Clofazimine Soft Gel Capsules
Clofazimine IP 50/100mg
- Treatment of lepromatous leprosy
- Treatment of borderline lepromatous leprosy
- Treatment of mid-borderline leprosy
- Treatment of erythema nodosum leprosum
PHARMACODYNAMIC PROPERTIES OF CLOFAZIMINE
Clofazimine exerts a slow bactericidal effect on Mycobacterium leprae. Clofazimine inhibits mycobacterial growth and binds preferentially to mycobacterial DNA. Clofazimine also exerts anti inflammatory properties in controlling erythema nodosum leprosum reactions. Clofazimine is highly lipophilic and tends to be deposited predominantly in fatty tissue and in cells of the reticuloendothelial system. It is taken up by macrophages throughout the body.
MECHANISM OF ACTION:Preferentially bind to mycobacterial DNA leading to disruption of the cell cycle and eventually kills the bacterium. It may also bind to bacterial potassium transporters, thereby inhibiting their function. Lysophospholipids have been found to mediate the activity of this drug.
PHARMACOKINETIC PROPERTIES OF CLOFAZIMINEABSORPTION:
Absorption varies from 45 to 62% following oral administration in leprosy patients. Bioavailability is approximately 70%. Food increases bioavailability and rate of absorption.
Clofazimine is bound to alpha- and beta-lipoproteins in serum, particularly the beta- lipoproteins, and the binding was saturable at plasma concentrations of approximately 10 mcg/mL. Binding to gamma-globulin and albumin was negligible.
Hepatic. Three metabolites have been identified - two conjugated and one unconjugated, however, it is not yet known whether these metabolites are pharmacologically active. Metabolite I is formed by hydrolytic dehalogenation of clofazimine, metabolite II presumably is formed by a hydrolytic deamination reaction followed by glucuronidation, and metabolite III appears to be a hydrated clofazimine glucuronide.
Clofazimine also passes into breast milk resulting in skin discolouration in the infant.
- Loss of appetite
- Scaling of skin
- Skin discolouration
- Eye discolouration.