cephalosporin activity/SE

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Author:
jliles
ID:
32993
Filename:
cephalosporin activity/SE
Updated:
2010-09-06 13:49:36
Tags:
cephalosporins
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For quiz #2
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  1. cephalexin (Keflex)
    • 1st generation
    • po only
  2. cephadroxil (Duracef)
    • 1st generation
    • po only
  3. cephazolin (Ancef)
    • 1st generation
    • IV only
  4. 1st generation Spectra of Activity
    • Good Gram + activity (resistant to B-lactamases)
    • Limited Gram - activity (covers some enteric bacilli, poor B-lactamase resistance)
    • Anaerobe activity limited to PCN susceptible strains (in oropharnyx)
  5. 1st Generation pharmacokinetics
    • High bioavailability of oral agents (food doesn't affect abs)
    • Good distribution throughout body but little CNS penetration
    • Primarily renally eliminated
    • Short half-life
  6. cefaclor (Ceclor)
    • 2nd generation
    • po only
  7. cefprozil (Cefzil)
    • 2nd generation
    • po only
  8. cefuroxime (Zinacef)
    • 2nd generation
    • IV
  9. cefoxitin (Mefoxin)
    • 2nd generation
    • IV only
  10. cephalothin (Keflin)
    • 1st Generation
    • IV only
  11. 2nd generation pharmacokinetics
    • Good oral bioavailability
    • (Cefuroxime axetil should be given w/ food)
    • Good distribution (only cefuroxime penetrates CNS)
    • Renally eliminated
  12. 2nd generation Spectrum of Activity
    • Gram + aerobes: not as active as 1st gen, primarily streptococci and staphylococci activity
    • Gram - aerobes: Improved activity from 1st gen against enteric bacilli (E.coli, Klebsiella, Enterobacter, Proteus)
    • Good activity against some B-lactamase producers (Haemophilus, Moraxella)
    • Anaerobes: limited overall. Exception: cephamycins (cefoxitin, cefotetan, cefmetazole)
  13. cefdinir (Omnicef)
    • 3rd generation
    • po only
  14. ceftriaxone (Rocephin)
    3rd generation (IV)
  15. ceftibuten (Cedax)
    • 3rd generation
    • po only
  16. ceftazidime (Fortaz)
    • 3rd generation
    • IV only
  17. 3rd generation pharmacokinetics
    • Good bioavailability of oral agents
    • (cefpodoxime & cefditoren should be given with food)
    • Good distribution throughout body (CNS penetration)
    • Primarily renally eliminated (except ceftriaxone & cefoperazone- 30-45% renal, remainder in bile)
  18. 3rd generation Spectrum of Activity
    • Gram+ aerobes: primarily streptococci and staphylococci, less active than other generations.
    • Gram- aerobes: Active against wide variety of organisms but still subject to inactivation by B-lactamases. (Excellent against Enterobacteriacae, Haemophilus, Moxarella, Neisseria)
    • Ceftazidime good against pseudomonas
    • Anaerobes: Limited to oropharyngeal strains
  19. cefepime (Maxipime)
    • 4th generation
    • IV only
  20. 4th generation Spectrum of Activity
    • Good Gram+ activity.
    • Excellent Gram- activity, inc pseudomonas aeruginosa
    • More stable against B-lactamases especially those made by enterobacteriaceae.
  21. 4th Generation pharmacokinetics
    • IV only- 100% bioavailability
    • Good CNS penetration
    • Short half-life
  22. Cephalosporin Adverse Effects
    • GI: n/v, abd pain, diarrhea
    • Skin: rash
    • CNS: stimulatory (tremors, insomnia, seizures)
    • Neutropenia, thrombocytopenia
    • Hypersensitivity in 1-3% pts
    • Ceftriaxone- billiary sludging
    • Agents w/NMTT side chain- hypoprothombinemia, disulfiram-like rxn (cefoperazone, cefmandole, cefotetan, cefmetazole)
    • C.diff, superinfection

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