Clofazimina [INN-Spanish]

• Antimycobacterials
• Leprostatic Agents
• Dyes
• Anti-Inflammatory Agents, Non-Steroidal
• ATC:J04BA01

• Chlofazimine
• Clofazimina [INN-Spanish]
• Clofazimine [USAN:BAN:INN]
• Clofaziminum [INN-Latin]
• Lampren
• Lamprene

• No information avaliable

C₂₇H₂₂Cl₂N₄

http://www.rxlist.com/cgi/generic3/clofazimine.htm

Clofazimina_[INN-Spanish] FDA

No information avaliable

473.396 g/mol

210-212 ^oC

0.225 mg/L (virtually insoluble)

Solid

7.132

Capsule (50 mg)

For the treatment of lepromatous leprosy, including dapsone-resistant lepromatous leprosy and lepromatous leprosy complicated by erythema nodosum leprosum.

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.

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

Oral, rabbit: LD₅₀ = 3.3 g/kg; Oral, mouse: LD₅₀ = > 4 g/kg. Severe abdominal symptoms have necessitated exploratory laparotomies in some patients on clofazimine therapy. Rare reports have included splenic infarction, bowel obstruction, and gastrointestinal bleeding. Deaths have been reported, following severe abdominal symptoms.

Patients should be warned that Lamprene may cause a discoloration of the skin from red to brownish-black, as well as discoloration of the conjunctivae, lacrimal fluid, sweat, sputum, urine, and feces. Patients should be advised that skin discoloration, although reversible, may take several months or years to disappear after the conclusion of therapy with Lamprene.

Patients should be told to take Lamprene with meals.

Mycobacteria