Antibiotics

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emac0408
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170397
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Antibiotics
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2012-09-12 14:01:52
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Antibiotics
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Antibiotics
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  1. Natural PCN
    • PCN-G
    • PCN-V:  e-withdrawal group (acid stable)
    • Mech:  B-lactam ring
    • Tx:  Gram+ Aero,
    • N.meningitidis(gram-)
    • Actinomycetes, Fusobacterium (anaero)
    • Resistant:  Staph (PCNase)
  2. AminoPCN
    • Ampicillin:  polar group 
    • Amoxicillin:  ^^ + e-withdrawal
    • Tx:  PCN (Gram+aero,N.meningitidis(gram-)Actinomycetes, Fusobacterium (anaero)) + H. influenza, E.coli, Proteus
    • Resist:  Klebsiella, Staph (both PCNase)
  3. UreidoPCN
    • Piperacillin:  polar (urea+piperazine)
    • Tx: PCN/aminoPCN (Gram+aero,N.meningitidis(gram-)Actinomycetes, Fusobacterium (anaero), H.influenzae, E.coli, Proteus) AND many Gram- (Klebsiella, P.auruginosa, N. gonorrhoeaa)
    • Resist:  Staph (PCNase)
  4. PCNase-resist PCN
    • Nafcillin:  bulky
    • Oxacillin:  ^^+ e-withdrawal
    • Dicloxicillin:  ^^
    • Tx:  Staph
    • Resist:  MRSA, MRSE
  5. CarboxyPCN
    Ticarcillin
  6. Beta-Lactamase Inh
    • Tazobactam w/ Piperacillin:  Pseudomonas
    • Clavulanate w/ Ticarcillin:  Pseudomonas (not w/Amoxicillin)
    • Sulbactam w/ Ampicillin:  not Pseudomonas
  7. Caphalospore
    decreased strain on B-lactam ring
  8. Cephalothin
    • 1st Gen Cephalosporin:  bulky group
    • Target:  PBP-3 (hyphal)
    • Tx:  PCN (Gram+aero, Gram-N.mening, anaero(actinomycetes, fusobacterium) + Staph, some Enterobact (E.coli, Kelbsiella,Proteus)
    • Resist:  Enterococcus, Haemophilus, Pseudomonas
  9. Cefazolin
    • 1st Gen Cephalosporin:  bulky group
    • Tx:  PCN (Gram+aero, Gram-N.mening, anaero(actinomycetes, fusobacterium) + Staph, some Enterobact (E.coli, Kelbsiella,Proteus)
    • Resist:  Enterococcus, Haemophilus, Pseudomonas
  10. Cephalexin
    • 1st Gen Cephalosporin:  PO absorption
    • Tx:  PCN (Gram+aero, Gram-N.mening, anaero(actinomycetes, fusobacterium) + Staph, some Enterobact (E.coli, Kelbsiella,Proteus)
    • Resist:  Enterococcus, Haemophilus, Pseudomonas
  11. Ceftriaxone
    • Advanced Cephalosporin:  Oxime 
    • ^^t1/2
    • Tx:  (=Cefotaxime) PCN, Staph, most Enterobacteria, Haemophilus
    • Resist:  Pseudomonas
    • S/E:  Hepatotoxic with sever liver dysfxn.
    • -never given to Neonates!!!
  12. Cefotaxime
    • Advanced Cephalosporin:  Oxime
    • Tx:  (=Ceftriaxone)  PCN, Staph, most Enterobacteria, Haemophilus
    • Resist:  Pseudomonas
  13. Ceftazidine
    • Advanced Cephalosporin:
    • R:  Propylcarboxy (vs. Pseudomonas) 
    • Tx:  Pseudomonas, Haemophilus, most Enterobacteria
    • Resist:  Gram+
    • Note:  Cefepime (zwitter: en mass porins): same as ceftazidine, but no Gram+
  14. Cefepime
    • Advanced Cephalosporine
    • Zwitterion:  en mass porins
    • Tx:  Pseudomonas, Haemophilus, most Enterobacteria AND Gram+ (same as Ceftazidiime, but Ceftazidime is not effective for Gram+)
  15. Cefpodoxime
    • Advanced Cephalosporin:
    • Ph/R group:  e-withdrawal
  16. Ceftaroline
    • Advanced Cephalosporine
    • Target:  PBP2a of MRSA (lose shape)
    • Tx:  MRSA, VISA, VRSA, PCN/cephalosporine resistant S. pneumoniae
  17. Carbapenem
    • R: steric block of PCNase
    • Target:  PBP-2 (lose shape) and most others
    • -Enters thru differ Porin than PCN/CEPH
    • Tx:  Life-threatening/polymicrobial infection
    • -Enterococcus stasis (need aminoglycoside)
  18. Imipenem
    • Carbapenem, =Meropenem
    • (R: steric block of PCNase)
    • (Target:  PBP-2 (lose shape) and most others-Enters thru differ Porin than PCN/CEPH)
    • Tx:  (Life-threatening/polymicrobial infection-Enterococcus stasis (need aminoglycoside))
    • -Gram+cocci, Gram-Rods, Anaerobes
  19. Meropenem
    • Carbapenem, =Imipenem
    • (R: steric block of PCNase)
    • (Target:  PBP-2 (lose shape) and most others-Enters thru differ Porin than PCN/CEPH)
    • Tx:  (Life-threatening/polymicrobial infection-Enterococcus stasis (need aminoglycoside))
    • -Gram+cocci, Gram-Rods, Anaerobes
  20. Ertapenem
    • Carbapenem
    • (R: steric block of PCNase)
    • (Target:  PBP-2 (lose shape) and most others-Enters thru differ Porin than PCN/CEPH)
    • ^^t1/2:  once daily (90% protein bound)
    • Tx:  (Life-threatening/polymicrobial infection)
    • -Gram+cocci, Enterobact, Anaerobes
    • Resist:  Enterococcus, Pseudomonas
  21. Doripenem
    • Gorillazine
    • Carbapenem
    • (R: steric block of PCNase)
    • (Target:  PBP-2 (lose shape) and most others-Enters thru differ Porin than PCN/CEPH)
    • Tx:  (Life-threatening/polymicrobial infection-Enterococcus stasis (need aminoglycoside))
    • -greatest activity vs. non-fermenters (Pseudomonas, Nocardia)
  22. Aztreonam
    • Monobactam
    • Target:  PBP-3 (hyphal)
    • R:  Propylcarboxy (vs. Pseudomonas)
    • No cross rxn w/ PCN allergy
    • Tx:  Aero Gram-Rods 
    • Resist:  Gram+, Anaerobes
  23. Vancomycin
    • Glycopeptide
    • Mech: bind D-Ala-D-Als, block bridging
    • Tx:  Gram+, Entercoccus with aminoglycoside, MRSA
    • Resist:  Gram- (too large for porin)
  24. Fosfomycin
    Bind building blocks of peptidoglycans
  25. Daptomycin
    • Lipopeptide
    • Form membrane cation channels (Ca-depend)
    • IV only (pep broken down)
    • Tx:  Gram+, MRSA/SE etc.
    • Resist:  Gram- (too large)
  26. Colistin
    • Polypeptide AB
    • Mech:  bind LPS/Plipids
    • Tx:  Gram-
    • Resist:  very common
  27. Fluoroquinolones
    • Fluoroquinolone:  inh Type II topoisomerase
    • Tx:  Gram-Rods, Gram+Cocci, Mycobacterium, intracellulars
    • -Protatitis, Mycobacteriosis
    • -inh DNA Gyrase (Gram-)
    • -inh Topoiso IV (Gram+)
    • S/E:  GI, CNS (delerium), Abnl Glc homeo (no DM)
    • -Arthropathy (no kids)
    • -Prolonged QT
    • Rx:
    • -Levofloxacin:  
    • -Moxifloxacin:  ^anaerobic 
    • -Gemifloxacin:
    • -Ciprofloxacin: ^aerobic (no effect on S.aureus, S.pneum)
  28. Metronidazole
    • Nitroimidazole:  Tinidazole also
    • Mech:  ^^Free Redicals damage DNA (NO2 group reduced by ferredoxin)
    • Tx:  Anarobes (not Actinomycetes), Protozoa
    • Resist:  Actinomycetes, Aerobes 
    • S/E:  Seizure, Encephalopathy, neuropathy, Red urine, gynecomastia, Antabuse Rxn
  29. Rifampin
    • Rifamycin
    • Mech:  binds RNA Polymerase
    • ^oral available, not given alone
    • Tx:  Staph, MRSA, Neisseria, Intracellular, Aspergillus/Cryptococcus
    • -Osteomyelitis, Endocarditis
    • S/E:  
    • -Induce CYP3A: decr contracept,warfarin,Azoles
    • -levels decr by AlOH3(antiacid), Azoles
    • -Orange/red urine/contacts
    • -rash, hepato/nephrotox, flu-like
  30. Rifabutin
    • Rifamycin
    • Mech:  inh RNA Pol
    • well absorbed
    • Tx:  M.avium, resistant MTb
  31. Rifaximin
    • Rifamycin
    • Mech:  inh RNA Pol
    • poorly absorbed:  Zwitterion!
    • Tx:  C. diff
  32. Aminoglycosides
    • Mech: bind 30S ribos: cause misread
    • ^^polar cation
    • only with severe infection
    • Tx:  Gram- Aerobic Rods, Enterococcus (w/ cell wall inh)
    • S/E:
    • Nephrotox:  absorb in prox. tubule, accum in lysos 
    • Ototoxic:  choclea (outerHC), vest (type1 HC)
    • NMJ Block:  decrease ACh release
    • Rx:
    • Gentamicin
    • Tobramycin
    • Amikacin
  33. Tetracyclines
    • Mech: bind 30S ribos
    • Tx:  Rickettsiae, mycoplasma, chlamydiae
    • S/E:  no preg!!! (hepatotox to mom, interfere w/ fetal teeth/bones: stain)
    • -esoph ulcers, diarrh, benign intracranial HT, vertigo
    • Interaction:  forms complexes with cations
    • -decr abs w/ milk/antacid,iron, cimetidine (h2-block)
    • -decr t1/2 w/ EtOH/anti-epilectics
    • Rx:
    • Tetracycline
    • Doxycycline
    • Minocycline
    • Tigecycline
  34. Macrolides & Axalides
    • Mech: bind 50S chromos
    • Tx:  Mycoplasma, Gram+/-, protozoa, spirochetes, intracellulars
    • Resist:  Enterobacteria
    • S/E:  GI upset, cholestatic hepatitis, 
    • -Hearing loss (transient)
    • -Prolonged QT
    • Rx:
    • Macrolides:  Erythromycin, Clarithromycin
    • Azalide:  Azythromycin
  35. Clindamycin
    • Mech:  bind 50S ribos
    • favorite of dentist/Sx
    • Tx:  Viridans strep, Aero Gram+cocci,
    • -Anaero: Fusobacteria, B.fragilis,Prevotella,Peptostrep
    • S/E:  AB Colitis:  C. diff overgrowth (pseudomem)
  36. Linezolid
    • Mech:  bind 50S ribos
    • Tx:  Gram+Cocci, MRSA, MRSE, VRE, PCN-resistant S.pneum.
    • S/E:  BM suppression (thrombocytopenia)
    • -Mito Tox:  Lactic Acidosis
  37. Sulfonamides 
    • Mech:  inh Folic Acid syn: replace PABA on pterydine synthase
    • Same as Trimethoprim:
    • Tx:  Bacteria, Parasites, Fungi
    • Ristant:  Anaerobes
    • S/E:  
    • -GI upset
    • -Steven-Johnson
    • -Hypouricemia
    • -leukopenia
    • -thrombocytopenia (also seen w/ Linezolid)
  38. Trimethoprim
    • Mech:  inh Folic Acid syn: last step (dihydropteroic-x-> FA)
    • Same as Sulfonamides:
    • Tx: Bacteria, Parasites, Fungi
    • Ristant: Anaerobes
    • S/E:
    • -GI upset
    • -Steven-Johnson
    • -Hypouricemia
    • -leukopenia
    • -thrombocytopenia (also seen w/ Linezolid)

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