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- Oldest,cheapest and most widely used
- Di-amino-Di-phenyl Sulfone
- Structurally similar to sulpha drugs
Mechanism of Action:- Similar to sulphonamides
- Lepra bacilli utilise PABA to synthesize folic acid. Dapsone competes with PABA inhibiting folate synthesis.
Pharmacokinetics:- Well absorbed orally
- Widely distributed into the skin,muscle, liver, kidneys etc.
- Metabolised by acetylation and conjugation in the liver. Undergoes enterohepatic cycling.
Adverse Effects:- Dose related:
- Hemolytic anemia especially in G6PD Deficiency.
- Methhemoglobinemia
- GI Adverse effects
- Dermatitis, pruritis and peripheral neuropathy
- Headache, drug fever
- Hepatitis
- May cause 'Sulfone syndrome' or Lepra reaction - -> Erythema nodosum Leprosum (ENL)
- occurs due to antigen release from lepra bacilli
Category:
Pharmacology Notes
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