Clofazimine is a medicine that is used for the treatment of Leprosy, Treatment of borderline lepromatous leprosy, Treatment of mid-borderline leprosy, Treatment of lepromatous leprosy, Treatment of erythema nodosum leprosum and other conditions. Indications:
The complete list of uses and indications for Clofazimine is as follows:
Treatment of borderline lepromatous leprosy
Treatment of mid-borderline leprosy
Treatment of lepromatous leprosy
Treatment of erythema nodosum leprosuPharmacology:Pharmacodynamic Properties Of Clofazimine
Clofazimine exerts a slow bactericidal effect on Mycobacterium leprae (Hansen's bacillus). Clofazimine inhibits mycobacterial growth and binds preferentially to mycobacterial DNA. Clofazimine also exerts antiinflammatory 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. Measurement of the minimum inhibitory concentration (MIC) of clofazimine against leprosy bacilli in vitro is not yet feasible. In the mouse footpad system, the multiplication of M.leprae is inhibited by introducing 0.0001%- 0.001% clofazimine in the diet. Although bacterial killing may begin shortly after starting the drug, it cannot be measured in biopsy tissues taken from patients for mouse footpad studies until approximately 50 days after the start of therapy. Pharmacokinetic Properties Of Clofazimine
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.
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 passes into breast milk and skin discoloration may occur in the infant.It should be administered to a breast-feeding woman only if clearly indicated.Contraindications
CLOFAZIMINE is contraindicated in patients with known hypersensitivity.Side Effects
Very rare but the common side effects are:
Changes in skin color
Dry and scaly skin
Do not store above 25C (77F). Protect from moisture.