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SULFONAMIDES
Prepared by,
Mrs. Rijo Lijo
INTRODUCTION
1. Sulfonamides is the first effective chemotherapeutic agents to be employed
systematically for the prevention and cure of bacterial infection in man.
Sulfonamides or sulpha drugs are the basis of several group of drugs.
2. This original anti-bacterial sulfonamide are synthetic antimicrobial agent that
contain the sulfonamide group.
3. Sulfonilamide is first synthesized by a German chemist Bayer in 1908.
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).
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)
CLASSIFICATION OF
SULFONAMIDES
INDICATION
 Typhoid and paratyphoid fever.
 Acute & chronic urinary tract infection.
 Tropical application for infected burn.
 Meningococcal meningitis(sulfadiazine).
 Bacillary dysentery.
 Uncomplicated gonorrhea.
 Dermatitis.
 Gut sterilization.
CONTRAINDICATION
 Pregnancy.
 Premature infant.
 Renal impairment.
 Dehydration.
ADVERSE REACTIONS OF
SULFONAMIDES
ADVERSE EFFECTS
– RENAL SYSTEM
– Sulfonamides precipitates in acidic urine & form crystal which pass the urine.
– Renal irritation.
– Crystalluria.
– Spasmodic pain(renal colic).
– Haematuria
– renal tubular necrosis.
– Oliguria.
– Anuria.
– HAEMOPOIETIC SYSTEM
– Bone marrow depression,
– Aplastic anaemia.
– Acute haemolytic anaemia.
– Thrombocytopenia.
– Eosinophilia.
– Agranulocytosis.
– Gastrointestinal tract
– Anorexia.
– Nausea.
– Vomiting.
– Diarrhoea .
– Hypersensitivity reaction
– Skin rashes.
– Photosensitivity.
– Exfoliative dermatitis.
– Contact dermatitis.
– Anaphylaxis.
– Steven johnson syndrome (Stevens-Johnson syndrome which includes
symptoms like aching joints, aching muscles, redness, blistering, and peeling of
the skin).
– Kernicterus in Neonates.( Can be precipitated especially in premature infants
since their blood brain barrier is not fully developed SULFONAMIDES
Displaces bilirubin from protein binding site Bilirubin passes through BBB
Deposited in Basal Ganglia + Subthalamic nuclei).
ADVANTAGES OF
SULFONAMIDES
DISADVANTAGES OF
SULFONAMIDES
Giving comparatively small doses of each component of a mixture of sulfonamides,
the danger of intrarenal drug precipitation should be only as great as if each
compound had been administered alone.
NURSES RESPONSIBILITY
 Inform doctor about all medical conditions you have — especially kidney, liver,
or blood disorders — before taking a sulfonamide.
 Sulfonamides may cause blood problems, especially if they're taken for a long
period of time.
 These medicines can also cause a serious, even life-threatening, skin rash.
Inform the doctor right away if you notice a rash or unusual skin changes.
 carefully monitor your body's response to this medicine with frequent
observation.
– These medicines shouldn't be given to infants under 2 months old.
– These drugs may make the skin more sensitive to the sun. Avoid unnecessary exposure to
sunlight, and wear sunscreen and protective clothing while outdoors.
Sulfonamides

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Sulfonamides

  • 2. INTRODUCTION 1. Sulfonamides is the first effective chemotherapeutic agents to be employed systematically for the prevention and cure of bacterial infection in man. Sulfonamides or sulpha drugs are the basis of several group of drugs. 2. This original anti-bacterial sulfonamide are synthetic antimicrobial agent that contain the sulfonamide group. 3. Sulfonilamide is first synthesized by a German chemist Bayer in 1908.
  • 3. 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).
  • 4. 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. INDICATION  Typhoid and paratyphoid fever.  Acute & chronic urinary tract infection.  Tropical application for infected burn.  Meningococcal meningitis(sulfadiazine).  Bacillary dysentery.  Uncomplicated gonorrhea.  Dermatitis.  Gut sterilization.
  • 7. CONTRAINDICATION  Pregnancy.  Premature infant.  Renal impairment.  Dehydration.
  • 9. ADVERSE EFFECTS – RENAL SYSTEM – Sulfonamides precipitates in acidic urine & form crystal which pass the urine. – Renal irritation. – Crystalluria. – Spasmodic pain(renal colic). – Haematuria – renal tubular necrosis. – Oliguria. – Anuria.
  • 10. – HAEMOPOIETIC SYSTEM – Bone marrow depression, – Aplastic anaemia. – Acute haemolytic anaemia. – Thrombocytopenia. – Eosinophilia. – Agranulocytosis.
  • 11. – Gastrointestinal tract – Anorexia. – Nausea. – Vomiting. – Diarrhoea .
  • 12. – Hypersensitivity reaction – Skin rashes. – Photosensitivity. – Exfoliative dermatitis. – Contact dermatitis. – Anaphylaxis. – Steven johnson syndrome (Stevens-Johnson syndrome which includes symptoms like aching joints, aching muscles, redness, blistering, and peeling of the skin).
  • 13. – Kernicterus in Neonates.( Can be precipitated especially in premature infants since their blood brain barrier is not fully developed SULFONAMIDES Displaces bilirubin from protein binding site Bilirubin passes through BBB Deposited in Basal Ganglia + Subthalamic nuclei).
  • 15. DISADVANTAGES OF SULFONAMIDES Giving comparatively small doses of each component of a mixture of sulfonamides, the danger of intrarenal drug precipitation should be only as great as if each compound had been administered alone.
  • 16. NURSES RESPONSIBILITY  Inform doctor about all medical conditions you have — especially kidney, liver, or blood disorders — before taking a sulfonamide.  Sulfonamides may cause blood problems, especially if they're taken for a long period of time.  These medicines can also cause a serious, even life-threatening, skin rash. Inform the doctor right away if you notice a rash or unusual skin changes.  carefully monitor your body's response to this medicine with frequent observation.
  • 17. – These medicines shouldn't be given to infants under 2 months old. – These drugs may make the skin more sensitive to the sun. Avoid unnecessary exposure to sunlight, and wear sunscreen and protective clothing while outdoors.