Pharmacology Exam II

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Rx2013
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65116
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Pharmacology Exam II
Updated:
2011-02-08 21:05:44
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Cephalosporins
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Cephalosporins
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  1. Cephalosporins are a class of
    beta lactam antibiotics
  2. Advantages of cephalosporins over PCNs
    • more stable against beta lactamases
    • broad specturm
  3. cephalosporins can by hydrolyzed by
    extended specturn beta lactamases
  4. cephalosporins are not active against
    • enterococci
    • L monocytogenes
  5. cephalosporins have a similar nucleus compared to PCNs but have
    a second R group option
  6. First synthetic cephalosporin
    cefalothin
  7. Cephalosporin mechanism of action
    • disruption of synthesis of the peptidoglycan layer of bacterial cell walls (same as other beta lactams)
    • less susceptible to penicillinases
  8. cephalosporins are grouped by "generation" which distinguishes their
    antimicrobial properties
  9. First generation cephalosporins are very active against
    gram positive cocci
  10. first generation cephalosporins are not generally active against
    methicillin resistant strains of staph
  11. Each newer generation of cephalosporins contains
    a broader spectrum of action
  12. First generation cephalosporins
    • cephalothin
    • cephalexin
    • cefazolin
    • cephradine
    • cephapirin
  13. First generation cephalospoins that may be used orally
    • cephalexin
    • cephradine
    • cefadroxil
  14. urin concentrations of 1st gen ceph.
    very high
  15. tissue vs blood concentrations of 1st gen ceph.
    lower in tissues than in blood
  16. excretion of 1st gen cephs.
    • renal
    • decreased by probenecid
  17. Only first gen. cephalosporin still in use
    • cefazolin
    • 0.5g-2g q8h
  18. Dose adjustments for 1st gen. ceph must be made based on
    renal function
  19. Uses of oral 1st gen cephalosporins
    • UTI
    • Streptococcal
    • cellulitis
    • soft tissue abscess
  20. Uses of cefazolin (IV)
    • surgical prophylaxis (drug of choice)
    • staph or strep infections in pt with PCN allergy
    • cannot be used for meningitis
  21. Second generation cephalosporins
    • cefamandole
    • cefonicid
    • cefuroxime
    • cefaclor
    • cefprozil
    • and structurally related cephamycins
  22. Cephamycins
    • cefoxitin
    • cefmetazole
    • cefotetan
    • activity against anaerobes
  23. 2nd generation cephalosporin spectrum
    • greater gram negative specturm than 1st
    • more resistant to b-lactamase
    • no activity against enterococci or pseudomonas
  24. Oral 2nd gen cephalosporins
    • cefuroxime
    • cefaclor
    • cefproxil
    • loracarbef
  25. Usual dose of 2nd gen cephs
    • adult 10-15mg/kg
    • higher in children (20-40mg/kg max of 1 gram)
  26. 2nd gen Cephs are not active against PCN resistant pneumococci except
    cefuroxime
  27. Second generation cephalosporin dosing depends on
    renal function
  28. oral 2nd gen cephs active against H influenzae or Moraxella are primarily used to treat
    • sinusitis
    • otitis
    • lower RTIs
  29. 2nd gen. cephs have activity against _____ and can therefore be used to treat ____ and ____.
    • activity against anaerobes
    • peritonitis
    • diverticulitis
  30. Used to treat community aquired pneumonia
    cefuroxime
  31. Cefuroxime should not be used to treat
    meningitis
  32. 3rd generation cephalosporins
    • cefoperazone
    • cefotaxime
    • ceftriaxone
    • ceftazidime
    • ceftizoxime
    • cefixime
    • cefpodoxime
    • cefdinir
  33. 3rd gen cephs have _____ when compared to 2nd generation
    expanded gram negtative coverage
  34. 3rd gen cephs are effective against
    b-lactamase producing strains of haemophilus and neisseria
  35. Only two drugs with useful activity against P aeruginosa (pseudomonas)
    • ceftazidime
    • cefoperazone
  36. achieve leves in CSF to inhibit most pathogens influding gram-negative rods except pseudomonas
    3rd generation cephalosporins
  37. Only 3rd gen cephs that do not require renal dosing
    • cefoperazone
    • ceftriaxone
  38. 3rd gen cephs should be avoided in treatment of
    enterobacter (emergence of resistance)
  39. Approved for treatment of meningitis except that caused by l monocytogenes
    • ceftriaxone
    • cefotaxime
  40. Clinical uses of Ceftriaxone and Cefotaxime
    • meningitis + vancomycin
    • treatment of sepsis of unknown cause
    • used in neutropenic immunocomprimised pt + aminoglycoside
    • treating hospital aquired infections
  41. Only recommended treatmenf for gonorrhea in the US
    • ceftriaxone
    • cefixime
  42. 4th generation cephalosporins
    • cefepime
    • cefluprenam
    • cefoselis
    • cefozopran
    • cefpirome
    • cefquinome
  43. Fourth Gen Cephalosporins
    • extended spectrum
    • greater b-lactamase resistance
    • can cross BBB
    • used in Pseudomonas aeruginosa
    • more resistance to lactamases produced by enterobacter
  44. Cefepime uses
    • pseudomonas
    • enterobacter
    • haemophilus
    • neisseria
    • penetrates CSF
  45. B-lactam antibiotics with activity against MRSA
    • currently under development
    • ceftaroline fosamil
    • ceftobiprole medocaril
    • increased PCN binding protein 2a
  46. Common ADRs with cephalosporins
    • diarrhea
    • nausea
    • rash
    • electrolyte disturbance
    • pain at injection site
  47. Infrequent ADRs with cephalosporins
    • vomiting
    • headache
    • dizziness
    • candidiasis
    • pseudomembranous colitis
    • eosinophilia and or fever
  48. Cephalosporin allergies
    hypersensitivity reactions identical to those of PCN
  49. Some patients with PCN allergy can tolerate cephalosporins, pt with history of anaphylaxis to PCN should _____
    not take cephalosporins
  50. Toxicities of cephalosporins
    • thrombophlebitis
    • interstitial nephritis (renal) or tubular necrosis
  51. Drug withdrawn from market due to tubular necrosis
    cephaloridine
  52. Cephalosporins containing a methylthiotetrazole group frequently cause ____. Can be avoided with the use of ____.
    • hypoprothrombinemia
    • bleeding disorders
    • disulfiram like reactions
    • vitamin K 10mg 2x weekly (for bleeding)

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