No

Leprostatic Agent

Orphan drug: Treatment of dapsone-resistant leprosy; multibacillary dapsone-sensitive leprosy; erythema nodosum leprosum; Mycobacterium avium-intracellulare (MAI) infections

C

Hypersensitivity to clofazimine or any component

Use with caution in patients with GI problems; dosages >100 mg/day should be used for as short a duration as possible; skin discoloration may lead to depression

>10%:

Dermatologic: Dry skin

Gastrointestinal: Abdominal pain, nausea, vomiting, diarrhea

Miscellaneous: Pink to brownish-black discoloration of the skin and conjunctiva

1% to 10%:

Dermatologic: Rash, pruritus

Endocrine & metabolic: Elevated blood sugar

Gastrointestinal: Fecal discoloration

Genitourinary: Discoloration of urine

Ocular: Irritation of the eyes

Miscellaneous: Discoloration of sputum, sweat

<1%: Edema, vascular pain, dizziness, drowsiness, fatigue, headache, giddiness, taste disorder, fever, erythroderma, acneiform eruptions, monilial cheilosis, phototoxicity, hypokalemia, bowel obstruction, GI bleeding, anorexia, constipation, weight loss, eosinophilic enteritis, cystitis, eosinophilia, anemia, hepatitis, jaundice, enlarged liver; increased albumin, serum bilirubin, and AST; bone pain, neuralgia, diminished vision, lymphadenopathy

Following GI decontamination, treatment is supportive

Decreased effect with dapsone (unconfirmed)

Protect from moisture

Binds preferentially to mycobacterial DNA to inhibit mycobacterial growth; also has some anti-inflammatory activity through an unknown mechanism

Absorption: Oral: 45% to 70% absorbed slowly

Distribution: Remains in tissues for prolonged periods; appears in breast milk; highly lipophilic; deposited primarily in fatty tissue and cells of the reticuloendothelial system; taken up by macrophages throughout the body; also distributed to breast milk, mesenteric lymph nodes, adrenal glands, subcutaneous fat, liver, bile, gallbladder, spleen, small intestine, muscles, bones, and skin; does not appear to cross blood-brain barrier

Metabolism: Partially in the liver to two metabolites

Half-life: Terminal: 8 days; Tissue: 70 days

Time to peak serum concentration: 1-6 hours with chronic therapy

Elimination: Mainly in feces; negligible amounts excreted unchanged in urine; small amounts excreted in sputum, saliva, and sweat

Oral:

Adults:

Dapsone-resistant leprosy: 100 mg/day in combination with one or more antileprosy drugs for 3 years; then alone 100 mg/day

Dapsone-sensitive multibacillary leprosy: 100 mg/day in combination with two or more antileprosy drugs for at least 2 years and continue until negative skin smears are obtained, then institute single drug therapy with appropriate agent

Erythema nodosum leprosum: 100-200 mg/day for up to 3 months or longer then taper dose to 100 mg/day when possible

Pyoderma gangrenosum: 300-400 mg/day for up to 12 months

Dosing adjustment in hepatic impairment: Should be considered in severe hepatic dysfunction

May be administered with meals; presence of food increases the extent of absorption

May cause drowsiness or giddiness

None reported

No information available to require special precautions

No effects or complications reported

May be taken with meals. Drug may cause a pink to brownish-black discoloration of the skin, conjunctiva, tears, sweat, urine, feces, and nasal secretions. Although reversible, it may take months to years for skin discoloration to disappear after therapy is complete. Report promptly bone or joint pain, GI disturbance, or vision disturbances. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to be pregnant. Do not breast-feed.

Monitor for GI complaints

Capsule, as palmitate: 50 mg

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"Effect of Combined Therapy with Ansamycin, Clofazimine, Ethambutol, and Isoniazid for Mycobacterium avium Infection in Patients With AIDS," J Infect Dis, 1989, 159(4):784-7.

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Hoy J, Mijch A, Sandland M, et al, "Quadruple-Drug Therapy for Mycobacterium avium-intracellulare Bacteremia in AIDS Patients," J Infect Dis, 1990, 161(4):801-5.

Kemper CA, Meng TC, Nussbaum J, et al, "Treatment of Mycobacterium avium Complex Bacteremia in AIDS With a Four-Drug Oral Regimen. Rifampin, Ethambutol, Clofazimine, and Ciprofloxacin" Ann Intern Med, 1992, 116(6):466-72.

Moore VJ, "A Review of Side Effects Experienced by Patients Taking Clofazimine," Lepr Rev, 1983, 54(4):327-35.

"Recommendations on Prophylaxis and Therapy for Disseminated Mycobacterium avium Complex for Adults and Adolescents Infected With Human Immunodeficiency Virus," MMWR Morb Mortal Wkly Rep, 1993, 42(RR-9):14-20.