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KG - Pharmacology > Cephalosporins > Flashcards

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
Q

DOC E. coli, Klebsiella, Proteus?

A

first or second generation cephalosporin

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26
Q

DOC Salmonella?

A

third generation cephalosporin

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27
Q

DOC penicillin resistant Strep pneum?

A

ceftriaxone

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28
Q

DOC Borrelia burgdorferi? (lyme dz)

A

ceftrioxone (late disease)

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29
Q

toxicity of cephalosporins?

A
  • 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)
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30
Q

characteristics of monobactams

A
  • 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)
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31
Q

list of monobactams

A

Aztreonam (Azactam) = only monobactam

32
Q

list of carbapenems

A
  • imipenem; cilastatin (primaxin)
  • meropenem (merrem)
  • ertapenem (invanz)
33
Q

characteristics of IMIPENEM & MEROPENEM (carbapenems)

A
  • given IV
  • broad spectrum activity (incl anaerobes, G+, G-
  • stable against B-lactamases
  • pseudomonas may develop resistance quickly so use w/ aminoglycosides recommended
34
Q

which carbapenem is the DOC for B-lactamase producing Enterobacter infections?

A

Imipenem or Meropenem

35
Q

Which carbapenem can cause seizures in high levels?

A

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
Q

“__________ is rapidly inactivated by renal tubule dihydropepdidases and must be given w/ ________, a dihydropeptidase inhibitor.”

A

“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
Q

characteristics of Ertapenem (carbapenem)

A
  • 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
Q

mechanism of VANCOMYCIN

A

prevents transpeptidation of peptidoglycan chain, binds to terminal D-ala-D-ala

39
Q

when to use Vancomycin?

A
  • 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
Q

what is DOC for clostridium dificil?

A

metronidazol (vancomycin not first choice)

41
Q

why is vancomycin drug of last resort for MRSA?

A

VRE - emergence of vancomycin resistant Enterococci and need for alternative MRSA treatment

42
Q

adverse effects of vancomycin?

A
  • can cause thrombophlebitis on IV injection
  • OTOTOXIC
  • NEPHROTOXIC
  • “red man syndrome” = flushing from histamine release
43
Q

mechanism of FOSFOMYCIN (monurol)

A

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
Q

characteristics of fosfomycin

A
  • 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
Q

mechanism of BACITRACIN?

A

interferes w/ final dephosphorylation step in phospholipid carrier cycle, can’t transport NAG-NAM across inner membrane

46
Q

characteristics of bacitracin

A
  • 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
Q

mechanism of CYCLOSERINE (seromycin)?

A

inhibits D-ala from being incorporated into peptidoglycan pentapeptide

48
Q

characteristics of cycloserine

A
  • second line, broad spectrum antibiotic used in treatment of active pulmonary and extra pulmonary TB & UTIs
  • can be bacteriosteric or bactericidal
49
Q

adverse effects of cycloserine

A
  • involve CNS (headache, depression, psychosis)
50
Q

what is used to treat moraxella catarrhalis? (G- cocci, aerobic)

A

TMP-SMZ, cephalosporin (2nd or 3rd gen)

51
Q

what is used to treat neisseria gonorrhoeae? (G- cocci, aerobic)

A

ceftriaxone or cefpodoxime

52
Q

what is used to treat neisseria meningitidis? (G- cocci, aerobic)

A

Pen G

53
Q

what is used to treat Enterovacter, Citrobacter, Serratia? (Gram - rods, aerobic)

A

TMP-SMZ, quinolone, carbapenem

54
Q

what is used to treat shigella? (Gram - rods, aerobic)

A

quinolone

55
Q

what is used to treat salmonella? (Gram - rods, aerobic)

A

TMP-SMZ, quinolone, cepholosporin (3rd gen)

56
Q

what is used to treat brucella species? (Gram - rods, aerobic)

A

doxycycline + rifampin or aminoglycosides

57
Q

what is used to treat helicobacter pylori? (Gram - rods, aerobic)

A

bismuth + metronidazole + tetracycline or amoxicillin

58
Q

what is used to treat psuedomonas? (Gram - rods, aerobic)

A

antipseudomonal penicillin + aminoglycoside

59
Q

what is used to treat stenotrophomonas maltophilia? (Gram - rods, aerobic)

A

TMP-SMZ

60
Q

what is used to treat legionella species?

A

azithromycin + rifampin or quinolone + rifampin

61
Q

what is used to treat Strep pneum? (Gram + cocci)

A

PCN

62
Q

what is used to treat Strep pyogenes? (Gram + cocci)

A

PCN, clindamycin

63
Q

what is used to treat Strep agalactiae? (Gram + cocci)

A

PCN (+ aminoglycoside?)

64
Q

what is used to treat viridans strep? (Gram + cocci)

A

PCN

65
Q

what is used to treat Staph aureus, B-lactamase neg? (Gram + cocci)

A

PCN

66
Q

what is used to treat Staph aureus, B-lactamase pos? (Gram + cocci)

A

PCN resistant PCN

67
Q

what is used to treat methicillin resistant? (Gram + cocci)

A

vancomycin

68
Q

what is used to treat Enterococcus species? (Gram + cocci)

A

PCN + aminoglycoside

69
Q

what is used to treat Bacillus species, non-anthracis? (Gram + rod, aerobic)

A

vancomycin

70
Q

what is used to treat listeria? (Gram + rod, aerobic)

A

Ampicillin (+ aminoglycoside?)

71
Q

what is used to treat Nocardia species? (Gram + rod, aerobic)

A

Sulfadiazine, TMP-SMZ

72
Q

What is used to treat Borrelia recurrentis? (Spirochetes)

A

doxycycline

73
Q

what is used to treat borrelia burgdorferi (early)? (Spirochetes)

A

doxycycline, amoxicillin

74
Q

what is used to treat borrelia burgdorferi (late)? (Spirochetes)

A

Ceftriaxone

75
Q

what is used to treat Leptospira species? (Spirochetes)

A

PCN

76
Q

what is used to treat Treponema? (Spirochetes)

A

PCN

KG - Pharmacology (8 decks)

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