Antibiotic Overview

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Antibiotic Overview
2011-01-21 04:06:48
Antibiotic Overview PHPR523

Antibiotic Overview
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  1. What is the MOA of beta-lactams?
    • bactericidal
    • bind to penicillin-binding proteins (PBP)
    • inhibit cell wall synthesis
  2. What Penicillins are given IV?
    • Pen G
    • Nafcillin
    • Oxacillin
    • Ampicillin (also oral)
    • Ticarcillin
    • Piperacillin
    • Unasyn (Amp/sulbactam)
    • Timentin (Ticarcillin/clavulanate)
    • Zosyn (Pip/tazobactam)
  3. What Penicillins are given PO?
    • Pen VK
    • Dicloxacillin
    • Amoxicillin
    • Ampicillin (IV also)
    • Carbenicillin (only used for UTIs)
    • Augmentin (Amox/clavulanate)
  4. What Penicillins are given IM?
    • benzathine Pen G
    • Procaine Pen G
    • Pen G benzathing + Pen G procaine
  5. What are the natural penicillins?
    • Pen G (and all variations)
    • Pen VK
  6. What are the penicillinase-resistant antistaphylococcal penicillins?
    • methicillin
    • nafcillin
    • oxacillin
    • dicloxacillin
  7. What are the extended-spectrum aminopenicillins?
    • ampicillin
    • amoxicillin
  8. What are the extended-spectrum antipseudomonal penicillins?
    • carbenicillin
    • ticarcillin
    • piperacillin
  9. What are the beta-lactam/beta-lactamase inhibitor combinations?
    • Augmentin (amoxicillin clavulanate)
    • Unasyn (ampicillin sulbactam)
    • Timentin (ticarcillin clavulanate)
    • Zosyn (piperacillin tazobactam)
  10. 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
  11. How are Penicillins eliminated?
    • renally: glomerular filtration and active tubular secretion
    • Oxacillin (renal and bile)
    • Navcillin (bile)
  12. What type of killing do Penicillins posess?
    time-dependent killing
  13. 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
  14. What pregnancy class are Penicillins?
    • class B
    • DOC in pregnancy
  15. What are the DI of Penicillins?
    • oral contraceptives (use condoms for 1 wk after antibiotics)
    • warfarin (increased INR d/t loss of gut flora)
  16. How are cephalosporins dosed?
    • IV
    • PO
  17. Which cephalosporins are dosed PO?
    • cephalexin
    • cefadroxil
    • cefaclor
    • cefuroxime axetil
    • cefprozil
    • cefixime
    • cefpodoxime proxetil
    • ceftibuten
    • cefdinir
    • cefditoren pivoxil
  18. What cephalosporins are 1st generation?
    • cefazolin
    • cephalexin
    • cefadroxil
  19. What cephalosporins are 2nd generation?
    • cefoxitin
    • cefuroxime
    • cefotetan
    • cefaclor
    • cefuroxime axetil
    • cefprozil
  20. What cephalosporins are 3rd generation?
    • cefotaxime
    • cefoperazone
    • ceftizoxime
    • ceftriaxone
    • ceftazidime
    • cefixime
    • cefpodoxime proxetil
    • ceftibuten
    • cefdinir
    • cefditoren pivoxil
  21. What cephalosporins are 4th generation?
    • cefepime
    • ceftaroline fosamil
  22. Which cephalosporins are good for anaerobes?
    • cefotetan
    • cefoxitin
  23. Which cephalosporins are good for pseudomonas?
    • ceftazidime
    • cefepime
  24. Which cephalosporins are good for MRSA, MRSE, and enterococcus
    ceftaroline fosamil
  25. Which cephalosporin is best for use in neonates?
  26. How are cephalosporins eliminated?
    • mostly renal: glomerular filtration and active tubular secretion)
    • cefoperazone (bile 70%)
    • ceftriaxone (bile 30-40%)
  27. How well do cephs penetrate the CNS?
    • cefuroxime
    • cefotaxime
    • ceftriaxone
    • ceftizoxime
    • ceftazidime
  28. How protein bound are cephs?
    ceftriaxone is concentration dependent: increasing dose increases fraction unbound, so higher doses and longer interval is better
  29. What are the SE of cephs?
    • hypersensitivity
    • increased INR in cephs that have MTT side-chain (cefoperazone)
    • NVD
    • disulfiram rxn in cephs with MTT side-chain
    • HA
    • dizziness
    • neurotoxicity (high dose in renal impaired)
    • bilirubin encephalopathy (ceftriaxone - highly PPB)
  30. Which ceph should not be used in neonates?
    ceftriaxone displaces bilirubin
  31. What are the DI of cephs?
    do not administer ceftriaxone with calcium-containing IV fluids in neonates (increased risk of precipitation)
  32. Which b-lactam is the only one that is monocyclic instead of bicyclic?
  33. How is aztreonam delivered?
  34. What type of beta-lactam is aztreonam?
    a monobactam
  35. How is aztreonam eliminated?
  36. What are the SE of aztreonam?
    • NVD
    • hypersensitivity: not much cross-reactivity with beta-lactams (safe in PCN allergy)
  37. Which type of PCN hypersensitivity is IgE mediated?
    immediate (< 72h) (type I)
  38. Which type of PCN hypersensitivity is not IgE mediated?
    late ( > 72h) (type II, III, or IV)
  39. What is the risk of cross-reactivity between cephalosporins/carbapenems and penicillin?
    about 10%
  40. What drugs are carbapenems?
    • imipenem/cilastatin (Primaxin)
    • meropenem
    • ertapenem
    • doripenem
  41. How are carbapenems delivered?
  42. Which carbapenem is used for pediatric menengitis?
  43. How are carbapenems eliminated?
  44. How do carbapenems penetrate the CNS?
    • well
    • imipenem not used for meningitis d/t risk of neurotoxicity
  45. What are the SE of carbapenems?
    • NVD
    • phlebitis
    • HA
    • confusion
    • seizures (highest with imipenem - no meningitis)
    • hypersensitivity (cross reactive with PCN and ceph)
    • nephrotoxicity (imipenem worse than meropenem)
  46. What pregnancy class are carbapenems?
    class B (imipenem is C)
  47. What are the DI of carbapenems?
    VPA levels reduced by meropenem
  48. What drugs are aminoglycosides?
    • gentamicin
    • tobramycin
    • amikacin
    • streptomycin (TB only)
    • neomycin (hepatic coma, bowel cleansing)
  49. What is the MOA of AGs?
    • bactericidal
    • inhibits protein synthesis by binding 30s subunit of bacterial ribosomes
  50. What type of killing do AGs have?
    concentration dependent killing
  51. How well are AGs absorbed PO?
  52. How well do AGs penetrate the CNS?
  53. How are AGs eliminated?
    glomerular filtration
  54. What are the SE of the AGs?
    • neprhotoxicity (proximal tubule selective)(Black-box Warning)
    • ototoxicity (cochlear and vestibular)
    • neuromuscular blockade (rare)
    • hypersensitivity (rare)
  55. What pregnancy class are AGs?
    D (teratogenic: ototoxicity)
  56. What are the DI of AGs?
    • loops (increased otoxicity - increase monitoring)
    • neuromuscular blockers
    • other nephrotoxic drugs (increase monitoring)
  57. What drugs are fluoroquinolones?
    • norfloxacin
    • ciprofloxacin
    • ofloxacin
    • levofloxacin
    • moxifloxacin
    • gemifloxacin
  58. How are FQs delivered?
    • IV
    • PO
  59. Which FQs can only be given orally?
    • norfloxacin
    • gemifloxacin
  60. What is the MOA of the FQs?
    • inhibit DNA gyrase (Topo II)
    • bactericidal
    • some inhibit Topo IV
  61. Which FQs inhibit Topo IV?
    • 3rd gen
    • 4th gen
  62. Which FQ are second generation?
    • norfloxacin
    • ciprofloxacin
    • ofloxacillin
  63. Which FQ are third generation?
  64. Which FQ are fourth generation?
    • moxifloxacin
    • gemifloxacin
  65. Which FQ have better systemic absorption?
    second generation
  66. Which FQ have better gram-negative activity?
    2nd generation
  67. Which FQ is used for UTIs and GI infections only?
  68. Which FQ are better for gram-positive, atypical, and/or anaerobic activity?
    4th generation
  69. How do serum concentrations compare between IV and PO FQ?
    they are equal except for ciprofloxacin (80% PO)
  70. What type of elimination do FQ have?
    • renal
    • moxifloxacin (hepatic)
  71. What type of killing to FQ have?
    concentration-dependent killing
  72. What are the SE of the FQ?
    • NVD (including infectious D)
    • dizziness
    • HA
    • somnolence
    • confusion
    • seizures (rare)
    • rash (gemifloxacin - limit to 7d)
    • photosensitivity
    • crystalluria
    • cartilage malformations
    • tendonitis/rupture
    • QT prolongation
    • dysglycemia (esp with diabetes)
  73. What pregnancy class are FQ?
    • class C
    • no nursing or pediatric patients either
  74. What are the DI of FQ?
    • CYP1A2 inhibition (cipro, oflox, norflox) affects R isomer of warfarin (least active)
    • decreased absorption with multivalent cations (separate by at least 4h)
    • decreased absorption with calcium and dairy (separate by at least 2h)
    • antiarrhythmics (qt prolongation)
    • sulfonylureas (dysglycemia)
  75. What type of drug is vancomycin?
  76. How is vancomycin delivered?
    • IV
    • PO (C. diff only)
  77. What is vancomycin's MOA?
    • inhibits bacterial cell wall synthesis
    • bacteriostatic and bactericidal
  78. How well does vanco penetrate the CNS?
  79. How is vanco eliminated?
    • IV: glomerular filtration
    • PO: feces
  80. What type of killing does vanco exhibit?
    time-dependent killing
  81. What is the goal trough level for vanco?
    10-20 mcg/ml
  82. What are the SE of vanco?
    • red man's syndrome
    • nephrotoxicity
    • ototoxicity
  83. What pregnancy class is vanco?
    class C
  84. What are the DI of vanco?
    other nephrotoxic or ototoxic drugs
  85. Which drugs are macrolides?
    • azithromycin
    • clarithromycin
    • erythromycin
  86. What is the MOA for macrolides?
    • inhibit protein synthesis
    • bind 50s ribosomal subunit
    • bacteriostatic
  87. How are macrolides delivered?
    • PO
    • IV
  88. Which macrolide can only be given PO?
  89. What infections are the macrolides the DOC for?
    • CAP
    • MAC (clarith)
    • H. Pylori (Clarith)
  90. How is azithromycin distributed?
    gets into tissues very well, so low serum concentration (not good for bacteremia)
  91. How well do macrolides penetrate the CNS?
    not well
  92. How are the macrolides metabolized?
    Erythromycin is metabolized by 3A4
  93. What are the SE of macrolides?
    • NVD (take with meals)
    • rash
    • HA
    • QT prolongation
    • cholestatic hepatitis
  94. What pregnancy class are the macrolides?
    class B (clarith is C)
  95. What are the DI of macrolides?
    • inhibit 1A2 and 3A4 (eryth and clarith)
    • antiarrhythmics
  96. What kind of drug is telithromycin?
    a ketolide
  97. What is the MOA of telithromycin?
    • inhibit protein synthesis
    • bind 50s ribosomal subunit
    • bacteriostatic
  98. How is telithromycin delivered?
  99. What are the SE of telithromycin?
    • diarrhea
    • hepatotoxicity
    • QT prolongation
  100. What pregnancy class is telithromycin?
    class C
  101. What is the black-box warning associated with telithromycin?
    respiratory failure in pts with myasthenia gravis
  102. What are the DI of telithromycin?
    substrate and inhibits 3A4
  103. What is the MOA of the TCNs?
    • inhibit protein synthesis
    • bind 30 ribosomal subunit
    • bacteriostatic
  104. What are the names of the TCNs?
    • tetracycline
    • demeclocycline
    • doxycycline
    • minocycline
  105. How are the TCNs delivered?
    • PO
    • IV
  106. Which TCN can be delivered IV?
  107. What are TCNs used for?
    • DOC for Rickettsial infections, chlamydia, and Lyme disease
    • Acne vulgaris
    • CAP pts on antiarrhythmics
  108. How are TCNs eliminated?
    renal and hepatic
  109. Which TCN can be used in renal impairment?
  110. What are the SE of TCNs?
    • discoloration of bone/teeth
    • NVD
    • esophogeal ulceration
    • photosensitivity
    • hepatotoxicity
    • renal toxicity
    • vertigo (minocycline)
    • hypersensitivity (rare)
  111. What are the DI of TCNs?
    • food
    • multivalent cations (except minocycline and doxycycline)
  112. What type of drug is tigecycline?
    a glycylcycline
  113. What is the MOA of tigecycline?
    • inhibit protein synthesis
    • bind 30s ribosomal subunit
  114. How is tigecycline delivered?
  115. What pregnancy class is tigecycline?
  116. What are the SE of tigecycline?
    • NVD
    • inj site reactions
    • discoloration of teeth in peds
    • hypersensitivity if allergic to TCNs
  117. Which drugs are sulfonamides?
    • sulfasalazine
    • sulfadiazine
    • sulfisoxazole
  118. How are sulfonamides delivered?
  119. What is the MOA for sulfonamides?
    • antagonize PABA synthesis
    • bacteriostatic
  120. What is the use for sulfonamides?
    uncomplicated UTI
  121. What are the SE of sulfonamides?
    • hypersensitivity
    • photosensitivity
    • bone marrow suppression
    • kernicterus
  122. What pregnancy class are sulfonamides?
    class B (except D in 3rd trimester)
  123. What are the DI of sulfonamides?
    significant increase in INR d/t 2C9 inhibition (S isomer of warfarin) (monitor q 2-3d)
  124. What is the MOA of trimethoprim?
    • inhibits the enzyme dihydrofolate reductase (DHFR)
    • bacteriostatic
  125. What is trimethoprim used for?
  126. How is bactrim dosed?
    weight-based dosing based on trimethoprim component
  127. What is the absorption of bactrim?
    give tmp/smx as a ratio of 1:5 to achieve serum concentrations of 1:20 (synergism)
  128. What are the SE of bactrim?
    • bone marrow suppression
    • hypersensitivity
    • kernicterus
  129. What pregnancy class is bactrim?
    class C (D in 3rd trimester)
  130. What are the DI of bactrim?
    2C9 inhibition - increase INR (warfarin S isomer) (monitor q 2-3d)
  131. What drugs are lincosamides?
    • clindamycin
    • lincomycin
  132. What is the MOA for lincosamides?
    • inhibit protein synthesis
    • bacteriostatic
  133. What are lincosamides used for?
    gram-positive or anaerobic skin infections or pneumonia
  134. What are the SE for lincosamides?
    black-box warning for clindamycin causing colitis (C. diff associated diarrhea - CDAD) (treat with metronidazole)
  135. What pregnancy class are lincosamides?
    class B
  136. What is the MOA of metronidazole?
    • toxic to bacterial DNA and RNA
    • bactericidal
  137. What is metronidazole used for?
    • anaerobes
    • protozoa
    • CDAD (C.diff associated diarrhea)
  138. What type of killing does metronidazole have?
    concentration-dependent killing
  139. What are the SE of metronidazole?
    • furry tongue
    • metallic taste
    • urine discoloration (red-brown)
    • peripheral neuropathy
    • carcinogenic (Black-box warning)
  140. What pregnancy class is metronidazole?
    class B (D in first trimester)
  141. What are the DI of metronidazole?
    • alcohol (disulfuram rxn)
    • 2C9 inhibitor increases INR
  142. What is the MOA of tinidazole?
    • toxic to bacterial DNA and RNA
    • bactericidal
  143. How is tinidazole delivered?
    PO with food
  144. What is tinidazole used for?
    • anaerobes
    • protozoa
  145. What are the SE of tinidazole?
    • NVA
    • bitter taste
    • carcinogenic (black-box)
  146. What pregnancy class is tinidazole?
    class C
  147. What are the DI of tinidazole?
    • alcohol - disulfuram rxns
    • 3A4 substrate
  148. What is the MOA of rifampin?
    • inhibits DNA-dependent RNA polymerase
    • bactericidal
  149. What is rifampin used for?
    • Tx and prophylaxis of TB
    • Tx of asymptomatic carriers of N. meningitidis
    • in combo with PCN or vanco for endocarditis or osteomyelitis (synergy)
  150. What are the SE of rifampin?
    • flu-like syndrome
    • reddish-orange excretions
  151. What pregnancy class is rifampin?
    class C
  152. What are the DI of rifampin?
    1A2, 2C9, 2C10, 3A4 inducer
  153. What is the MOA of rifaximin?
    • inhibits DNA-dependent RNA polymerase
    • bactericidal
    • non-systemic
  154. What is rifaximin used for?
    traveler's diarrhea (E. coli)
  155. What pregnancy class is rifaximin?
    class C
  156. What are the DI of rifaximin?
    none clinically
  157. What is the MOA of nitrofurantoin?
    • inhibits acetyl CoA to inhibit carb metabolism
    • also inhibits cell wall synthesis
    • bacteriostatic at low dose
    • bactericidal at high dose
  158. What is nitrofurantoin used for?
  159. What are the SE of nitrofurantoin?
    • discolors urine brown
    • pulmonary toxicity
  160. What pregnancy class is nitrofurantoin?
    class B
  161. What is the MOA of chloramphenicol?
    • inhibits protein synthesis
    • bacteriostatic
  162. What is chloramphenicol used for?
    serious infections for which potentially dangerous drugs are ineffective or contraindicated when caused by susceptible strains, especially meningitis or brain abscess
  163. How well does chloramphenicol penetrate the CNS?
    very well
  164. What are the goals for chloramphenicol concentrations?
    • peak: 15-25 mcg/ml
    • trough: 5-15 mcg/ml
    • monitor CBC q 2-3d
  165. What are the SE of chloramphenicol?
    • bone marrow suppression (black box)
    • monitor q 2-3d
  166. What drugs are the streptogramins?
    quinupristin/dalfopristin (synercid)
  167. What is the MOA of synercid?
    inhibit protein synthesis
  168. How is synercid delivered?
  169. What is synercid used for?
    • serious gram-positive aerobic infections
    • reserved for vanco-resistant
  170. What are the SE of synercid?
    infusion-site rxns
  171. What pregnancy class is synercid?
    class B
  172. What are the DI of synercid?
    3A4 inhibitor
  173. What drug is an oxazolidinone?
  174. What is the MOA of linezolid?
    • inhibit protein synthesis
    • bacteriostatic
  175. What kind of killing does linezolid have?
    time-dependent killing
  176. How is linezolid delivered?
    • PO
    • IV
  177. What is linezolid used for?
    serious gram-positive aerobic infections only
  178. What are the SE of linezolid?
    thrombocytopenia (rare) (monitor CBC weekly if on longer than 2 wks)
  179. What pregnancy class is linezolid?
    class C
  180. What are the DI of linezolid?
    inhibits MAO
  181. What kind of drug is daptomycin?
    a cyclic lipopeptide
  182. What is the MOA of daptomycin?
    inhibits DNA/RNA/protein synthesis
  183. What type of killing does daptomycin have?
    concentration-dependent killing
  184. How is daptomycin delivered?
  185. What is daptomycin used for?
    • gram-positive aerobes including MRSA and VRE
    • skin infections
    • bacteremia (not pneumonia)
  186. What is an advantage of daptomycin?
    low resistance potential
  187. What are the SE of daptomycin?
    can increase CPK at high doses (monitor weekly)
  188. What pregnancy class is daptomycin?
    class B
  189. What are the DI of daptomycin?
    consider d/c statins while on daptomycin to decrease risk of myopathy
  190. What should patients be counseled on for antibiotics?
    • what the medication is and what it is for
    • how to take it
    • when to expect symptom improvement
    • need for compliance
    • SE
    • DI (esp. OC)
  191. How should antibiotic efficacy be monitored?
    • sx resolution
    • temp
    • WBC
    • compliance
    • serum drug concentrations
    • other tests (x-rays, TEE, lumbar puncture, bone scan, etc)
  192. how should antibiotic safety be monitored?
    • SE
    • DI
    • CI
    • serum drug concentrations