FallExam2Drugs_Antibiotics.txt

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FallExam2Drugs_Antibiotics.txt
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Antibiotics
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  1. Fluoroquinolones

    (drugs, use, MOA, MOR, adverse reactions)
    • Drugs: CIPROFLOXACIN (broad spect, gram -), LEVOFLOXACIN (broad spect, gram + and -)
    • Use: Give oral or IV but antacids decrease oral availability. Ear and eye drops agianst pseudomonas (-), staph (+) and strept (+). Levo also good for atypical respiratory bugs (mycoplasma and legionella)
    • MOA: Inhibit DNA gyrase (topo II) and topo IV. Bactericidal
    • MOR: 1. target modificaton 2.altered uptake/efflux 3. plasmid mediated modification by quinolone transacetylase
    • Adverse Reactions: Arthropathy (no pregnant, children, joint paint in elderly). QT interval prolongation (contra for antiarrythmic drugs or those that induce bradycardia)
  2. Rifampin

    (use, MOA, MOR, adverse reactions)
    • Use: First line drug for mycobacterium tuberculosis. Give Oral or IV with great CNS and intracellular dist
    • MOA: Inhibit RNA polymerase (bactericidal)
    • MOR: target site mutation in rpoB subunit
    • Adverse Reactions: liver problems, induce cyt p450 enzymes (bad or HIV meds), turns body fluid orange
  3. Metronidazole

    (use, MOA, MOR, adverse reactions)
    • Use: Gaurdia, Trichomonas, Anaerobes, Protozoa. Also bismuth and amoxicillin for triple therapy against H. Pylori.
    • MOA: Produce DNA toxic metabolites via pyruvate:ferredoxin oxireductase interference (bastericidal)
    • MOR: unknown
    • Adverse Reactions: Renal retention of lithium and ergot derivatives (NO ALCOHOL!!!)
  4. Sulfonamides

    (drugs, use, MOA, MOR, adverse reactions)
    • Drugs: SULFAMETHOXAZOLE, SULFADIAZINE, DAPSONE (leprosy, pneumo. carinii). ALL broad sprectrum against gram + and -.
    • Use: synergistic with trimethoprim "TMP-SMX" (Bactrim) for UTIs, Nocardia, Chlamydia. Give PO or IV. Topical cream with silver ions
    • MOA: PABA analog blocks folic acid synthesis (dihyropteroate synthetase inhibitor)
    • MOR: target site mutation, upregulates new genes, altered uptake/efflux via plamid and chromosomes
    • Adverse Reactions: Allergic reactions, Prophylaxis in HIV but can cause neutropenia and dermatitis, Not for patients who are pregnant, with folic acid deficiency or G6P deficiency
  5. Trimethoprime

    (Use, MOA, MOR, adverse reactions)
    • Use: synergistic with sulfonamide "TMP-SMX" (Bactrim) for UTIs, Shigella, Salmonella, Pneumo carinii
    • MOA: DHF acid analog blocks folic acid synthesis (DHF acid reductase inhibitor)
    • MOR: target site mutation, up-regulation of new genes, altered uptake/efflux
    • Adverse Reactions: Allergic reactions, Prophylaxis in HIV but can cause neutropenia and dermatitis, Not for patients who are pregnant, with folic acid deficiency or G6P deficiency
  6. Penicillin G/V

    (class, use, MOA, MOR, adverse reactions)
    • class: natural penicillin
    • Use: Oral or IV, crosses BBB, broad spectrum against gram + and - however decreased usage due to resistance
    • MOA: Binds transpeptidases to prevent cross linking and inhibits cell wall synthesis (bactericidal
    • MOR: mutated transpeptidases, beta-lactamases, altered uptake
    • Adverse Reactions: Allergic reactions, Hemolytic anemia
  7. Nafcillin

    (class, use, MOA, MOR, adverse reactions)
    • Class: artificial penicillinase resistant penicillin
    • Use: Oral or IV, crosses BBB, STAPH Aureus
    • MOA: Binds transpeptidases to prevent cross linking and inhibits cell wall synthesis (bactericidal)
    • MOR: mutation of transpeptidases, beta-lactamases, altered uptake
    • Adverse Reactions: Allergic reactions, hemolytic anemia
  8. Dicloxacillin

    (class, use, MOA, MOR, adverse reactions)
    • Class: artifical penicillinase resistant penicillin
    • Use: Oral or IV, crosses BBB, same as other penicillins
    • MOA: Binds transpeptidases to prevent cross linking and inhibits cell wall synthesis (bactericidal)
    • MOR: mutation of transpeptidases, beta-lactamses, altered uptake
    • Adverse reactions: hypersensitivity
  9. Ampicillin

    (class, use, MOA, MOR, adverse reactions)
    • Class: artificial pencillin; Use: Oral or IV, crosses BBB, HELPS kill enterococci (Haemophilus influenza, E. coli, Listeria monocytogenes, Proteus mirabilis, Salmonella, enterococci)
    • MOA: Binds transpeptidases to prevent cell wall synthesis (bactericidal)
    • MOR: mutation of transpeptidases, beta-lactamases, altered uptake
    • Adverse reactions: hypersensitivity, rash
  10. Amoxicillin

    (class, use, MOA, MOR, adverse reactions)
    • Class: artificial penicillin
    • Use: Oral or IV, crosses BBB, HELPS kill enterococci (Haemophilus influenza, E. coli, Listeria monocytogenes, Proteus mirabilis, Salmonella, enterococci)
    • MOA: Binds transpeptidases to prevent cell wall synthesis (bactericidal)
    • MOR: mutation of transpeptidases, beta-lactamases, altered uptake
    • Adverse reactions: hypersensitivity
  11. Amoxicillin/Clavulanate

    (class, use, MOA, MOR, adverse reactions)
    • Class: art. penicillin plus beta-lactamase inhibitor
    • Use: Oral when IV is not possible. Everything else is same as plain amoxicillin but clavulunate prevents resistance by inhibiting beta-lactamases
  12. Ampicillin/Sulbactam

    (class, use, MOA, MOR, adverse reactions)
    • Class: art. penicillin plus beta-lactamase inhibitor
    • Use: Everything is same as ampicillin but sulbactam prevents resistance by inhibiting beta-lactamases
  13. Piperacillin/Tazobactam

    (class, use, MOA, MOR, adverse reactions)
    • Class: art. penicillin plus beta-lactamase inhibitor
    • Use: IV only!! Pseudomonas. Similar to other pencillins but inhibits beta-lactamases
  14. Cephalexin

    (class, use, MOA, adverse reactions)
    • Class: Cephalosporin (1st gen.)
    • Use: PEaK (gram + cocci, Proteus mirabilis, E. coli, Klebsiella pneumoniae)
    • MOA: beta-lactam that inhibits cell wall synthesis but less susceptible to penicillinases (bastericidal)
    • Adverse Reactions: 5-10% PCN allergy cross hypersensitivity
  15. Ceftazidime

    (class, use, MOA, adverse reactions)
    • Class: Cephalosporin (3rd gen.)
    • Use: Pseudomonas, meningitis, serious gram neg. infections resistant to other beta-lactams
    • MOA: beta-lactam that inhibits cell wall sythesis but less susceptible to penicillinases (bactericida)
    • Adverse Reactions: 5-10% PCN allergy cross hypersensitivity
  16. Cefotaxime
    (class, use, MOA, adverse reactions)
    • Class: Cephalosporin (3rd gen.)
    • Use: serious gram - infections resistant to other beta-lactams, pseudomonas
    • MOA: beta-lactam that inhibits cell wall synthesis but less susceptible to penicillinase (bactericidal)
    • Adverse Reactions: 5-10% PCB allergy cross hypersensitivity
  17. Ceftriaxone

    (class, use, MOA, adverse reactions)
    • Class: Cephalosporin (3rd gen.)
    • Use: serious gram - infections resistant to other beta-lactams, pseudomonas
    • MOA: beta-lactam that inhibits cell wall synthesis but less susceptible to penicillinase (bactericidal)
    • Adverse Reactions: 5-10% PCB allergy cross hypersensitivity
  18. Imipenem/Cilastatin

    (class, use, MOA, adverse reactions)
    • Class: Carbapenem
    • Use: broad spectrum use with gram + cocci, gram - rods, and anaerobes. Enterobacter
    • MOA: beta-lactam inhibits cell wall synthesis by binding transpeptidases and blocking cross-linking. Cilastatin inhibits dihydropeptidase I to increase t1/2 life (normally inactivates in renal tubule in presence of dihydropeptidase I). Resistant to beta-lactamase
    • Adverse Reactions: PCN allergy cross-hypersensitivity, GI distress, skin rash, CNS toxicity at high plasma levels
  19. Aztreonam

    (class, use, MOA, adverse reactions)
    • Class: Monobactem
    • Use: For penicillin allergic patients and those with renal insufficiency who cannot tolerate aminoglycosides. Gram negative rods only (pseudomonas, klebsiella, serratia)
    • MOA: Inhibits cell wall synthesis by binding PBP3 and preventing cross-linking. Resistant to beta-lactamse.
    • Adverse Reactions: Few. No cross sensitivity with penicillin or cephalosporin
  20. Vancomycin

    (class, use, MOA, MOR, adverse reactions)
    • Class: Glycopeptidase; Use: MRSA!!!!! Against gram + organisms resistant to beta-lactams
    • MOA: Binds D-alanine to prevent crosslinking and inhibit cell wall synthesis (bactericidal)
    • MOR: Transposon- bacterial enzymes use D-serine or D-lactate to make cell wall
    • Adverse Reactions: Rapid IV administration can cause Red Man Syndrome (histamine mediated), nephortoxicity with aminoglycosides
  21. Bacitracin

    (class, use, MOA, adverse reactions)
    • Class: Polypeptide
    • Use: Topical with neomycin and polymyxin B neosporin
    • MOA: Blocks lipid carrier (inhibits dephosphorylation) used for cell wall components (bactericidal)
    • Adverse Reactions: Few, allergy
  22. Tetracyline

    (drugs, use, MOA, MOR, adverse reactions)
    • Drugs: TETRACYCLINE, DOXYCYCLINE (adm. less frequently than tetra, good for patients with renal failure cause fecal elimination), TIGECYCLINE (not affected by resistance mechanism)
    • Use: Broad spectrum including protozoa
    • MOA: blocks protein synthesis by inhibiting 30S ribosome (bacteriostatic)
    • MOR: (not for Tigecycline) Efflux pumping, ribosome binding protein
    • Adverse reactions: Anatogonistic with Beta-lactams. Discoloration of teeth (not for children or prenant), nausea, photosensitivity, rash (sun exposure). Can not with milk, antacids or iron containing cus divalent cation inhbits absorption in gut.
  23. Macrolides

    (drugs, use, MOA, MOR, Adverse reactions)
    • Drugs: ERYTHROMYCIN (seldom used due to QT prolongation and more nausea), AZITHROMYCIN (children and preganant women, long half life so take less frequently), CLARITHROMYCIN (extended release version available)
    • Use: broad spectrum including respiratory pathogens. Used in patients with penicillin allergy
    • MOA: block protein synthesis by binding 50S ribosome
    • MOR: methylation of ribosome, efflux pumping
    • Adverse reactions: Erythromycin can cause QT prolongation
  24. Clindamycin

    (class, use, MOA, MOR, Adverse reactions)
    • Class: Lincosamides
    • Use: IV, PO or topical gram + and anaerobes (protozoa). Not for gram - (can not cross outer membrane)
    • MOA: binds 50S ribosome to block protein synthesis
    • MOR: ribsome RNA methylation, altered proteins, and adenylatio
    • Adverse Reactions: Allergy
  25. Linezolid

    (class, use, MOA, MOR, Adverse reactions)
    • Class: oxazolidinone
    • Use: give IV or PO for gram positives, multiple resistant staph and entercocci
    • MOA: binds 50S ribosomes
    • MOR: mutation of 23s rRNA
    • Adverse Reactions: Thrombocytopenia with long term use, Contra with SSRI
  26. Chloramphenicol

    (use, MOA, MOR, Adverse reactions)
    • Use: seldom used today but broad spectrum IV or PO
    • MOA: binds 50S ribosome
    • MOR: acetylation, efflux pumping
    • Adverse reactions: aplastic anemia, bone marrow suppression, gray syndrome, dose adjustment with liver problems
  27. Quinupristin-Dalfopristin

    (class, use, MOA, MOR, Adverse reactions)
    • Class: streptogramins
    • Use: IV admin. for drug resistant enterococci (gram +)
    • MOA: binds 50s ribosome
    • MOR: efflux pumping or methylation only if one of the two are given
    • Adverse Reactions: Athralgias, Myalgias
  28. Mupirocin

    (use, MOA, MOR, Adverse Reactions)
    • Use: Topical drug resistant gram + (S aureus)
    • MOA: blocks protein synthesis of bacterial ribosomes by inhibiting isoleucine tRNA synthetase
    • MOR: target site mutation
    • Adverse reactions: unclear
  29. Polymyxins

    (use, MOA)
    • Use: topical use for gram negatives. Also IV or IM
    • MOA: distrupts bacterial membrane by charge alteration
  30. Daptomycin

    (use, MOA, Adverse reactions)
    • Use: IV admin for drug resistant gram +
    • MOA: cyclic lipopeptide that disrupts membrane by pore formation
    • Adverse reactions: elevated liver function tests, muscle weaknes, and pain with increased CPK
  31. Nitrofurantoin

    (Use, MOA, MOR, Adverse reactions)
    • Use: PO admin for uncomplicated UTIs (concentrated in the urine)
    • MOA: unclear, mimics radiation damage, enzymatic reduction for activity
    • MOR: altered levels of reduction enzyme
    • Adverse Reactions: turns urine brown, lung problem with prolonged use
  32. Aminoglycosides
    • Drugs: streptomycin, gentamicin, tobramycin; Post-ABX effect: persistent suppression after drug removal, Conc-dep killing: high conc better killing
    • Use: IV or MI against gram negatives (not for anaerobes)
    • MOA: binds 30S ribosome and also distrupts bridges between LPS
    • MOR: Modifying enzymes, efflux pumping, and altered ribosome binding
    • Adverse reactions: nephrotoxicity and ototoxicity FUCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCKKKKKKKK!!! I'm not making anymore cards ever again!

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