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2011-06-14 02:08:40

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  1. Bacteriostatic vs Bacteriocidal
    • Bacteriostatic- stop growth, need good immune sys to clear the bugs. DO NOT use in immunocompromised pts, meningitis, endocarditis!
    • - Erythromycin, Clindamyclin, Sulfamethoxazole, Trimethoprim, Tetracyclines, Chloramphenicol.

    • Bacteriocidal- kill!
    • -Peniciliin, Vancomycin, Fluoroquinolone, Aminoglycoside, Cephalosporins, Metronidazole
  2. Combos of antibacterials
    NEVER mix Bactericidal + Bacteriostatic!

    Penicillin + Aminoglycoside= synergy!

    Penicillin + Tetracycline= antagonism!
  3. Drugs that inhibit bacterial cell wall synthesis
    bacteriocidals! (lactams!)

    • Penicillin
    • cephalosporins
    • imipenem/ meropenem
    • aztreonam
    • vancomycin (not lactam)
  4. Drugs that inhibit bacteral protein synthesis

    • Aminoglycoside (bacteriocidal)
    • Chloramphenicol
    • macrolide
    • tetracycline
    • streptogramins
    • linezolid
  5. Drugs that inhibit nucleic acid synthesis

    • Fluoroquinolones
    • Rifampin
  6. Drugs that inhibit folic acid synthesis
    • Sulfonamide
    • Trimethoprim
    • Pyrimethamine
  7. Beta Lactams
    • bacteriocidals with beta-lactam ring structure : D-ala-D-ala analog
    • -bind Penicillin-binding proteins (PBP)
    • -inhibit transpeptidation (block crosslinking PG-final step in cell wall syn)

    • Penicillins (b-lactam+5C ring)
    • Cephalosporins (+6C ring)
    • Imipenem,Meropenem (carapenems)
    • Aztreonam (monobactams)
  8. Resistance to Beta lactams
    • beta-lactamases ex. Staph
    • change transpeptidase structure ex.MRSA
    • change porins (gram- so drug can't enter) ex. Pseudomonas

    All Mycoplasma are resistant to all beta-lactams! b/c no cell wall!
  9. Penicillin G, V
    • 1st gen penicillin
    • narrow spectrum b-lactam
    • short half life
    • beta-lactamase sensitive

    • USE- Syphillis!
    • some gram+ streps, meningococci
    • SE- hypersensitivity (+coombs- hapten), Hemolytic anemia
    • Jarisch-Herxheimer reaction (from syphillis rx)

    • Benzathine Penicillin G-repository form for syphilis (2week half life!)
  10. Nafcillin, Methicillin, Oxacillin, Dicloxacillin
    • 2nd gen penicillin
    • very narrow spectrum
    • beta-lactamase resistant (bulky R)

    • USE- Staph! except MRSA
    • (use Vancomycin for MRSA)

    • SE- Methicillin- interstitial nephritis
    • Nafcillin, oxacillin- hepatotoxic (b/c eliminate by bile)
  11. Amipicillin, Amoxicillin
    • 3rd gen penicillin
    • broader spectrum!
    • beta-lactamase sensitive
    • Amoxicillin better oral-bioavailability

    • USE-Gram+: Streps,Enterococci listeria !
    • Gram-: E.coli, H. influenzae, Proteus
    • H.pylori (Amoxicillin)
    • Borrelia (Amoxicillin)

    • SE-Hypercensitivity (ampicillin rash!)
    • Pseudomembranous colitits (Rx- metronidazole)
  12. Ticarcillin, Piperacillin, Azlocillin, Carbenicillin
    • 4th gen Penicillin
    • antipsuedomonals!!
    • extended spectrum
    • beta-lactamase sensitive

    • USE- Pseudomonas!
    • more Gram- rods (enterobacteracea)

  13. Clavulanic acid, Sulbactam, Tazobactam
    • suicide inhibitors of beta-lactamases
    • add to penicillins (except Nafcillin, Methicillin)
  14. Keep in mind for Penicillins
    -enhance activity with clavulanic acid, sulbactam..

    • -synergy with aminoglycosides
    • (amoxicillin+ aminoglycoside-->Enterococci)
    • (Ticarcillin + aminoglcoside-->pseudomonas)

    - all eliminated by kidney except Nafcillin, Oxacillin (bile)!- so adjust dose for bad kidneys!

    -Cross-allergenicity betwm penicilins!
  15. Drug hypersensitivity reactions
    Type1: IgE- rapid onset, anaphylaxis, andioedma, laryngospasm

    Type2: IgM, IgG- fixed to cells--> vasculitis, neutropenia, +Coombs

    Type3: Immune-complex-->vasculitis, serum sickenss, glomerulo/interstitial nephritis

    Type4: Tcell med--> urticarial maculopapular rashes, Stevens-Johnson syndrome
  16. Cephalsporins
    • beta-lactams w/ 6c ring
    • -less susceptable to penicillinases
    • -bacteriocidal!

    • 1st gen: Cefazolin, Cephalexin
    • 2ng gen: Cefotetan, Cefaclor, Cefuroxime
    • 3rd gen: Ceftriaxone, Cefotaxime, Cefdinir, Cefixime, Cefoperazone
    • 4th gen: Cefepime
  17. Cephalexin, Cefazoline
    • 1st gen cephalosporin
    • same mech as penicillin
    • long half life

    • USE- gram+ cocci
    • gram- : Proteus, E.coli, Klebsiella
    • (PEcK), dur Surgery!

    • SE- hypersensitivity, Vit-K deficiency
    • ,increase nephrotoxicity with Aminoglycosides!
  18. Cefotetan, Cefaclor, Cefuroxime
    • 2nd gen cephalosporin
    • same mech as penicillin
    • -does NOT cross BBB!
    • -Cefuroxime does!

    • USE-gram + cocci
    • more gram- coverage (HEN PEcK)- H. influenzxa, Enterobacter, Neisseria, Proteus, E.coli, Klbesiella

    SE-Disulfram-like effect w/Cefotetan! Hypersensitivity, Nephrotoxicity with aminoglycosides

  19. Ceftriaxone, Cefoperazone, Cefotaxime,Ceftazidime, Cefdinir, Cefixime
    • 3rd gen cephalosporins (the work horse!)
    • -Cross BBB!! except Cefoperazone
    • -broad spectrum!
    • -Ceftriaxone, Cefoperazone eliminated by bile, NOT kidney.
    • -Cefoperazone is too lipid soluble to be free to cross BBB.

    • USE- Meningitis, Sepsis!
    • -many gram+, gram-
    • -Ceftriaxone- Meningitis,Gonorrhea
    • -Ceftazidime - pseudomonas!

    • SE- Disulfram-like effects w/ Cefperazone, Hypersensitivity,
    • Hepatotoxicity w/ Ceftriaxone, Cefoperazone (bile)
  20. Cefepime (IV)
    • 4th gen cephalosorin
    • very broad spectrum
    • resistant to penicillinase
    • cross BBB, IV only

    USE- Pseudomonas, more gram +s

    SE- Hypersensitivity, nephrotoxicity w/ Aminoglycosides
  21. Bugs NOT killed by cephalosporins

    • -Listeria (use amoxicillin/ampicillin)
    • -Atypicals (mycoplasma, Chlamydia) (use, macrolides)
    • -MRSA (use vancomycin)
    • -Enterococci (use amoxicillin/ampicillin)
  22. NOTE about cephalosporins
    • -Cross allergenicity with Penicillins!
    • -just use Macrolides (gram+), Aztreonam (gram- rods)

    -Disulfram-like effects w/ Cefoperazone, Cefotetan

    • -Renal clearance similar to Penicillins (active tubular secr. blocked by Probenecid)
    • -Ceftriaxone, Cefoperazone eliminated by bile, not kidney.
  23. Imipenem/ Cisplatin
    • Carbapenem
    • broad spectrum beta-lactam!
    • -same mech as penicilin
    • -resistant to penicillinase
    • -must use w/ Cisplatin (dehydropeptidase inhibitor) to block inactivation in kidney.

    • USE- almost anything! (not MRSA)
    • -gram+ cocci, gram- rods, anaerobes
    • -used in hospital for severe-life-threatening infections!!
    • SE- Seizure! GI distress, hypersensitivity, dose adjust for kidney
  24. Meropenem
    • Carbapenem
    • broad spectrum beta-lactam!
    • -same mech as penicilin
    • -resistant to penicillinase

    • USE- almost anything! (NOT MRSA)
    • -gram+ cocci, gram- rods, anaerobes
    • -used in hospital for severe-life-threatening infections!

    SE-GI distress, hypersensitivity, dose adjust for kidney, NO seizures
  25. Aztreonam
    • Monobactam (beta lactam)
    • -same mech as penicillin
    • -resistant to penicillinase
    • -NO cross allergenicity w/ Penicilliins, cephalosporins!!
    • -synergistic w/ aminoglycosides
    • -does NOT cross BBB!

    • USE- only gram - rods!!
    • -good for penicilin-allergic pt
    • -good for kidney failure pt who can't tolerate aminoglycoside
    • -NOT for gram+, or anaerobes

    SE-GI distress but not much..
  26. Vancomycin
    • NOT beta lactam
    • -inhibit PG elongation (transglycosylation) by binding at D-ala-D-ala muramyl pentapeptide
    • -bacteriocidal
    • -IV, oral (not absorbed, stay in gut)
    • -goes everywhere except BBB
    • -kidney eliminated

    USE- gram + only! -MRSA, Enterococci, C.Difficile (PO, backup. Metronidazole better)

    SE-red man syndrome (typeI-histamine), ototoxicity, nephrotoxicity, thrombophlebitis

    • Resistance-VRSA, VRE emerging! VRE change target as D-ala-D-lactate!
    • -use Linezolid, Streptogramins for these nasty ones!
  27. Protein synthesis inhibitors
    all bacteriostatic except aminoglycosides

    • 1.Block initiation complex formation
    • Aminoglycosides (30S),
    • Linezolid (50S)-VRSA, VRE
    • -block mRNA assoc w/ 50S ribosome (static)- cause misreading of mRNA (cidal-aminoglycoside)

    • 2.block AA incorporation to A site-
    • Tetracycline (30S), Dalfopristin/Quinupristin(50S)

    • 3.Block peptide bond formation-peptidyltransferase
    • -Chlormaphenicol (50S)

    • 4.Block translocation-
    • Macrolides, Clindamycine (50S)
  28. Gentamicin, Neomycin, Amikacin, Tobramycin, Sterptomycin
    • Aminoglycosides
    • -bacteriocidal
    • -block initiation complex form, cause misread (frameshift)in mRNA
    • -require O2 for uptake! go thru ETC
    • -CANNOT kill anaerobes, streps!
    • -synergy w/ Beta lactams
    • -polar, not good orally, poor distribute (stay in ECF)
    • -low TI (once/day dose good)

    • USE-gram - rods!
    • -synergy w/ampicllin-->enterococci
    • -synergy w/4th gen penicillin-->pseudomonas

    • SE-nephrotoxicity (esp w/cephalosporins), ototoxicity, esp w/ loos), NMJ blockade (block Ach release like botox!) contact dermatitis w/ Neomycin
  29. Resistance to aminoglycosides
    bugs make conjugation enzyme that inactivate aminoglycoside!
  30. Sterptomycin

    USE- TB, choice for Bubonic Plague, Tularemia

    NOT nephrotoxic!
  31. Neomycin, Polymyxin, Bacitracin
    topical aminoglycoside

    SE-contact dermatitis!
  32. Once/daily dosing
    • Antibacterial effects depend mainly on peak drug levels (rather than time) and continue w/ blood levels less than MIC
    • = Post-antibiotic effect!

    depends on both blood level and time that levels are greater than threshold (ex. total dose)
  33. Tetracycline, Doxycycline, Demeclocycline, Minocycline
    • Tetracycline
    • -bacteriostatic
    • -inhibit A site on 30S (block attachment of AA-tRNA)
    • -broad spectrum! actively taken up by bug-->accum in cell
    • -chelate cations, so do NOT take w/food (esp. antiacids, milk, Ca, decr absoption)
    • -antagonistic w/ penicillins!!

    • USE-good for intracellular, atypicals
    • -Chlamydia, Rickettsia, Borrelia, Vibrio, Treponema (backup)

    • SE-chelate Ca, Mg, Fe..
    • - decr bone! brown teeth, inhibit bond growth in kids!, phototoxicity
    • -vestibular disfunction (minocycline)
    • -kidney dose adjust except Doxycycline
    • do NOT use in pregnancy and kids!!
  34. Resistance to tetracycline
    transport PUMPS pump drug out of the cell
  35. Doxycycline
    • tetracycline
    • -bacteriostatic
    • -block A site on 30s
    • -NO nephrotoxicity b/c eliminated by liver!
    • -more lipid soluble

    • USE- Borrelia burgdorferi (Lyme disease!)
    • -good for prostatitis (chlamydia, gonnorrea)

    • SE-inhibit bone, phototoxicity
    • do NOT use in pregnancy, kids!
  36. Minocycline
    • Tetracycline
    • -bacteriostatic
    • block A site on 30S
    • -too water soluble

    • USE- dental issues, gingivitis
    • get in high conc in saliva, tears

    • SE- bone inhibit, vestibular dysfunctinon, kidney
    • do NOT use in pregnancy, kids!
  37. Demeclocycline
    • Tetracycline
    • -bacteriostatic
    • -block A site on 30s
    • -inhibit ADH receptor in collecting duct!!
    • --> cause nephrogenic diabetes insipidus!!

    USE- SIADH (paraneoplastic in renal cell carcinoma, bronchogenic squaous cell carcinoma)
  38. Chloramphenicol
    • bacteriostatic
    • -inhibit 50S peptidytransferase (peptide bond formation)
    • -very wide spectrum
    • -lipid soluble, cross BBB
    • -glucuronidated by liver
    • -cross placenta!

    • USE- meningitis! (H.influenza, N.meningitis, S.pneumonia)
    • -backup for Samonella typhi, B.fragilis, Rickettsia

    • SE-does dependent marrow suppression (like anticancer),
    • gray baby syndrome! (baby's liver can't handle, can't eliminate-->kernicterus), hemolysis in G6PD
    • ,inhibit Cyps!!
    • do NOT use in pregnancy!

    Resistance- inactivating acetyltransferases
  39. Erythromycin, azithromycin, clarithromycin
    • Macrolide
    • -bacteriostatic
    • -block translocation by binding to 23S rRNA on 50S
    • -wide-spectrum
    • -inhibit CYPS!
    • -can use Azithromycin in pregnancy b/c more water soluble.

    • USE- atypical pneumonia (mycoplasma, chalmydia, legionella!)
    • -URIs, STDs (Neisseria), MAC
    • -gram + cocci (not MRSA)esp. penicillin-allergic pts
    • -GI motility disorders (activate motilin receptors)

    • SE- Prolong QT (esp. Erythromycin), GI distress (motilin), reversible deafness, acute cholestatic hepatitis, eosinophilia, increase conc. of theophyllines, oral anticoagulants
    • -inhibit CYPS!
  40. Resistance to Macrolide
    methylation of 23S rRNA so Macrolide cannot recognize it!
  41. Drug for Macrolide resistant Strep pneumonia?
    Telithromycin - ketolide
  42. Clindamycin
    • bacteriostatic
    • -block traslocation at 50s
    • -narrow spectrum
    • -accum high conc in bone!
    • (anaerobes above diaphram)

    • USE- gram+ anaerobic infections! (B. fragilis, Clostridium perfringens)
    • -aspiration pneumonia
    • -osteomyelitis (S. aureus)
    • NOT gram- osteomyelitis ex. Sickle cell osteomyelitis (salmonella), Diabetic osteomyelitis (pseudomonas)

    SE-pseudomembramous colitis (Rx w/ Metronidazole or Vancomycin (backup)
  43. Linezolid
    • bacteriostatic
    • -block formation of initiation complex (same as aminoglycosides but at 50s)
    • -very toxic!

    • USE- VRSA, VRE, drug-resistant pneumococci
    • -both E. faecalis and E. faecium!

    SE-bone marrow suppression! (esp. thrombocytopenia)
  44. Quinupristin-Dalfopristin
    • Streptogramins
    • -bacteriostatic
    • -block A site (like tretracycline) from 50S
    • block release of peptide from ribosome.

    • USE-VRSA, VRE (alternative to Vancomycin resistance-D-ala-D-lactate)
    • -E. faecium, but NOT E. faecalis
  45. antibiotics to NOT use in pregnancy
    • Aminoglycosides
    • Fluoroquinolones
    • Sulfonamides
    • Tetracyclines
  46. Sulfomethoxazole
    Sulfisoxasole, Sulfadiazine
    • inhibitor of bacterial folic acid synthesis
    • -bacteria make their folate from PABA + Pteridine w/ Dihydropteroate synthetase
    • -inhibit dihydropteroate synthetase
    • -bacteriostatic
    • -acetylated by liver-->less soluble metabolite!!-->renal excreted

    • USE- see w/ Trimethoprim
    • -synergy w/ dihydrofolate reductase inhibitors
    • -sulfonamides alone useless b/c multiple drug resistance!!

    • SE- hypersensitivity (rash, steven-johnson syndrome)
    • Hemolysis in G6PD deficiency, crystalluria in kidney!, phototoxic
    • high protein binding-->kernicterus in neonates! (displace bilirubin from albumin)
  47. Trimethoprim, Pyrimethamine
    • inhibitor of bacterial folic acid synthesis
    • -bock dihydrofolate reductase (in humans too)
    • -bacteriostatic

    USE- combo w/ sulfonamides

    • SE-anticancer like effects!
    • -Megaloblastic anemia, leukopenia, granuloytopenia (give leucovorin!)
  48. Trimethoprim-sulfomethoxazole TMP-SMX
    inhibit Dihydropteroate synthetase + dihydrofolate reductase (synergy)

    • USE-Nocardia! Listeria (backup to amoxicillin) UTIs!
    • -gram- (E.coli, samonella, shigella, H.influenza)
    • -gram+ (staph, MRSA)
    • -Pneumocystis jiroveci !! CD4<200
  49. Sulfadiazine + Pyrimethamine
    USE- Toxoplasma gondii (CD4 <100)
  50. Sulfa allergies
    • Sulfa-allergic pts:
    • do NOT give

    • -sulfa drugs- sulfasalazine, sulfonylureas
    • -thiazides
    • -acetazolamide
    • -furosemide
    • -celecoxib
    • -probenecid
  51. Ciprofloxacin, Norfloxacin, Levofloxacin, Sparfloxacin, Nalidixic acid

    • Fluororquinolones
    • -direct DNA synthesis inhibitor
    • -bacteriocidal
    • -block DNA gyrase (topoiosomerase II)-neg supercolis
    • -block topoisomerase IV- separate replicated DNA
    • -Fe,Ca limit absopriton (like tetracyclines)-don't eat w/ food
    • -renal excretion (inhibited by probenecid)

    • USE-UTIs, STDs, PID (Chlamydia, gonorrhea)
    • - gram- skin, soft tissue, bone infections (salmonella, pseudomonas)
    • -Diarrhea by Shigella, Salmonella, E.coli, Campylobacter
    • -drug resistant pneumococci (levofloxacin)
    • -Anthax!

    • SE-Phototoxcity, rash, insomnia/headache, Tendonitis, tendon rupture, QT prolong!
    • do NOT use in pregnancy and Kids!
  52. Metronidazole
    • bacteriocidal
    • -form free radicals--> damage bacterial DNA
    • -anaerobes below diaphram

    • USE- 1st choice for Giardia,Entamoeba,Trichomonas
    • -most anaerobes: Bacteroides, Clostridium (not Actinomyces)
    • -1st choice for C.diff Pseudomembranous colitis!
    • -triple therapy for H. Pylori (Bismuth +tetracycline/amoxicillin)

    SE- metallic taste, Disulfram-like effect, peripheral neuropathy
  53. H. Pylori regimen
    • 1. BMT regimen:
    • Bismuth, Metronidazole, Tetracycline

    2. Clarithromycin, amoxicillin, omeptrazole

    -decrease peptic ulcer, decrease risk of adenocarcinoma, MALT lymphoma
  54. Anti-TB drugs
    name 5
    and backups
    • Isoniazid
    • Rifampin
    • Ethambutol
    • Pyrazinamide
    • Streptomycin

    • backups:
    • Aminoglycosides (Streptomycin, amikacin, kanamycin)
    • Fluoroquinolones
    • Capreomycin (hearing loss)
    • Cycloserine (neurotoxic)
  55. Isoniazid
    • anti-TB drug
    • -inhibit mycolic acid synthesis
    • -must be activated by bacterial catalase (KatG-gene)
    • -HIGH resistance (mutate KatG gene)

    • USE- only one for solo prophylaxis for TB
    • -combo therapy for TB
    • - give with vit B6!

    SE- hepatotoxic! Pyridoxine deficiency!! (use up all B6--> neurotoxicity from sideroblastic anemia (high Ferritin, %sat, low TIBC) (give Pyridoxine B6), SLE-like in slow acetylators
  56. Rifampin
    • anti-TB drug
    • -block bacterial transcription of DNA
    • (RNA polymerase inhibitor)

    • USE- combo therapy for TB
    • -meningococcal prophylaxis
    • -prophylaxis of H. influenza
    • -Leprosy

    • SE- hepatotoxic, induce CYPs!
    • -Red oragne body fluids!!
  57. Ethambutol
    • anti-TB drug
    • -inhibit cell wall carbohydrate polymerization by blocking arabinosyltransferase

    USE- combo therapy for TB

    SE- optic neuritis! can't tell red vs green!!
  58. Pyrazinamide
    • anti-TB drug
    • -prodrug
    • -effective in acidic pH of phagolysosomes of Macs where TB lives

    USE- combo therapy for TB

    SE- hepatotoxic, Hyperuricemia (compete w/ uric acid for excretion)
  59. Streptomycin

    USE- IV for TB

    SE- ototoxicity, nephrotoxicity, NMJ blockade
  60. Regimen for TB
    Prophylaxis- Isoniazid

    Rx- Isoniazid, Rifampin, Pyraxinamide, Ethambutol
  61. Regimen for Mycobacterium avium-intracellulare
    Prophylaxis- Azihromycin or Clarithromycin

    Rx-Rifampin, Azithromycin, Ethambutol, Streptomycin
  62. Regimen for Mycobacterium leprae
    Prophylaxis- none

    Rx- Dapsone, Rifampin, Clofazimine
  63. Prophylaxis for Meningococcal
    • Rifampin
    • Minocycline (backup)
  64. Prophylaxis for Gonorrhea
    Ceftiaxone (cephalosporin)
  65. Prophylaxis for Syphilis
    Benzathine Penicillin G
  66. Drug of choice for
    History of recurrent UTIs
  67. Prophylaxis for Pneumocystis jiroveci

    Pentamidine (backup)
  68. Prophylaxis for
    Endocarditis w/ surgical/dental procedure
  69. Prophylaxis for M. avium intracellulare