pharm(abx)

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sun_flower87
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156834
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pharm(abx)
Updated:
2012-06-01 22:53:36
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ABXs
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starred in class
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  1. What are 4 wrongs of pen G?
    • 1. Narrow spectrum
    • 2. Acid sensitive
    • 3. Beta lactamarase sensitive
  2. pen V?
    Oral form of pen G
  3. herpes virus infection indicaiton?
    Pen G
  4. If staph aureus is resistant to methicillin what do you use instead?
    Vancomycin
  5. Aminopen?
    • Extended spectrum (include gram-)
    • Ampicillin, amoxilcillin
    • Nitrogen group allows it to penetrate gram- cell wall
  6. What do you use tx pseudomonas?
    • Carboxypen (cabenicillin, ticarcillin)
    • Ureidopenicillin (piperacillin, azlocillin, mezlocillin)
    • But these are sensitive to beta lactamase so must combine with b-lactamase inhibitors (clavulanic acid, sulbactan, tazolbactam
  7. Beta latamase inhibitor?
    • Clavulanic acid
    • Sulbactam
    • Tazobactam
  8. What do you use to tx staph aureus?
    • Methicillin
    • nafcillin
    • Isozazyolyl pen
    • Addition of bulky R group makes it resistant to beta lactamase
  9. Mechanism of pen?
    • *Binds to PBP (pen binding protein) or transpeptidase and inhibit cell wall synthesis
    • *creating pores in membrane; collapse of mem potential
    • --> eventual cell lysis
  10. How pen blocks cell wall synthesis?
    • Stereochem similarity
    • B-lactam ring CO-N bone is very similar to bacterial CO-N bond In cell wall --> so prevent cross linking
  11. Slow release form of pen?
    Procaine, benzathine
  12. Which pen has to be given by IV?
    • Pen G
    • Antipseudomonals (mezlocillin, piperacillin)
    • Ticarcillin
  13. Probenicid?
    Inhibits tubular secretion and so can be used to elevate blood level
  14. Adverse effect of pen
    • - Allergic rxn (hypersensitivity rxn - most common) (high with ampicillin)
    • - acute anaphylactic rxn (tx with epi)
    • - superinfection
    • - hyperkalemia (possible arrythmia or cardiac arrest)
  15. Mechanism of resistance of pen
    Change in PBP (important in g+; s aureus resistnace to methicillin, pneumococcus
  16. Presence of pen triggers b lactamase production?
    True
  17. Use of pen in dentistry
    • Amoxicillin orally
    • Ampicillin parenterall
  18. Cephalosporins
    • 6membered dihydrothiazine ring + beta lactam ring
    • Bacteriocidal
  19. 1st gen of Cephalosporins
    • Cefazoline
    • Cephalothin
    • Cephalex (oral)
    • Greayest activity vs g+
  20. 2nd gen of Cephalosporins
    • Cafaclor (oral)
    • Cefoxitin (actice vs bacteriodes fragilis, serratia marcescens)

    • Extended spectrun (gram-) due to increase in
    • affinity to PBP
    • Penetration to g- cell wall
    • Resistance to b-lactamase
  21. Third gen of Cephalosporins
    • Cafriaxone (vs pseudomonas)
    • Cefotaxime
    • Caftazidime (vs pseudomonas)
    • Ceftizoxime
    • Cefpodoximine proxetil (oral)

    Useful for menigitis by g-

    Addition of AMINOTHIZOKE MOIETY to beta lactam increased the activity va g-
  22. Fourth gen of cephalosporins
    Active vs pseudomonas

    Cafepime is ZWITTERION and has enhanced activity to penetrate the porin in g-
  23. Adverse effect of cephalosporin
    • Convulsion
    • MTT (cafamandole, cafotetan, cafoperazone, cafopnicid)★★★
    • Interferes with vK formation -clotting problem
    • 5-10% ppl allergic to pen also allergic to this
  24. Azetreonam
    Monocyclic lactam - unique spectrum (aerobic g-) (pseudomonas)

    Mechanism: sulfonic acid group binds to PBP3

    im or iv

    Alternative when allergic to pen
  25. What can you use when pt is allergic to pen?
    Azetreonam
  26. Vancomycin
    • Tricyclic glycopeptide
    • Used to tx SERIOUS RESISTANT TO STAPH ENTEROCOCCUS AND STREPH INFECTION or pen allergy

    IV

    Adverse effect: red man or red neck syndrone, ototoxic -permanant hearing loss

    Resistance: replace D-ala with D-lactate
  27. Carbapenem
    • Imipenem/cilastatin given together★★
    • A carbon instead of sulfur

    Pulmonary intra ab and soft tissue infection

    • Meropenem (imipenem) is resistant to degradation by dehydropeptidase 1
    • So it must be given with cilastatin (competitive dehydropeptidase1 inhibitor)

    Iv or im
  28. Bacitracin
    • Bactericidal vs g+
    • Use it only as topically bc too toxic
  29. Fosfomycin
    Inhibit cell wall synthesis by blocking formation kf n-acetylmuramic acid
  30. Cycloserine
    To tx TB that is resistant to first line choices

    • Toxic - not the First line drug
    • Inhibit alanine ligase or alanine racemase
  31. Tetracycline
    • Wk base supplied as hydrochloride salt
    • Doxycyclune most used now

    Borrelia burgdorferi - lyme dz - carried by tick - amoxicillin or tetracycline

    Inhibit protein synthesis (30S)

    Oral

    • Absorption:
    • Best under acidic condition
    • Impaired by milk products (chelastion, increase in PH)

    During formation of bone, dentin, enamel of unerupted teeth: discoloration

    • Adverse effects: discolored band, growth inhibition, photosensitization
    • Contraindicated in pregnancy

    Resistance: increase efflux
  32. Chlorolamphenicol
    Broad spectrum (only for SERIOUS INFECTION: meningitis, typhoid fever when others don't work)

    50S

    Adverse effects: toxic bone marrow depression, Aplastic anemia, gray baby syndrome
  33. Gray baby syndrome
    Chloramphenicol
  34. Aplastic anemia
    Chloramphenicol
  35. Red neck or redman syndrome?
    Vancomycin
  36. Aminoglycoside
    Synergistic action with pen to tx enterococcal endocarditis

    Tx penumonia cause by pseudomonas!!

    • Neomycin for topical infection of skin
    • Neosporin (neomycib, polymyxinB, bacitracin)

    30S - BACTERIOCIDAL!! Conc dependent

    Basic so may react with pen (acidic) or cephaloporin in high conc

    • Adverse effects:
    • 1.renal damage (nephrotoxicity)
    • 2.ototoxicity (destruction of vestibular (headache) or cochlear (tinnitus) sensory cells)
    • 3.fetal exposure in pregnancy
    • 4.respiratory paralysis

    • Resistance:
    • Acetyltransferase, phosphotransferase, adenyltransferase
  37. Ab distention, vomiting, cyanosis, hypothermia, irregular respiration, vasomotor collapse from chloramohenicol
    Gray baby syndrome
  38. Mcrolides
    Macro - many rings

    • Erythromycin (alternative for pen)
    • Azithromycin (acid stable)

    • Peptic ulcer dz (helicobacter pylori)
    • Clarithromycin + omeprazole + amoxicillin

    • Legionella pneumonia
    • Azithromycin bc
    • 1.excellent activity
    • 2.Sup tissue conc
    • 3.easy admin as single daily dose
    • 4.Better tolerability
    • 5.Longer half life

    • Chlamydia trachomatis (trachoma, urethritis) - eye dz, inflammation
    • Azithromycin and erythromycin can be used during pregnancy

    50S

    Erythromycin best absorbed under alkaline condition - acid sensitive

    • Adverse effects:
    • Cholestatic hepatitis (mainly by erythromycin)
    • Inhibit P450 isoenzyme

    • Resistance:
    • Production of methylase enzyme - modify ribosomal target. Can no longer inhibit protein synthesis
  39. Clindamycin
    Anaerobic g- : used in dentistry

    • Lung and pleural infection
    • No predictable for brain access as poor penetration into CSF

    50S

    Flavored suspension for peds use

    • Adverse effects:
    • PSEUDOMEMBRANEOUS COLITIS due to superinfection with chlostridium difficile

    (Bc its free radical wipe off all chlostridium; not selective)

    Combined with beta lactams for serious infection
  40. Pseudomembraneous colitis
    Clindamycin
  41. Adverse effect of clindamycin?
    Pseudomembraneous colitis
  42. Metronidazole
    Enters abcess!! Important for dentists

    • Free radicals
    • Conc dependent killers - diffuse into cells and nitro grouo is reduced to metabolites that damages DNA leading to cell death★

    Adverse effects: disulfiram rxn with ethanol (nausea and flushing) -inhibit alcohol metabolism★

    • Use in dent?
    • Progressive periodontitis with combination of beta lactam
  43. Sulfonamide & trimethiprim
    • Sulfa in names
    • (Except mefanide)

    • Co-trumoxazole: Trimethiprim combined with sulfamethoxazole
    • Useful for peumocystis carinii infection in AIDS pts★

    Alleric rxn, skin rash, serum sickness★

    Synergistic effect
  44. what is the mechanism of sulfonamides and trimethoprim?
    inhibition of folic acid production
  45. which of the followin gdoes not inhibit dihydrofolate reductase?
    1. sulfonimides2. trimethoprim3. methotrexate4. pyrimthamine
    • answer: sulfonimides
    • sulfonimides inhibits dihydrofolate synthase
  46. fluoroquinolones
    • cliprofloxacin (cipro) - choice for post-exposure prophylaxis of inhalation anthrax ***
    • (floxacin in names)

    aerobic gram-

    mechanism: inacativate DNA gyrase (g-) and topoisomerase IV (g+) and promote DNA trand break

    contraindicated in pragancy
  47. adverse effects of sulfonamides and trimethoprim?
    • kernicterus in infants
    • (displacement of bilirubin)
  48. kernicterus in infants?
    sulfonamides and trimethoprim
  49. TB agent
    • isoniazid
    • rifampin
    • pyrazinamide
    • ethambuterol

    • streptomycin
    • aminosalicyic acid
    • ethionamide
  50. isoniazid
    TB agents

    peripheral neuritis - more common in slow acetylators; protecdt with pyridoxine
  51. rifampin
    TB agent

    reduce rate of emergence of resistance if used in combination

    • inhibits DNA dependent RNA polymerase
    • Binds to (b subunit) and inhibit DNA-dependent
    • RNA polymerase of mycobacteria and other microorganisms.
    • (*)

    • inducer of cytochrome p450
  52. orange red brown color?
    clofazidine
  53. ethanbutol
    TB

    optic neuritis with decrease in visual acuity and loss of ability to discrimate colors
  54. streptomycin
    TB

    • used in resistant cases
    • very good for treating TB
  55. Dapsone
    • mechanism of action**
    • interfere with the synthesis of folic acid by acting as competitive inhibitors of dihydrofolate synthetase

    (structurally similar to sufonamides obviously)

    • advers effect: methemoglobinemia
  56. methemoglobinemia
    dapsone
  57. leprosy agents?
    • dapsone
    • clofazimine
  58. clofazimine
    leprosy

    • adverse effect*
    • color urine, feces, sputum, sweat red*
  59. antifungal agnets
    • amphotericin B
    • nystatin
    • flucytosin
    • azoles
    • iodide
    • griseofulvin
    • pneumocadins and papulocandins
  60. amphotericin B
    binds to sterols (ergosterol - fungal cholesterol) in cell membrane forming pores or channels

    you dont want to use amphotericin B with imidazoles
  61. nystatin
    candidal infection of the oral cavity (oral moniliasis, thrush, denture stomititis)
  62. flucytosine
    antifungal

    combined with amphotericinB for cryptococcal meningitis in AIDS pts
  63. most broad spectrum ABX?
    tetracycline!!
  64. Azoles
    • imidazole (2Ns): systemic candidiasis
    • triazoles (3Ns): topical

    • mecahnism of action
    • azole inhibit the synthesis of ergosterol by inhibiting sterol 12-a-demethylase, a cytochrom p450 dependent enzyme system

    • adverse effects:
    • hepatotoxicity and increase in liver enzyme
    • fetal hepatic necrosis
    • ketoconazole causes gynecomastia and menstrual irrecularities by lowering steroid biosynthesis ***
  65. griseofulvin
    antifungal

    • spectrum of action
    • use liumited to infection of the skin, hair, and nails
  66. fungal infection of skin, nail, hair?
    what do you treat with?
    griseofulvin
  67. Pneumocandins and papulocandins
    new antifungal

    inhibit cell wall synthesis by inhibiting b-1,3-glucan synthetase (not in human cells - safe)

    effective vs azole resistant C albicans
  68. Agents to treat AIDS!
    • neucleoside reverse transcriptase inhibitors
    • 1. zidovudine (retrovir)
    • 2. didanosine
    • 3. zalcitabine
    • 4. stavudine
    • 5. lamivudine
    • 6. abacavir

    • non-neucleoside reverse transcriptase inhibitors
    • (these directly inhibit RT w/o being incorporated into the DNA)
    • 1. nevirapine
    • 2. delavirdine
    • 3. efavirenze

    • HIV protease inhibitors
    • 1. saquinavir
    • 2. ritonavir
    • 3. indinavir
    • 4. nelfinavir
    • 5. amprenavir
  69. what is the adverse effect of using HIV protease inhibitors?
    HIV protease inhibitors1. saquinavir2. ritonavir3. indinavir4. nelfinavir5. amprenavir

    buffalo humps - fat deposit and redistribution
  70. VIRAL respiratory infections (influenza)
    • amantadine
    • rimantadine

    • mechanism of action
    • - prevent viral replication
    • - prevent fusion of viral memebrane with host cell membrane - interfere with release of new virus

    • zanamivir
    • oseltamivir
    • (neuraminidase inhibitor)
  71. herpes virus
    • mechanism:
    • Converted to triphosphate with viral-specific thymidine kinase. Triphosphate selectively inhibits virus DNA-polymerase and thus inhibits viral DNA replication
  72. herpes virus infection indicaiton?
    ganciclovir useful for CMV retinitis in imunnocompromised pt

    • Initial and recurrent herpes genitalis,
    • Herpes simplex encephalitis, mucocutaneous
    • infections in immunocompromised
    • patients. Useful in Herpes zoster infections (shingles)
  73. 30S
    • tetracyclin
    • aminoglycosides (bacteriocidal)
  74. 50s
    • chloramphenicol
    • macrolides
    • clindamycin

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