ICARE: ID FINAL Antibiotics

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VASUpharm14
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189209
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ICARE: ID FINAL Antibiotics
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2012-12-13 00:17:57
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FINAL! good luck!!!
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  1. 4 MOA of antibiotics
    • 1) inhibition of cell wall synthesis
    • 2) inhibition of ribosomal protein synthesis
    • 3) inhibition of folate (RNA purines)
    • 4) inhibition of DNA synthesis
  2. MOA beta lactams
    inhibits cell wall synthesis by binding to PBPs
  3. 4 classifications of penicillins
    • 1) natural penicillins
    • 2) penicillinase-resistant penicillins
    • 3) aminopenicillins
    • 4) beta-lactam/beta-lactamase inhibitors
  4. 2 natural penicillin drugs and dosage forms
    • 1) pen G - IV
    • 2) pen VK - PO
  5. 3 clinical uses of natural penicillins
    • 1) strep infections
    • 2) syphilis
    • 3) dental infections
  6. natural penicillins - spectrum 
    • narrow
    • gram + , some gram - (not that good), anaerobes, spirochetes
  7. elimination of natural penicillins
    renally
  8. Penicillinase - resistant penicillins (antistaph)
    3 agents + dosage form
    • NOD
    • nafcillin (Unipen) - IV
    • oxacillin  - IV
    • dicloxacillin (Diclox) - PO
  9. penicillinase-resistant penicillins (antistaph)
    spectrum
    • beta-lactamase staph a. - best for cellulitis
    • NOT mrsa
    • strep (but not as well as PCN)
  10. aminopenicillins
    2 agents + dosage form
    • 1. ampicillin - po/iv
    • 2. amoxicillin - po
  11. aminopenicillins
    spectrum
    more gram NEGATIVE 
  12. aminopenicillins
    clinical uses
    • 1) acute OTITIS MEDIA
    • 2) bacterial sinusitis
    • 3) prophylaxis endocarditis before DENTAL procedures
  13. beta lactam/lactamase inhibitors
    4 agents + dosage form
    • 1) amoxicillin/clavulanic acid (Augmentin) PO
    • 2) ampicillin/sulbactam (Unasyn) IV
    • 3) ticarcillin/clavulanic acid (Timentin) IV
    • 4) pipercillin/tazobactam (Zosyn) IV
  14. 9 beta-lactamase producing organisms
    • gram -  = HNM PEK
    • Haemoph, N. Gonnor, Morexalla, proteus, ecoli, klebsiella
    • gram + = staph a
    • anaerobes = bacteriodes
  15. Sinusitis tx
    • Augmentin  - PO
    • amoxicillin/clavulanic acid
  16. IV equivalent of Augmentin
    • Unasyn - IV
    • ampicillin/sulbactam
  17. beta-lactamase inhibitors
    cover PSEUDO
    • 1. ticarcillin/clavulanic (Timentin) - IV
    • 2. pipercillin/tazobactam (Zosyn) - IV

    also aspiration pneumonia (covers anaerobe bacteroides)
  18. Adverse Drug reactions***
    penicillins
    • Hypersensitivity
    • - rash,pruritis

    penicillin --> degraded --> penicilloic acid, or forming antigens --> antibody formation
  19. ADR
    penicillin
    hypersensitive - 3 options
    • 1) alternative antibiotic
    • 2) skin testing - major and minor antigenic determinants
    • 3) desensitization - gradual increasing doses of penicillin
  20. # generations of cephalosporins
    5
  21. cephalosporins
    coverage
    gram NEGATIVE coverage INCREASES , except ceftaroline
  22. cephalosporins are INACTIVE against
    • AtLE
    • atypicals
    • listeria
    • enterococcus
  23. listeria for, age group, and tx
    • meningitis
    • young and elderly
    • ampicillin
  24. MTT side chain
    • 2nd gen
    • cefotetan (TT)
    • - bleeding and disulfiram (no alcohol)
  25. 1 st gen cephalosporins (3) + dosage form
    • 1. cefazolin (Ancef/Kefzol) - IV
    • 2. cephalexin (Keflex) - PO
    • 3. cefadroxil (Duricef) - PO
  26. 2nd gen cephalosporins (6) + dosage forms
    • 1. cefoxitin (Mefoxin) - IV
    • 2. cefuroxime (Zinacef) - IV, (ceftin) - PO
    • 3. cefotetan (Cefotan) - IV
    • 4. cefaclor (Ceclor) - PO
    • 5. cefprozil (Cefzil) - PO
    • 6. loracarbef (Lorabid) - PO
  27. 3 rd gen cephalosporins (9) + dosage forms
    • 1. cefotaxime (Claforan) - IV
    • 2. ceftizoxime (Cefizox) - IV
    • 3. ceftazidime (FORTAZ) - IV PSEUDO
    • 4. cefibuten (Cedax) - PO
    • 5. cefdinir (Omnicef) - PO
    • 6. cefpodoxime (Vantin) - PO
    • 7. Ceftriaxone (Rocephin) - IV
    • 8. cefixime (Suprax) - PO
    • 9. cefditoren (Spectracef) - PO
  28. cephalosporin
    PSEUDO coverage
    ceftazidime - Fortaz - IV
  29. 4th gen cephalosporin (1) + dosage form
    cefepime (Maxipime) - IV
  30. 4th gen cephalosporin
    spectrum
    • improved +, - and PSEUDO
    • cefepime (Maxipime) - IV
  31. 4th gen PSEUDO
    cefepime (Maxipime) - IV
  32. 5th gen cephalosporin (1) + dosage form
    ceftaroline (Teflaro) - IV
  33. 5th gen cephalosporin
    spectrum + indication
    • MRSA
    • gram positive, negative
    • indication: skin structure infections 
    • CAP - Mssa only and others
  34. Carbapenems (4) + dosage forms
    • DIME (DIM/E) - GORILLA-cillins
    • 1) imipenem/cilastatin (Primaxin) - IV
    • 2) meropenem (Merrem) - IV
    • 3) ertapenem (Invanz) - IV
    • 4) doripenem (Doribax) - IV
  35. Carbapenems 
    spectrum
    • PAN coverage 
    • positive
    • negative
    • anaerobes
  36. Carbapenems 
    PSEUDO
    • DIM
    • 1) doripenem (Doribax) - IV
    • 2) imipenem/cilastatin (Primaxin) - IV
    • 3) meropenem (Merrem) - IV
  37. ertapenem (Invanz) - IV
    LACKS coverage
    NO PEA

    • pseudomonas
    • enterococcus
    • acinetobacter
  38. CAN'T USE CARBAPENEMS
    • Seizures - imipenem
    • 3-5% cross reactivity with beta-lactams (ALLERGY)
  39. Monitor in carbapenems??
    RENAL impairment
  40. Monobactams
    agent (1) + dosage form
    aztreonam (Azactam) - IV
  41. Monobactam
    spectrum
    • aztreonam (Azactam) - IV
    • gram NEGATIVE ONLY
    • PSEUDO

    no cross reactivity with other beta-lactams!!!
  42. 4 ways for beta-lactam resistance 
    IMPORANT
    • 1) altered PBP
    • - MRSA
    • -Strep pneumo and enterococci (pen resist)
    • 2) altered outer membrane permeability (gram NEG)
    • 3) production of beta-lactamases or other deactivating enzymes
    • -pens, cephs, carbapenems
    • 4) efflux pump (gram NEG)
  43. Otitis media - in kids
    - avoid resistance
    HIGH dose AMOX 80-90 mg/kg/day
  44. Aminoglycosides
    2 toxicities
    • 1) ototoxicity
    • 2) nephrotoxicity
  45. aminoglycosides
    spectrum
    • gram NEGATIVE ... synergy with beta-lactams = positive
    • PSEUDO
  46. aminoglycosides 
    spectrum with beta-lactams
    • SYNERGY for ENDOCARDITIS (gram + cocci)
    • 1) enterococcus faecalis 
    • 2) staph a 
  47. aminoglycosides
    MOA
    30 s RIBOSOMAL to inhibit protein synthesis
  48. aminoglycosides
    resistance
    transferase enzyme inactivate aminoglycosides
  49. aminoglycosides
    PK info
    • concentration DEpendent killing (dose-dependent killing)
    • Post antibiotic effect (PAE)

    • PEAK/MIC ratio
    • -traditional vs once daily dosing
  50. aminoglycoside agents (4)
    TAGS

    • 1) tobramycin (Nebcin)- IV - better PSEUDO
    • 2) amikacin (Amikin) - IV - RESISTANT bacteria use
    • 3) gentamicin (Garmycin) - IV - most widely used
    • 4) Streptomycin - IV-  2nd line TB in combo
  51. Macrolides agents (3) + dosage form
    • ACE
    • 1. azithromycin (Zithromax, Zmax) - PO/IV
    • 2. clarithromycin (Biaxin) - PO
    • 3. erythromycin - PO/IV
  52. atypicals (3)
    • mycoplasma
    • legionalla
    • chlamydia
  53. Macrolides: potent 3A4 inhibitors/drug interactions (2)
    IMPORTANT
    • 1. erythromycin - PO/IV
    • 2. clarithromycin (Biaxin) - PO
    • avoid STATINS, benzos, carbamazepine, cyclosporin, theophylline
  54. not to use Macrolides??
    Strep pneumo infections (watch for resistance!)
  55. Lincosamides agent (1) + dosage form
    clindamycin (Cleocin) - PO/IV

    D- TEST!!!!
  56. Lincosamides
    spectrum
    • gram +/- ANaerobes
    • gram + aerobes - CA-MRSA

    vs metronidazole - anaerobes, parasites
  57. lincosamides
    Side effect (1)
    C. DIFF
  58. chloramphenicol (Chloromycetin)
    spectrum
    • BROAD
    • positive, negative, anaerobes
  59. chloramphenicol (Chloromycetin)
    Adverse effects
    • bone marrow suppression
    • gray baby syndrome (preggo category C) 
    • - not used much
  60. tetracyclines agents (4) + dosage form
    • 1) doxycycline (Vibramycin) - IV/PO
    • 2) tetracycline (Sumycin) - PO
    • 3) minocycline (Minocin) - PO
    • 4) demclocycline (Declomycin) - PO
  61. tetracyclines
    spectrum
    • fair positive, negative, mycoplasma
    • TICKS! - rickettsia
    • chlamydia, plasmodium
  62. tetracyclines
    MOA
    ribosome 30 s - inhibit protein synthesis
  63. Tetracyclines
    clinical uses
    • TICKS
    • CA-MRSA - but BACTRIM IS FIRST CHOICE
  64. SIADH tetracycline
    demeclocycline (Declomycin) - PO
  65. Tetracyclines
    Drug interactions
    • di-tri- valent cations
    • = decrease absorption! (bind up so space use)
  66. tetracyclines
    Adverse effects
    • teeth discoloration < 8 yo AVOID
    • photosensitivity
  67. glycylcline agent (1) + dosage form
    tigecycline (Tygacil) - IV
  68. Glycylcycline
    Spectrum
    • positive - MRSA, VRE!!!
    • negative - NO PSEUDO
    • anaerobes 
  69. glycylcycline
    moa
    • inhibit binding to 30 s ribosome
    • all similar to tetracycline!!!
  70. trimethoprim/sulfamethoxazole (Bactrim)
    spectrum
    • DOC: UTI, PCP, Upper resp infections (URI)
    • -gram negative URINARY pathogens, positive, CA-MRSA
  71. trimethoprim/sulfamethoxazole (Bactrim)
    drug interactions
    warfarin, phenytoin
  72. trimethoprim/sulfamethoxazole (Bactrim)
    dosing? 
    important
    • SS tab = 80 mg TMP/ 400 SMX PO
    • DS tab = 160 mg TMP/800 SMX PO
  73. 2nd gen FQ agents (2) + indication
    • 1. ciprofloxacin (Cipro) - PSEUDO
    • 2. ofloxacin (Floxin)
    • use: UTI
  74. 3rd gen FQ agents (3) + indication
    • 1. levofloxacin (Levaquin) - PSEUDO
    • 2. gemifloxacin (Factive)
    • 3. moxifloxacin (Avelox)
    • use: RESPIRATORY FQ (Strep PNEUMO)
  75. FQ MOA
    inhibit TOPO 2 (gyrase), and 4 - inhibit DNA synthesis
  76. FQ - PSEUDO
    • 1. ciprofloxacin (Cipro) - 2nd gen
    • 2. levofloxacin (Levaquin) - 3rd gen
  77. FQ
    spectrum
    • gram -
    • not really for staph
    • strep pneumo is 3rd gen  respiratory quinolones
    • atypicals: chlamydia, mycoplasma, legionella, brucella 
    • anaerobic = MOXIFLOXACIN (Avelox)
  78. FQ
    pk/absorption
    EXCELLENT BA (80-95%) - iv:po
  79. FQ
    clinical use
    NOT for UTIs (1)
    moxifloxacin (Avelox)
  80. FQ
    Adverse effects (5)
    • 1. CNS - seizures
    • 2. QT prolongation
    • 3. tendonitis, tendon rupture - elderly
    • 4. joint cartilage damage/arthropathy <18 yo immature beagle puppies!!!
    • 5. C. DIFF
  81. FQ 
    drug interactions
    • di-, tri- valent cations
    • (antacids)

    like tetracyclines!
  82. ciprofloxacin (Cipro)
    spectrum
    • FQ 2nd gen
    • UTI, pyelonephritis , etc.
    • PO/IV,etc 
  83. Vancomycin
    MOA
    • inhibits cell wall synthesis
    • d-ala, d-ala
  84. Vancomycin
    spectrum
    • DOC: MRSA
    • MSSA - staph/strep - slow - use NOD first!!!
    • synergy with aminoglycosides - entero faecium and faecalis
    • resistance VISA/GISA, VRSA
  85. Vancomycin
    clinical use
    • PO - C DIFF
    • IV - everything else, alternative to PCN
  86. Vancomycin
    adverse effects 
    • nephrotoxicity
    • ototoxicity

    "RED MAN syndrome" - not an allergy = slow infusion rate or increase infusion time
  87. telavancin (Vibativ)
    spectrum + efficacy
    • similar to Vancomycin
    • MSSA, MRSA
    • -GISA
    • HAP
  88. telavancin (Vibativ)
    Adverse effects
    • taste disturbance, n/v, foamy urine
    • cyp 3A4 
    • QTc, red man syndrome
  89. metronidazole (Flagyl)
    spectrum + pk/Absorption
    • anaerobes   vs CLINDAmycin (gram + aerobes too)
    • parasites

    BA 100%
  90. metronidazole (Flagyl)
    Adverse effects + Drug interactions
    • GI, peripheral neuropathy
    • big: disulfiram-like reaction (avoid alcohol), warfarin (INC INR)
  91. metronidazole (Flagyl)
    clinical use
    • anaerobic infections
    • C. DIFF - mild to moderate
  92. tinidazole (Tindamax)
    spectrum and dosing
    • antiprotozoal (antiparasitic?)
    • ONCE DAILY DOSING
  93. linezolid (Zyvox)
    MOA
    ribosome RNA of 50s subunit
  94. linezolid (Zyvox)
    spectrum
    MRSA, VRE (faecium), entero faecalis, MSSA
  95. linezolid (Zyvox) 
    indication + pk/absorption
    • VRE
    • pneumonia (HAP), MRSA, MSSA
    • CAP
    • complicated, uncomplicated skin structures (DIABETIC FOOT infections)
    • pk/absorption: BA 100% (hepatic adjust not renal adjust!!!!)
  96. linezolid (Zyvox)
    Adverse effect (2)
    • THROMBOCYTOPENIA
    • Neuro
  97. linezolid (Zyvox)
    Drug Interactions
    IMPORTANT
    • weak, monoamine oxidase inhibitor
    • AVOID SSRIs, decongestant (HTN)
  98. quinupristin/dalfopristin (Synercid)
    MOA
    ribosomal 50 S
  99. quinupristin/dalfopristin (Synercid)
    spectrum
    • MSSA, MRSA, VRE, atypicals
    • no faecalis!!!!!
  100. quinuprisint/dalfopristin (Synercid)
    Adverse effect
    • PAIN (local) 
    • give CENTRAL LINE
  101. quinupristin/dalfopristin (Synercid)
    Drug interaction
    CYP3A4 inhibitor!!!
  102. daptomycin (Cubicin)
    MOA
    cell membrane, insert tail and let potassium out (efflux)
  103. daptomycin (Cubicin)
    spectum
    • like linezolid in terms of gram positive coverage
    • MSSA, MRSA, faecalis, faecium (VRE)
  104. daptomycin (Cubicin)
    NOT to use in?
    Adverse monitoring?
    Drug interaction (1)?
    • NOT for respiratory tract infections = bad with surfactant - strep pneumo)
    • CPK elevation weekly
    • HMG-CoA reductase inhibitors - STATINS avoid!!!
  105. colistimethate sodium  
    spectrum
    Adverse effects
    • gram-negative 
    • nephrotoxicity (worse than aminoglycosides)
  106. rifampin (Rifadin)
    clinical use
    Adverse event
    • classic CYP450 enzyme INDUCER
    • TB, N. men, H.influ, S. aureus (MRSA)
    • ADR: orange discoloration
  107. nitrofurantoin (Macrodantin, Macrobid)
    Avoid?
    renal dysfunction CrCl < 60 ml/min
  108. fosfomycin (Monurol)
    • Single dose for UTI 
    • PO

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