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22 Cards in this Set

  • Front
  • Back

Cycloserine

Class- structural analogue of D-Ala


SOA- 1st stage of CW synthesis, low MW precursors synthesized


Bacteriocidal


Broad G+ and G-, mostly used for TB


CNS toxicity (restricted to TB rx)

Bacitracin

Class- polypeptide with thiazoline ring


SOA- 2nd stage of CW synthesis. inhibits dephosphorylation of lipid pyro-po4


Bacteriocidal


G+ bacteria


Systemic toxicity, use topically

Beta Lactams


(penicillin and cephalosporins)

Class- Beta Lactams


SOA- 3rd Stage of CW synthesis. covalently bind PBP (transpeptidase) to prevent x-ling between last glycine and penultimate d-ala


Bacteriocidal


Broad Spectrum


Oral and Parenteral

Vancomycin

Class- Glycopeptide


SOA- Cell Wall, blocks transglycolation


Bacteriocidal


Gram +


Parenteral (except C. Difficile = oral)


overuse can lead to Van R enterococci/staph

Aminoglycosides


(gentamicin, tobramycin, amikacin, neomycin, streptomycin)

Class- aminoglycosides


SOA- Irreversibly bind 30s subunit, interrupt cycle at initiation of protein synthesis


Bacteriocidal


Broad G+ and G- but not anaerobes


Parenteral only


nephrotoxic/ototoxic


synergistic with B-lactams

Tetracyclines

Class- Tetracyclines


SOA- bind reversibly to 30s subunit. prevents polypeptide synthesis


Bacteriostatic


Broad spectrum


Iron/antacids/dairy/food impair absorption


depression of bone w/ sustained use


intracellular activity

Chloramphenicol

Class- chloromycetin (nitrobenzene ring)


SOA- Binds 50s subunit reversibly, prevents transpeptidation/elongation


Bacteriostatic


Broad spectrum


Oral and parenteral


cause bone marrow suppression --> aplastic anemia


good for some anaerobes


last resort

Erythromycin

Class- Macrolides


SOA- bind 50s subunit reversibly, blocks translocation/elongation


Bacteriostatic (high level - cidal)


Broad spectrum (mainly G+, some G-)


Good for pt allergic to penicillin


intracellular activity

Lincomycin and Clindamycan

Class- Lincosamides


SOA- Binds 50s subunit and inhibit peptide bond formation


Bacteriostatic (cidal at high conc)


Mostly G+ and anaerobes


no interference with food

Sulphonamides

Class- Sulfa drugs


SOA- analogue of PABA- interferes with folic acid metabolism (purine/pyrimidine)


Bacteriostatic


Broad spectrum, some parasites and protozoa


Distributed throughout body


synergistic with trimethoprim


nausea, vomiting, diarrhea, hypersensitivity


(take a lot of water)

Trimethoprim

Class- Trimethoprim


SOA- Selective inhibitor of dihydrofolate reductase (anti folic acid)


Bacteriostatic (high concentration = cidal)


Broad spectrum


synergistic with sulfa

Quinolones


(ciprofloxacin, levoquin, moxifloxacin, nalidixic acid)

Class- Fluoroquinolone


SOA- inhibits DNA gyrase and topoisomerase


Bacteriocidal


Broad G- and G+


Doesn't work against MRSA


Gyrase = supercoling, Topo IV = separation of daughter strands


increased R because of overuse

Rifampin (macrocyclic)

Class- aromatic ring system spanned by long aliphatic bridge


SOA- binds RNA polymerase, inhibits mRNA synthesis


Bacteriocidal


Broad spectrum


R develops rapidly in vitro/ in vivo



Amphotericin B

Class- Polyenes


SOA- binds egosterol causing membrane pores


Fungicidal


Used on Fungi (yeast and mold)


fungi contain sterols (ergosterol) unlike humans

Azoles

SOA- interferes with cytochrome p-450 in ergosterol synthesis


Fungistatic


Fungi (yeast and mold)


hepatic elimination (avoid in pt with hepatic insufficiency)

Polymyxins

Class- Polymyxin B (cationic cyclic peptide)


SOA- detergent-like properties increase cell permeability


Bacteriocidal


Gram -, including pseudomonas


nephrotoxic and neurotoxic

Cell Wall

Cycloserine- 1st stage (precursors synthesized) (G+ and G-, TB)




Bacitracin- 2nd stage (dephosphorylation)


(G+)




B-lactam (penicillin/cephalosporin)- 3rd stage (transpeptidase / PBP) (Broad)




Vancomycin- prevents precursors into growing PG (G+)




ALL BACTERIOCIDAL

30s Ribosomal subunit

Aminoglycoside- irreversible, causes nonsense proteins (G+ and G-, not anaerobes)


-bacteriocidal




Tetracycline- reversible (broad spectrum)


-bacteriostatic

50s ribosomal subunit

Chloramphenicol- binds reversibly (broad)


-static




Erythromycin- reversible (mostly G+, some G-)


-static (high conc = cidal)




Clindamycin/Lincomycin- reversible (G+ and anaerobes)


-static (high conc = cidal)

Metabolic disruption

Sulfonamides- interfere with folic acid metabolism / purine pyrimidine synthesis


-broad/parasites, static




Trimethoprim- selective inhibitor of dyhydrofolate reductase


-broad, static




SYNERGISTIC

Nucleic Acid Synthesis disruption

Quinolones- Inhibit gyrase and topoisomerase


-G- and G+, bacteriocidal




Rifampin- bind RNA polymerase, inhibit mRNA synthesis


-Broad, bacteriocidal

Membrane Disruption

Polymyxin B- detergent-like, G- including pseudomonas


-bacteriocidal, neurotoxic/nephrotoxic




Amphotericin- Bind ergosterol --> pore


- fungicidal




Azoles- interfere with cytochrome p-450 in ergosterol synthesis


-fungistatic