Cfofazime Pharmaceutical Chemistry -2

Clofazimine is used in the treatment of lepromatous leprosy, including dapsone-resistant forms of the disease. In addition to its antibacterial action, the drug appears to possess anti-inflammatory and immune-modulating effects that are of value in controlling neuritic complications and in suppressing erythema nodosum leprosum reactions associated with lepromatous leprosy. It is frequently used in combination with other drugs, such as dapsone or rifampin.

The mechanisms of antibacterial and anti-inflammatory actions of clofazimine are not known. The drug is known to bind to nucleic acids and concentrate in reticuloendothelial tissue. It can also act as an electron acceptor and may interfere with electron transport processes.

The oral absorption of clofazimine is estimated to be about 50%. It is a highly lipid-soluble drug that is distributed into lipoidal tissue and the reticuloendothelial system. Urinary excretion of unchanged drug and metabolites is negligible. Its half-life after repeated dosage is estimated to be about 70 days. Severe gastrointestinal intolerance to clofazimine is relatively common. Skin pigmentation, ichthyosis and dryness, rash, and pruritus also occur frequently.

Clofazimine has also been used to treat skin lesions caused by Mycobacterium ulcerans.

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