shosh: antibiotics

  1. Mechanism of penicillin
    Inhibits transpeptidase cross-linking of bacterial cell wall
  2. Name 3 penicillinase-resistant penicillins
    What is their clinical use?
    • Methicillin
    • Nafcillin
    • Oxacillin

    Use for staph aureus (except for MRSA)
  3. Two extended spectrum penicillins
    -what needs to be added to treatment plan?
    • Ampicillin and amoxicillin
    • Use with clavulanic acid or sulbactam to protect against penicillinase
  4. Treatment of choice for listeria and e. coli
    Ampicillin or amoxicillin
  5. Three anti-pseudomonal penicillins
    Ticarcillin, piperacillin, carbenicillin + clavulanic acid, sulbactam, or tazobactam
  6. Two first generation cephalosporins and their main clinical use
    • Cefazolin, cephalexin
    • Use for surgical prophylaxis, due to their long half lives
  7. Three third generation cephalosporins and their major clinical uses
    • Cefotaxime, ceftazidime, ceftriaxone
    • Use to treat gonorrhea, sepsis, and meningitis (can cross the BBB)
  8. Name four bacteria that third generation cephalosporins do not work on
    • Listeria--penicillin
    • Atypicals--macrolides
    • MRSA--vancomycin
    • Enterococci--amoxicillin
  9. Mechanism and clinical use of aztreonam
    • Inhibits cell wall synthesis
    • Synergistic with aminoglycosides
    • No cross-allergenicity with penicillin--can be used as an alternative in patients with penicillin allergy
    • ONLY works on gram negative rods
  10. What needs to be administered with imipenem?
    Cilastatin, to inhibit renal inactivation
  11. Major side effect of imipenem
  12. Mechanism and clinical use of vancomycin
    • Inhibits D-ala D-ala in bacterial cell walls
    • Use for bad gram positives (S. aureus, clostridium)
  13. Why can't furosemide or gentamycin be used with vancomycin?
    Risk of ototoxicity
  14. Drug that causes red man syndrome, due to hypersensitivity reaction
  15. Name five aminoglycosides, and their mechanism of action
    Gentamycin, neomycin, amikacin, tobramycin, streptomycin

    • Inhibit formation of the initiation complex, block mRNA translation
    • Require oxygen for uptake, so don't work against anaerobes
  16. Side effects of aminoglycosides
    • Nephrotoxicity
    • Ototoxicity (especially when used with furosemide)
    • Teratogenic
  17. Antibiotic that acts like the botulinum toxin, and causes neuromuscular blockade
    Aminoglycosides (streptomycin, neomycin, amikacin, gentamycin, tobramycin)
  18. Mechanism of tetracycline
    Binds to 30S subunit, blocks binding of aminoacyl-tRNA
  19. Why can't tetracycline be taken with antacids or milk products?
    • Tetracycline binds to divalent cations in the gut, which inhibits its absorption (and absorption of the cations)
    • Inhibition of Ca absorption can cause dysplastic changes to teeth and bones
  20. Drug of choice for lyme disease
  21. Demeclocycline
    A tetracycline that acts as an ADH antagonist. Used to treat SIADH, not used as an antibiotic
  22. Mechanism and use of macrolides
    • Bind to 50S subunit, block translocation
    • (names all end in ...thromycin)
    • Use for atypicals (mycoplasma, legionella, chlamydia, MAC)
  23. Side effects of macrolides
    • Prolongation of QT interval
    • GI discomfort, due to activation of motilin receptors
    • Acute cholestatic hepatitis
    • Increased concentration of oral anticoagulants
  24. Drug that causes aplastic anemia and gray baby syndrome
  25. Drug of choice for gram positive osteomyelitis
    Clindamycin--good for osteomyelitis because has good penetrance into bone, but DOES NOT WORK against gram negative osteomyelitis (i.e. salmonella)
  26. Drug of choice for macrolide-resistant pneumonia
  27. Drugs for VRE
    • Quinupristin, dalfopristin--bind to 50S ribosomal subunit
    • Linezolid--blocks initiation complex formation
  28. Enzyme inhibited by TMP-SMX
    Dihydropteroate synthetase
  29. Drug of choice for PCP
  30. Drug of choice for Chagas disease
    Nifurtimox (arsenic)
  31. Antibiotics that cause tendonitis
  32. Triple therapy
    • Bismuth
    • Metronidazole
    • Amoxicillin/tetracycline
  33. Side effect of metronidazole
    Disulfiram like reaction with alcohol
  34. Anti-TB drug that exacerbates gout
  35. Drug that causes red-green color blindness
  36. Drug of choice for P. vivax and P. ovale
  37. Side effects of isoniazid
    • Neurotoxicity, due to similarity with B6, and impaired B6 absorption
    • B3, niacin, deficiency, since B6 is needed to make B3
    • Hepatotoxicity
    • DI lupus
  38. Mechanism and clinical use of AMB
    • Binds to ergosterol, causes pores to form in cell membrane
    • Use for systemic mycoses (coccidioidomycosis, blastomycosis, aspergillosis, candida, mucor)
  39. Mechanism and use of nystatin
    • Binds to ergosterol, disrupts fungal membranes
    • Use for oral candida (too toxic for systemic use)
  40. Mechanism and use of azoles
    • Inhibit P450 14alpha demethylase, block sterol synthesis
    • Use for systemic mycoses
    • (Drug of choice in invasive aspergillosis)
  41. Drug of choice for pinworm infections
    Mebendazole (disrupts glucose uptake and microtubule structure)
  42. Mechanism of praziquantel
    Opens Ca channels in helminth cell membranes
  43. Mechanism of flucytosine
    • Inhibits RNA synthesis by conversion to 5-FU and incorporation into RNA change, inhibits DNA synthesis by inhibition of thymidine synthase
    • Use of systemic fungal infections
  44. Mechanism of caspofungin
    Inhibits synthesis of beta glucans, blocks cell wall formation
  45. Mechanism and clinical use of terbinafine
    • Inhibits squalene epoxidase
    • Use to treat dermatophytoses
  46. Mechanism and clinical use of griseofulvin
    • Deposits in keratin-rich tissues, inhibits microtubule function
    • Use for dermatophyte infection
    • Disulfiram-like reaction
  47. Mechanism and clinical use (2) of amantadine
    • Blocks viral penetration and uncoating
    • Causes release of DA from nerve terminals
    • Used to treat influenza A and Parkinson's
  48. Mechanism and use of zanamivir and oseltamivir
    • Inhibits influenza neuraminidase
    • Side effects are flu-like symptoms. Heehee.
  49. Mechanism and clinical use of ribivarin
    • Inhibits IMP dehydrogenase, blocks synthesis of gaunine nucleotides.
    • Use to treat CMV and chronic hep C, in combo with alpha interferons
  50. Side effect of ribivarin
    Hemolytic anemia
  51. Mechanism and clinical use of acyclovir
    • A prodrug that is activated by bacterial thymidine kinase and causes chain termination.
    • Use for HSV, VZV, and EBV
  52. Mechanism and clinical use of gancyclovir
    • A prodrug that is activated by human cellular kinases and inhibits viral DNA polymerase
    • First line treatment for CMV
  53. Dose limiting side effect of gancyclovir
  54. Mechanism and clinical use of foscarnet
    • Inhibits viral DNA polymerase. Not a prodrug.
    • Use to treat CMV retinitis when gancyclovir doesn't work
  55. Side effects of foscarnet
    • Nephrotoxicity
    • Hypocalcemia, due to Ca chelation--can be life threatening if patient is also on pentamidine, for PCP
  56. Names and side effects of protease inhibitors
    • Squinavir, indinavir, ritonavir
    • Ritonavir has lots of interactions with other drugs
    • All protease inhibitors cause insulin resistance and lipodystrophy (buffalo hump, central obesity)
  57. Advantage of atazanavir
    Causes less hyperglycemia and lypodystrophy than most protease inhibitors
  58. Non-nucleoside reverse transcriptase inhibitors (3)
    • Nevirapine
    • Efavirenz
    • Delaviridine
  59. Side effect of efavirenz
    Insomnia, nightmares
  60. Class and side effect of abacivir
    • NRTI
    • Severe allergic reactions
  61. Drug that blocks GP-41 and sterically inhibits HIV fusion with host cell
  62. Drug that binds to CCR4
  63. HIV integrase inhibitor
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shosh: antibiotics