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Sulfonamides(1)
Sulfonamides(1)
Sulfonamides(1)
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Sulfonamides(1)

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  • Considerable resistance has emerged
  • Trimethoprim is 20-100X as potent as the sulfonamide.
  • Unlikely in normal patients in recommended doses.
  • Transcript

    • 1. SULFONAMIDES Recognized since 1932. In clinical usage since 1935. First compounds found to be effective antibacterial agents in safe dose ranges. Mainstay of therapy before penicillins.
    • 2. SULFONAMIDES Now largely superceded by antibiotics and trimethoprim-sulfamethoxazole. They continue to occupy a small place in therapy.
    • 3. Gram-negative Wheel of Bugs Neissseria spp H. influenzae E. Coli (coliforms) Bacteroides spp AnaerobicP. aeruginosa Clostridium spp S. aureus Enterococcus spp Streptococcus spp Gram-positive
    • 4. FOLIC ACID BIOSYNTHESIS DIHYDROPTERIDINE 2 ATP PYROPHOSPHATE DERIVATIVEDihydropteroate 2HN COOHSynthetase HN SO2NH2 DIHYDROPTEROIC ACID 2 Glutamic Acid DIHYDROFOLIC ACID
    • 5. BLOOD Protein Bound Kidney MetabolitesOral Other-Sweat, Free Saliva,X Topical Prostatic fluid,Parenteral Stool Body Fluids & Tissues CSF
    • 6. KERNICTERUS IN THE NEWBORN Displacement of bilirubin from plasma protein binding sites.
    • 7. METABOLISM O H3 HC C N SO2N RAcetylated sulfonamides-inactive, toxic,and less soluble
    • 8. EXCRETION They are excreted in the urine partly as the parent and partly as the metabolite. Some sulfonamides are very insoluble in the acid urine.
    • 9. EXCRETION Half life of the sulfonamides depends on renal function. Dosage should be modified or the sulfonamides should not be used in renal failure.
    • 10. SULFONAMIDE PREPARATIONS Rapidly absorbed and rapidly eliminated (prototype- sulfisoxazole). Poorly absorbed sulfonamides (sulfasalazine). Topical sulfonamides (sulfacetamide, silver sulfadiazine). Long-acting sulfonamides (sulfadoxine)
    • 11. CONTRAINDICATIONS
    • 12. DRUG-DRUG INTERACTIONS Inhibit metabolism of some drugs. Displace certain drugs from plasma albumin.
    • 13. TRIMETHOPRIM-SULFAMETHOXAZOLE OCH3 2 HN CH OCH3 2 OCH3 80 mg TRIMETHOPRIM 2 HN SO2NH N CH3 O 400 mg SULFAMETHOXAZOLE
    • 14. COTRIMOXAZOLE Optimal ratio of the two drugs is 5:1 sulfa :trimethoprim.
    • 15. Synergism
    • 16. ADVANTAGES Expanded number of organisms inhibited. Bactericidal . Decreased resistance. Decreased toxicity.
    • 17. THERAPEUTIC USES
    • 18. hcd2.bupa.co.uk/.../ html
    • 19. PNEUMOCYSTIS PNEUMONIA(PCP)
    • 20. PNEUMOCYSTIS PNEUMONIA(PCP) www.learningradiology.com/
    • 21. PNEUMOCYSTIS PNEUMONIA (PCP) The most common opportunistic infection in advanced AIDS (80% of AIDS patients have at least one episode). Now considered a fungus (P.jurovecii). Multiple infections are often present simultaneously with the PCP.
    • 22. PROPHYLAXIS Routine prophylaxis has been successful in improving survival. PCP prophylaxis is indicated if the patient has a CD4 T lymphocyte count lower than 200 cells/mm3, or has oral candidiasis regardless of the CD4 count.
    • 23. TREATMENT OF PCP Early therapy is essential as success of therapy is related to severity of the disease at the time of initiation of therapy.
    • 24. TMP-SMX Treatment of choice. Oral form used for mild-moderate cases or after initial response to IV therapy and for prophylaxis.
    • 25. TMP-SMX Excellent tissue penetration. Produces a rapid clinical response.
    • 26. DRUG INTERACTIONS Same as with sulfonamides
    • 27. other sulphonamides Sulphonylureas (anti-diabetic agents) Carbutamide Acetohexamide Chlorpropamide Tolbutamide Tolazamide Glipizide Gliclazide Glibenclamide (glyburide) Glibornuride Gliquidone Glisoxepide Glyclopyramide Glimepiride
    • 28.  Anticonvulsants Acetazolamide Ethoxzolamide Sultiame Zonisamide Dermatologicals Mafenide
    • 29.  Other Celecoxib (COX-2 inhibitor) Darunavir (Protease Inhibitor) Fosamprenavir (Protease Inhibitor) Tipranavir (Protease Inhibitor) Probenecid (PBN) Sotalol (Beta-blocker) Sulfasalazine (SSZ) Sumatriptan (SMT)
    • 30.  Diuretics Acetazolamide Bumetanide Chlorthalidone Clopamide Dorzolamide Furosemide Hydrochlorothiazide (HCT, HCTZ, HZT) Indapamide Mefruside Metolazone Xipamide
    • 31. Viable organisms 6 control 4 sulfonamide 2 0 1 2 3 4 5 6 7 8 9 Time of incubation (hrs)
    • 32. RESISTANCE Results from multiple mechansims. Altered dihydropteroate synthetase. Cross-resistance among all sulfonamides.
    • 33. PABA + PteridineDihydropteroate SULFONAMIDESynthetase DIHYDROPTEROIC ACIDDihydrofolate Synthetase DIHYROFOLIC ACID Dihydrofolate Reductase TRIMETHOPRIM TETRAHYDROFOLIC ACID
    • 34. ADVERSE EFFECTS Hypersensitivity reactions -common  allergic rashes  photosensitivity  drug fever  Stevens-Johnson syndrome
    • 35.  hypersensitivity reaction to sulfa drugs are rash and hives. However, there are several life-threatening manifestations of hypersensitivity to sulfa drugs, including Stevens–Johnson syndrome, toxic epidermal necrolysis, agranulocytosis, hemolytic anemia, thrombocytopenia, and fulminant hepatic necrosis, among others.
    • 36. 
    • 37. CRYSTALLINEAGGREGATES,HEMATURIA,OBSTRUCTION
    • 38. ADVERSE EFFECTS Headache, nausea, vomiting and diarrhea. Hematological effects -anemia, agranulocytosis.
    • 39. ADVERSE REACTIONS Dermatological reactions including skin rashes. GI (nausea and vomiting).

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