Pharm 46 Sulfonamides,

Front 1

antifolate drugs that inhibit microbial enzymes involved in folic acid synthesis

Back 1

sulfonamides

Front 2

selective inhibitor of dihydrofolate reductase

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trimethoprim

Front 3

weakly acidic compounds that have a common chemical nucleus resembling PABA

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sulfonamides

Front 4

where are sulfonamides metabolized

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liver

Front 5

what happens to sulfonamides with acidic urine

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decreases solubility - increased risk for stones

Front 6

What organism is stimulated by sulfonamides?

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Rickettsiae

Front 7

Name the enteric bacteria that is inhibited by sulfonamides.

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E. coli, klebsiella, salmonella, shigella, enterobacter

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What is the activity against anaerobes?

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Activity is poor

Front 9

What is the clinical use of the oral but nonabsorbable sulfonamide agents?

Back 9

Sulfasalazine is widely used in UC , enteritis, and other inflammatory bowel disease

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which sulfa can you give to reduce the liklihood of precipitation

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triple sulfa

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short acting sulfonamide

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sulfisoxazole

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intermediate acting sulfonamide

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sulfamethoxazole

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long acting sulfonamide

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solfadoxine

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drug structurally similar to folic acid and is excreted in high concentrations in prostatic and vaginal fluids, large amount excreted unchanged in the urine

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trimethoprim

Front 15

What is the mechanism of action of sulfonamide?

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bacteriostatic inhibitor of folic acid synthesis; COMPETITVE INHIBITOR OF DIHYDROPTEROATE SYNTHASE

Front 16

What is the treatment of acute toxoplasmosis?

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Sulfadiazine in combination with pyrimethamine

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_______ plus pyrimethamine is combination treatment for malaria.

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Sulfadoxine

Front 18

What is the clinical use of mafenide acetate?

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It is used topically for burn sites

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What is the difference between mafenide acetate and silver sulfadiazine?

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Both are used for topical burn use. Mafenide and its primary metabolite inhibit carbonic anhydrase and causes carbonic anhydrase and can cause metabolic acidosis. Silver sulfadiazine is much less toxic and is preferred to mafenide for prevention of infection of burn wounds

Front 20

why do sulfonamides not harm mammallian folate synthesis

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because mammalian cells use preformed folic acid, not denovo formed

Front 21

What is the mechanism of action of trimethoprim ?

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dihydrofolate reductase that prevents formation of the active form of folic acid

Front 22

what is treatment with both trimethoprim and sulfonamide called

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sequential blockade

Front 23

increased production of what from bacteria will increase resistance to sulfonamides

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PABA

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what are sulfonamides active against

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gram positive and gram negative

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what two organisms are sulfonamides active against

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chlamydia and nocardia

Front 26

simple UTI, ocular infections, burn infections, ulcerative colitis and rheumatoid arthritis and toxoplasmosis can be treated with what class

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sulfonamides

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effective orally in the tx of UTIs and in respiratory, ear and sinus infections by h influenzae and moraxella catarrhalis

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TMP SMZ

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what is used for infections of aeromonas hydrophilia in immunocompromised patients

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TMp - SMZ

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what to use for prevention and treatment of pneumocystitis pneumonia

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TMp SMZ

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listeria monocytogenes treatment

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TMP smz

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toxicity of sulfonamides (hypersensitivity)

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skin rashes and fever,

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GI toxicity associated with sulfonamides

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nausea, vomiting and diarrhea, hepatic dysfunction

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what can occur in patients taking sulfonamides with a G6P deficiency

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acute hemolytic anemia

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hematotoxicity of sulfonamides

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ganulocytopenia, thrombocytopenia and aplastic anemia

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nephrotoxicity of sulfonamides

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can precipitate in the urine at low Ph - cause stones

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sulfonamides can increase the plasma levels of what two drugs by competeint for plasma binding spots

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warfarin and methotrexate

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this drug can cause megaloblastic anemia, leukopenia and granulocytopenia

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trimethoprim

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TMP SMZ toxicity

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with aids - fever, rash, leukopenia and diarrhea

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What is the mechanism of action for quinolones ?

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Quinolones block bacterial DNA synthesis by inhibiting bacterial topoisomerase II (DNA gyrase) and topoisomerase IV

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Inhibition of DNA gyrase prevents______

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the relaxation of positively supercoiled DNA that is required for normal transcription and replication

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Inhibition of topoisomerase IV prevents______

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the separation of replicated chromosomal DNA into the respective daughter cells during cell division

Front 42

Which of the fluoroquinolones have the least activity against both gram positive and gram negative organisms.

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Norfloxacin

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Which of the fluoroquinolones has the most activity against gram negative organisms.

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Ciprofloxacin

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what is norfloxacin used for

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UTI

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what are ciprofoxacin and ofloxacin used for (5)

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gram negatives; gonococcus ; gram positive cocci ;mycobacteria ;atypical pneumonia

Front 46

What type of malaria is pyrimethamine with sulfodoxine used to treat?

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Falciparum malaria

Front 47

What STI are cipro and levofloxacin effective in treating?

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Chlamydial urethritis or cervicitis

Front 48

Pyrimethamine selectively inhibits dihydrofolic acid reductase in ______ but Trimethoprim inhibits it in ____

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protozoa; bacteria

Front 49

Why are fluoroquinolones not recommended for patients under 18 years of age.

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Fluoroquinolones may damage growing cartilage and cause an arthropathy

Front 50

What are the respiratory fluoroquinolones?

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Levofloxacin, gatifloxacin, gemifloxacin, and moxifloxacin. They have enhanced gram positive; atypical pneumonia (mycoplasma, legionella, chlamydia)

Front 51

What is a rare but serious complication in fluoroquinolone use in adults?

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tendinitis; there is a risk of tendon rupture.

Front 52

levofloxacin, gemifloxacin and moxifloxacin used for?

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S pneumonae, MRSA, gram positive (better than 2nd gen) ; gram negative (worse than 2nd gen)

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gemifloxacin and moxifloxacin are useful against what

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anaerobes

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what GI drug interferes with fluoroquinolones

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antacids with multivalent cations

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which should you not use for systemic infections

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norfloxacin

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how are fluoroquinolones eliminated from the bloodstream

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kidneys

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what can slow fluoroquinolone excretion

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probnecid

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which should not be used in UTI

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moxifloxacin

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MOA for fluoroquinolones

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topoisomerase II inhibitors (gram neg)
topoisomerase IV in gram positive

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which fluoroquinolones have the widest spectrum of activation

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gemifloxacin and moxifloxacin

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what is the most common fluoroquinolone side effet

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GI toxicity

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insomnia, abnormal liver function, phototoxicity, tendonitis and tendon rupture

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fluoroquinolones toxicity

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opportunitstic infections from what with fluoroquinolones

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c albicans and streptococci

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can you use fluoroquinolones with children and pregnant women

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no