Clofazimine Soft Gel Capsules

Clofazimine, is a medication used to treat Leprosy. This medication is indicated for treatment of lepromatous leprosy including dapsone-resistant leprosy complicated by erythema nodosum leprosum. It is generally used to prevent the emergence of drug resistance.
The complete list of uses and indications for Clofazimine is as follows:
  • 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 CLOFAZIMINE

ABSORPTION:
Absorption varies from 45 to 62% following oral administration in leprosy patients. Bioavailability is approximately 70%. Food increases bioavailability and rate of absorption.

DISTRIBUTION:
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.

METABOLISM:
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 may be used in pregnant women with leprosy if the potential benefits justify the risk to the fetus. The World Health Organisation recommends that clofazimine be continued during pregnancy, as the symptoms of leprosy appear to worsen over this time. Clofazimine crosses the placenta, and skin discolouration has been seen in neonates.
Clofazimine also passes into breast milk resulting in skin discolouration in the infant.
No known contraindications. Use cautiously in patients with GI dysfunction, such as abdominal pain or diarrhea. 
Very rare but the common side effects are:
  • Vomiting
  • Nausea
  • Diarrhoea
  • Loss of appetite
  • Rash
  • Itching
  • Scaling of skin
  • Skin discolouration
  • Eye discolouration.
Do not store above 25˚C (77˚F). Protect from moisture.