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Term can ONLY modify the R group at the amino group on the bottom no substituents on the phenyl ring other than the amine (which has to be primary) drugs with the highest activity have a pKa close to that of PABA (pKa = 6.5). to do this you have to add EWGs on the R position, commonly heterocycles.	Definition SAR of sulfonamides
Term bacteriostatic effect (when used alone) folic acid inhibitors = antimetabolites folic acid PABA is very similar to sulfonamides. the drug will be inserted instead of the normal building block in the synthesis of folic acid. dihydropteroate synthetase will recognize the sulfonamide instead of the normal building block of folic acid synthesis	Definition MOA of sulfonamides
Term decreases	Definition as the pKa of sulfonamides increases, what happens to the activity of the drugs?
Term increased production of PABA alterations in the dihydropteroate synthetase reduced drug uptake (permeability barrier and/or efflux pumps) regulational changes in the target enzymes	Definition mechanisms of bacterial resistance to sulfonamides
Term BROAD SPECTRUM small molecules so can cross porins and membranes urinary tract infections combinations - to reduce resistance	Definition spectrum of activity of sulfonamides
Term well absorbed from the GI tract binding to plasma proteins (differs between different classes) pass into body fluids (peural, synovial, ocular, and cerebrospinal) excretion via renal	Definition absorption, distribution, and excretion of sulfonamides
Term metabolism by acetylation of the para amino group: acetylsulfonamides are toxic: toxicity is related to the precipitation of the metabolite during excretion, can be prevented if patient drinks a lot of water to dissolve it better both sulfonamide and acetylsulfonamide are excreted renally sulfonamides are filtered and exhibit reabsorption metabolism by glucuronidation: less common than acetylation	Definition metabolism of sulfonamides
Term hypersensitivity toxicity to the hematopoietic system toxicity to the urinary tract	Definition adverse effects of sulfonamides
Term long acting sulfonamides: sulfamethoxypiridazine and sulfamethoxydiazine	Definition which class of sulfonamides are associated with Steven-Johnson syndrome?
Term very long acting sulfonamides: sulfadoxine administered once weekly	Definition what class of sulfonamides is used in combination with pyrimethamine for prophylaxis of malaria?
Term inhibitor of dihydrofolate reductase used for urinary tract infections in combination with sulfonamides trimethoprim binds to the enzyme in the last step of the synthesis of folic acid	Definition MOA of trimethoprim
Term available PO and IV volume of distribution greater than sulfonamides excreted in the urine metabolism by acetylation	Definition pharmacology of trimethoprim
Term GI upset folate deficiency may occur in some patients CONTRAINDICATED in pregnant women to avoid folate deficiency trimethoprim and sulfonamides are SELECTIVE b/c humans do not synthesize folate, we get it from our diets.	Definition adverse effects of trimethoprim
Term plasmid-encoded TMP resistance chromosomal TMP resistance	Definition bacterial resistance of trimethoprim
Term bactericidal broad spectrum urinary tract infections, respiratory tract infections, GI tract infections	Definition spectrum of trimethoprim/sulfonamide combinations