Antibacterial Agents

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Antibacterial Agents
2011-09-19 02:08:18
Antibacterial Agents

Antibacterial Agents
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  1. What is the MOA of beta-lactams?
    • bactericidal
    • Penicillin-binding proteins (PBP) make up the cell
    • bind to (PBP)
    • inhibit cell wall synthesis
  2. What is penicillinase-resistant penicillins?
    have substitutions to the beta-lactam ring that sterically inhibit penicillinase
  3. Which Penicillins are given IV?
    • Pen G
    • Nafcillin
    • Oxacillin
    • Ampicillin (also oral)
    • Ticarcillin
    • Piperacillin
    • Unasyn (Amp/sulbactam)
    • Timentin (Ticarcillin/clavulanate)
    • Zosyn (Pip/tazobactam)
  4. Which Penicillins are given PO?
    • Pen VK
    • Dicloxacillin
    • Amoxicillin
    • Ampicillin (IV also)
    • Carbenicillin (only used for UTIs)
    • Augmentin (Amox/clavulanate)
  5. Which Penicillins are given IM?
    • benzathine Pen G
    • procaine Pen G
    • Pen G benzathing + Pen G procaine
  6. What are the natural penicillins?
    • Pen G (and all variations)
    • Pen VK (Veetids)
  7. What are the spectrum of activity for natural PCNs?
    • Streptococcus pyogenes
    • Streptococcus pneumoniae
    • Streptococcus viridans
    • Clostridium perfringes (gas gangrene)
  8. Why are natural PCNs are ineffective against staphylococcus aureus?
    because they are readily hydrolyzed by penicillinases (Beta-lactamases) to become resistant to penicillin
  9. Which natural PCN are more active toward Gram-negative organisms?
    Pen G is 5-10x more active than Pen V
  10. What are the penicillinase-resistant penicillins or antistaphylococcal penicillins?
    • methicillin
    • nafcillin
    • oxacillin
    • dicloxacillin
  11. What are the spectrum of activity for penicillinase-resistant penicillins/antistaphylococcal penicillins?
    • MSSA
    • streptococci (but not enterococci)
  12. What are the extended-spectrum aminopenicillins?
    • ampicillin
    • amoxicillin (Trimox, Amoxil)
  13. What are the extended-spectrum antipseudomonal penicillins?
    • carbenicillin
    • ticarcillin
    • piperacillin
  14. What are the beta-lactamase inhibitors?
    • clavulanic acid
    • sulbactam
    • tazobactam
  15. What are the beta-lactam/beta-lactamase inhibitor combinations?
    • Augmentin (amoxicillin clavulanate)
    • Unasyn (ampicillin sulbactam)
    • Timentin (ticarcillin clavulanate)
    • Zosyn (piperacillin tazobactam)
  16. What are the main coverage of Augmentin & Timentin?
    • H. flu
    • Moraxella catarrhalis
    • Klebsiella pneumonia
    • MSSA
    • Anaerobes
  17. How are beta-lactam/beta-lactamase inhibitors formulated?
    • amount of beta-lactam changes as dose increases
    • amount of beta-lactamase is constant
    • 2x250 does not equal 1x500, the inhibitor concentration would be too high = more SE
  18. How are Penicillins eliminated?
    • renally: glomerular filtration and active tubular secretion
    • Oxacillin (renal and bile)
    • Nafcillin (bile)
  19. What type of killing do Penicillins posess?
    time-dependent killing
  20. What are the SE of Penicillins?
    • NVD (infectious and non-infectious D)
    • hypersensitivity
    • anemia
    • decreased platelets
    • increased INR
    • acute interstitial nephritis (methicillin, nafcillin)
    • excess sodium load (ticarcillin worst)
    • excess potassium load (Pen G)
    • superinfection
  21. What pregnancy class are Penicillins?
    • class B
    • DOC in pregnancy
  22. What are the DI of Penicillins?
    • oral contraceptives (use condoms for 1 wk after antibiotics)
    • warfarin (increased INR d/t loss of gut flora)
  23. What is the MOA of cephalosporins?
    • bactericidal
    • inhibition of mucopeptide synthesis in bacterial cell wall
    • cause cell wall lysis
  24. How are cephalosporins dosed?
    • IV
    • PO
    • IM
  25. How are cephalosporins grouped?
    grouped into generations based on their antimicrobial coverage
  26. What cephalosporins are 1st generation?
    • cefazolin (Ancef)
    • cephalexin (Keflex)
    • cefadroxil (Duricef)
  27. Which 1st generation cephalosporins are given PO?
    • cephalexin (Keflex)
    • cefadroxil (Duricef)
  28. What are the groups of microorganisms that 1st generation cephalosporins cover?
    Gram (+) more than Gram (-)
  29. What cephalosporins are 2nd generation?
    • cefoxitin (Mefoxin)
    • cefuroxime (Zinacef)
    • cefotetan (Cefotan)
    • cefaclor (Ceclor)
    • cefprozil (Cefzil)
  30. Which 2nd generation cephalosporins are dosed PO?
    • cefaclor (Ceclor)
    • cefprozil (Cefzil)
  31. Which 2nd generation cephalosporins are dosed both IV & IM?
    • cefuroxime (Zinacef)
    • cefotetan (Cefotan)
  32. What cephalosporins are 3rd generation?
    • cefdinir (Omnicef)
    • ceftriazone (Rocephin)
    • ceftazidime (Fortaz)
    • cefotaxime (Claforan)
  33. Which 3rd generation cephalosporins are dosed PO?
    cefdinir (Omnicef)
  34. Which 3rd generation cephalosporins are dosed IV & IM?
    • ceftriazone (Rocephin)
    • ceftazidime (Fortaz)
  35. What cephalosporins are 4th generation?
    • cefepime (Maxipime)
    • IV & IM
  36. What cephalosporins are 5th generation?
    • ceftaroline (Teflaro)
    • IV only
  37. What kind of killing does cephalosporins possess?
    • time-dependent killing
    • above the MIC
  38. Which cephalosporins are good for anaerobes?
    • cefoxitin (Mefoxin)
    • cefotetan (Cefotan)
  39. Which cephalosporins are good for pseudomonas?
    • ceftazidime (Fortaz)
    • cefepime (Maxipime)
  40. Which cephalosporins are good for MRSA, MRSE, and enterococcus?
    ceftaroline (Teflaro)
  41. Which cephalosporin is best for use in neonates?
    cefotaxime (Claforan)
  42. How are cephalosporins eliminated?
    • mostly renal: glomerular filtration and active tubular secretion
    • ceftriaxone (bile 30-40%)
  43. Which cephs can penetrate the CNS?
    • cefuroxime (2nd-gen)
    • cefotaxime (3rd-gen)
    • ceftriaxone (3rd-gen)
    • ceftazidime (3rd-gen)
  44. How protein bound are cephs?
    ceftriaxone is concentration dependent: increasing dose increases fraction unbound, so higher doses and longer interval is better
  45. What are the SE of cephs?
    • hypersensitivity
    • increased INR/bleeding/hypoprothrombinemia in cephs that have MTT side-chain (cefotetan)
    • NVD
    • HA
    • dizziness
    • neurotoxicity (high dose in renal impaired)
    • bilirubin encephalopathy (ceftriaxone - highly PPB)
  46. Which ceph should not be used in neonates?
    ceftriaxone displaces bilirubin
  47. What are the DI of cephs?
    do not administer ceftriaxone with calcium-containing IV fluids in neonates (increased risk of precipitation)
  48. How can bacteria becomes immune or resistance to cephalosporins?
    through the production of beta-lactamases