Anti-Hansen Drugs Flashcards
What is the MOA of Sulfone?
Inhibits folic acid synthesis
What is the mode of action of Sulfone?
Bacteriostatic (against M.leprae)
Sulfone: Pharmacokinetics
Slow but complete absorption orally
Well distributed in tissues
Enterohepatic circulation
Acetylated in the liver
Sulfone: Adverse Effects
Hematologic
GIT disturbance
CNS
Sulfone Syndrome
What is Sulfone Syndrome?
Exacerbation of Lepromatous Leprosy
What are the different Anti-Hansen drugs?
Sulfone
Dapsone
Clofazimine
Rifampicin
At what Dapsone dose will resistance emerge (in large M.leprae populations)?
Low doses
What is the indication for Dapsone use?
Intermediate and tuberculoid leprosy
Prophylaxis for household contacts of those with borderline & lepromatous-type leprosy
Pneumocystis carinii pneumonia (with AIDS)
What drug decreases Dapsone levels by increasing its plasma clearance?
Rifampicin
What is the chief secondary drug for leprosy and when is it used?
Clofazimine; Used for Sulfone-resistant patient
Clofazimine Pharmacokinetics
Well absorbed orally
Accumulates in tissue causing reddish discoloration of tears and conjunctiva
Very slow excretion (1/2 life = 70 days)
Clofazimine Adverse Effects
Reddish discoloration of skin
Eosinophilic enteritis
Decrease sweating
Photosensitivity
Why use combination therapy in leprosy?
Reduce development of resistance
For adequate therapy with existing resistance
Decreased duration of treatment (minimum still 2 years)
Standard Leprosy Chemotherapy for Paucibacillary form (Intermediate, Tuberculoid)
Dapsone + Rifampicin
Standard Leprosy Chemotherapy for Multibacillary form (lepromatous, borderline)
Rifampicin + Dapsone + Clofazimine (x2 years)