr
Aztreoname (monobactam): 1.7hr

58
Q

Aztreonam traits

A
  • Used to treat serious Gram - infections
  • LIttle cross allergenecity with penicillins and cephalosporins
  • Avoids risk of nephrotoxicity from aminoglycosides
59
Q

Carbapenem traits

A
  • May have cross-allergenicity w/ penicillins and cephalosporins
  • “Shotgun” use, but should be replaced with narrow spectrum when possible
60
Q

Toxicities common to cephalosporins, aztreonams, and carbapenems

A
  • GI: Nausea, diarrhea, colitis
  • Allergic
  • Hematologic: neutropenia, hemolytic anemia (rare)
  • Renal: interstitial nephritis (rare)
  • SUPERINFECTION
61
Q

Cefotetan and Cefoperazone unique toxicities

A

Antabuse-like reactions to alcohol

62
Q

Imipenem unique toxicity

A

Occationally precipitates seizures in elderly or those w/ impaired renal function

63
Q

Ceftriaxone unique toxicity

A

More frequent diarrhea and can cause biliary “sludge”… avoid in infants!

64
Q

Vancomycin pharmacokinetics

A
  • Low oral absorption
  • Painful IM, but given IV
  • T 1/2=6 hrs; 9 hrs w/ renal failure
  • Excreted renally–glom filtration
  • wide distribution, except CNS, EYE, and PROSTATE
65
Q

Vancomycin coverage

A
  • All Gram + (except VRE)

- No activity against Gram -

66
Q

Tx for pseudomembranous colitis

A

ORAL Vancomycin

67
Q

Vancomycin Toxicity

A

Dose-related toxicities:

  • Mild nephrotoxicity (bad if combined w/ aminoglycosides)
  • Ototoxicity–Cochlear
  • *Must measure peak & trough blood levels and renal fxn during therapy

-Hypersensitivity
>”RED NECK” Syndrome (from Histamine)–> give slowly to avoid

68
Q

Televancin differences to Vancomycin

A
  • Greater activity against resistant S. aureus
  • Longer 1/2 life (8 hours)
  • More nephrotoxic
  • Contraindicated in preg
  • Freq nausea and tasts perversion
69
Q

Daptomycin inactivation

A

In lung by surfactant

|&raquo_space; can’t use for pneumonia!

Pharmacology Antimicrobials (4 decks)

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