clofazimine (Lamprene)
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Indications
- treatment of dapsone-resistant leprosy
- multibacillary dapsone-sensitive leprosy
- erythema nodosum leprosum
- Mycobacterium avium intracellulare (MAI) infection
- pyoderma gangrenosum[3]
Contraindications
Caution:
- patients with gastrointestinal (GI) problems
- skin discoloration may lead to severe depression
Dosage
- well tolerated in doses < 100 mg/day
- doses > 100 mg/day should be used for as short a duration as possible
- take doses with meals
- dapsone-resistant leprosy:
- multibacillary dapsone-sensitive leprosy
- 100 mg PO QD in combination with 2 or more antileprosy agents for at least 2 years
- continue until negative skin smears are obtained, then
- single drug therapy with appropriate agent
- erythema nodosum leprosum
- Mycobacterium avium intracellulare (MAI) infection
- leprosy in children: 1 mg/kg/day in combination with dapsone & rifampin
Capsules: 50 & 100 mg.
Pharmacokinetics
- oral absorption: 45-70%, aborbed slowly
- tissue distribution
- distributed principally to fatty tissues & reticulo- endothelial cells
- appears in breast milk
- crosses placenta
- does not distribute into brain or CSF
- remains in tissues for prolonged periods of time
- metabolized partially in the liver
- mainly excreted in the feces
- elimination 1/2life
- 70 days (tissue)
- 8 days (terminal)
elimination via feces
elimination via liver
1/2life = 70 days tissue
1/2life = 8 days terminal
Adverse effects
- common (> 10%)
- dry skin, abdominal pain, nausea/vomiting, diarrhea, pink to brownish-black discoloration of skin & conjunctiva*
- less common (1-10%)
- rash, pruritus, hyperglycemia, fecal discoloration*, urine discoloration*, eye irritation, sputum discoloration*, sweat discoloration*
- uncommon (< 1%)
- edema, vascular pain, dizziness, drowsiness, fatigue, headache, giddiness, taste disturbance, fever, erythroderma, acne, monilial cheilosis, phototoxicity, hypokalemia, bowel obstruction, GI bleeding, anorexia, constipation, weight loss, eosinophilic enteritis, cystitis, eosinophilia, anemia, hepatitis, jaundice, bone pain, neuralgia, decreased visual acuity, lymphadenopathy
* pink to brownish-black discoloration of skin, conjunctiva, tears, sweat, urine, feces, nasal secretions; may take months to years to disappear after therapy is complete
Drug interactions
- dapsone:
- possibly diminished anti-inflammatory effect
- anti-mycobacterial effect is unaffected
Mechanism of action
- highly lipophilic agent
- leprostatic