Clofazimine

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Clofazimine
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Indications

  • Lepromatous leprosy.
  • Multibacillary leprosy (in combination with rifampicin and dapsone).
  • Erythema nodosum leprosum.
  • Chronic discoid lupus erythematosus
  • Granulomatous cheilitis
  • Chronic graft-versus-host disease.
  • Neutrophilic dermatoses (pyoderma gangrenosum, Sweet syndrome) .
  • Granuloma faciale.
  • Orofacial granulomatosis.
  • Granulomatous cheilitis.
  • Ashy dermatosis.
  • Acne fulminans.
  • keloidal blastomycosis.
  • Other infections : (mycobacterial, malacoplakia, rhinoscleroma).

Dosage

  • 50–400 mg orally daily(Larger doses are usually divided into two to four times daily).
  • Multibacillary leprosy. : Clofazimine 300 mg (Monthly supervised) + Clofazimine 50 mg (daily self‐administered) for 12 months.
  • Erythema nodosum leprosum. : Clofazimine 300 mg/day for several months.
  • Ashy dermatosis: Clofazimine 100 mg/day for 3 months in inflammatory cases.
  • Acne fulminans: Clofazimine 200 mg three times a week.
  • Orofacial granulomatosis: Clofazimine 100 mg twice daily 10 days, then twice weekly for 4 months.
  • Granulomatous cheilitis: Clofazimine 100 mg twice daily for 10 days, then twice weekly for 4 months.
  • keloidal blastomycosis: combination of itraconazole,100 mg/day, and clofazimine, 100 mg/day. .
  • Granuloma faciale: Clofazimine (300 mg daily).
  • pyoderma gangrenosum: Clofazimine 100 mg three times daily( 4 weeks).
  • Sweet syndrome: Clofazimine 200 mg/day for 4 weeks followed by 100 mg/day for 4 weeks.

Mechanism of action

  • Antimycobacterial -Anti-inflammatory-Selective immunomodulation.
  • Clofazimine binds to mycobacterial DNA leading to disruption of the cell cycle and eventually kills the bacterium.
  • It disrupts cell membranes and inhibits bacterial proliferation (activation of phospholipase A2 leads to generation of membrane-destabilizing lysophospholipids).
  • Clofazimine enhances superoxide production .
  • It inhibits neutrophil motility and lymphocyte proliferation.

Monitoring

Baseline Monitoring

  • Baseline electrolyte panel.

Follow Up Monitoring

  • Periodic LFTs if daily doses >100 mg.
  • Periodic evaluation for GI side effects and skin discoloration.

Side effects

  • Reversible orange-brown discoloration of the skin.
  • Discoloration of cornea, conjunctiva, and body fluids (urine, sweat, tears).
  • Xerosis, ichthyosis.
  • Gastrointestinal symptoms:(abdominal pain, nausea, vomiting, diarrhea)
  • Ocular irritation.
  • Elevated hepatic enzymes.
  • Fatal enteropathy (rarely).
  • Cardiac arrhythmias (rarely; associated with electrolyte disturbances).
  • Exacerbation of vitiligo.
  • Depression secondary to skin discoloration.

Contraindications

  • Prior hypersensitivity reaction.

Interactions

  • A degree of caution is encouraged for concomitant use with either rifampin or isoniazid.
  • Dapsone may inhibit the anti-inflammatory activity of clofazimine( have not been confirmed).
  • Clofazimine and deutetrabenazine both increase QTc interval. Avoid or Use Alternate Drug.
  • Ivosidenib and clofazimine both increase QTc interval. Avoid or Use Alternate Drug.
  • Macimorelin and clofazimine both increase QTc interval. Avoid or Use Alternate Drug.
  • Ribociclib and clofazimine both increase QTc interval. Avoid or Use Alternate Drug.
  • Clofazimine and gemtuzumab both increase QTc interval. Use Caution/Monitor.
  • Clofazimine and lofexidine both increase QTc interval. Use Caution/Monitor. ECG monitoring is recommended.
  • Oxaliplatin will increase the level or effect of clofazimine. Use Caution/Monitor.
  • Monitor for ECG changes if therapy is initiated in patients with drugs known to prolong QT.
  • Clofazimine decreases levels of rifampin by inhibition of GI absorption. Applies only to oral form of both agents.

Pregnancy & Lactation

  • Clofazimine should be avoided during pregnancy (formerly category C)
  • Lactation (concentrated in breast milk).
  • Breast milk may turn pink and nursing infants of mothers taking clofazimine have developed skin discolouration.

Precautions

  • Avoid long-term administration of >200 mg daily.
  • Clofazimine should be used with caution in patients who have gastrointestinal problems such as abdominal pain and diarrhea.
  • Severe abdominal symptoms have necessitated exploratory laparotomies in some patients receiving clofazimine.
  • For skin dryness and ichthyosis, oil can be applied to the skin.
  • Discoloration of soft contact lenses may also occur.

Drug Info

  • The pigmentation usually fades within 6–12 months of stopping clofazimine, although traces of discoloration may remain for up to 4 years.
  • When taken with food, absorption is increased.
  • Patients should be warned that clofazimine 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.

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