2. INTRODUCTION
1. Sulfonamides are the first antimicrobial agents effective against the pyogenic
bacteria (pus forming bacteria).
2. They are p-amino benzene sulfonamide derivatives forms the active moiety
sulfanilamide.
3. Sulfonamides are primarily bacteriostatic against most of Gram +ve and
Gram –ve bacteria.
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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.
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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)
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10. ADVERSE EFFECTS
1. Crystalluria (major)
2. Hypersensitivity- Steven-Jhonson syndrome
3. Epigastric pain
4. Haemolytic Anamia – in G-6PD deficient patient
5. Hepatitis (in 0.1 % patients)
6. Kernicterus- It is the precipitation of bilirubin inside the brain of newborn
due to displacement of bilirubin from plasma protein binding site
7. Nausia ,vomiting
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