SULFONAMIDES

• They have broad-spectrum antimicrobial activity against gram-positive cocci, gram-negative bacilli, mycobacteria, rickettsiae, chlamydiae, and some fungi.
• chemical chameleons 


  Sulfones
• Antidote for Folic Acid toxicity

  Leucovorin or Folinic acid
• Sulfonamides applications

  Anti-cancer

  Anti-glaucoma

  Anti-convulsions

  Inhibitor of gamma-reductase
• Side effects of Sulfonamides

  Lethargy

  Diarrhea

  Anorexia

  Steve-Johnson syndrome

  Headache

  Nausea

  Vomiting

  Photosensitivity
• Sulfonamide's general structure consist of:

  P-amino group

  Sulfanilamide structure

  Aromatic ring

  N¹-substitution group
• P-amino group


  Mimics PABA
• Aromatic ring

  promotes target binding

  increase lipophilicity

  increase bioavailability
• Sulfanilamide group

  Increase potency and affinity
• Tx for UTI, respiratory system, and. GI tract; a derivative of sulfanilamide

  Sulfamethoxazole
• Blocks synthesis of folic acid

  Sulfonamide
• Synthesized from PABA, pteridine, and glutamate

  Folic acid
• Drug of choice for toxoplasmosis

  Sulfadiazine
• Causative agent of toxoplasmosis

  Toxoplasma gondii
• Sulfadiazine is used together with?

  Pyrimethamine
• Tx for malaria

  Sulfadoxine with Pyrimethamine
• Discontinued in 2006 due to severe side effects


  Sulfacytine
• Topical sulfonamide for eye infection is Sulfacetamide
• Sulfacetamide is available in the market with 10%, 20%, and 30% concentrations
• Topical sulfonamides for skin infections

  Silver sulfadiazine, Mefanide acetate
• Treatment for burns and it is contraindicated for children and pregnant women.

  Silver sulfadiazine
• Mefanide acetate


  Tx for bacterial infections or fungus infections.
• Co-trimoxazole is composed of:

  Trimethoprim and Sulfamethoxazole
• Antidote for Methotrexate

  Leucovorin
• Causes Sulfamethoxazole and Trimethoprim to bind

  Synergistic Effect
• Second line treatment for otitis media

  Sulfadiazine
• Another name for Sulfonamides


  Sulfa medicines
• DHFR meaning


  Dihydrofolate Reductase