This document discusses anti-leprotic drugs used to treat leprosy. It classifies these drugs into sulfones like dapsone, phenazine derivatives like clofazimine, and anti-tubercular drugs like rifampin and ethionamide. It provides details on the classification, mechanisms of action, adverse effects and reactions of dapsone and clofazimine, which are the primary sulfone and phenazine derivatives used respectively. Common adverse effects include haemolysis, methemoglobinemia, and various skin reactions. Proper usage and monitoring is important due to potential adverse reactions.

1. ANTI LEPROTIC DRUGSANTI LEPROTIC DRUGS

2. CLASSIFICATIONCLASSIFICATION
 SULFONESULFONE : Dapsone(DDS): Dapsone(DDS)
 PHENAZINE DERVATIVEPHENAZINE DERVATIVE : Clofazimine: Clofazimine
 ANTI TUBERCULAR DRUGSANTI TUBERCULAR DRUGS : Rifampin,: Rifampin,
EthionamideEthionamide
 OTHER ANTIBIOTICSOTHER ANTIBIOTICS : Ofloxacin,: Ofloxacin,
Minocycline,Minocycline,
Clarithromycin.Clarithromycin.

3. SULFONE DERIVATIVESULFONE DERIVATIVE
 DAPSONEDAPSONE::
 It is diamino diphenyl sulfone (DDS)It is diamino diphenyl sulfone (DDS)
 It is structurally related to sulfonamides.It is structurally related to sulfonamides.
 It is bacteriostatic for MycobacteriumIt is bacteriostatic for Mycobacterium
leprae.leprae.
 It is used in the treatment ofIt is used in the treatment of
Pneumocystis pneumoniaPneumocystis pneumonia in HIVin HIV
patients.patients.

4. MECHANISM OF ACTION:
PABA (-)Dapsone
Dihydro pteroate synthetase
Folic acid
Synthesis of purine and pyrimidine
Precursors of DNA & RNA
Cellular growth & replication.

5. ADVERSE REACTIONS:ADVERSE REACTIONS:
• HaemolysisHaemolysis
• MethemoglobinemiaMethemoglobinemia
• Nausea and AnorexiaNausea and Anorexia
• Cutaneous reactions include Allergic rashes, Photo toxicity, HyperCutaneous reactions include Allergic rashes, Photo toxicity, Hyper
melanosis and rarely exfoliative dermatitis.melanosis and rarely exfoliative dermatitis.
CONTRA INDICATIONS:CONTRA INDICATIONS:
• It should not be used in patients suffering with severe anaemia withIt should not be used in patients suffering with severe anaemia with
Haemoglobin <7g% and in those showing hyper sensitivityHaemoglobin <7g% and in those showing hyper sensitivity
reactions.reactions.

6. ADVERSE EFFECTSADVERSE EFFECTS::
SKINSKIN::
 Reddish discolouration of skin.Reddish discolouration of skin.
 Discolouration of hair and body secretions occurs.Discolouration of hair and body secretions occurs.
 Dryness of skin & itching often occurs.Dryness of skin & itching often occurs.
 Acne form eruptions & photo toxicity.Acne form eruptions & photo toxicity.
GI SYMPTOMSGI SYMPTOMS::
 Enteritis with intermittent loose stools, nausea, abdominal pain, anorexiaEnteritis with intermittent loose stools, nausea, abdominal pain, anorexia
& weight loss.& weight loss.
 Higher doses are used to control lepra reaction.Higher doses are used to control lepra reaction.
CONTRA INDICATIONSCONTRA INDICATIONS::
 It is avoided during early pregnancy & in patients with liver or kidneyIt is avoided during early pregnancy & in patients with liver or kidney
damage.damage.

7. PHENAZINE DERIVATIVEPHENAZINE DERIVATIVE
 CLOFAZIMINE (Clo)CLOFAZIMINE (Clo) ::
MECHANISM OF ACTIONMECHANISM OF ACTION::
 It is a phenazine dye that binds to DNA and inhibits templateIt is a phenazine dye that binds to DNA and inhibits template
function.function.
 This drug have redox properties may lead to generation of cytotoxicThis drug have redox properties may lead to generation of cytotoxic
oxygen radicals that are also toxic to bacteria.oxygen radicals that are also toxic to bacteria.
 It is bactericidal to M.leprae and has some activity against M.avium.It is bactericidal to M.leprae and has some activity against M.avium.
 It is an orally active drug (40-70% absorbed)It is an orally active drug (40-70% absorbed)
 It accumulates in many tissues, especially in fat, in crystalline form.It accumulates in many tissues, especially in fat, in crystalline form.
 Half life t ½ = 70 days.Half life t ½ = 70 days.

8.  It is a Jarish Herxheimer (Arthus) type of reaction due to release ofIt is a Jarish Herxheimer (Arthus) type of reaction due to release of
antigen from killed bacilli.antigen from killed bacilli.
 It may be mild, severe or life threatening.It may be mild, severe or life threatening.
HOW IT WILL COMES ?HOW IT WILL COMES ?
• It is the reaction which develops 4-6 weeks after DAPSONE treatmentIt is the reaction which develops 4-6 weeks after DAPSONE treatment
is called asis called as SULFONE SYNDROMESULFONE SYNDROME..
SYMPTOMS:SYMPTOMS:
• Fever, malaise, lymph node enlargement & anaemia.Fever, malaise, lymph node enlargement & anaemia.
• It is generally seen in malnourished patientsIt is generally seen in malnourished patients..
LEPRA REACTION:LEPRA REACTION:

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Keerthi.RKeerthi.R

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