Lamprene

• Phenazine dye with antimycobacterial and anti-inflammatory activity.1 2 4 37 70 76 78 117 118 119 139 141 Commercially available as capsules containing micronized clofazimine suspended in an oil-wax base.1

• Mechanism of action against mycobacteria not fully elucidated.1 2 37 118 120 Appears to exert antimycobacterial effect by binding preferentially to mycobacterial DNA and inhibiting replication and growth.1 2 119 120 121 122 124

• Exerts anti-inflammatory and immunosuppressive effects in vitro and in vivo.1 2 37 54 58 60 61 66 80 101 102 139 146 Precise mechanisms of these effects not fully elucidated,1 37 60 61 80 but appears to cause dose-dependent inhibition of neutrophil motility54 61 80 101 102 and also inhibits mitogen-induced lymphocyte transformation.54 60 61 80 101 May enhance phagocytic activity of polymorphonuclear cells and macrophages2 99 103 and enhance membrane-associated oxidative metabolism in these cells.58 61

• Clofazimine’s anti-inflammatory and immunosuppressive effects, in addition to antimycobacterial effects, appear to contribute to efficacy in the treatment and prevention of ENL reactions.2 37 54 58 61 66 80 101 102 139

• Slowly bactericidal against Mycobacterium leprae in vivo.1 36 37 76 118 119 123 Bactericidal against M. tuberculosis163 and M. marinum98 in vitro, but appears to be only bacteriostatic in vitro against other mycobacteria,2 including M. avium complex (MAC).35

• M. leprae resistant to clofazimine reported only rarely.24 26 27 87 163 193

• Cross-resistance between clofazimine and dapsone or rifampin not reported to date.1 2 135 139 163 However, there are rare reports of M. leprae resistant to both clofazimine and dapsone, but susceptible to rifampin.26

In the U.S.

• Lamprene

Available Dosage Forms:

• Capsule

Therapeutic Class: Leprostatic

Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor immediately if any of the following side effects occur:

• Bloody or black, tarry stools
• colicky or burning abdominal or stomach pain
• mental depression
• yellow eyes or skin—may be an orange color if already have a pink to brownish-black skin or eye discoloration

Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

• Diarrhea
• dry, rough, or scaly skin
• loss of appetite
• nausea or vomiting
• pink or red to brownish-black discoloration of skin and eyes
• skin rash and itching

• Changes in taste
• dryness, burning, itching, or irritation of the eyes
• increased sensitivity of skin to sunlight

Clofazimine commonly causes discoloration of the feces, lining of the eyelids, sputum, sweat, tears, and urine. Usually this side effect does not require medical attention, but the discoloration may not go away. However, clofazimine may also cause bloody or black, tarry stools. This side effect may be a symptom of serious bleeding problems that do require medical attention.

Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

Lamprene is indicated in the treatment of lepromatous leprosy, including dapsone-resistant lepromatous leprosy and lepromatous leprosy complicated by erythema nodosum leprosum. Lamprene has not been demonstrated to be effective in the treatment of other leprosy-associated inflammatory reactions.

      Combination drug therapy has been recommended for initial treatment of multibacillary leprosy to prevent the development of drug resistance.