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26 Cards in this Set

  • Front
  • Back
Mechanism of action of sulfonamides
competes with PABA during folate synthesis to inhibit dihydropteroate synthase
Why don't sulfonamides have an effect on human folate?
sulfonamides only inhibit folate SYNTHESIS. humans don't synthesize folate. sulfonamides have no effect on folate use
Dihydropteroate synthase is inhibited by high levels of...
sulfonamides
Trimethoprim inhibits which enzyme?
DHFR, dihydrofolate reductase. now dihydrofolate cannot become FH4 (tetrahydrofolate) to be used in purine synthesis
3 ways of resistance to sulfonamides
very high PABA levels, folate production enzyme with low sulfonamide affinity, low sulfonamides permeability, mutant target enzymes
Major mode of distribution of sulfonamides
oral
Sulfonamide-trimethoprim together have what sort of effect?
synergistic. both work on sequential steps of folate synthesis/usage
Sulfacetamide, a topical sulfonamide, has a side effect of metabolic acidosis. Why?
it is a carbonic anhydrase inhibitor = no CO2 removal in the lung = acidosis
Stevens-Johnson syndrome is a fatal side effect of which class?
sulfonamides
Major sulfonamide adverse reactions
crystalluria, rashes (even the fatal Steven-Johnson syndrome), hemolytic/aplastic anemia
Why doesn't trimethoprim (inhibitor of folate usage) lead to human cell death?
human DHFR is way less reactive to trimethoprim (50,000x less active against humans)
Sulfonamides alone are (bactericidal or bacteriostatic)?
bacteriostatic
Sulfonamides + trimethoprim are (bactericidal or bacteriostatic)?
bactericidal
Trimethoprim is usually given by what route?
alone orally; with sulfa drugs it is IV
Trimethoprim concentrates in what parts of the body?
prostate and vagina
Megaloblastic anemia is seen in patients on which drug?
trimethoprim (mimics folate deficiency)
Quinolones mechanism of action
block DNA gyrase (topoisomerase 2) + topoisomerase 4. both
DNA gyrase function
relaxation of DNA coils. helps unwind DNA
Topoisomerase 4 function
relax DNA coils
Function of Qnr proteins against quinolones
protects DNA gyrase from the quinolones
Anthrax is treated with...
ciprofloxacin
Trimethoprim + Sulfamethoxazole is first line therapy for ...
P. jiroveci pneumonia
Pyrimethamine + sulfadiazine is first line therapy for what infection?
toxoplasmosis
Pyrimethamine + sulfadiazine is second line therapy for what infection?
malaria
Arthritis-like symptoms are a common side effect of which drug?
Fluoroquinolones
Chlamydial urethritis and cervicitis is best treated with which drugs?
levofloxacin and ciprofloxacin;