كلوفازيمين

PHARMACOKINETICS:

Absorption: Clofazimine is absorbed slowly and variably from the gastrointestinal tract after oral administration. Its bioavailability can be influenced by food intake.

Distribution: It is highly lipophilic and extensively distributed in body tissues, especially in fatty tissues, skin, liver, and spleen. Clofazimine accumulates in macrophages and reticuloendothelial tissues, leading to a prolonged half-life.

Metabolism: Clofazimine undergoes minimal metabolism in the body.

Elimination: The drug is primarily eliminated via the bile into the feces, with only a small amount excreted in the urine. Due to tissue accumulation, it has a very long terminal half-life, ranging from several weeks to months.

PHARMACODYNAMICS:

Clofazimine produces its antimicrobial action by binding to mycobacterial DNA, interfering with DNA replication and transcription processes, thereby inhibiting bacterial growth and reproduction. Additionally, it generates reactive oxygen species (ROS) within the bacteria, causing oxidative damage that contributes to its bactericidal activity. Beyond its antimicrobial properties, clofazimine also has anti-inflammatory effects, which help reduce inflammation and immune-mediated tissue damage associated with diseases like leprosy. Its accumulation in macrophages and tissues enhances both its antimicrobial and anti-inflammatory actions, contributing to its prolonged therapeutic effects.

DOSAGE AND ADMINISTRATION:

Typical Adult Dosage:

• Multibacillary Leprosy:
  100 mg taken orally once daily, along with a supervised dose of 300 mg once a month.
• Paucibacillary Leprosy:
  Used in combination with other medications according to established treatment protocols.

Administration:

Clofazimine is given orally and is best taken with food to enhance absorption.
The duration of treatment is generally long-term, often lasting from several months to a few years, depending on the severity and type of infection.

DRUG INTERACTIONS:

Some drugs should be avoid while taking clofazimine as it get interact with other drugs causing adverse effects. Below are the some drugs mentioned that should be avoid while taking clofazimine.

Antibiotics -  Azithromycin, Trimethoprim, sulfamethoxazole, trimethoprim

Antacids – Aluminium hydroxide, magnesium hydroxide, simethicone

FOOD INTERACTIONS: 

Avoid taking alcohol.

CONTRAINDICATIONS:

Contraindicated in patients with hypersensitivity to clofazimine and severe gastrointestinal disorders.

ADVERSE EFFECTS:

• Loss of appetite
• Nausea
• Discoloration
• Diarrhea
• Change in taste
• Fever
• Headaches
• Hives
• Jaundice

OVERDOSE:

Taking overdose of clofazimine can cause some toxic effects.

• Cardiotoxicity
• Phototoxicity
• Change in skin colour