ANTILEPROTIC DRUGS

Siddhartha Maji
Assistant professor
Ramesh Institute of Vocational and Technical
Education
+91-8757218056
 INTRODUCTION

• Leprosy, also known as Hansen's disease, is a chronic infectious disease caused by

Mycobacterium leprae (gram positive bacteria)

• The disease mainly affects the skin, the peripheral nerves, mucosal surfaces of the
upper respiratory tract and the eyes.

• Spread is thought to occur through a cough or contact with fluid from the nose of a
person infected by leprosy.

• Leprosy is curable with multidrug therapy. Treatment of leprosy is done with the
medications dapsone, rifampicin, and clofazimine for six to twelve months.
MECHANISM OF ACTION

(Dapsone , Solapsone)

Thiambutosine

Clofazimine
Folic Acid synthesis pathway
 CLASSIFICATION

1. SULPHONES :- DAPSONE , SOLAPSONE

2. PHENAZINE DERIVATIVE : - CLOFAZIMINE

3. DI SUBSTITUTED :- THIAMBUTOSINE
➢ 4-[(4-aminobenzene)sulfonyl]aniline.
DAPSONE

❑ Physico-chemical Properties:
• Chemical Formula: C12H12N2O2S
• Molecular Weight 248.3 g/mol
• Slightly soluble in water, freely soluble in Alcohol
• White crystalline powder
• Melting Point: 175 °C
• Plasma t1/2 >24 hrs
• Log P : 0.97

❑MOA: Inhibition of PABA; incorporation into folic acid by folate synthase.

❑ Use: It is used to treat a certain type of skin disorder caused during Hansen's disease.
It works by decreasing swelling (inflammation) and stopping the growth of bacteria

❑ Brand Names : Dapsone; Novophone.

❑ Storage : should be stored in room temperature and avoid direct sunlight.

 SOLAPSONE

❑Solapsone is a tetrasodium sulphonate derivative of Dapsone.

❑Physico-chemical Properties:
• Chemical Formula: C30H28N2Na4O14S5
• Molecular Weight 892.8 g/mol
• soluble in water
• White crystalline powder
• Acid Catalysed Hydrolysis decomposes Solapsone giving Cinnamaldehyde.

❑MOA: Inhibition of PABA; incorporation into folic acid by folate synthase.

❑ Use: It is a sulfonamide antibiotic used in the treatment of leprosy but It is less
potent than Dapsone.
❑ Brand Names :Sulphetrone, Solusulfone, Salapsone
❑ Storage : should be stored in room temperature and avoid direct sunlight.
 THIAMBUTOSINE

➢ 1-(4-butoxyphenyl)-3-[4-(dimethylamino)phenyl]thiourea.
➢ Physico-chemical Properties:
• Chemical Formula: C19H25N3OS
• Molecular Weight 343.5 g/mol
• Insoluble in water
• White crystalline powder
• Melting Point: 175 °C

❑MOA: Inhibition of PABA; incorporation into folic acid by folate synthase.

Dihydrofolate reductase inhibitor.
❑ Use: It is used as anti-inflammatory drug. It is basically used as a second line
drugs in dapsone resistant cases.
❑ Brand Names : Cibe-1906,DPT,Su-1906
❑ Storage : should be stored in room temperature and avoid direct sunlight.
 CLOFAZIMINE

➢ N,5-bis(4-chlorophenyl)-3-(1-methylethylimino)-5H-phenazin-2-amine.
➢ Physico-chemical Properties:
• Chemical Formula: C27H22Cl2N4
• Molecular Weight 473.4 g/mol
• Slightly soluble in water: 0.225 mg/L
• Dark Red Crystal
• Melting Point: 211.0 °C

❑MOA: DNA intercalation. Blocks the template function of the DNA and
inhibits bacterial proliferation.
❑ Use: It is used to treat a certain type of skin disorder caused during
Hansen’s disease. It works by decreasing swelling (inflammation) and
stopping the growth of bacteria

❑ Brand Names: Lamprene; Hansepran.

❑ Storage : should be stored in room temperature and avoid direct sunlight.

Thank You

Siddhartha Maji
Assistant professor
Ramesh Institute of Vocational and Technical
Education
+91-8757218056