Antimicrobials

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ldewanz
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120171
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Antimicrobials
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2011-12-02 22:36:03
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antimicrobials
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  1. Penicillin G
    • penicillin
    • Acid-labile
    • Parentral (IM-procaine or benzathine/IV)
    • Gram +/- cocci
    • SE: allergies/neurotox/seizures/Stevens-Johnsons
  2. Pencillin V
    • penicillin
    • Acid stabile/Oral
    • Gram +/- cocci
    • SE: allergies/neurotox/seizures/Stevens-Johnsons
  3. Oxacillin
    • beta-lactamase resistant (methicillin)
    • Acid stable/food interferes
    • Use: Staphylococci/streptococci (penicillinase-producing)
    • Resist: MRSA/PBP w/lower affinity for drugs
    • SE: hepatitis at high dose
  4. Amoxicillin
    • Extended spectrum
    • Destroyed by beta-lactamases
    • Acid stable/Oral/greater absorb than ampicillin/not food effected
    • Use: non-lactamase gram- bacilli/prophylaxis against bacterial endocarditis
  5. Ampicillin
    • Extended spectrum
    • Acid stable/Oral
    • Use: non-lactamase gram- bacilli/prophylaxis against bacterial endocarditis
  6. Piperacillin
    • Extended spectrum
    • Parenteral
    • Anti-Pseudomonal/Klebsiella
    • Combo w/aminoglycoside
  7. Ticarcillin
    • Extended spectrum
    • Parenteral
    • Ani-Pseudomonal
    • not used alone
  8. Clavulanic acid
    • beta lactamase inhibitor
    • Used w/ extended spectrum penicillins
    • MOA: Beta-lactamase suicide inhibitors
  9. Sulbactam
    • beta lactamase inhibitor
    • Used w/ extended spectrum penicillins
    • MOA: Beta-lactamase suicide inhibitors
  10. Tazobactam
    • beta lactamase inhibitor
    • Used w/ extended spectrum penicillins
    • MOA: Beta-lactamase suicide inhibitors
  11. Cephalexin
    • 1st generation cephalosporin
    • MOA: inhibit cell wall synthesis
    • SE: allergy (worse than penicillins)/Disulfiram-like rxn
    • Renal excretion/Oral/IV/IM/Vary distribution
    • Resist: Amp C/low affinity PBP
    • Use: broadest gram+ cocci (surgical prophyl)/gram- bacilli
  12. Cefuroxime
    • 2nd generation cephalosporin
    • MOA: inhibit cell wall synthesis
    • SE: allergy (worse than penicillins)/Disulfiram-like rxn
    • Renal excretion/Oral/IV/IM/Vary distribution
    • Resist: Amp C/low affinity PBP
    • Use: Anaerobes
  13. Ceftazidime
    • 3rd generation cephalosporin
    • MOA: inhibit cell wall synthesis
    • SE: allergy (worse than penicillins)/Disulfiram-like rxn
    • Renal excretion/Oral/IV/IM/Vary distribution
    • Resist: Amp C/low affinity PBP
    • Use: Pseudomonas/Pneumococcal/serious Gram-/ children
  14. Cefepime
    • 4th generation cephalosporin
    • MOA: inhibit cell wall synthesis
    • SE: allergy (worse than penicillins)/Disulfiram-like rxn
    • Renal excretion/Oral/IV/IM/Vary distribution
    • Resist: Amp C/low affinity PBP
    • Use: Pseudomonas/high resist beta-lactamases/ enterobacter/penicillin-resist strep
  15. Imipenem
    • carbapenem
    • MOA: bind more efficiently to PBP (than pens/cephs)
    • Use: gram- (aero/anaer)/2nd line serious nosocomial
    • Broadest spectram (antagonize cidal effects of pen/ceph)
    • Resist: alter PBPs
    • Parenteral/Renal met (admin w/cilastatin)
    • SE: cross-allergic to pen/GI/neurotox
  16. Meropenem
    • carbapenem
    • MOA: bind more efficiently to PBP (than pens/cephs)
    • Use: gram- (aero/anaer)/2nd line serious nosocomial
    • Broadest spectram (antagonize cidal effects of pen/ceph)
    • Resist: alter PBPs
    • Parenteral/Renal met (admin w/cilastatin)
    • SE: cross-allergic to pen/GI/neurotox
  17. Cilastatin
    • Peptidase inhibitor
    • Inhibit dehydropeptidases
    • Prevent kidney met/elimination of Imipenem
  18. Aztreonam
    • monobactam
    • MOA: binds PBPs/resist beta-lactamases
    • IV/IM/penetrates CNS
    • NO cross-allergy with pen
    • Narrow: gram- aerobes (includ pseudomonas)
    • Use: gram- UTIs/LRI/systemic infections
  19. Bacitracin
    • MOA: depletes lipid carrier for PDG
    • Topical only
    • Narrow: gram+/neisseria/T. pallidum
    • SE: nephrotoxicity (if not topical)
    • Use: skin/opthalmic/combo w/polymyxin B
  20. Daptomycin
    • Cell membrane agent
    • MOA: membrane depolarization/Cidal
    • IV/renal elim
    • Use: sim to vancomycin/tx VRE/VRSA (last resort)
    • SE: myopathy
  21. Fosfomycin
    • Non-beta lactam drug
    • MOA: analog of PEP/blk PDG synth
    • Well absorbed/distributed/excreted unchanged in urine
    • broad spectrum
    • Rapid resistance w/multiple doses
    • Single dose UTI
    • SE: diarrhea/vaginitis
  22. Vancomycin
    • MOA: binds D-Ala-D-Ala terminus of pentapeptide/blks X-linking
    • Cidal if dividing/static in enterococci
    • IV only/distribute good (CNS/bone)
    • Narrow: gram+/MRSA/S. pneumonia/combo w/ aminoglycosides
    • SE: Red man syndrome/oto/nephro
    • VRE: enterococci dec binding
    • VRSA: S. aureus overexpress D-Ala-D-Ala
  23. Amikacin
    • Aminoglycoside
    • Use: resist to gent/tobra/M. tuberculosis combo tx
    • MOA: irrverse bind 30s/blk initiation/blk further translat/ incorrect AA
    • Cidal/concentration depend kill
    • Gram- bacilli/combo pen/vanco for S. aureus/S. epidermidis
    • Resist: mut ribosome/dec uptake or efflux/enz inact
    • IV/IM
    • High conc inner ear/renal cortex
    • Renal elim
    • SE: oto/vestibular/renal tox
  24. Gentamicin
    • Aminoglycoside
    • MOA: irrverse bind 30s/blk initiation/blk further translat/ incorrect AA
    • Cidal/concentration depend kill
    • Gram- bacilli/combo pen/vanco for S. aureus/S. epidermidis
    • Resist: mut ribosome/dec uptake or efflux/enz inact
    • IV/IM
    • High conc inner ear/renal cortex
    • Renal elim
    • SE: oto/vestibular/renal tox
    • Use: severe Gram-
  25. Neomycin
    • Aminoglycoside
    • Use: resist gent/tobra
    • MOA: irrverse bind 30s/blk initiation/blk further translat/ incorrect AA
    • Cidal/concentration depend kill
    • Gram- bacilli/combo pen/vanco for S. aureus/S. epidermidis
    • Resist: mut ribosome/dec uptake or efflux/enz inact
    • IV/IM
    • High conc inner ear/renal cortex
    • Renal elim
    • SE: oto/vestibular/renal tox
  26. Tobramycin
    • Aminoglycoside
    • Use: Pseudomonas/cystic fibrosis pts
    • MOA: irrverse bind 30s/blk initiation/blk further translat/ incorrect AA
    • Cidal/concentration depend kill
    • Gram- bacilli/combo pen/vanco for S. aureus/S. epidermidis
    • Resist: mut ribosome/dec uptake or efflux/enz inact
    • IV/IM
    • High conc inner ear/renal cortex
    • Renal elim
    • SE: oto/vestibular/renal tox
  27. Spectinomycin
    • Aminocyclitol
    • MOA: binds 30s (no misread)
    • Static
    • Gram-/some Gram+
    • Use: MRSA and enterococci/AB resist gonorrhea
    • IM
  28. Streptomycin
    • Aminoglycoside
    • High resist to this drug
    • Use: mycobacterial infections
    • Cause deafness in newborns
    • MOA: irrverse bind 30s/blk initiation/blk further translat/ incorrect AA
    • Cidal/concentration depend kill
    • Gram- bacilli/combo pen/vanco for S. aureus/S. epidermidis
    • Resist: mut ribosome/dec uptake or efflux/enz inact
    • IV/IM
    • High conc inner ear/renal cortex
    • Renal elim
    • SE: oto/vestibular/renal tox
  29. Tigecycline
    • Gylcylglycine
    • MOA: sim to tetracycline w/higher affinity
    • Static against Hershey isolate of MRSA
    • Use: strains that are tet-resist/Vanco-resist
  30. Tetracycline
    • Tetracycline
    • MOA: reverse bind to 30s/blk tRNAs from A site
    • Broad: superinfection/Gram+ more so
    • Static
    • Resist: dec influx/inc efflux/enz inactive/protect ribosomes
    • Oral/dec with food and milk/dec if dec gastric pH
    • Wide distribute/accum in liver/bone/enamel/cross placenta
    • Elim kidney/bile
    • Use: acne/rickettsial disease
    • SE: GI/superinfections/photosens/hepatotox/renal tox/ discolor teeth
    • Dec efficacy of pens/digoxin/warfarin/hypoglycemic
  31. Doxycycline
    • Tetracycline
    • MOA: reverse bind to 30s/blk tRNAs from A site
    • Broad: superinfection/Gram+ more so
    • Static
    • Resist: dec influx/inc efflux/enz inactive/protect ribosomes
    • Oral/dec with food and milk/dec if dec gastric pH
    • Wide distribute/accum in liver/bone/enamel/cross placenta
    • Use: acne/rickettsial disease
    • SE: GI/superinfections/photosens/hepatotox/renal tox/ discolor teeth
    • Dec efficacy of pens/digoxin/warfarin/hypoglycemic
    • Elim as chelate in feces
  32. Minocycline
    • Tetracycline
    • MOA: reverse bind to 30s/blk tRNAs from A site
    • Broad: superinfection/Gram+ more so
    • Static
    • Resist: dec influx/inc efflux/enz inactive/protect ribosomes
    • Oral/dec with food and milk/dec if dec gastric pH
    • Wide distribute/accum in liver/bone/enamel/cross placenta
    • Use: acne/rickettsial disease
    • SE: GI/superinfections/photosens/hepatotox/renal tox/ discolor teeth
    • Dec efficacy of pens/digoxin/warfarin/hypoglycemic
    • Met by liver/Eim by feces
  33. Azithromycin
    • Macrolides
    • MOA: reverse to 50s/blk move from A to P site
    • Static (inhib streptogamins/clindamycin/chloramphenicol
    • Narrow: Gram+/anerobes
    • Cross resist possible (Efflux/modify ribosome/ hydrolyse by esterases from enterobacter)
    • Acid stable
    • Poor CNS pen/everywhere else/placenta
    • Use: alternate to pen/resp from atypical microbe
    • SE: GI
    • DOES NOT Inhibit CYP3A4
  34. Clarithromycin
    • Macrolide
    • MOA: reverse to 50s/blk move from A to P site
    • Static/inhib streptogamins/clindamycin/chloramphenicol
    • Narrow: Gram+/anerobes
    • Cross resist possible (Efflux/modify ribosome/ hydrolyse by esterases from enterobacter)
    • Acid stable
    • Poor CNS pen/everywhere else/placenta
    • Use: alternate to pen/resp from atypical microbe
    • SE: GI
    • Inhibit CYP3A4
  35. Erythromycin
    • Macrolide
    • Acid labile
    • Abscess penetration
    • Cholestatic hepatitis/allergic
    • MOA: reverse to 50s/blk move from A to P site
    • Static/inhib streptogamins/clindamycin/chloramphenicol
    • Narrow: Gram+
    • Cross resist possible (Efflux/modify ribosome/ hydrolyse by esterases from enterobacter)
    • Acid stable
    • Poor CNS pen/everywhere else/placenta
    • Use: alternate to pen/resp from atypical microbe
    • SE: GI
    • Inhibit CYP3A4
  36. Telithromycin
    • Ketolide
    • MOA: binds 50s @ 2 sites
    • Conc depended cidal for S. pneumoniae
    • Acid stable
    • Dec resist
    • Oral/no food prob/liver met/liver and renal elim
    • Resist: MLSb aureus and pyogenes
    • Use: CA-RTI
    • SE: GI/blurry vision/inc myasthenia gravis
    • Drug: inc levels of CYP3A4/cisapride/simvastatin
  37. Clindamycin
    • Lincomycin
    • MOA: 50s of bacteria exclusively
    • Use: Gram+/anaerobes (esp B. fragilis non-CNS)
    • Cidal for some
    • Resist: slow by methylase
    • Oral/IV/Wide distribute even bone/low in CNS
    • Met liver/elim renal
    • Use: RTI by anerobes/abscess/group A strep/ osteomyelitis
    • SE: diarrhea/rash/S-J syndrome/anaphylaxis
  38. Quinupristin
    • Streptogramin
    • MOA: binds 50s (same as macrolides)
    • Combo=cidal
    • Use: MRSA/life threaten Vanco-resist gram+
    • SE: pain at injection site/drug interactions
    • Resist: erm methylases/vgb lactonases
  39. Dalfopristin
    • Streptogramin
    • MOA: bind 50s by quinupristin (synergistic)
    • combo=cidal
    • Use: MRSA/life threaten Vanco-resist gram+
    • SE: pain at injection site/drug interactions
    • Resist: vat/sat acetyltransferases//vga/vgb efflux proteins
  40. Chloramphenicol
    • MOA: bind to peptidyltransferase site of 50s (near clindamycin/macrolides so cross resist)
    • Static
    • Broad: anaerobic/Gram- bacilli
    • Resist: acetyltransferases
    • Oral/placenta/CNS/liver met/renal elim
    • Use: tx tetracycline stuff if cant have tetra
    • SE: hematological/aplastic anemia/allergy/gray baby
    • Drug: inhib P450
  41. Linezolid
    • MOA: 23s of 50s ribosome
    • Static
    • Oral
    • Use: MRSA/drug-resist S. pneumoniae/VRE
    • NO corss-resist with other protein inhibitors
  42. Mupirocin
    • MOA: inhib tRNA synthetase
    • Topical only!
    • Use: impetigo from MRSA/group A strep
    • Rapid met
    • rare resist
  43. Sulfamethoxazole
    • sulfonamide
    • MOA: competitive inhib PABA binding to DHPS enz
    • Static (if used alone)
    • Oral/IV
    • Wide distribution/CNS and CSF
    • Liver met/renal elim
    • Broad: gram+/-//Plasmodium/toxoplasma gondii
    • Resist: wide spread/inc PABA/mutant DHPS/efflux
    • SE: GI/rash/marrow/liver tox/hemolytic anemia (G6PD deficiency)/kernicterus/S-J syndrome
    • Use: malaria/CNS toxoplasmosis
  44. Trimethoprim
    • DHFR inhibitor
    • MOA: blk DHFR
    • Static (if used alone)
  45. TMP-Sulfa
    • DHFR inhibitor/Bactrim/Septra
    • Cidal because a combo
    • Oral
    • Wide distribute/renal elim
    • Broad: gram+/-//NOT pseudomonas/anaerobes/atypical
    • Resist: Inc DHFR/Mutate DHFR
    • SE: same as sulfas/marrow dec/neutropenia/anti-folate effect
    • Use: UTIs/Pneumocystis in AIDS and transplant/ sinusitis/otitis media/CA-MRSA
  46. Ciprofloxacin
    • Fluoroquinolone
    • Cidal
    • MOA: DNA gyrase/topoisomerase/irreversable DNA damage
    • Oral/IV/Hepatic or renal elim
    • Wide distribution/dec with food/low CSF
    • Gram+/-//Not anaerobes/nosocomial/atypical
    • NO synergy
    • Resist: dec permeability/efflux/mut enz
    • SE: GI/Achilles tendon rupture/hep tox/super infect/
    • Use: complicated UTIs/bacterial prostatitis/pneumonia/ STDs
  47. Levofloxacin
    • Fluoroquinolone
    • Cidal
    • MOA: DNA gyrase/topoisomerase/irreversable DNA damage
    • Oral/IV/Hepatic or renal elim
    • Wide distribution/dec with food/low CSF
    • Gram+/-//Not anaerobes/nosocomial/atypica
    • lNO synergy
    • Resist: dec permeability/efflux/mut enz
    • SE: GI/Achilles tendon rupture/hep tox/super infect
    • Use: complicated UTIs/bacterial prostatitis/pneumonia/ STDs
  48. Moxifloxacin
    • Fluoroquinolone
    • Cidal
    • MOA: DNA gyrase/topoisomerase/irreversable DNA damage
    • Oral/IV/Hepatic or renal elim
    • Wide distribution/dec with food/low CSF
    • Gram+/-//Not anaerobes/nosocomial/atypical
    • NO synergy
    • Resist: dec permeability/efflux/mut enz
    • SE: GI/Achilles tendon rupture/hep tox/super infect
    • Use: complicated UTIs/bacterial prostatitis/pneumonia/ STDs

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