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Lamprene (Clofazimine) - Description and Clinical Pharmacology

 
 



Lamprene®

Lamprene ®

clofazimine  

Soft Gelatin Capsules

 

Prescribing Information

Rx only

DESCRIPTION

Lamprene, clofazimine, is an antileprosy agent available as soft gelatin capsules for oral administration. Each capsule contains 50 mg of micronized clofazimine suspended in an oil-wax base. Clofazimine is a substituted iminophenazine bright-red dye. Its chemical name is 3-(p -chloroanilino)-10-(p -chlorophenyl)-2, 10-dihydro-2-isopropyliminophenazine, and its structural formula is

Clofazimine is a reddish-brown powder. It is readily soluble in benzene; soluble in chloroform; poorly soluble in acetone and in ethyl acetate; sparingly soluble in methanol and in ethanol; and virtually insoluble in water. Its molecular weight is 473.4.

      Inactive Ingredients. Beeswax, butylated hydroxytoluene, citric acid, ethyl vanillin, gelatin, glycerin, iron oxide, lecithin, p-methoxy acetophenone, parabens, plant oils, propylene glycol.

CLINICAL PHARMACOLOGY

Lamprene exerts a slow bactericidal effect on Mycobacterium leprae (Hansen’s bacillus). Lamprene inhibits mycobacterial growth and binds preferentially to mycobacterial DNA. Lamprene also exerts anti-inflammatory properties in controlling erythema nodosum leprosum reactions. However, its precise mechanisms of action are unknown.

Pharmacokinetics

Lamprene has a variable absorption rate in leprosy patients, ranging from 45%-62% after oral administration. The average serum concentrations in leprosy patients treated with 100 mg and 300 mg daily were 0.7 µg/mL and 1.0 µg/mL, respectively. After ingestion of a single dose of 300 mg, elimination of unchanged Lamprene and its metabolites in a 24-hour urine collection was negligible. Lamprene is retained in the human body for a long time. The half-life of Lamprene following repeated oral doses is estimated to be at least 70 days. Part of the ingested drug recovered from the feces may represent excretion via the bile. A small amount is also eliminated in the sputum, sebum, and sweat.

      Lamprene 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. In autopsies performed on leprosy patients, clofazimine crystals were found predominantly in the mesenteric lymph nodes, adrenals, subcutaneous fat, liver, bile, gall bladder, spleen, small intestine, muscles, bones, and skin.

Microbiology

Measurement of the minimum inhibitory concentration (MIC) of Lamprene 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% Lamprene 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.

      Lamprene does not show cross-resistance with dapsone or rifampin.

      The following in vitro data are available, but their clinical significance is unknown. Lamprene has been shown in vitro to inhibit M. avium and M. bovis at concentrations of approximately 0.1-1.0 µg/mL. The MIC for M. avium-intracellulare isolated from patients with acquired immunodeficiency syndrome (AIDS) ranged from 1.0 to 5.0 µg/mL. With a few exceptions, microorganisms other than mycobacteria are not inhibited by Lamprene.

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