Sulphonamides with its use classification adverse effects

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

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.

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)

7. 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).

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

9. CONTRAINDICATION
Pregnancy.
Premature infant.
Renal impairment.
Dehydration.

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