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Cephalosporins Flashcards

1
Q

Name Beta-Lactams

A
  1. penicillins
  2. cephalosporins
  3. monobactams
  4. cardapenems
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2
Q

name other inhibitors of cell wall synthesis (NOT B-lactams)

A
  1. vancomycin
  2. phosphomycin
  3. bacitracin
  4. cycloserine
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3
Q

mechanism of action - cephalosporins?

A

activate cell wall autolytic enzymes through blocking of terminal cross-linking of peptidoglycan (will interfere w/ forming new cell walls)

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4
Q

how are cephalosporins classified?

A

semisynthetic cephalosporins for clinical use classified as:

  1. first generation
  2. second generation
  3. third generation
  4. fourth generation
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5
Q

re: cephalosporins, what do “R1” or “R2” mean?

A
  • R1 = substitutions determine degree of antibacterial activity
  • R2 = affects pharmacokinetic properties
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6
Q

to which group are cephalosporins related to CHEMICALLY?

A
  • penicillins
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7
Q

what structure do cephalosporins have?

A
  • beta lactam ring structure
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8
Q

what in cephalosportins increases resistance to beta lactamase?

A

7-methyl group

similar to penicillins, but protected from degradation by beta lactamase

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9
Q

characteristics of FIRST GEN CEPHALOSPORINS

A 
NARROW SPECTRUM CEPHALOSPORINS
- good activity against G+ bacteria 
- moderate activity against G- organisms (E coli, Kleb, Proteus)
- MOST G+ COCCI ARE SUSCEPTIBLE, MSSA! (enterococci, MRSA, S.epidermis = resistant)
- alternative for penicillin allergies
- some acid resistant
- increased b-lactamase resistance
- renal excretion
cefazolin = DOC for surgical prophylaxis
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10
Q

what is the DOC for surgical prophylaxis?

A

cefazolin

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11
Q

list first generation cephalosporins

A

CEFAZOLIN (kefzol, ancef) - IV, IM
cephalothin (keflin) - IN, IM
cephalexin (keflex) - oral

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12
Q

characteristics SECOND GEN CEPHALOSPORINS

A

INTERMEDIATE SPECTRUM CEPHALOSPORINS

  • lower activity against G+
  • somewhat INCREASED activity against G- negatives (E coli, pleb, proteus)
  • NO ANTISPEUDOMONAL activity
  • increased b-lactamase resistance
  • some acid resistant
  • mostly renal excretion
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13
Q

list second generation cephalosporins

A

CEFACLOR (ceclor) - oral
cefuroxime (zinacef) - IV, IM
cefprozil (cefzil) - oral

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14
Q

characteristics THIRD GEN CEPHALOSPORINS

A

BROAD SPECTRUM CEPHALOSPORINS

  • less active against G+ cocci
  • much more active against Enterobacteriaceae incl penicillinase producing strains
  • some active against Pseudomonas (when combined w/ aminoglycosides)
  • some acid resistant
  • increased B-lactamase resistance
  • most excreted by kidney
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15
Q

list third generation cephalosporins

A
  • CEFTRIAXONE (rocephin) - neisseria
  • Cefotaxime sodium (claforan)
  • Cefoperazone (Cefobid) - P. aeruginosa
  • Ceftazidime (fortaz)
  • Cefixime (suprax) - oral
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16
Q

list third generation cephalosporins CNS PENETRATION

A
  • CEFTRIAXONE (rocephin) - neisseria
  • Cefotasime sodium (claforan)
  • Cefoperazone (Cefobid) - P. aeruginosa
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17
Q

which third generation cephalosporin DOC for N. gonorrhoeae? (and contraindications?)

A
  • CEFTRIAXONE (rocephin) - neisseria

- not for use in neonates (bilirubin displacement)

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18
Q

which third generation cephalosporin should be avoided for use in patients with hepatic insufficiency? Why?

A
  • Cefoperazone (Cefobid) - P. aeruginosa

- metabolized by liver

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19
Q

characteristics FOUR GEN CEPHALOSPORINS

A
  • comparable to 3rd gen
  • more resistant to some B-lactamase
  • ANTIPSEUDOMONAL
  • BETTER G+ coverage
  • renal excretion
  • BROADEST COVERAGE: enterobacteriaceae, MSSA, pseudomonas
  • empirical therapy, particularly when resistance to B-lactamases are anticipated
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20
Q

list fourth generation cephalosporins

A

Cefepime (maxipime) - IV

- best overall coverage of cephalosporins (esp for G+ w/ resistance to B-lactamase)

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21
Q

characteristics of “UNNAMED” GEN CEPHALOSPORINS

A
  • FDA approved 2010
  • NO ANTIPSEUDOMONAL ACTIVITY
  • activity against G+ and G-, approved for CABP
  • renal excretion
  • MRSA & VRSA COVERAGE - ONLY BETA LACTAM ACTIVE AGAINST MRSA
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22
Q

list “unnamed” generation cephalosporins

A
  • ceftaroline fosamil (teflaro) - IV

can bind to PBP2A w/ high affinity that other beta lactams can’t bind to

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23
Q

DOC moraxella catarrhalis?

A

second or third gen cephalosporin

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24
Q

DOC neisseria gonorrhoeae?

A
  • ceftriaxone

- cefixime

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25
DOC E. coli, Klebsiella, Proteus?
first or second generation cephalosporin
26
DOC Salmonella?
third generation cephalosporin
27
DOC penicillin resistant Strep pneum?
ceftriaxone
28
DOC Borrelia burgdorferi? (lyme dz)
ceftrioxone (late disease)
29
toxicity of cephalosporins?
- fairly safe - SUPERINFECTIONS (enterococci, G- bacilli, pseudomembranous colitis or candida) - disulfiram-like run after alcohol consumption - ALLERGY (10% cross sensitivity w/ PCN), rash, urticaria, fever, eosinophilia - direct & indirect positive Coombs test - GI --> anorexia, nausea, vomiting, diarrhea - DOSE DEPENDENT RENAL TUBULAR NECROSIS (synergistic nephrotoxicity w/ aminoglycosides)
30
characteristics of monobactams
- drugs w/ monocyclic b-lactam ring - relatively resistant to b-lactamases - ACTIVE ONLY AGAINST AEROBIC G-RODS (incl pseudomonas, serratia, klebsielle, proteus) - no activity against G+ or anaerobes - parenteral admin - few side effects (phlebitis, skin rash, abnormal liver function) - no cross sensitivity w/ other b-lactams (good for PCN allergic)
31
list of monobactams
Aztreonam (Azactam) = only monobactam
32
list of carbapenems
- imipenem; cilastatin (primaxin) - meropenem (merrem) - ertapenem (invanz)
33
characteristics of IMIPENEM & MEROPENEM (carbapenems)
- given IV - broad spectrum activity (incl anaerobes, G+, G- - stable against B-lactamases - pseudomonas may develop resistance quickly so use w/ aminoglycosides recommended
34
which carbapenem is the DOC for B-lactamase producing Enterobacter infections?
Imipenem or Meropenem
35
Which carbapenem can cause seizures in high levels?
IMIPENEM - use cautiously w/ patients in renal failure, brain lesions, head trauma, hx of CNS disorders (ie: seizures) *MEROPENEM less likely to cause seizures
36
"__________ is rapidly inactivated by renal tubule dihydropepdidases and must be given w/ ________, a dihydropeptidase inhibitor."
"IMIPENEM is rapidly inactivated by renal tubule dihydropepdidases and must be given w/ CILASTATIN, a dihydropeptidase inhibitor." *MEROPENEM is not activated by dihydropeptidases and does NOT need cilastatin!
37
characteristics of Ertapenem (carbapenem)
- highly stable against B-lactamases - activity against wide variety of G+, G- and anaerobic microorganisms, particularly Enterobacteriaceae - less active against Pseudomonas (should not be used) - IV, IM admin - 95% protein binding, renal elimination
38
mechanism of VANCOMYCIN
prevents transpeptidation of peptidoglycan chain, binds to terminal D-ala-D-ala
39
when to use Vancomycin?
- against penicillin and MRSA infections - to treat G+ infections in PCN allergic pts (parenteral) (effective only G+) - to treat super infections of Staph, Clostridium dificil (even though first choice = METRONIDAZOL)
40
what is DOC for clostridium dificil?
metronidazol (vancomycin not first choice)
41
why is vancomycin drug of last resort for MRSA?
VRE - emergence of vancomycin resistant Enterococci and need for alternative MRSA treatment
42
adverse effects of vancomycin?
- can cause thrombophlebitis on IV injection - OTOTOXIC - NEPHROTOXIC - "red man syndrome" = flushing from histamine release
43
mechanism of FOSFOMYCIN (monurol)
inhibits cell wall synthesis at one of first steps in synthesis of peptidoglycan analog of phosphoenolpyruvate (prevents NAG to NAM reduction), structurally unrelated to other drugs
44
characteristics of fosfomycin
- active against both G+ and G- - oral, excreted by kidney - used for uncomplicated lower UTIs in women - combo of fosfomycin & B-lactam, amino glycoside or fluoroquinolone may be synergistic
45
mechanism of BACITRACIN?
interferes w/ final dephosphorylation step in phospholipid carrier cycle, can't transport NAG-NAM across inner membrane
46
characteristics of bacitracin
- parenteral (rare) and topical polypeptide antibiotic - active against G+ bacteria - commonly used in combo w/ neomycin & polymyxins, which are active against G- bacteria - parenteral bacitracin used rarely due to risk of NEPHROTOXICITY - usually used to prevent superficial skin/eye infections following minor injuries
47
mechanism of CYCLOSERINE (seromycin)?
inhibits D-ala from being incorporated into peptidoglycan pentapeptide
48
characteristics of cycloserine
- second line, broad spectrum antibiotic used in treatment of active pulmonary and extra pulmonary TB & UTIs - can be bacteriosteric or bactericidal
49
adverse effects of cycloserine
- involve CNS (headache, depression, psychosis)
50
what is used to treat moraxella catarrhalis? (G- cocci, aerobic)
TMP-SMZ, cephalosporin (2nd or 3rd gen)
51
what is used to treat neisseria gonorrhoeae? (G- cocci, aerobic)
ceftriaxone or cefpodoxime
52
what is used to treat neisseria meningitidis? (G- cocci, aerobic)
Pen G
53
what is used to treat Enterovacter, Citrobacter, Serratia? (Gram - rods, aerobic)
TMP-SMZ, quinolone, carbapenem
54
what is used to treat shigella? (Gram - rods, aerobic)
quinolone
55
what is used to treat salmonella? (Gram - rods, aerobic)
TMP-SMZ, quinolone, cepholosporin (3rd gen)
56
what is used to treat brucella species? (Gram - rods, aerobic)
doxycycline + rifampin or aminoglycosides
57
what is used to treat helicobacter pylori? (Gram - rods, aerobic)
bismuth + metronidazole + tetracycline or amoxicillin
58
what is used to treat psuedomonas? (Gram - rods, aerobic)
antipseudomonal penicillin + aminoglycoside
59
what is used to treat stenotrophomonas maltophilia? (Gram - rods, aerobic)
TMP-SMZ
60
what is used to treat legionella species?
azithromycin + rifampin or quinolone + rifampin
61
what is used to treat Strep pneum? (Gram + cocci)
PCN
62
what is used to treat Strep pyogenes? (Gram + cocci)
PCN, clindamycin
63
what is used to treat Strep agalactiae? (Gram + cocci)
PCN (+ aminoglycoside?)
64
what is used to treat viridans strep? (Gram + cocci)
PCN
65
what is used to treat Staph aureus, B-lactamase neg? (Gram + cocci)
PCN
66
what is used to treat Staph aureus, B-lactamase pos? (Gram + cocci)
PCN resistant PCN
67
what is used to treat methicillin resistant? (Gram + cocci)
vancomycin
68
what is used to treat Enterococcus species? (Gram + cocci)
PCN + aminoglycoside
69
what is used to treat Bacillus species, non-anthracis? (Gram + rod, aerobic)
vancomycin
70
what is used to treat listeria? (Gram + rod, aerobic)
Ampicillin (+ aminoglycoside?)
71
what is used to treat Nocardia species? (Gram + rod, aerobic)
Sulfadiazine, TMP-SMZ
72
What is used to treat Borrelia recurrentis? (Spirochetes)
doxycycline
73
what is used to treat borrelia burgdorferi (early)? (Spirochetes)
doxycycline, amoxicillin
74
what is used to treat borrelia burgdorferi (late)? (Spirochetes)
Ceftriaxone
75
what is used to treat Leptospira species? (Spirochetes)
PCN
76
what is used to treat Treponema? (Spirochetes)
PCN

KG - Pharmacology (8 decks)

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