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72 Cards in this Set
- Front
- Back
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antifolate drugs that inhibit microbial enzymes involved in folic acid synthesis |
sulfonamides
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selective inhibitor of dihydrofolate reductase
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trimethoprim
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weakly acidic compounds that have a common chemical nucleus resembling PABA
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sulfonamides
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where are sulfonamides metabolized
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liver
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what happens to sulfonamides with acidic urine
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decreases solubility - increased risk for stones
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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 |
Sulfadoxine |
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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
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MOA of sulfonamide
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bacteriostatic inhibitor of folic acid synthesis
COMPETITVE INHIBITOR OF DIHYDROPTEROATE SYNTHASE |
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why do sulfonamides not harm mammallian folate synthesis
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because mammalian cells use preformed folic acid, not denovo formed
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trimethoprim MOA
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dihydrofolate reductase that prevents formation of the active form of folic acid
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what is treatment with both trimethoprim and sulfonamide called
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sequential blockade
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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
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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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MRS listeria monocytogenes Nocardiosis Cholera, typhoid fever, shigellosis treatment
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TMP smz |
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toxicity of sulfonamides (hypersensitivity) |
skin rashes and fever Crossallergenicity between sulfonamide, oral hypoglycemics and thiazides Rare Exfoliative dermatitis Steven Johnson syndrome Polyarteritis nodosa |
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GI toxicity associated with sulfonamides |
Commonly nausea, vomiting and diarrhea,
mild hepatic dysfunction
Uncommon Hepatitis |
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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 |
ganulocytopenia, thrombocytopenia and aplastic anemia Rare |
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nephrotoxicity of sulfonamides |
can precipitate in the urine at low Ph - cause stones Crystalluria, hematuria |
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sulfonamides can increase the plasma levels of what by competing for plasma binding spots |
warfarin and methotrexate Bilirubin- kernicterus (3trimester of pregnancy) |
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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 |
with aids - fever, rash, leukopenia and diarrhea
Normal adverse effects of antifolate drugs Megaloplastic anemia, leukopenia, granulocytopenia |
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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) 2nd generation |
gram negatives gonococcus gram positive cocci mycobacteria atypical pneumonia (Mycoplasma pneumoniae, chlamydophila pneumoniae) |
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levofloxacin gemifloxacin and moxifloxacin used for? |
gram positive (better than 2nd gen) s pneumonae gram negatvie (worse than 2nd gen) MRSA Entercocci
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gemifloxacin and moxifloxacin are useful against what |
anaerobes Broadest spectrum |
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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 |
Active tubular secretion 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 |
moxifloxacin
But doesn't need dosage reduction with renal dysfunction because of biliary excretion and hepatic metabolism |
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MOA for fluoroquinolones |
topoisomerase II inhibitors (gram neg) topoisomerase IV in gram positive Bactericidal Postantibiotic effect |
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which fluoroquinolones have the widest spectrum of activation |
gemifloxacin and moxifloxacin Including gram positive and gram negative, atypical pneumonia agents, anaerobic agents |
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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
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Half life of fluoroquinolone |
3-8h |
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Resistance in fluoroquinolone |
Rapid resistance in 2nd generation Especially campylobacter jejuni, gonococcal, Gram positive (MRSA) Pseudomonas aerugionsa Serratia |
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Resistance in fluoroquinolone |
Rapid resistance in 2nd generation Especially campylobacter jejuni, gonococcal, Gram positive (MRSA) Pseudomonas aerugionsa Serratia |
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Resistance in fluoroquinolone by efflux mechanism |
M tuberculosis S aureus S pneumonia |
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Resistance in fluoroquinolone |
Rapid resistance in 2nd generation Especially campylobacter jejuni, gonococcal, Gram positive (MRSA) Pseudomonas aerugionsa Serratia |
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Resistance in fluoroquinolone by efflux mechanism |
M tuberculosis S aureus S pneumonia |
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Resistance by gyrA gene |
Encodes DNA gyrase Resistance for gonococci |
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Which organism in uGt and GIT does fluoroquinolone treat |
Gram negative-Gonococci E coli Enterobacter Pseudomonas aerugionsa Salmonella Shigella |
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Which organism in uGt and GIT does fluoroquinolone treat |
Gram negative-Gonococci E coli Enterobacter Pseudomonas aerugionsa Salmonella Shigella |
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Which treatment is now less effective bc of resistance |
Infections of Respiratory tract, skin, soft tissue |
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Which organism in uGt and GIT does fluoroquinolone treat |
Gram negative-Gonococci E coli Enterobacter Pseudomonas aerugionsa Salmonella Shigella |
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Which treatment is now less effective bc of resistance |
Infections of Respiratory tract, skin, soft tissue |
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Which fluoroquinolone is used as an alternative for ceftriaxone and Cefixime in gonorrhoae, but not recommended bc of resistance |
Ciproflaxin and ofloxacin as single dose |
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Other clinical uses of fluoroquinolone |
Meningococcal carrier state Tuberculosis Prophylactic management of neutropenia |
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DOC for nocardiosis |
1.TMP-SMZ 2. Sulfadiazine + pyrimethamine
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DOC for nocardiosis |
1.TMP-SMZ 2. Sulfadiazine + pyrimethamine
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Effects of sulfadiazine in AIDS |
Prophylaxis in pneumocystis pneumonia |
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Treatment with Ciprofloxacin |
UTI Otitis media including H influenzae and pneumococci 50% resistance to MRSA |
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Most common adverse effects of sulfonamide |
Hypersensitivity- skin rash Neurological dysfunction and hematuria is less common |
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Most common adverse effects of sulfonamide |
Hypersensitivity- skin rash Neurological dysfunction and hematuria is less common |
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Action of sulfasalazine |
Significant anti inflammatory action Goo 50-75% Improvement in ulcerative colitis Effect in rheumatoid arthritis |
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Treatment of gonorrhea + urethritis when sulfonamide allergy |
Single dose cefixime and azithromycine |
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Treatment of gonorrhea + urethritis when sulfonamide allergy |
Single dose cefixime and azithromycine |
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DOC in rocky spotted mountain fever |
Chloramphenicol |
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Treatment of gonorrhea + urethritis when sulfonamide allergy |
Single dose cefixime and azithromycine |
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DOC in rocky spotted mountain fever |
Chloramphenicol |
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DOC for travellers diarrhea |
2nd generation of fluoroquinolone Effective against gram negative E. coli Shigella Salmonella |
