SULFONAMIDES with its classification use

Sulphonamides with its use classification adverse effects

1. SULFONAMIDES PRESENTED BY, MITESH LUNGASE GUIDED BY, MRS. DEEPIKA PRAJAPATI ACADEMIC YEAR 2023-24

2. INTRODUCTI ON Sulfonamides are the first antimicrobial agents effective against the pyogenic bacteria (pus forming bacteria). They are p-amino benzene sulfonamide derivatives forms the active moiety sulfanilamide. Sulfonamides are primarily bacteriostatic against most of Gram + ve and Gram – ve bacteria.

3. history In 1935, sci Domagk discovered the first sulfonamide dye prontosil red (chemically sulfonamido chrysoidine ) which was effective against streptococcal infection in the mice . In 1937, this dye also cured infant infected by staphylococcal septicaemia (100 % fatal that time). Sulfanilamide was the active moiety in prontosil red which was effective against streptococcal infection in mice.

4. CLASSIFICATION OF SULFONAMIDES

5. MECHANISM OF ACTION Folic Acid is very essential for the growth of bacteria as it is crucial for nucleic acid synthesis. Many bacteria synthesize their own folic acid from PABA. Sulfonamides are structural analogues of PABA ,enters the sequence in place of PABA. Sulfonamides compete for enzyme dihydropteroic acid synthase to create a non- functional analogue of folic acid. This is of no use to bacteria hence. GROWTH CEASES (BACTERIOSTATIC ACTION)

6. PHARMACOKINETIC Route of administration : Oral (well absorbed from upper GIT). Disribution: CSF, Placenta(widely disributed) 20-90 percent drugs protein bound. Metabolism: Liver (acetylation). Excretion: Kidney (tubular secretion &glumerular filtration).

7. uses Sulfadiazine –meningitis sulfamethoxazole -it is used in combination with trimethoprime combination as cotrimoxazole Sulfacetamide sodium –ophthalmic preparation Silver sulfadiazine & mefenide –in Burn therapy Sufasalazine (prodrug) –Ulcerative colitis(5 –ASA) Sulfamethopyrazine -in combination with pyrimethamine for malaria , pneumocystic jiroveci,taxoplasmosis gondii

8. CONTRAINDICATION Pregnancy. Premature infant. Renal impairment. Dehydration .

9. ADVERSE EFFECTS Crystalluria (major) Hypersensitivity- Steven- Jhonson syndrome Epigastric pain Haemolytic Anamia – in G-6PD deficient patient Hepatitis (in 0.1 % patients) Kernicterus- It is the precipitation of bilirubin inside the brain of newborn due to displacement of bilirubin from plasma protein binding site Nausia ,vomiting

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