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