CLOFAZEMINE 100MG TABLET

Indications

• Leprosy (Hansen's disease)
• Mycobacterial infections

Dosage

Children: Refer to the BNF for Children for appropriate dosing based on age and weight.

Adults: Refer to established guidelines or the BNF for specific dosing information, as it varies based on the condition being treated and patient factors.

Mechanism of action

Clofazimine works by binding to the mycobacterial DNA, disrupting the function of the DNA and inhibiting bacterial replication. It also has anti-inflammatory properties, which may help in the management of chronic inflammatory conditions associated with mycobacterial infections.

Pharmacodynamics

Clofazimine exhibits bactericidal activity against Mycobacterium leprae and has demonstrated efficacy against other mycobacterial species. Its unique mechanism involves interference with the bacterial DNA and modulation of the immune response, leading to a reduction in inflammation and bacterial burden. The drug's anti-inflammatory effects are particularly beneficial in alleviating the symptoms of leprosy.

Pharmacokinetics

Clofazimine is well absorbed from the gastrointestinal tract and is highly lipophilic, allowing it to accumulate in tissues, particularly in the adipose tissue. It has a long elimination half-life, typically ranging from 70 to 100 days, which allows for once-daily dosing in many cases. The drug is metabolized in the liver and excreted mainly through the bile. Its long half-life necessitates monitoring for potential accumulation and side effects during treatment.

Contra-indications

• Hypersensitivity to clofazimine or any of its components
• Severe liver impairment

Adverse effects

• Skin discoloration (pink to brown)
• Gastrointestinal disturbances (nausea, vomiting, diarrhea)
• Dry skin
• Abdominal pain
• Fatigue
• Potential for QT prolongation

Interactions

• May interact with drugs that are substrates of CYP450 enzymes
• May increase the effect of digoxin
• Potential interaction with antiretroviral drugs

Precautions

• Use with caution in patients with liver disease
• Monitor for signs of hypersensitivity reactions
• Periodic monitoring of cardiac function is advised due to the risk of QT prolongation

Pregnancy

Clofazimine is classified as category C. Its safety in pregnancy has not been established, and it should be used only if the potential benefit justifies the potential risk to the fetus.

Breast-feeding

Clofazimine is excreted in breast milk. Caution is advised when administered to nursing mothers.

Storage

Store in a cool, dry place, away from direct sunlight. Keep out of reach of children.

Formulations

• Capsules (100 mg)
• Tablets (50 mg)